SUPER PHARMA TABLE

Maria Yña Eluisia T. Pereyra RPh, MD,

MBA

DRUG MOA and INDICATION ADVERSE EFFECTS NOTABLE PROPERTIES

1. AUTONOMIC DRUGS
Cholinomimetics
A. Direct Acting Choline Esters
i. Acetylcholine Muscarinic agonist; activates M1 through M3 CNS stimulation, miosis, cyclospasm, very short lived DOA: 5-30sec, apidly
receptors in all peripheral tissues. Results to brochoconstriction, excessive GI and GU smooth hydrolyzed by AChE; acts on both M and N
increased secretion, smooth muscle contraction muscle contraction, increased secretory activity receptors
(except in vascular smooth muscles where it causes of sweat gland, airways etc, vasodilation
relaxation) and changes in heart rate
ii.Betanechol Muscarinic agonist; activates M1 through M3 Cylospasm, diarrhea, urinary urgency, Results in smooth muscle contraction
receptors in all peripheral tissues (same as Ach) ; for vasodilation, reflex tachycardia, sweating except in vascular smooth muscles where it
Bladder and bowel atony causes relaxation; resistant to AChE, orally
active, act on M receptors only
iii. Carbachol Nonselective muscarinic and nicotinic agonist; similar Cylospasm, diarrhea, urinary urgency, acts on both M and N receptors, DOA:
to betanechol; used topically for glaucoma treatment vasodilation, reflex tachycardia, sweating 30mins-2hrs

B. Direct Acting Muscarinic Alkaloids

i. Pilocarpine Partial muscarinic agonist; used for treatment of Miosis, blurring of vision good lipid solubility compared to choline
Glaucoma, Sjogren's syndrome and Sicca syndrome esters

C. Direct Acting Nicotinic Agonists

i. Nicotine Agonist at both NN and NM receptos; activates Generalized ganglionic stimulation Able to enter the CNS and activates NN
autonomic post ganglionic neurons (both (hypertension, tachycardia, nausea, vomiting, receptors ; DOA: 1-6h only
sympathetic and parasympathetic) and skeletal diarrhea)
muscle neuromuscular end plates ; for Smoking
Cessation
ii. Varenicline Selective partial agonist at nicotinic receptors; used Generalized ganglionic stimulation longer DOA than nicotine: 12-24h
exclusively for smoking cessation (hypertension, tachycardia, nausea, vomiting,
diarrhea)
D. Short Acting Cholinesterase
Inhibitor (Alcohol)
i. Edrophonium Binds briefly to active site of acetylcholinesterase Miosis, salivation, nausea, vomiting, diarrhea, parenteral, very short lived DOA: 5-15min
(AChE) and prevents access of acetylcholine (Ach); bradycardia
Amplifies all actions of Ach; increases
parasympathetic activity and somatic neuromuscular
transmission ; for Myasthenia gravis diagnosis
(Tensilon test)
E. Intermediate Acting Cholinesterase
Inhbitors (Carbamates)
 i. Neostigmine Forms covalent bonds with AChE, but is hydrolyzed Miosis, salivation, nausea, vomiting, diarrhea, poor lipid solubility, oral, DOA: 30min-2h
and released; Longer acting than Edrophonium ; for bradycardia
Myasthenia gravis treatment; reversal of
nondepolarizing muscular blockade, Ogilvie
syndrome
ii. Pyridostigmine Longer acting effect compared to Neostigmine Miosis, salivation, nausea, vomiting, diarrhea, poor lipid solubility, oral, DOA: 4-8h
bradycardia
iii. Physostigmine Natural alkaloid tertiary amine, similar to Miosis, salivation, nausea, vomiting, diarrhea, good lipid solubility: able to enter the CNS,
neostigmine bradycardia DOA: 4-8h
F. Long Acting Cholinesterase
Inhibitors (Organophosphates)
i. Echothiophate Similar to neostigmine but with slower release Miosis, salivation, nausea, vomiting, diarrhea, moderate lipid solubiliy, DOA: 2-7days
bradycardia
ii. Malathion, Parathion malathion: scabicide, parathion: insecticide Miosis, salivation, nausea, vomiting, diarrhea, high lipid solubiliy, DOA: 7-30 days
bradycardia
Cholinoceptor Blocking Drugs
i. Scopolamine Competitively blocks all muscarinic receptors, Drowsiness, blurring of vision, dry eyes, known as Hyoscine-N-Butyl-Bromide
antagonizes histamine and serotonin ; for motion constipation, dry mouth, urinary retention (Buscopan)
sickness, dec. acid secretion in the GIT
ii. Atropine Nonselective competitive antagonism at all Tachycardia, mydriasis, cyloplegia, skin flushing, DOC for organophosphate poisoning;
muscarinic receptors in the CNS and peripheral delirium, hallucinations, urinary retention, notorious for causing hyperthermia
tissues; causes mydriasis and cycloplegia; mandatory constipation
antidote for severe cholinesterase inhibitor poisoning
; Mydriatic, cycloplegic, antidote for
organophosphate poisoning (DOC), for bradycardia,
hypersalivation and to decrease airway secretion
during general anesthesia

iv. Homatropine Similar to atropine but with a shorter duration of Mydriatic, cycloplegic
action (12-24h) ; Mydriatic, cycloplegic in eye
examinations
v. Cyclopentolate Similar to atropine but with a shorter duration of Mydriatic, cycloplegic
action (3-6h), Mydriatic, cycloplegic in eye
examinations
vi. Tropicamide Similar to atropine but with the shortest duration of shorter DOA among cholineceptor blockers
action (15-60min); Mydriatic, cycloplegic in eye (15-60min)
examinations
vii. Ipratropium Competitive nonselective antagonist at muscarinic Dry mouth, cough, nasal dryness not as effective as SABAs but less
receptors ; for BA and COPD tachycardia and arrhythmia ; few
muscarinic effects outside the lungs
viii. Tiotropium Similar to Ipratropium but with longer duration of Dry mouth, cough, nasal dryness not as effective as SABAs but less
action tachycardia and arrhythmia ; few
muscarinic effects outside the lungs
 ix. Oxybutinin Nonselective muscarinic antagonist which reduces Tachycardia, mydriasis, cyloplegia, skin flushing, for urinary urgency and incontinence
detrussor smooth muscle tone spasms ; for delirium, hallucinations, urinary retention,
decreasing urgency in mild cystitis and dec. bladder constipation
spasm after urologic surgery
x. Pralidoxime Regenerates active acetylcholinesterase; can relieve muscle weakness Must be administered before 6-8 hours of
skeletal muscle and endplate block ; Usual antidote organophosphate bond with cholinesterase
for early stage cholinesterase inhibitor poisoning occurs ; has oxime group which has high
affinity for phosphorus
xi. Hexamethonium, Mecamylamine, Competitively blocks all Nn nicotinic Ach receptors ; Postural hypotension, dry mouth, blurred vision, first successful agents in treating HTN
Trimethaptan for Hypertensive emergencies (obsolete) constipation, sexual dysfunction

Sympathomimetics
i. Epinephrine Non-selective, direct acting sympathomimetic; Hypertension, tachycardia, ischemia, DOC for Anaphylaxis ; inactive per orem ;
activates A and B adrenergic receptors; A1 - hyperglycemia do not enter CNS significantly ; short DOA
vasoconstriction and increased BP; B1 - increased HR,
conduction and contractility; B2 - bronchodilatation ;
used for Cardiac arrest, anaphylaxis, asthma, COPD,
Hemostasis
ii. Norepinephrine Non-selective, direct acting sympathomimetic; Extreme vasospasm, tissue necrosis, excessive Compensatory vagal reflexes tend to
activates A and B adrenergic receptors; A1 - BP increase, arrhythmias, infarction, reflex overcome the direct postive chronotropic
vasoconstriction and increased BP; B1 - increased HR, bradycardia effects ; alpha activity > beta activity;
conduction and contractility; B2 - bronchodilatation ; inactive per orem ; do not enter CNS
used for Neurogenic shock, cardiogenic shock significantly ; short DOA

iii. Dopamine Non-selective, direct acting sympathomimetic; Cardiovascular disturbances, arrhythmias inactive per orem ; do not enter CNS
activates A, B and D1 adrenergic receptors; A1 - significantly ; short DOA; very effective in
vasoconstriction and increased BP; B1 - increased HR, renal failure associated with shock
conduction and contractility; D1 - vasodilation in
splanchnic and renal blood vessels ; for cardiogenic
Shock and heart failure
iv. Isoproterenol Beta nonselective sympathomimetic; nonselectively Cardiovascular disturbances, arrhythmias synthetic catecholamine, not readily taken
activates B adrenergic receptors; B1 - increased HR, up into nerve endings
conduction and contractility; B2- bronchodilatation ;
for Asthma
vi. Phenylephrine A1 agonist used for short term maintenance of BP in Rebound nasal congestion (Rhinitis Mydriasis without cycloplegia
acute hypotension; also used intranasally to produce medicamentosa), hypertension, stroke, MI
local vasoconstriction as a decongestant ; mydriatic,
for drug-induced hypotension, spinal shock

vii. Clonidine A2 agonist that inhibits adenylyl cyclase and interacts Sedation, rebound hypertension, dry mouth When taken per orem, there is initial inc in
with other intracellular pathways; marked BP then will go down once the drug enters
vasodilation by central sympatholytic effect ; for the CNS
Hypertension, Cancer pain, opioid withdrawal
 viii. Methyldopa, Guanfacine and Central sympatholytics analogous to clonidine ; Sedation, positive Coomb's test (Hemolytic Methyldopa - positive Coomb's test
Guanabenz Methyldopa is used for Pre-eclampsia anemia) (Hemolytic anemia)
xi. Apraclonidine, Brimonidine A2 agonist; reserved for ophthalmologic use in eye discomfort, hyperemia and pruritus, blurred NONE
glaucoma for reduction of intraocular pressure vision
xii. Dobutamine B1 agonist that activates adenylyl cyclase, increasing Tachyarrhythmia, Hypertension, Eosinophilic Beta1 selective
myocardial contractility; with positive inotropic effect myocarditis, Premature ventricular beats,
; Clinically used for cardiogenic shock and acute heart Angina, Dyspnea, Fever, Headache, Nausea,
failure Palpitation
xiii. Albuterol/Salbutamol B2 agonist with adenylyl cyclase activation; results to Nausea , Fever, Bronchospasm, Vomiting, Rapid development of tolerance; DOC as
bronchial smooth muscle dilation ; for Bronchial Headache, Dizziness, Cough, Allergic reactions Asthma reliever
Asthma
xiv. Fenoldopam D1 agonist that activates adenylyl cyclase; results to Angina, Cardiac dysrhythmia, Dizziness, D1 agonist
vascular smooth muscle relaxation ; for Hypertension Flushing, Heart failure, Hypotension, Myocardial
infarction, Tachycardia
xv. Bromocriptine D2 agonist that inhibits adenylyl cyclase and interacts Nausea, Hypotension, Headache, Dizziness D2 agonist
with other intracellular pathways; restores dopamine
actions in the CNS for Parkinson's disease,
prolactinemia
Sympatholytics
i. Phenoxybenzamine Irreversibly blocks A1 and A2 receptors resulting to Orthostatic hypotension, Reflex tachycardia, GI Irreversible blockade
indirect baroreflex activation. Decreases blood irritation
pressure but increases heart rate due to baroreflex
activation ; for Pheochromocytoma
ii. Phentolamine Reversible A1 and A2 receptor antagonist with low Orthostatic hypotension, Reflex tachycardia, GI Reversible blockade
half life ; for Pheochromocytoma and Rebound irritation
hypertension
iii. Prazosin, Doxazosin, Terazosin Blocks A1 but not A2 receptors; leads to reduction in Dizziness, Drowsiness, Headache, Weakness, Used in patients with HTN and BPH at the
blood pressure ; for Benign Prostatic Hyperplasia, Asthenia, Nausea, Palpitation, Edema, same time
Hypertension Orthostatic hypotension
iv. Tamsulosin Slightly selective A1a blockade causing relaxation of Headache, Orthostatic hypotension, Rhinitis, Slightly selective A1a blockade causing
prostatic smooth muscles > vascular smooth muscle ; Abnormal ejaculation, Dizziness, Arthralgia, relaxation of prostatic smooth muscles >
for BPH Infection vascular smooth muscle
vi. Labetalol Beta blockade > A1 blockade; still with BP depressant Bronchospasm, cardiac depression, AV block, safe in pregnant patients
effects and limited HR increase hypotension, dizziness, headache; Use in
caution with DM Px: Masks symptoms of
hypoglycemia in diabetics
vii. Propranolol, Nadolol, Timolol Blocks B1 and B2 receptors; lowers both HR and BP Propranolol has local anesthetic effect
and reduces the release of renin ; for Angina
prophylaxis, hypertension, arrhythmias, migraine,
performance anxiety, hyperthyroidism
 viii. Metoprolol, Atenolol, Alprenolol, B1 > B2 blockade; lowers both HR and BP, reduces Nebivolol has vasodilating effect ;
Betaxolol, Nebivolol the release of renin BUT is considered safer for metoprolol reduce moratlity in heart failure
patients with asthma ; for Angina prophylaxis,
hypertension, arrhythmias, migraine, performance
anxiety, hyperthyroidism
x. Pindolol, Acebutolol, Carteolol, B1, B2 with intrinsic sympathomimetic (partial Pindolol is a partial agonist, therefore safer
Bopindolol, Oxprenolol, Celiprolol, agonist) effect; lowers BP with modest reduction in in bronchial asthma
Penbutolol HR
xi. Carvedilol, Medoxalol, Bucindolol, Beta blockade > A1 blockade; still with BP depressant Carvedilol reduce mortality in heart failure
Labetalol effects and limited HR increase ; for Heart Failure

xii. Esmolol B1 > B2 blockade; for rapid control of BP and Used in for perioperative thyroid storm
arrhythmias, thyrotoxicosis and myocardial ischemia
intraoperatively ; for Supraventricular tachycardia

2. CARDIOVASCULAR-RENAL DRUGS
Antihypertensives
lower BP by decreasing volume and a direct vascular
A. Diuretics effect that is not yet fully understood

Inhibit Na/Cl transporter in distal convoluted tubule.

Cause moderate diuresis and reduced excretion of Hypokalemic metabolic alkalosis, Dilutional
i.Thiazide: Hydrochlorothiazide, calcium; for mild to moderate hypertension (FIRST hyponatremia, Potassium wasting, causes hypercalcemia in contrast with loop
Chlorthalidone, Metolazone, LINE), Heart failure, Nephrogenic Diabetes Insipidius, hyperlipidemia, hyperuricemia, sulfa allergy, diuretics which cause hypocalcemia ; FIRST
Indapamide Renal calcium stones hyperglycemia, hypercalcemia LINE for mild to moderate hypertension
Inhibit Na/K/2Cl transporter in thick ascending limb
of loop of Henle, Cause powerful diuresis and Hypokalemic metabolic alkalosis, Potassium
increased CA excretion; for heart failure, wasting, ototoxicity, hyperuricemia, causes hypocalcemia in contrast with
ii. Loop: Furosemide, Torsemide, hypertension, acute renal failure, Pulmonary edema, nephrotoxicity, dehydration, hypomagnesemia, thiazide diuretics which cause
Bumetanide, Ethacrynic Acid hypercalcemia, Anion overdose sulfa allergy hypercalcemia
decrease venous return, decrease HR, decrease
contractile force, decrease cardiac output, decrease
B. Sympathoplegics TPR
dry mouth, sedation, rebound hypertension, Taper use prior to discontinuation to avoid
i.Sympathetic Outflow Blocker: activates a2 adrenergic receptors ; for hypertensive hemolytic anemia: (+) Coomb's test rebound hypertension ; readily enter the
Clonidine, Methyldopa urgency (clonidine), pre eclampsia (methyldopa) (methyldopa), sedation CNS

ii. Ganglion blockers: competetively blocks Nn nicotinic Ach receptors; for Postural hypotension, blurred vision,
Hexamethonium,Trimethaphan hypertension (obsolete), hypertensive emergencies constipation, dry mouth, sexual dysfunction NONE
 Reserpine Irreversibly blocks the vesicular
monoamine transporter (VMAT) while Guanethidine
and Guanadrel inhibit the vesicular release of NE
iii. Nerve terminal blockers: from the presynaptic neuron; for Hypertension Sedation, suicidal ideation, severe psychiatric
Reserpine, Guanethidine, Guanadrel (obsolete) depression NONE
iv. Adrenergic antagonists: Tamsulosin is most selective for prostatic
Prazosin,Doxazosin, Terazosin, selectively blocks a1 adrenergic receptors; for Reflex tachycardia (less chance), first dose smooth muscle ; Doxazosin and Terazosin
Tamsulosin, Silodosin hypertension, benign prostatic hyperplasia orthostatic hypotension has longer duration of action than prazosin
C. Vasodilators
Release NO from endothelial cells, Relaxes arteriolar
smooth muscle, causing vasolidation. Decreases combination treatment with ISDN for heart
afterload ; for pre-eclampsia, hypertension, heart Edema, myocardial ischemia, drug induced failure is more effective than ACEIs in
i. Oral Vasolidator: Hydralazine failure lupus (hydralazine), reflex tachycardia blacks
Opens K+ channels in vascular smooth muscle,
causing hyperpolarization, muscle relaxation and Edema, Angina, Reflex tachycardia, Pulmonary
vasolidation; for alopecia / male pattern baldness, hypertension, Pericarditis, Hirsutism, salt and require concomitant use of diuretics and
Minoxidil hypertension water retention BBs to block compensatory responses
ii. Calcium Channel Blockers
block voltage-gated L-type calcium channels (cardiac Constipation, Nausea, flushing,gingival
Non-dihydropyridine calcium > vascular); for Angina, Supraventricular tachycardia, hyperplasia, AV block, sinus node depression,
channel blocker: Verapamil, Diltiazem migraine, hypertension Pretibial edema, dizziness excessive cardiac depression may occur
Dihydropyridine calcium channel
blocker: Nifedipine, Amlodipine,
Nicardipine, Nisoldipine, Isradipine, block voltage-gated L-type calcium channels (vascular Nausea, Flushing, dizziness, pretibial edema, greater vasodilator effect that
Felodipine > cardiac); for Angina, hypertension constipation cardiodepressant effect
iii. Parenteral Vasodilators
relaxes venous and arteriolar smooth muscle; for not commonly used because it is very light
acute heart failure, controlled hypotension, sensitive, has short Duration of action ;
Nitroprusside cardiogenic shock, hypertensive emergency hypotension, headache, CN toxicity given as continuous infusion
a thiazide derivative without a diuretic
Opens K+ channels in vascular smooth muscle, effect ; also reduces insulin release (can be
causing hyperpolarization, muscle relaxation and used to treat hypoglycemia in insulin-
Diazoxide vasolidation; for hypertension hypotension, headache producing tumors)
causes arteriolar vasolidation of the afferent and
efferent arterioles. Increases renal blood flow; for
Fenoldopam hypertensive emergency hypotension, hypokalemia short duration of action: 10mins
D. Angiotensin antagonists and renin
inhibitor
cough, hyperkalemia, rash, hypotension,
palpitations, renal damage in patients with slows down the progression of DM
i. ACE inhibitors: Captopril, Enalapril, inhibit angiotensin converting enzyme ; for preexisting renal vascular disease but is nephropathy and cardiac remodelling in
Lisinopril, Benazepril hypertension, heart failure protective for DM nephropathy ; CI in pregnancy heart failure
 ii. Angiotensin receptor blocker:
Losartan, Valsartan, Irbesartan, competetively blocks Angiotensin 1 receptor site ; for fatigue / weakness, hypoglycemia, anemia,
Candesartan hypertension diarrhea, cough, CI in pregnancy as effective as ACEi but less cough
diarrhea, cough, rash, hyperkalemia, increase in
inhibitor of renin's action on its substrate serum creatinine, renal impairment, no reproductive toxicity but is also CI
iii. Renin inhibitor: Aliskerin angiotensinogen angioedema because of the toxicity of ACEi and ARBs
Vasodilators and anti-Angina Pectoris
A. Nitrates

releases nitric oxide (NO), relaxes smooth muscle,

i. Ultrashort-acting nitrate: Amyl especially vascular, increases cGMP (cyclic guanosine Reflex tachycardia, Orthostatic hypotension,
Nitrite monophosphate); for cyanide poisoning methemoglobinemia inhalational route, but now rarely used
releases nitric oxide (NO), increases cGMP (cyclic Dangerous hypotension with PDE inhibitors
ii. Short-acting nitrate: Nitroglycerin, guanosine monophosphate) and relaxes smooth such as Sildenafil ; First Pass effect is ~90%
Isosorbide Dinitrate, Isosorbide muscle especially vascular; for Angina, acute Reflex tachycardia, orthostatic hypotension, (NTG), NTG also decrease platelet
Mononitrate coronary syndromes headache, tolerance (transdermal) aggregation
B. Calcium Channel Blockers
block voltage-gated L-type calcium channels (cardiac Constipation, Nausea, flushing,gingival
i. Non-dihydropyridine calcium > vascular); for Angina, Supraventricular tachycardia, hyperplasia, AV block, sinus node depression,
channel blocker: Verapamil, Diltiazem migraine, hypertension Pretibial edema, dizziness excessive cardiac depression may occur
ii. Dihydropyridine calcium channel
blocker: Nifedipine, Amlodipine,
Nicardipine, Nisoldipine, Isradipine, block voltage-gated L-type calcium channels (vascular Nausea, Flushing, dizziness, pretibial edema, greater vasodilator effect that
Felodipine > cardiac); for Angina, hypertension constipation cardiodepressant effect
Drugs used in Heart Failure

Other drugs for heart failure include Diuretics

(Furosemide is the DOC for acute heart failure),
Angiotensin Antagonists (ACEi is the DOC for chronic
heart failure), Beta1 blockers (dopamine and
dobutamine), Non-selective Beta Blockers
(Carvedilol, Labetalol, Metoprolol), PDEi (Inamrinone,
Milrinone), Vasodilators (Nitroprusside,
A. Cardiac Glycoside Nitroglycerin)
inhibits Na/K ATPase; increases intracellular Ca, Arrhythmogenesis increased by
increasing cardiac contractility; for heart failure, Narrow therapeutic index, Arrhythmias, hypokalemia, hypercalcemia,
i. Digoxin Nodal arrythmias diarrhea, vomiting, visual changes hypomagnesemia
Anti-Arrhythmics
A. Class 1 Antiarryhtmics
 Use- and state-dependent block of INa channels;
some block of Ik channels. Slowed conduction Arrhythmias, lupus-like syndrome
velocity and pacemaker activity; prolonged action (procainamide), hypotension, cinchonism
potential duration and refractory period; for atrial (quinidine), thrombocytopenia (quinidine),
i. Class 1A: Procainamide, and ventricular arrhythmias especially after antimuscarinic effect (disopyramide), quinidine
Disopyramide, Quinidine, myocardial infarction reduces digoxin clearance Hyperkalemia exacerbates cardiac toxicity

highly selective use and state-dependent INa block; Hyperkalemia, exacerbates cardiac toxicity.
minimal effect in normal tissue; no effect on IK; DOC Lidocaine is the least cardiotoxic among
for ventricular arrhythmia post-myocardial infarction, conventional anti-arrhythmics ; only affect
ii. Class 1B: Lidocaine, Mexiletene, Digoxin-induced arrhythmia ; Mexilitine can be used CNS stimulation, Allergy, Arrhythmias, ischemic tissue; lidocaine is never given P.O
Tocainide, Phenytoin for neuropathic pain depression, Agranulocytosis due to significant first pass effect
Selective use and state-dependent block of INa;
iii. Class 1C: Flecainide, Propafenone, slowed conduction velocity and pacemaker activity; Increased arrhythmias (proarrhythmic effect), hyperkalemia exacerbates cardiac toxicity
Encainide, Moricizine for refractory arrhythmias CNS excitation contraindicated for post MI arrhythmias
B. Class 2 Antiarrythmics

Block of beta-receptors, decrease in cAMP results to

decreased Na and Ca current and suppression of
cardiac pacemaker activity; for Post MI prophylaxis In CHF, reduces progression and decreases
against sudden death, thyrotoxicosis, acute incidence of potentially fatal arrhythmias.
perioperative and thyrotoxic arrhythmias, Bronchospasm, AV block, Hypotension, Cardiac Sotalol is a beta-blocker anti arrhythmic
i. Propranolol, Esmolol Supraventricular tachycardia depression that has class 3 properties
C. Class 3 Arrhythmics Group with the greatest risk for TDP
Selective Ik block ; prolonged action potential and QT
interval; for treatment and prophylaxis of atrial
i. Dofetilide, Ibutilide, fibrillation Torsade de pointes NONE
Ik block and beta-adrenoceptor block; for ventricular
arrhythmias, Supraventricular tachycardia, Atrial Dose-related torsade de pointes, excessive beta-
ii. Sotalol fibrillation blockade (sinus bradycardia, asthma) NONE

Strong Ik block produces marked prolongation of

action potential and refractory period. Group 1
activity slows conduction velocity; groups 2 and 4 Amiodarone has Class 1, 2 3 and 4 activity
activity confer additional anti arrhythmic activity; for Microcrystalline deposits in cornea and skin, therefore is the MOST EFFICACIOUS of all
refractory arrhythmia, used off label in many paresthesias, Pulmonary fibrosis, Tremor, anti-arrhythmics, amiodarone has longest
iii. Amiodarone, Dronedarone arrhythmia Thyroid dysfunction (hyper- or hypo-) among all anti-arrhythmics (1-10 weeks)
D. Class 4 Antiarrythmatics

Block voltage-gated L-type calcium channels (cardiac

>vascular), decreased AV conduction velocity ; for Constipation, Pretibial edema, Nausea, Flushing,
i. Non-dihydropyridine calcium Angina, Hypertension, Supraventricular tachycardia, Gingival hyperplasia, heart failure, AV block, should be avoided in Ventricular
channel blocker: Verapamil, Diltiazem migraine, Raynaud's Phenomenon, Vasospasm dizziness, sinus node depression tachycardia
E.Miscellaneous Antiarrythmics
 Increase in diastolic Ik of AV node that causes
marked hyperpolarization and conduction block; DOC for paroxysmal supraventricular
reduced ICa; For AV nodal arrhythmias, DOC for Flushing, Transient chest pain, Dyspnea, tachycardia, Duration of action is only
i. Adenosine paroxysmal supraventricular tachycardia Hypotension 15sec
Diuretics
A. Carbonic Anhydrase Inhibitors
Inhibits carbonic anhydrase. In proximal tubule, In
glaucoma, secretion of aqueous humor is reduced Drowsiness, Sulfa Allergy, Renal calcium stones,
i. Acetazolamide, Dorzolamide, and in mountain sickness, metabolic acidosis Paresthesias, hyperchloremic metabolic
Brinzolamide, Dichlorphenamide, increases respiration; for glaucoma, diuresis for acidosis, hepatic encephalopathy in cirrhotic
Methanolamide edema with alkalosis. patients, potassium wasting diuresis is self-limiting after 2-3 days
B. Loop Diuretic
Inhibit Na/K/2Cl transporter in thick ascending limb Synergistic ototoxicity with
of loop of Henle, Cause powerful diuresis and Hypokalemic metabolic alkasis, dehydration, aminoglycosides. Efficacy decreased by
increased Ca excretion; for Heart failure, Ototoxicity, Potassium wasting, Sulfa allergy, NSAIDs ; causes hypocalcemia in contrast
i.Furosemide, Bumetanide, Hypertension, Pulmonary Edema, Hypercalcemia, Hyperuricemia, Hypocalcemia, with thiazide diuretics which cause
Torsemide Acute renal failure, Anion overdose Hypomagnesemia, Nephritis hypercalcemia
C. Thiazide Diuretics
Inhibit Na/Cl transporter in distal convolutes tubes.
Causes moderate diuresis and reduced excretion of Hypokalemic metabolic alkalosis, Potassium Synergistic effect with loop diurectics.
i. Hydrochlorothiazide, calcium; For hypertension Hypercalciuria, Heart wasting, dilutional hyponatremia, Efficacy decreased by NSAIDs ; causes
Chlorthalidone, Indapamide, failure, Nephrogenic diabetes insipidius, renal Hyperglycemia, hyperuricemia, sulfa allergy, hypercalcemia in contrast with loop
Metolazone calcium stones hyperlipidemia diuretics which cause hypocalcemia
D. Potassium-Sparing Diuretics
Steroid inhibitors of cytoplasmic aldosterone
receptor in cortical collecting ducts. Reduce K Hyperkalemia, impotence, Benign prostatic
i. Spironolactone, Eplerenone excretion; for Hyperaldosteronism, Heart failure, hyperplasia, Hyperchloremic metabolic acidosis, Eplerenone reduces progression of DM
(Aldosterone Antagonist) Hypokalemia, Hypertension anti-androgenic effect (Spironolactione) nephropathy and reduces mortality post MI
Hyperkalemia, kidney stones, metabolic
Inhibitor of ENaC (Epithelial sodium channels) in acidosis, Acute renal failure (with
ii. Amiloride, Triamterene (Na cortical collecting duct, reduces Na reabsorption and indomethacin), should never be given with should never be given with potassium
channel Blocker) K excretion; for hypokalemia potassium supplements supplements
E. Osmotic Diuretics

Osmotically retains water in tubule by reducing

reabsorption in proximal tubule, descending limb of
Henle's loop, and collecting ducts; in the periphery,
mannitol extracts water from cells; for Transient volume expansion (hyponatremia,
i. Mannitol, Glycerin, Isosorbide, Rhabdomyolysis, Hemolysis, Increased intracranial pulmonary edema; followed by hypernatremia)
Urea pressure, Acute glaucoma nausea, headache, dehydration, vomiting used to maintain high urine flow
F. ADH Agonists/ Antagonists
 Agonists at V1 and V2 ADH receptors. Activate
insertion of aquaporin water channels in collecting
tubule. Vasoconstriction; For central diabetes Increases the factor VIII activity of patients
i. Antidiuretic hormone, insipidus, hemophilia, Nocturnal enuresis, von with mild hemophilia A or von Willebrand
Desmopressin, Vasopressin Willebrand's disease Hypertension, Hyponatremia disease
Infusion site reactions, hyperkalemia,
G. ADH Antagonists: Conivaptan, Nephrogenic diabetes insipidus, Bone and Teeth
Tolvaptan, Lixivaptan, Demeclocycline, Antagonist at V1, V2 receptors; for SIADH and abnormalities(demeclocycline), Renal failure Central Pontine Myelinosis may occur with
Lithium Hyponatremia (Lithium, demeclocycline) rapid correction of hyponatremia

3. DRUGS WITH IMPORTANT ACTION ON SMOOTH MUSCLES

Histamine, Serotonin and the Ergot Alkaloids
A. H1 antagonists diminish or abolish the major actions of histamine in Sedation, should not be given to neonates Possess antimuscarinic, adrenaline-
the body by competitive, reversible blockade of because they are more susceptible to antagonising, serotonin antagonising, and
histamine H1-receptor sites on tissues ; used antimuscarinic effects local anaesthetic effects. Some have
primarily for the alleviation of conditions such as calcium-channel blocking activity ; Sedating
urticarial rashes and nasal allergy that are antihistamines may enhance the sedative
characterised by type I hypersensitivity ; are of value effects of CNS depressants including
in preventing urticaria and are used to treat urticarial alcohol, barbiturates, hypnotics, opioid
rashes and mild angioedema analgesics, anxiolytic sedatives, and
antipsychotics ; all are PO but can be given
topical (nose and eyes) ; negligible effect
on H2 receptors
i. 1st Generation: Diphenhydramine, Reversible blockade of histamine H1-receptor sites Anticholinergic effects, orthostatic hypotension more likely to block autonomic receptors,
Dimenhydrinate, Chlorpheniramine, on tissues ; anti-nausea and antiparkinsonism effect, (promethazine), sedation also has alpha1 blocking and local
Meclizine, Promethazine for allergic reactions, for sedation and motion anesthetic effect ; Cyclizine (more anti-
sickness (Diphenhydramine Dimenhydrinate, motion sickness action less sedative and
Cyclizine, Meclizine, Promethazine), for and autonomic effects); Promethazine (less
chemotherapy-induced vomiting (Diphenhydramine) anti-motion sickness, more sedative and
autonomic effects ; Usual half-life: 4-12h

ii. 2nd Generation: Loratadine, Reversible blockade of histamine H1-receptor sites headache, dry mouth, hyperkinesia, malaise, No sedation and antimuscarinic effects ;
Desloratadine, Cetirizine, on tissues ; for allergic reactions may cause arrhythmia due to blockade of usual half-life: 12-24h
Levocertirizine, Fexofenadine cardiac potassium channels (acrivastine,
astemizole, cetirizine, loratadine, and
terfenadine)
B. H2 antagonists No blocking action on H1 receptor
i. Cimetidine, Ranitidine, Famotidine, Surmountable competitive pharmacologic block of CYP450 inhibitor, antiandrogen effects, used in the ICU setting to prevent gastric
Nizatidine H2 receptors, reduction of nocturnal acid secretion in decreased hepatic blood flow (cimetidine), weak erosion and hemorrhage ; usual half-life: 1-
gastirc and duodenal ulcer, accelerate healing and enzyme inhibitory effect (Ranitidine) 3h
prevent recurrences ; for PUD, GERD and ZES

C. Serotonin Agonists
 i. 5HT1D receptor agonist: Agonist at the 5HT1D receptor in the blood vessels Injection site reaction, paresthesia, dizziness, all are per orem only except for
Sumatriptan, Naratriptan, causing vasocontriction ; 1st line treatment for Acute warm/hot sensation, chest pain, coronary Sumatriptan which can also be given
Almotriptan, Eletriptan, Frovatriptan, migraine and cluster headache attacks vasospasm intranasally, transdermal and IV ; All has 2-
Rizatriptan, Zolmitriptan 27hrs DOA exc for sumatriptan DOA: 2-4h
D. Serotonin Antagonists
i. 5HT3 receptor antagonist: Selectively block 5HT3 receptors ; For antiemesis in Constipation, headache, malaise Dolasetron can increase QRS and QT
Ondansetron, Granisetron, patients post-chemotherapy or post-operation (proarrhythmic effect) duration so never
Dolasetron, Alosetron use in patients with heart disease
E. Ergot Alkaloids most are partial agonists at alpha receptors and 5HT
receptors but some are potent agonist at dopamine
receptors
i. Vasoselective: Ergotamine Mixed partial agonist effects at 5-HT2 and a- gangrene (secondary to ischemia) in overdose, can cause epinephrine reversal due to
adrenoceptors, causes vasoconstriction; For Migraine unusual hyperplasia of the retroperitoneal, partial agonist effect on alpha receptors
attacks (but 5HT1D are preferred) retropleural or subendocardial cavity --> (REMEMBER: All partial agonist will act as
hydronephrosis, cardiac valvular and conduction antagonist in the present of a full agonist)
system malfunction
ii. Uteroselective: Ergonovine Mixed partial agonist effects at 5-HT2 and a- marked uterine contraction, GI upset (nausea, uterus becomes more sensitive to ergots
adrenoceptors, causes vasoconstriction; For control vomiting, diarrhea) during pregnancy, produce very powerful
of post-partum bleeding and long-lasting contraction leading to
decreased bleeding, Never give before
delivery of placenta
The Eicosanoids: Prostaglandins, Thromoboxanes, Leukotrienes and related compounds
A. Prostaglandin E1 analog
i. Misoprostol, Gemeprost PGE1 analogue, activated EP receptor, causes Abdominal pain, Uterine cramping, teratogen, Misoprostol's intended use is for NSAID-
increased HCO3 and mucus secretion in stomach and miscarriage induced gastritis, may also be used
uterine contraction; For prevention of ulcer in together with Mifepristone or
patients who take high doses of NSAIDs due to Methotrexate as safe abortifacient
arthritis, abortifacient
ii. Alprostadil PGE1 analogue, causes vascular smooth muscle Apnea, hypotension, priapism, lightheadedness, given as injection into the cavernosa for
relaxation and vasolidation; For Maintenance of arrhythmia erectile dysfunction
patent ductus arteriosus (PDA), Erectile dysfunction

B. Prostaglandin E2 analog
i. Dinoprostone, Sulprostone Low concentrations contract, higher concentrations Cramping, Fetal trauma approved abortifacient in the 2nd
relax uterine and cervical smooth muscle, soften trimester, although effective in inducing
cervix at term before induction with oxytocin; For labor, it produces more SE than other
cervical ripening, induction of labor, abortifacient oxytocics

C. Prostaglandin F2a analog

i. Latanoprost, Arboprost, PGF2a analogue, increases outflow of aqueous vomiting, diarrhea, transient Latanoprost may cause changes in the color
Bimatoprost, Travoprost, humor thus reduces intraocular pressure; For bronchoconstriction of the iris and may lengthen eyelashes
Unoprostone glaucoma
D. Prostaglandin I2 analog
 i. Epoprostenol, Beraprost, Iloprost, PGI2 analogue, activates IP receptor, causes Hypotension, headache, flusing used primarily for pulmonary hypertension
Treprostinil vasolidation and reduces platelet aggregation; For (esp Treprostinil IV)
severe pulmonary Hypertension and reducing
platelet aggregation in dialysis machines
E. Leukotriene antagonists
i. Lipoxygenase inhibitor: Zileuton see entry on Drugs used for Asthma
ii. LT receptor blocker: Montelukast, see entry on Drugs used for Asthma
Zafirlukast
F. Corticosteroids see entry on Drugs used for Asthma
G. Non-steroidal anti-inflammatory see entry on Analgesics
drugs
Drugs used in Asthma
A. Beta2-selective agonist (short-
acting)
i. Albuterol/Salbutamol, Activates beta2-receptors in bronchial smooth Tachycardia, Nervousness, tremors, Increase toxicity when used for COPD (May
Levalbuterol, Terbutaline, muscle leading to bronchodilation ; DOC for acute restlessness, arrhythmias when used precipitate arrythmias) and in patients with
Metaproterenol, Pirbuterol, asthma attacks excessively, loss of responsiveness (tolerance, heart disease; usual DOA: 2-4hrs, all are
Procaterol, Fenoterol tachyphylaxis) given inhalational, Salbutamol and
terbutaline is also available PO, terbutaline
can also be given IV
B. Beta2-selective agonist (long acting)
ii. Salmeterol, Formoterol, Activates beta2-receptors in bronchial smooth Tachycardia, Nervousness, tremors, Increase asthma mortality when used
Cleneterol, Bambuterol muscle leading to bronchodilation, potentiates restlessness, arrhythmia when used excessively, alone; May precipitate arrhythmias; usual
corticosteroid action; For Asthma prophylaxis loss of responsiveness (tolerance, tachyphylaxis) DOA: 12hrs
C. Muscarinic receptor agonist
i. Ipratropium, Tiotropium Blocks muscarinic receptors in bronchial smooth anti-muscarinic effects (dry mouth, blurred More effective and less toxic than beta
muscle and prevent bronchoconstriction mediated by vision etc.) agonists for COPD, Tiotropium has longer
vagal discharge; For acute BA attack and COPD DOA than Ipratropium, Ipratropium given
as aerosol has little systemic effects, has no
effect on the chronic inflammation aspect
of BA
C. Methylxanthine
i. Theophylline, Aminophylline, Phosphodiesterase inhibitor, Adenosine receptor CNS stimulation (Insomnia, seizure, Anorexia), Antidote in overdosage is BB. Higher
Pentoxifylline antagonist, causes bronchodilation and increased Cardiac stimulation (Arrhythmias), Tremors, clearance in adolescents and smokers.
strength of contraction of diaphragm; For asthma increased BP, diuresis, inc GI motility Narrow therapeutic window; usual DOA:
especially in nocturnal attacks, Intermittent 12hrs
claudication (pentoxifylline), very useful in COPD

D. Mast cell Stabilizer

 i. Cromolyn, Nedocromil, Prevents calcium influx and stabilizes mast cells, Cough, Airway irritation No bronchodilator action but can prevent
Lodoxamide preventing degranulation and release of histamine, bronchoconstriction caused by antigens
leukotrienes and mediators; for Asthma prophylaxis (both in the early and late BA responses),
and allergies (oral, nasal and ophthalmic drops) unusually insoluble chemicals so rarely
used
E. Corticosteroid
i. Fluticasone, Beclomethasone, Inhibit synthesis of arachidonic acid by inhibiting Oropharyngeal candidiasis, mild growth For status asthmaticus: use IV prednisolone
Budesonide, Flunisolide, Phospholipase A2, Reduces expression of COX and retardation observed in children, Minimal or hydrocortisone ; prednisolone is the
Mometasone, Triamcinolone, LT, inc responsiveness of Beta receptors in the systemic steroid steroid toxicity (eg, adrenal active metabolite of prednisone
Ciclosenide airway, bind to intracellular receptors and activate suppression), Mild growth retardation
Glucocorticoid response elements in the nucleus
leading to synthesis of substances that prevent full
expression of inflammation and allergy ; DOC for
Asthma prophylaxis, First line treatment for
moderate to severe BA, COPD, Allergic rhinitis, also
used as anti-inflammatory for other conditions such
as auto-immune diseases and cancer, also for
immune suppression

F. Leukotriene synthesis inhibitor

i. Zileuton Inhibitor of 5-lipoxygenase. Reduces synthesis of Flulike syndrome, headache, drowsiness, No bronchodilator action, not
leukotrienes. Prevents airway inflammation and dyspepsia, hepatitis, elevation of liver enzymes recommended for acute BA attack
bronchoconstriction; For asthma prophylaxis (more than LT receptor blockers)
G. Leukotriene Antagonist
i. Montelukast, Zafirlukast, Blocks leukotriene-1 receptor, prevents airway Gastrointestinal upset, Insomnia, elevation of No bronchodilator action, not
Pranlukast inflammation and bronchoconstriction; For asthma liver enzymes recommended for acute BA attack
prophylaxis
H. Anti-IgE antibody
i. Omalizumab Binds IgE antibodies on sensitized mast cells and Long term toxicity not yet well documented humanized murine monoclonal antibody,
prevents activation by BA triggers and subsequent very expensive and only administered IV
release of inflammatory mediators; For prophylaxis
of severe, refractory asthma not responsive to all
other drugs

4. DRUGS THAT ACT ON THE CENTRAL NERVOUS SYSTEM

Sedative-Hypnotics
A. Short-acting benzodiazepines
 bind GABA-A receptor subunits to increase frequency additive CNS depression if used with
of chloride channel opening which causes membrane causes anterograde amnesia, decreased ethanol, antihistamines, antipsychotics,
hyperpolarization ; For acute anxiety, panic attacks, psychomotor skills, unwanted daytime sedation, opioids and TCAs, decreased REM sleep,
i. Midazolam, brotizolam, triazolam, anesthesia induction and preoperative sedation (esp tolerance, dependence liability and rebound use lower doses in the elderly when used
oxazepam, etizolam Midazolam), insomnia (Triazolam) insomnia or anxiety. for insomnia
B. Intermediate-acting
benzodiazepines

additive CNS depression if used with

bind GABA-A receptor subunits to increase frequency ethanol etc, decreased REM sleep, High
of chloride channel opening which causes membrane dose BZD and Barbs may suppress seizure
hyperpolarization; For anxiety disorders even panic but at the expenses of marked sedation
disorders (Alprazolam and Clonazepam), insomnia EXCEPT Clonazepam and Phenobarbital,
(Estazolam), skeletal muscle relaxation, seizure causes anterograde amnesia, decreased Lorazepam is preferred over Diazepam in
i. Lorazepam, Alprazolam, Estazolam, disorders (Clonazepam), status epilepticus psychomotor skills, unwanted daytime sedation, Status Epilepticus due to its long
Clonazepam, Lormetazepam, (Lorazepam), tranquilizers, Bipolar disorder tolerance, dependence liability and unwanted distribution halflife, use lower doses in the
Nitrazepam, Temazepam (Clonazepam), infantile spasm (Clonazepam) daytime sedation. elderly when used for insomnia
C. Long-acting Benzodiazepine

bind GABA-A receptor subunits to increase frequency

of chloride channel opening which causes membrane
hyperpolarization; For anxiety disorders, insomnia
(Flurazepam), skeletal muscle relaxation (e.g. causes anterograde amnesia, decreased additive CNS depression if used with
cerebral palsy - Diazepam), seizure disorders, psychomotor skills (esp Diazepam and ethanol etc., decreased REM sleep,
i. Diazepam, chlorazepate, tranquilizers, for status epilepticus (Diazepam), Flurazepam), unwanted daytime sedation, Flunitrazepam is used as a date-rape drug,
chlordiazepoxide, flurazepam, anesthesia (Diazepam), alcohol withdrawal tolerance, dependence liability and rebound use lower doses in the elderly when used
quazepam, flunitrazepam (Diazepam and Chlordiazepoxide) insomnia or anxiety. for insomnia
D. Benzodiazepine antagonist
agitation, confusion, and precipitates Seizures and arrhythmias may occur when
antagonist at benzodiazepine sites on GABA-A benzodiazepine withdrawal syndrome for those administered in patients who took both
i. Flumazenil receptor ; for benzodiazepine overdose. with benzodiazepine dependence. TCAs and benzodiazepines
E. Ultrashort-acting barbiturates

bind to GABA-A receptor sites (distinct from

benzodiazepines) to increase duration of chloride
channel opening, block glutamic acid additive CNS depression if used with
i. Thiopental, Methohexital, neurotransmission, at high doses can block NA dependence liability is greater than ethanol etc., CYP450 inducer, Thiopental
Thiamylal channels ; For anesthesia induction (esp Thiopental) benzodiazepine, acute intermittent porphyria. has highest lipid solubility
F. Short and intermediate-acting
barbiturates
 bind to GABA-A receptor sites (distinct from
benzodiazepines) to increase duration of chloride
channel opening, block glutamic acid
i. Pentobarbital, secobarbital, neurotransmission, at high doses can block Na
amobarbital, butalbital, butabarbital, channels ; For insomnia and preoperative sedation dependence liability is greater than additive CNS depression if used with
talbutal, aprobarbital (Secobarbital), for status epilepticus (Phenobarbital) benzodiazepine, acute intermittent porphyria. ethanol etc., CYP450 inducer
G. Long-acting barbiturate

additive CNS depression if used with

bind to GABA-A receptor sites (distinct from ethanol, CYP450 inducer, Phenobarbital
benzodiazepines) to increase duration of chloride may be excreted unchanged in the urine,
channel opening, block glutamic acid dependence liability is greater than High dose BZD and Barbs may suppress
neurotransmission, at high doses can block Na benzodiazepine, acute intermittent porphyria, seizure but at the expenses of marked
i. Phenobarbital, mephobarbital, channels ; For insomnia, seizure disorders severe respiratory and cardiovascular sedation EXCEPT Clonazepam and
primidone (Phenobarbital), status epilepticus (Phenobarbital) depression Phenobarbital
H. Imidazopyridine sedative-hypnotics
lack anti-convulsant, anti-anxiety and
muscle relaxant effects, effects are
reversed with Flumazenil, very rapid onset
of action, may dec. REM sleep, rebound inc
bind selectively to a subgroup of GABA-A receptors, on withdrawal from chronic use, increasing
acting like benzodiazepines to enhance membrane day-after psychomotor depression, few use due to rapid onset with minimal effects
hyperpolarization, only interact with GABA-A amnestic effects; tolerance, dependence liability on the sleep pattern and cause less
receptors with alpha-1 subunit ; For insomnia and and withdrawal symptoms is less than that of daytime cognitive impairment as compared
i. Zolpidem, Zaleplon, Eszopiclone sleep disorder esp. when sleep onset is delayed benzodiazepines to BZD
I. Atypical Sedative-Hypnotics
minimal abuse liability, minimal CNS
depressant effects, tolerance and
non-specific chest pain, tachycardia, withdrawal ; no anticonvulsant or muscle
partial agonist at 5-HT1A receptors and possibly D2 palpitations, dizziness, nervousness, tinnitus, GI relaxant property ; slow onset of action
i. Partial Serotonin Agonist: receptors, precise MOA of anxiolytic effect is unkown distress, paresthesias, dose-dependent pupillary (>1week), metabolized by CYP3A4, safe for
Buspirone ; For generalized anxiety disorders constriction pregnant patients
minimal rebound insomnia or withdrawal
symptoms, minimal abuse liability,
activates melatonin receptors (MT1 and MT2 metabolized by CYP450 (increased levels in
ii. Melatonin receptor agonist: receptors) in the suprachiasmatic nuclei in the CNS -- Dizziness, fatigue, decreased testosterone, the presence of CYP1A2 or CYP2D6
Ramelteon > decreased latency of sleep onset increased prolactin inhibitors
Antiseizure Drugs
CYP450 inducer , metabolism is non-linear
(elimination shift from 1st order to zero
nystagmus, diplopia, sedation, gingival order at moderate to high dose levels) ,
hyperplasia, hirsutism, anemias, peripheral Fosphenytion is a water-soluble prodrug of
block voltage-gated Na channel ; DOC for generalized neuropathy (absent DTRs), osteoporosis, fetal phenytoin ; phenytoin is preferred in
i. Phenytoin, Fosyphenytoin, tonic-clonic seizures, DOC for partial seizures, status hydantoin syndrome, abnormalities in Vit D prolonged therapy for status epilepticus
Mephenytoin, Ethotoin epilepticus, arrhythmias, migraine metabolism because it is less sedating.
 CYP450 inducer, Oxcarbazepine has less
diplopia, cognitive dysfunction, drowsiness, drug interactions, metabolism may be
block voltage-gated Na channels and decreases ataxia, blood dyscrasias, Stevens-Johnson inhibited by other drugs such as
glutamate release ; DOC for trigeminal neuralgia, syndrome, erythematous rash, teratogen (spina Propoxyphene and valproic acid ; may be
DOC for generalized tonic-clonic seizures, DOC for bifida and craniofacial anomalies), used for acute manic phase and as
ii. Carbamazepine, Oxcarbazepine partial seizures, for bipolar disorders hyponatremia (Oxcarbazepine) prophylaxis in the depressive phase

CYP450 inhibitor ; also have the same

blocks high-frequency firing of neurons which effect on Ca currents like Ethosuximide ;
modifies amino acid metabolism ; DOC for bipolar Other MOA include enhancing K channel
disorder (acute mania), DOC for generalized tonic- drowsiness, nausea, tremor, alopecia, weight permeability ; BZDs are commonly required
clonic seizures and absence seizure, partial seizures, gain, hepatotoxicity (esp in infants), neural tube at initiation therapy of valproic acid ; DOC
iii. Valproic acid myoclonic seizures, also used for Bipolar disorders defects for acute manic illness
May also act on Na channels and as
antagonist at some glutamate receptors ;
primary anticonvulsant in infants, children
iv. Phenobarbital see notes above ; For status epilepticus in children cognitive dysfunction, dependence and pregnant patients
v. Ethosuximide, Phensuximide, inhibit low threshold (T-type) Ca currents esp in GI distress, lethargy, headache and behavioural
Methsuximide thalamic neurons ; DOC for absence seizure changes. Long half-life
vi. Diazepam see entry on Sedative-Hypnotics
eliminated in the kidneys in their
unchanged form ; structural analogues of
blocks Ca++ channels, increases GABA release ; For GABA but does not activate GABA receptor
neuropathic pain such as postherpetic neuralgia, directly ; also have the same effect on Ca
vii. Gabapentin, Pregabalin partial seizures, migraine dizziness, sedation, ataxia, nystagmus, tremor currents like Ethosuximide
blocks Na and Ca++ channels and decreases
glutamate , Zonisamide only blocks Na channels ; For primarily undergoes glucuronidation
generalized tonic-clonic seizures, DOC for partial reaction ; Lamotrigine may be used for
seizures, myoclonic seizures, absence seizures, dizziness, ataxia, nausea, rash, SJS / TEN acute manic phase and as prophylaxis in
viii. Lamotrigine, Zonisamide bipolar disorder. (lamotrigine), severe skin reaction (Zonisamide) the depressive phase

Bind synaptic protein selectively inhibiting It is not metabolized by CYP450 enzymes,

hypersynchronization of epileptiform burst firing ; dizziness, sedation, weakness, irritability, eliminated in the kidneys in their
ix. Levetiracetam For generalized tonic-clonic seizures, partial seizures hallucinations, psychosis unchanged form

multiple actions on synaptic function, probably via

actions on phosphorylation (Na, Ca, GABA, AMPA- drowsiness, dizziness, ataxia, psychomotor Antiseizure drugs with the most number of
glutamate, carbonic anhydrase), Felbamate also slowing, memory impairment, paresthesias, MOA, undergo both hepatic and renal
facilitate the inhibitory actions of GABA but its exact weight loss, acute myopia, glaucoma, myopia, metabolism, Topiramate can also block Na
MOA is still unknown ; For generalized tonic-clonic urolithiasis ; felbamate causes hepatic failure channels and potentitae action of GABA
seizures, partial seizures, absence seizures, migraine ; and hematotoxic (can cause ITP, aplastic and block glutamate receptor, Felbamate
x. Topiramate, Felbamate Felbamate is only for severe refractory seizure states anemia) may also block glutamate receptors
Irreversibly inactivates GABA aminotransaminase
(GABA-T) which terminates the action of GABA ; For
xi. Vigabatrin GTC seizure visual field defects None
 Inhibits GABA transporter (GAT-1) in neurons and glia
thus inhibiting its reuptake, leading to prolongation
xii. Tiagabine of GABA effects ; For partial seizures asthenia or weakness, dizzines None
General Anesthetics
This group in general increase the threshold for
A. Inhalational General Anesthetics firing of CNS neurons
Lowest Potency (highest MAC) and least
Facilitates GABA-mediated inhibition, block brain cardiotoxic; additive CNS depression with
NMDA and Ach-N receptors; used as anesthesia for megaloblastic anemia on prolonged exposure; many agents especially opioids and
i. Nitrous Oxide minor surgery and dental procedures Euphoria (laughing gas), bronchodilation sedative-hypnotics
additive CNS depression with many agents
especially opioids and sedative-hypnotics ;
Facilitates GABA-mediated inhibition, block brain all inhaled anesthetcis cause
ii. Desflurane NMDA and Ach-N receptors ; For general anesthesia bronchospasm, peripheral vasodilation bronchodilation except Desflurane

Facilitates GABA-mediated inhibition, block brain peripheral vasodilation, renal insufficiency (due additive CNS depression with many agents
iii. Sevoflurane NMDA and Ach-N receptors; For general anesthesia to Flourine release), bronchodilation especially opioids and sedative-hypnotics

Facilitates GABA-mediated inhibition, block brain catecholamine-induced arrhythmias, peripheral additive CNS depression with many agents
iv. Isoflurane NMDA and Ach-N receptors ; For general anesthesia vasodilation, bronchodilation especially opioids and sedative-hypnotics
spike-and-wave activity in EEG, muscle
twitching, breath-holding, myocardial additive CNS depression with many agents
Facilitates GABA-mediated inhibition, block brain depression, renal insufficiency (due to Flourine especially opioids and sedative-hypnotics ;
v. Enflurane NMDA and Ach-N receptors ; For general anesthesia release), dec cardiac output, bronchodilation has pungent odor which limits its use
catecholamine-induced arrhythmias, myocardial
Facilitates GABA-mediated inhibition, block brain depression, post-operative hepatitis, dec cardiac additive CNS depression with many agents
vi. Halothane NMDA and Ach-N receptors ; For general anesthesia output, bronchodilation especially opioids and sedative-hypnotics
Highest potency and lowest MAC (very
slow onset and recovery); additive CNS
Facilitates GABA-mediated inhibition, block brain renal insufficiency (due to Flourine release), depression with many agents especially
vii. Methoxyflurane NMDA and Ach-N receptors ; For general anesthesia bronchodilation opioids and sedative-hypnotics
B. Intravenous General Anesthetics
i. Barbiturates: Thiopental, are respiratory and circulatory depressants -->
Methohexital, Thiamylal see notes above dec cerebral blood flow --> dec ICP rapid entry into the brain (<1min)
ii. Benzodiazepine: Midazolam, Midazolam is a usual adjunct with
Brotizolam, Triazolam, Oxazepam, inhalational anesthetics and IV opioids, has
Etizolam see notes above see notes above a slow onset but longer DOA

Blocks excitation by glutamate at NMDA receptors; CV stimulation, hypertension, increased ICP, Reduces delirium by pretreatment with
iii. Phencyclidine derivative: For dissociative anesthesia (analgesia, amnesia and delirium, Dissociative anesthesia, post-op benzodiazepine, congener of Phencyclidine
Ketamine catatonia but with retained consciousness) effects: disorientation, hallucination, excitation / angel dust
Modulates GABA-A receptors containing beta3 pain at injection site, myoclonus, postoperative Minimal effects on CV and respiratory
subunits; For general anesthesia to patients with nausea and vomiting, adrenocortical functions, no analgesic properties, short
iv. Imidazole derivative: Etomidate limited cardiac or respiratory reserve suppression (on prolonged administration) DOA
 Antidote is Naloxone / Naltrexone ;
Neuroleptanesthesia (analgesia + amnesia)
happens when Fentanyl, Droperidol and
Interacts with mu, sigma, kappa receptors for respiratory depression, chest wall rigidity (which Nitrous oxide are given together ; faster
v. Opioid analgesics: Fentanyl, endogenous opioid peptides ; For high risk patients may cause impaired ventilation) and recovery with remifentanil ; these drugs
morphine, alfentanil, remifentanil who might not survive general anesthesia constipation have fast onset of action
"milk of anesthesia", additive effects with
sedative-hypnotic drugs ; as rapid as
bradycardia, vasodilation, hypotension, negative thiopental and also with fast recovery ;
Potentiates GABA-A receptors, blocks Na channels; inotropism, pain at injection site, anterograde antiemetic action ; Fospropofol is the
For prolonged sedation esp in ICU patients and also amnesia, dystonia, priapism, paresthesia water-soluble prodrug form of propofol but
vi. Propofol, Fospropofol in OPD surgeries (Fospropofol) with slower onset and recovery
Local Anesthetics
this group can cause antibody formation in
A. Ester Local Anesthetics some patients
Blockade of Na channels slows which prevents axon light-headedness, sedation, restlessness,
i. Procaine potential propagation; For local anesthesia nystagmus, seizures, respiratory, CV depression Shortest half-life among local anesthetics
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia, topical light-headedness, sedation, restlessness,
ii. Benzocaine anesthesia nystagmus, seizures, respiratory, CV depression Use cautiously in sunburns, Topical only
with intrinsic sympathomimetic activity so
it does not need an alpha agonist (like
epinephrine) to limit its systemic
Blockade of Na channels slows which prevents axon light-headedness, sedation, restlessness, absorption; causes mood elevation due to
potential propagation, with intrinsic nystagmus, seizures, respiratory, CV depression, action on dopamine receptor ; All local
sympathomimetic activity; For local anesthesia, abuse liability, severe hypertension, cerebral anesthetics are vasodilators EXCEPT
iii. Cocaine topical anesthesia hemorrhage, cardiac arrhythmia, MI cocaine ; Topical only
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia, spinal
anesthesia, epidural anesthesia, topical ophthalmic light-headedness, sedation, restlessness,
iv. Tetracaine anesthesia nystagmus, seizures, respiratory, CV depression also available as Ophthalmic solution
B. Amide Local Anesthetics
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia,
antiarrhythmia (group 1B activity), used for post-MI light-headedness, sedation, restlessness, Frequently administered with Epinephrine
i. Lidocaine and for digitalis toxicity nystagmus, seizures, respiratory, CV depression to avoid systemic absorption
Blockade of Na channels slows which prevents axon
potential propagation; For local anesthesia, dental light-headedness, sedation, restlessness, causes methemoglobinemia (antidote:
ii. Prilocaine anesthesia nystagmus, seizures, respiratory, CV depression methylene blue)
Blockade of Na channels slows which prevents axon light-headedness, sedation, restlessness, Use with caution in pregnant women and
potential propagation; For local anesthesia, epidural nystagmus, seizures, respiratory, CV depression, patients with cardiac disease (may cause
iii. Bupivacaine anesthesia, intrathecal anesthesia severe CV toxicity, hypotension and arrhythmias heartblock, arrhyhtmia and hypotension)
Blockade of Na channels slows which prevents axon light-headedness, sedation, restlessness,
potential propagation; For local anesthesia, epidural nystagmus, seizures, respiratory, CV depression,
iv. Ropivacaine anesthesia cardiotoxicity Longest half-life among local anesthesia
Skeletal Muscle Relaxant
A. Depolarizing Neuromuscular
Blocker
muscle pain, hyperkalemia, increased
Agonist at Ach-N receptors causing initial twitch then intragastric pressure leading to regurgitation Metabolized by pseudocholinesterase ;
persistent depolarization ; For skeletal muscle (aspiration), increased intraocular pressure, may cause malignant hyperthermia if given
i. Succinylcholine relaxation during intubation and general anesthesia malignant hyperthermia together with inhaled anesthetics
B. Non-Depolarizing Neuromuscular effects are easily reversed by giving AChE
Blocker a common SE for this group is Histamine release inhibitors such as Neostigmine
Competitive antagonists at skeletal muscle nicotinic
i. Mivacurium (short-acting: 10- acetylcholine receptors; For skeletal muscle respiratory paralysis, apnea, and moderate Metabolized by pseudocholinesterase;
20mins DOA) relaxation during intubation and general anesthesia histamine release reverse effects with Neostigmine
Undergoes Hoffman elimination (rapid
spontaneous breakdown); reverse effects
respiratory paralysis, apnea, and moderate with Neostigmine ; converted to
ii. Atracurium (intermediate-acting) histamine release and bronchospasm Laudanosine which can cause seizures
Undergoes elimination in bile; reverse
iii. Vecuronium (intermediate-acting) respiratory paralysis and apnea effects with Neostigmine
reverse effects with Neostigmine;
Suggamadex is a novel reversal agent for
rocuronium; most rapid onset time (60-120
iv. Rocuronium (intermediate-acting) respiratory paralysis and apnea, hypersensitivity sec)
respiratory paralysis, apnea, hypotension and Relatively contraindicated in myocardial
v. Tubocurarine (long-acting) recurarization ischemia; reverse effects with neostigmine

Competitive antagonists at skeletal muscle nicotinic

acetylcholine receptors; For skeletal muscle
relaxation during intubation and general anesthesia, respiratory paralysis, apnea, tachycardia, Reverse effects with Neostigmine, may
vi. Pancuronium (long-acting) euthanasia, lethal injection, strychnine poisoning hypertension, recurarization cause heart block
Anti-Parkinsonism and other drugs for movement disorders
A. Dopamine Precursor
Contraindicated in patients with history of
psychosis; hypertensive crisis occurs when
GI upset (emesis), dyskinesia (choreoathetosis), used with MAO inhibitors, ameliorates
behavioural changes (anxiety, agitation, signs of parkinsonism and decreases
Levodopa is a dopamine precursor, carbidopa inhibits confusion, delusion), on-off phenomena, mortality rate ; patient response decreases
peripheral metabolism via dopa decarboxylase; Drug wearing-off phenomena, postural hypotension, with time but is improved when given
i. Levodopa-carbidopa of choice for parkinson’s disease tachycardia together with COMT inhibitors
B. Dopamine Agonist
anorexia, nausea, vomiting, dyskinesia, postural
Partial agonist at dopamine D2 receptors in brain; For hypotension, behavioural changes,
Parkinson’s disease which is levodopa intolerance, erythromelalgia (Bromocriptine), pulmonary
i. Bromocriptine, Pergolide hyperprolactinemia infiltrate (Bromocriptine) Ergot alkaloids
 Contraindicated for patients with active
peptic ulcer disease, psychotic illnesss or
anorexia, nausea, vomiting, dyskinesia, postural recent MI ; decrease dose in renal
Partial agonist at dopamine D3 receptors in brain, hypotension, behavioural changes (more dysfunction ; Neuroprotective ; Ropirinole
ii. Pramipexole, Ropinirole Roprinole is a D2 agonist; For Parkinson’s disease prominent compared to levodopa) is metabolized by CYP1A2

Partial agonist at dopamine D3 receptors, antagonist

at 5-HT and alpha adrenoceptors; For off-periods of
Parkinson’s disease, alcoholism, opiate addiction, severe nausea, dyskinesia, hypotension, Premedicate with Trimethobenzamide to
iii. Apomorphine erectile dysfunction, alzheimer’s disease drowsiness and sweating prevent severe nausea
C. MAO type B inhibitor
Selective inhibitors of MAO type B leading to serotonin syndrome occurs when used with
decreased degradation of dopamine, increases SSRI and Meperidine ; Selegiline is
response to levodopa/carbidopa; Only as adjunct to hepatically metabolized into desmethyl
levodopa for parkinson’s disease but Rasigiline can insomnia, mood changes, dyskinesias, GI selegiline (which is neuroprotective) and
i. Selegiline, Rasagiline be given alone (more potent) distress and hypotension amphetamine
D. COMT inhibitor
Block L-dopa metabolism by inhibiting catechol-O-
methyltransferase in periphery and CNS, prolongs dyskinesias, GI distress, postural hypotension,
response to levodopa; used in the wearing-off sleep disturbance, orange discoloration of urine, Entacapone only acts in the periphery while
phenomena of parkinson’s disease, as adjuncts to hepatotoxicity (tolcapone only), neuroleptic Tolcapone acts both in the periphery and
i. Entacapone, Tolcapone levodopa malignant syndrome, rhabdomyolysis CNS.
E. Antiviral
enhances dopaminergic transmission by unknown behavioural changes (restlessness, agitation,
mechanism, maybe by influencing the synthesis, insomnia, hallucination, psychosis), livedo
release or reuptake of dopamine; For Parkinson’s reticularis, GI disturbances, urinary retention, May improve bradykinesia, rigidity and
i. Amantadine disease and influenza postural hypotension, peripheral edema tremor ; has antimuscarinic action
F. Anticholinergic
Decrease the excitatory actions of cholinergic
neurons on cells in the striatum by blocking Exacerbate tardive dyskinesias that result
muscarinic receptors; as adjunct for parkinson’s from prolonged use of antipsychotic drugs;
i. Benztropine, Biperiden, disease and extrapyramidal symptoms caused by drowsiness, inattention, confusion, delusions, improve tremor and rigidity with little
Trihexyphenidyl, Orphenadrine antipsychotics hallucinations, atropine-like effects effect on bradykinesia
Antipsychotics and Lithium
A. Typical Antipsyhotics may also be used for pruritus and as sedatives has no effect on negative symptoms
extrapyramidal dysfunction, tardive dyskinesia,
hyperprolactinemia, atropine-like effects, failure
of ejaculation, postural hypotension, marked
Blocks D2 receptors >> 5-HT2 receptors; For sedation, corneal and lens deposits, neuroleptic
i. Phenothiazine: Chlorpromazine schizophrenia and other psychotic disorders malignant syndrome, contact dermatitis prototype of all typical antipsychotics
 Thioridazine has the Strongest autonomic
effects; only antipsychotic with fatal
extrapyramidal dysfunction, tardive dyskinesia, overdose ; Fluphenazine and
ii. Other Phenothiazines: hyperprolactinemia, atropine-like effects, failure Trifluoperazine have very significant
Thioridazine, Fluphenazine, Blocks D2 receptors >> 5-HT2 receptors; For of ejaculation, postural hypotension, retinal parkinson-like effect ; Fluphenazine has
Perphenazine, Prochlorperazine, schizophrenia and other psychotic disorders, deposits (thioridazine), cardiotoxicity less sedation compared to other anti-
Trifluoperazine antiemesis (prochlorperazine) (arrhythmias - thioridazine) psychotics
Blocks D2 receptors >> 5-HT2 receptors; For extrapyramidal dysfunction, tardive dyskinesia, causes the most extrapyramidal symptoms
iii. Butyrophenol: Haloperidol, schizophrenia and other psychotic disorders, hyperprolactinemia, neuroleptic malignant of all typical anti-psychotics ; has the
Droperidol huntington’s disease and tourette’s syndrome syndrome weakest autonomic effects
may be used for mania and psychotic symptoms in
B. Atypical Antipsychotics Alzheimer's dementia and Parkinsons disease cure both negative and positive symptoms
Extrapyramidal dysfunction (less),
hyperprolactinemia (less), postural hypotension, Only antipsychotic that reduces the risk of
Blocks 5-HT2 receptors >> D2 receptors; For weight gain, hyperglycemia, hyperlipidemia, suicide ; may be effective for drug-resistant
schizophrenia (refractory, suicidal) and other myocarditis, agranulocytosis, seizures, ileus, types ; weight gain, agranulocytosis, seizure
i. Clozapine psychotic disorders hypersalivation (sialorrhea) and hyperglycemia is prominent
Blocks 5-HT2 receptors >> D2 receptors; For Extrapyramidal dysfunction (less),
schizophrenia, bipolar disorders, anorexia nervosa hyperprolactinemia (less), postural hypotension, weight gain and hyperglycemia is
ii. Olanzapine and depression weight gain, hyperglycemia, hyperlipidemia prominent, safe in pregnancy
Extrapyramidal dysfunction (less),
hyperprolactinemia (less), postural hypotension,
weight gain, somnolence, fatigue, sleep
Blocks 5-HT2 receptors >> D2 receptors; For paralysis, hypnagogic hallucinations, cataracts,
iii. Quetiapine schizophrenia, bipolar disorders (manic) priapism, QT prolongation (TDP) can cause TDP, safe in pregnancy
Blocks 5-HT2 receptors >> D2 receptors; For Extrapyramidal dysfunction (less),
schizophrenia, bipolar disorders, depression, hyperprolactinemia (marked), insomnia, Only antipsychotic approved for
iv. Risperidone intractable hiccups, tourette syndrome photosensitivity schizophrenia in the youth
Blocks 5-HT2 receptors >> D2 receptors; For Extrapyramidal dysfunction (less), postural Increased mortality in elderly patients with
v. Ziprasidone schizophrenia, bipolar disorders (acute mania) hypotension, QT prolongation (TDP) dementia-related psychosis ; can cause TDP
Blocks 5-HT2 receptors >> D2 receptors; For
schizophrenia, bipolar disorders, depression, autism, Extrapyramidal dysfunction (less), GI upset,
vi. Aripiprazole cocaine dependence tremor, hypersensitivity (rare) Least sedating atypical antipsychotics
Contraindicated in sick sinus syndrome;
Tremor, sedation, ataxia, aphasia, thyroid treat overdose with hemodialysis ; high
Uncertain MOA but the proposed MOA is by enlargement, hypothyroidism, reversible volume of distribution ; clinical benefit is
inhibiting the enzyme involved in the recycling of nephrogenic diabetes insipidus, edema, seen only after weeks of use ;
neuronal membrane phosphoinositides which causes acneiform skin eruption, leukocytosis, teratogen antipsychotic agents or BZDs are commonly
depletion of phosphatidylinositol bisphosphate, thus (ebstein’s anomaly), bradycardia, some drugs required at initiation therapy of Li and
consequently decreasing IP3 and DAG --> decrease in (NSAIDs, ACEi, diuretis etc) can increase Lithium valproic acid ; Contraindicated in lactation ;
neurotransmission ; For bipolar disorder, recurrent toxicity while caffeine and theophylline can Natriuresis stimulates reflex increase in the
vii. Lithium (mood stabilizer) depression, schizoaffective disorder decrease its toxicity reabsorption of Li and Na in the PCT
Antidepressants
A. Tricyclic Antidepressants
 Additive depression of the CNS with other
central depressants ; Imipramine is
metabolized to desipramine while
amitriptyline is metabolized to nortriptyline
Block NE and 5-HT transporters leading to ; longterm use may lead to down-
potentiation of NT action at postsynaptic receptors; excessive sedation, fatigue, confusion, regulation of Beta receptors leading to a
For MDD (most effective), bipolar disorder, acute sympathomimetic effects, atropine-like effects, decrease in BP and depression of cardiac
panic attacks, ADHD, chronic pain states, as sleeping orthostatic hypotension, cardiomyopathies, conduction ; has significant muscarinic
i. Imipramine, Clomipramine, aid, OCD (Clomipramine) ; this group is very useful arrhythmias, tremors, paresthesias, weight gain receptor blocking effect esp Amitriptyline ;
Desipramine, Amitryptyline, for patients with psychomotor retardation, sleep ; 3Cs of overdose: Coma, Cardiotoxicity, lower seizure threshold ; may interfere
Nortryptiline disturbance, poor appetite and weight loss Convulsions with antihypertensive action of Clonidine
B. SSRI
Serotonin syndrome when used with
MAOIs ; minimal inhibitory effect on
cholinergic or adrenergic receptors ; lower
Inhibits neuronal reuptake of serotonin by inhibiting seizure threshold ; this group can decrease
Serotonin Transporter (SERT); DOC for OCD, for MDD, nausea, vomiting, headache, anxiety, agitation, appetite leading to weight loss ; Increased
anxiety, panic attacks, phobias, PTSD, GAD, bulimia, drowsiness, insomnia, erectile dysfunction, EPS, risk for suicide in children and adolescents ;
i. Fluoxetine, Paroxetine, Citalopram, premenstrual dysphoric disorder, alcohol QT prolongation (citalopram), withdrawal Fluoxetine, Fluvoxamine and Paroxetine
Escitalopram, Sertraline, Fluvoxamine dependence syndrome are CYP450 inhibitors
C. SNRI
venlafaxine has less affinity for NE
dizziness, insomnia, sedation, GI distress, transporter than desvenlafaxine and
Inhibits neuronal reuptake of serotonin and hypertension (venlafaxine), hepatotoxicity duloxetine ; differ from TCA in lacking
norepinephrine by binding to transporters for both (duloxetine), withdrawal syndrome even in just blockade of H1, M and alpha receptors ;
i. Venlafaxine, Duloxetine, 5HT and NE; For MDD, fibromyalgia, neuropathic one missed dose, CNS stimulation (Venlafaxine), Increased risk for suicide in children and
Desvenlafaxine pain, menopausal symptoms liver dysfunction (Duloxetine) adolescents
D. Serotonin antagonist
May cause arrhythmias in px with pre-
existing cardiac disease ; short t1/2 so
given BID to TID, has significant muscarinic
Blocks 5-HT2A receptors, weak inhibitor of NE and sedation, GI disturbance, orthostatic receptor blocking effect esp Nefazodone ;
5HT transporters; For MDD, as sleeping aid hypotension, priapism, hyperprolactinemia, liver CYP450 inhibitors ; Trazodone also has
i. Trazodone, Nefazodone (trazodone) dysfunction (nefazodone) significant alpha1 and H1 blocking effect
Increased risk for suicide in children and
E. Tetracyclics adolescents
Strong norepinephrine reuptake inhibitor and weak autonomic effects, akathisia, parkinsonism (due
serotonin reuptake inhibitor, blocks dopamine D2 to dopamine receptor blockade), seizures, Lowers seizure threshold, has significant
i. Amoxapine receptors; For MDD cardiotoxicity muscarinic receptor blocking effect
Increases amine release from nerve endings by
antagonism of presynaptic a2 adrenoceptors, also
blocks serotonin 5-HT2A receptors; For MDD, weight gain, marked sedation, dizziness, blurred has significant muscarinic receptor and
ii. Mirtazapine appetite stimulation, as sleeping aid vision and nightmares alpha2 blocking effect
 Inhibits neuronal reuptake of dopamine and Lowers seizure threshold, for smoking
norepinephrine, increase dopamine and weight loss, agitation, anxiety, dizziness, dry cessation ; no effect on 5HT or NE
norepinephrine activity; For MDD and smoking mouth, aggravation of psychosis, seizures, receptors or amine transporters ; CYP450
iii. Bupropion cessation, alcohol dependence priapism inhibitor
F. MAO Inhibitors
Hypertensive crisis when taken with
tyramine-rich food, serotonin syndrome
Inhibits MAO type A and type B, increases CNS levels when taken with SSRI ; this group is
of NE and serotonin, Phenelzine and structurally related to amphetamine ;
Tranylcypromine are nonselective MAO inhibitors CYP450 inhibitors ; longterm use may lead
while Selegiline is a MAO-B selective inhibitor; For to down-regulation of Beta receptors
MDD unresponsive to other agents ; useful in dizziness, insomnia, orthostatic hypotension, (leading to decrase in BP) ; lower seizure
i. Phenelzine, tranylcypromine, patients with significant anxiety, phobic features and blurred vision, arrhythmia, diarrhea, threshold ; selegiline may be given as skin
selegiline hypochondriasis hyperthermia, CNS stimulation, seizure patch
Opioid Analgesics and Antagonists
Additive CNS depression with other
A. Full Agonist TRIAD: miosis, coma, respiratory depression depressants
Exerts hemodynamic effects on the
pulmonary circulation ; significant first-pass
miosis, restlessness, respiratory depression, effect ; metabolized in the body to
Strong agonist at u receptors; For severe pain, pain increased ICP, postural hypotension, urinary morphine-6-glucuronide which has equal
i. Morphine associated with acute MI, for pulmonary edema retention, pruritus, addiction liability analgesic activity as morphine
Strong agonist at u receptors; For severe pain, restlessness, respiratory depression, increased
adjunct in anesthesia, chronic pain and breakthrough ICP, postural hypotension, urinary retention, May be given transdermally or via lollipop;
ii. Fentanyl cancer pain pruritus, addiction liability ohmefentanyl is the most potent opioid
Only opioid that does not cause miosis and
biliary contraction ; opioid of choice for
pain relief in pancreatitis ; metabolized to
normeperidine which can cause seizure
Strong agonist at u and k receptors, inhibits pain therefore contraindicated in patients with
neurotransmission, muscarinic blocking actions; For restlessness, respiratory depression, increased seizure disorder ; if given with MAOi -->
moderate to severe pain, labor analgesia, spasmodic ICP, postural hypotension, urinary retention, Hyperpyrexic coma, if given with SSRI -->
iii. Meperidine pain (biliary, renal), preoperative sedation pruritus, addiction liability, seizures Serotonin syndrome
Strong agonist at u receptors, inhibits pain
neurotransmission, binds NMDA receptors and Used in methadone maintenance therapy
antagonizes the effects of glutamate; For moderate miosis, restlessness, respiratory depression, (MMT) for opioid dependence; currently
to severe pain, opioid dependence, opioid increased ICP, postural hypotension, urinary being investigated as a novel treatment for
iv. Methadone withdrawal retention, pruritus, addiction liability leukemia
B. Partial Agonist / Moderate Agonist
Strong agonist at u receptors, inhibits pain
neurotransmission, binds NMDA receptors and
antagonises the effects of glutamate; For moderate miosis, restlessness, respiratory depression,
to severe pain, opioid dependence, opioid increased ICP, postural hypotension, urinary there is genetic variation in the metabolism
i. Hydrocodone, oxycodone withdrawal retention, pruritus, addiction liability of codeine and its derivatives
 Decreases sensitivity of cough receptors, depressing hallucination, confusion, excitation, increased or
the medullary cough center through sigma receptors decreased pupil size, nystagmus, seizures, coma, codeine is metabolized by CYP2D6 to
ii. Dextrometorphan, codeine stimulation; For cough suppression respiratory depression, addiction liability morphine
C. Weak Agonist
Weak agonist at u receptors, inhibits pain miosis, respiratory depression, increased ICP,
i. Propoxyphene, levopropoxyphene, neurotransmission; For mild to moderate pain, postural hypotension, urinary retention,
dextropropoxyphene restless leg syndrome pruritus, addiction liability, fatal arrythmias Withdrawn because of fatal cardiotoxicity
D. Mixed Agonist-Antagonist
Strong agonist at k receptors, weak antagonist
activity at u receptors; For moderate to severe pain, sedation, dizziness, sweating, nausea, anxiety,
opioid dependence, alcohol dependence, balance hallucinations, nightmares, respiratory Buprenorphine reduces craving in alcohol
i. Nalbuphine, buprenorphine, anesthesia, for opioid withdrawal states depression (less), tolerance, dependence dependence, buprenorphine and
butorphanol, pentazocine (buprenorphine) liability nalbuphine is resistant to Naloxone
E. Opioid Antagonist
Competitively blocks u, sigma and k receptors, Precipitates abstinence syndrome in Px
rapidly reverses effects of opioid agonists; For opioid with opioid dependence ; Naloxone and
overdose, opioid and alcohol dependence Nalmefene is IV (DOA: 12-24 hrs) while
i. Naloxone, naltrexone, nalmefene (naltrexone) pruritus, nausea, vomiting Naltrexone is PO (DOA: 48h)
F. Dual-acting
Weak agonist at u receptors, inhibits neuronal
reuptake of serotonin and norepinephrine; For
moderate pain, chronic pain syndrome, neuropathic seizures, nausea, dizziness, pruritus, Lower seizure threshold ; CI in Px taking
i. Tramadol pain constipation SSRI and those with history of seizure

5. DRUGS USED TO TREAT DISEASES OF THE BLOOD, INFLAMMATION, & GOUT

Agents Used in Anemias and Hematopoietic Growth Factors
A. Hematopoietic growth factor
i. Ferrous sulfate, Ferrous gluconate, Required for the biosynthesis of heme and heme Black stools, shock, lethargy, dyspnea,
Ferrous Fumarate, Iron dextran, containing proteins, including hemoglobin and abdominal pain, necrotizing gastroenteritis,
Sodium Ferric Gluconate complex, myoglobin; For Iron deficiency anmia, iron death, organ failure, hemochromatosis,
Iron sucrose supplementation metabolic acidosis None
B. Heavy metal chelator
Chelates excess iron; For acute and chronic iron Hypotension, Neurotoxicity, ARDS, Increased
i. Deferoxamine, Deferasirox poisoning susceptibility to infections None
C. Hematopoietic growth factor
 Cofactor required for essential enzymatic reactions
that form tetrahydrofolate, convert homocysteine to Hydroxocobalamin has a longer t1/2 than
i. Cyanocobalamin, methionine and metabolize methylmalonyl-CoA; For cyanocobalamin ; has a storage of up to
Hydroxocobalamin vitamin B12 deficiency, megaloblastic anemia No significant toxicity 5yrs in the liver
D. Hematopoietic growth factor
Precursor of an essential donor of methyl groups
used for synthesis of amino acids, purines and
deoxynucleotide; For Megaloblastic anemia,
i. Folic acid, Folacin (Pteroylglutamic prevention of neutral tube defects (spina bifida), only modest amounts are stored in the
acid), Folinic acid prevention of coronary artery disease No significant toxicity body
E. Hematopoietic growth factor
Performance-enhancing drug in athletes ;
darbepoietin is once a week
i. Epoetin Alfa, Darbepoetin alfa, Agonist of erythropoietin receptors expressed by red administration, while Methoxy
Methoxy Polyethylene Glycol- Epoetin cell progenitors; For Anemia, associated with chronic Polyethylene Glycol- Epoetin Beta is 1-2x
Beta renal failure, cancer, HIV infection and prematurity Hypertension, Thrombosis, Pure red cell aplasia per month administration
F. Myeloid growth factor

Binds receptors on myeloid progenitors and

stimulates cell maturation and proliferation ;
Accelerates neutrophil recovery and reduces
incidence of infection; For neutropenia associated
i. (G-CSF) Filgrastim, Sargamostim with chemotherapy, myelodysplasia, and aplastic
(GM-CSF), Pegfilgrastim anemia Edema, Fever, Arthralgia Pegfilgrastim has longer t1/2
G. Megakaryocyte growth factor
Recombinant form of an endogenous cytokine;
activates IL -11 receptors ; For secondary prevention
of thrombocytopenia in patients undergoing fatigue, headache, anemia, fluid accumulation in
i. Oprelvekin(IL-11), Thrombopoietin chemotheraphy the lungs, dizziness, transient atrialarrythmias given SC OD
Agents Used in Dyslipidemia
has direct anti-atherosclerotic effect, and
can prevent bone loss ; Increased risk of
myopathy and rhabdomyolysis when used
with fibrates ; Given before bedtime
because cholesterol synthesis
predominantly occurs at night ; simvastatin
and lovastatin are prodrugs, all the rest are
in their active form already ; Rosuvastatin,
Inhibits rate-limiting enzyme in cholesterol Atorvastatin and Simvastatin have greater
biosynthesis (HMG-CoA reductase), Increased maximal effect than other statins ; if given
A. HMG-CoA Reductase Inhibitors: hepatic cholesterol uptake, Increased high affinity together with resins give at least 1hr before
Simvastatin, Atorvastatin, LDL receptors which leads to decreased LDL levels ; or 4hrs after resin administration (resins
Rosuvastatin, Fluvastatin, Pravastatin, DOC for hypercholesterolemia (high LDL), decreases Hepatoxicity, Myopathy, Rhabdomyolysis, decrease the absorption of statins) ; has
Lovastatin, Pitavastatin, Cerivastatin, risk of acute coronary syndromes, ischemic stroke Gastrointestinal distress, Teratogen CYP450 dependent metabolism
 non-absorbable polymers that bind bile acids and
similar steroids in the intestines preventing their
reabsorption, increases cholesterol utilization for Increases TGs and VLDL in patients with
replacement, modestly lowers LDL levels by high TGs and combined hyperlipidemia ;
B. Bile Acid Binding Resin: increasing hepatic LDL receptors ; For Constipation, Bloating, Gritty taste, Gallstone Treat constipation with fiber
Colesevelam, Colestipol, hypercholesterolemia (high LDL), pruritus in formation, steatorrhea, malabsortion of fat supplements/psyllium ; Avoid in patients
Cholestyramine cholestasis, digitalis toxicity soluble substances (vitamin k, folate) with diverticulitis

Selective inhibitor of the NPC1L1 transporter

decreasing intestinal absorption of cholesterol and
other phytosterols, decreases cholesterol hepatic
C. NPC1L1 transporter inhibitor: pool, increases hepatic LDL receptors ; For Hepatoxicity (increased with statin use), Synergistic LDL-lowering effect with statins
Ezetimibe Hypercholesterolemia (High LDL), phytosterolemia Myositis ; is a prodrug

Cholesterol analog, takes the place of dietary and

billiary cholesterol, decreasing intestinal absorption
of cholesterol and other phytosterols ; For Gastrointestinal upset, bloating, impotence
D. Sterol absorption blocker: Sitosterol Hypercholesterolemia (high LDL), phytosterolemia (rare), coronary events NONE

Decreases VLDL synthesis and LDL cholesterol

concentrations, decreases hormone-sensitive lipase decreases fibrinogen and increases t-PA ;
activity leading to decreased LDL levels, Increases Flushing, nausea, vomiting, Pruritus, Acanthosis NSAIDs pre-treatment reduces flushing ;
HDL cholesterol by decreasing its catabolism ; DOC nigricans, Rashes, Gastrointestinal irritation, Avoid in patients with peptic ulcer disease ;
for increasing HDL levels, for Hypercholesterolemia Hepatoxicity (mild), Hyperuricemia, Impaired Potentiates effects of antihypertensives
E. Nicotinic Acid derivatives: Niacin (low HDL, high LDL/VLDL), hypertriglyceridemia glucose tolerance, Arrhythmias, Ambylopia (vasodilators, ganglion blockers)
Increased risk of myopathy and
rhabdomyolysis when used with statins ;
Avoided in patients with hepatic or renal
Activates PPAR-α and increases expression of dysfunction ; may increase LDL in patients
lipoprotein lipase and apolipoproteins (apoA-I, apoA- with familial combined
II) leading to enhanced clearance of TG-rich hyperlipoproteinemia ; has little or no
F. Fibrates: Gemfibrozil, Fenofibrate, lipoproteins, Lowers triglycerides, Increases HDL ; Nausea, Rashes, Leukopenia, nausea, vomiting, effect on LDL ; higher risk of gallstone
Bezafibrate DOC for hypertriglyceridemia increased risk of cholesterol gallstones formation if given together with resins
Drugs for Coagulation
A. Antiplatelet For arterial thrombosis only

Nonselective, irreversible COX 1&2 inhibitor. Reduces

platelet production of thromboxane A2, temporarily
inhibit Prostacyclin synthesis ; For prevention or Gastrointestinal toxicity, nephrotoxicity,
arterial thrombosis (MI, TIA, CVD), Inflammatory tinnitus, hyperventilation, hypersensitivity, Uncoupler of oxidative phosphorylation,
disorders (rheumatic fever, juvenile rheumatoid HAGMA, Increased bleeding time, associated with Reye syndrome in children
i. Aspirin arthritis, kawasaki disease) Nephrotoxicity (AKI and Interstitial Nephritis) ; Do not use as NSAID for gout
 Reversbily inhibits the binding of fibrin and other
ligands to the platelet GPIIb-IIIa receptor ; For
ii. GPIIb-IIIa inhibitor: Abciximab, antithrombosis during PCI, Acute coronary
Eptifibatide,Tirofiban syndromes (unstable angina, NSTEMI) Bleeding, Thrombocytopenia Adjunct to thrombolysis

Inhibits phosphodiesterase III and increases cAMP in

platelets and blood vessels, Inhibits platelet
aggregation and causes vasolidation ; For prevention additional MOA: inhibit uptake of
of thromboembolic complications of cardiac valve adenosine by endothelial cells and RBC,
replacement (as adjunct to warfarin), secondary thus increasing adenosine levels leading to
iii. PDE III inhibitor: Dipyridamole, prevention of ischemic stroke (with aspirin), inhibition of platelet aggregation ;
Cilostazol Intermittent claudication (Cilostazol only) Headache, palpitations Cilostazol is contraindicated in heart failure
Irreversibly inhibits binding of ADP to platelet
receptors,thus reducing platelet aggregation ; For
prevention and treatment of arterial thrombosis Bleeding, nausea, hematologic (neutropenia, GI & Hematologic SE are more common
iv. ADP inhibitor: (stroke, TIA, unstable angina), Acute coronary leukopenia), thrombotic thrombocytopenic with ticlopidine. Additive effects with
Clopidogrel,Ticlopidine, Prasugel syndromes, Prevention of re-stenosis after PCI purpura (Ticlopidine), dyspepsia aspirin
B. Anticoagulant For both venous and arterial thrombosis

Activates antithrombin III which Inactivates thrombin

or factor IIa, factor IXa & factor Xa by forming stable
complexes with them ; For deep venous thrombosis,
myocardial dysfunction, Pulmonary embolism,
adjuvant to percutaneous coronary intervention (PCI)
and thrombolytics, Atrial fibrillation, Pulmonary
embolism, given with thrombolytics for Bleeding, transient Heparin-induced DOC for anticoagulation during pregnancy ;
i. Heparin (indirect thrombin revascularization procedures, given with GPIIb-IIIa thrombocytopenia, Osteoporosis with chronic administered IV or SC ; Monitor with aPTT,
inhibitor) inhibitors for angioplasty and stent placement use Antidote: Protamine Sulfate

Binds and potentiates effect of antithrombin III on

factor Xa (more selective for Xa); For Deep venous Does not require aPTT monitoring,
thrombosis, Pulmonary embolism, unstable angina, Protamine sulfate is only partially effective
myocardial infarction, adjuvant to percutaneous in reversing effects ; advantage over
ii. LMWH: Enoxaparin, Dalteparin, coronary intervention (PCI) and thrombolytics, Atrial regular heparin is higher bioavailability and
Tinzaparin, Fondaparinux fibrillation Bleeding, less risk of thrombocytopenia t1/2 ; Fondaparinux is given SC OD
Binds to thrombin's ative site and inhibits its
enzymatic action; For anticoagulation in patients Monitor with aPTT. No reversal agents exist
iii. Direct Thrombin Inhibitors: with heparin induced thrombocytopenia (HIT), ; Dabigatran is PO while all the rest are
Lepirudin, Desirudin, Bivalirudin, percutaneous coronary angioplasty (Bivalirudin with Bleeding, Anaphylactic reactions, Effect- parenteral ; Bivalirudin also inhibits platelet
Argatroban, Dabigatran aspirin) prolonging antibodies activation

iv. Direct Oral Factor Xa inhibitor: bind to free and bound factor Xa ; For prevention of
Rivaroxaban, Apixaban Venous thrombosis, in stroke patients with Afib bleeding No reversal agent
 Inhibits vitamin K epoxide reductase (responsible for
y-carboxylation of the vitamin K- dependent clotting
(factors II, VII, IX, X, Protein C & Protein S) ; For Bleeding, Teratogen (bone defects, Monitor effects with PT-INR. Antidote is
chronic anticoagulation (DVT, atrial fibrillation, valve hemorrhage), warfarin-induced skin necrosis vitamin K or FFP. Narrow therapeutic
v. Warfarin, Dicumarol replacement) EXCEPT in pregnancy (transient hypercoagulability) window ; 99% protein-bound
C. Antidote
Chemical antagonist of heparin. Reverses excessive
anticlotting activity of unfractionated heparin; For hypotension, flushing, bradycardia, dyspnea,
i. Protamine Sulfate heparin overdosage hypersensitivity Partially reverses effect of LMWHs

Increases supply of reduced vitamin K, which is

required for synthesis of functional vitamin K-
ii. Endogenous Vitamin: Vitamin K1, dependent clotting and anticlotting factors ; For
K2, K3 (Phytonadione, Menaquinone, Vitamin K deficiency, Antidote to warfarin, Severe infusion reaction when administered at a
Menadione) prevention of hemorrhagic diatheses in newborns fast rate (dyspnea, chest and back pain) Vit K1 may be given PO or IV
Tx should be done within 6 hrs, better if
within 3hrs ; Antidote is AMINOCAPROIC
Tissue plasminogen activator analog. Converts ACID ; Streptokinase forms a complex with
D. Thrombolytic: Alteplase, plasminogen to plasmin, which degrades the fibrin endogenous plasminogen, thus catalyzing
Anistreplase, Reteplase, and fibrinogen, causing thrombolysis ; For acute Bleeding, Reperfusion, Cerebral hemorrhage, the conversion of plasminogen to plasmin ;
Streptokinase, Tenecteplase, myocardial infarction, pulmonary embolism, Ischemic Arrhythmias ; Loss of effectiveness (on 2nd use) tPA is selective for fibrin-bound
Urokinase stroke and allergic reactions (streptokinase) plasminogen

Competitively inhibits plasminogen activation thus

inhibiting fibrinolysis ; For prevention and treatment
of acute bleeding episodes in patients with high risk Contraindicated in disseminated
of bleeding (hemophilia, intracranial aneurysms, intravascualr coagulation (DIC) and
E. Antiplasmin drug: Tranexamic acid menstrual, obstetrics, thrombolytics, postperative) Thrombosis, hypotension, Myopathy, Diarrhea genitourinary bleeding
Vasopressin V2 receptor agonist, Increases factor VIII
activity of patients with mild hemophilia A or VWD;
For hemophillia A, von Willebrand's disease, central headaches, nausea, flushing, seizures, may cause immunologic reactions and
F. ADH agonist: Desmopressin diabetes insipidus hyponatremia infections
Non-steroidal Anti-Inflammatory Drugs, Disease-Modifying Anti-rheumatic Drugs, Non-opioid Analgesics & Drugs Used in Gout
A.Non-selective NSAID
low doses undergo first order kinetics while
high doses undergo zero order reaction ;
Long term use reduces the risk of colon
i. Aspirin, Sodium Salicylate See entry on Drugs for caogulation Disorder See entry on Drugs for caogulation Disorder cancer
 Ibuprofen and Indomethacin can be used
to close PDA ; Ibuprofen and naproxen
have moderate effectiveness ; Ibuprofen is
relatively safe but with short half-life of
ii. Ibuprofen, Diclofenac, Diflunisal, 2hrs ; Naproxen and Piroxicam have longer
Etodolac, Fenoprofen, Flurbiprofen, half-lives ; Ketorolac has significant
Ketoprofen, Meloxicam, Nabumetone, analgesic effect but not anti-inflammatory
Naproxen, Oxaprozin, Piroxicam, Nonselective reversible COX-1 and COX-2 inhibitor. Gastrointestinal bleeding (less than aspirin), effect ; use Ketorolac only for 72hrs due to
Sulinidac, Tolemtin, Mefenamic acid, Inhibits prostaglandin and thromboxane synthesis ; Nephrotoxicity (AKI and Interstitial Nephritis), GI and renal damage ; NSAIDs may
Ketorolac For analgesia, fever and as anti inflammatory Hypersensitivity reaction interfere with ASA's antithrombotic action
Nonselective reversible COX-1 and COX-2 inhibitor.
Inhibits prostaglandin synthesis and inhibit crystal
phagocytosis by macrophages ; For anti inflammatory Gastrointestinal toxicity, pancreatitis, Indomethacin has greater anti-
(gout arthritis, ankylosing spondylitis), for closing Nephrotoxicity, Serious hematologic reactions, inflammatory effect compared to other
iii. Indomethacin PDA BM suppression NSAIDs
Selective COX-2 inhibitor. Inhibits prostaglandin Gastrointestinal bleeding, Nephrotoxicity (same
B. COX-2 Selective NSAID: Celecoxib, synthesis ; For Analgesia, Anti inflammatory, risk as nonselective NSAIDs), Myocardial Rofecoxib and Valdecoxib withdrawn due
Etoricoxib, Parecoxib Antipyretic infarction and stroke to incereased incidence of thrombosis
Selectively inhibits COX-3 in the CNS, Weak COX-1
C. Non-opioid Analgesic (COX3 and COX-2 inhibitor in the periphery, Inhibits Hepatoxicity (antidote: NAC), Renal papillary
inhibitor) Paracetamol prostaglandin synthesis ; For Analgesia and necrosis and Interstitial nephritis, Preferred antipyretic in children (does not
(Acetaminophen) antipyretic Methemoglobinemia, Hemolytic anemia cause reye's syndrome) ; t1/2 is only 2-3h
D. Disease Modifying Anti-Rheumatic
Drug
Inhibits AICAR transformylase and thymidylate
synthase, with secondary effects on
polymorphonuclear chemotaxis ; For rheumatoid Nausea, Mucosal ulcers, hepatoxicity,
arthritis, SLE, JRA, psoriatic arthritis, Ankylosing hypersensitivty, Pseudolymphomatous reaction, DMARD of choice for Rheumatoid arthritis,
i. Methotrexate spondylitis, Polymyositis teratogen, hematotoxicity Rescue agent: Leucovorin (Folinic acid)
Bacterial infections (URTIs), reactivation of
latent tuberculosis, lymphoma, Demyelination,
Reactivation of Hepatitis B, Auto antibody
ii. TNF-alpha inhibitor: Infliximab, Binds or inhibits to TNF-a ; For Crohn's disease, formation (ANA, anti dsDNA), infusion reactions,
Adalimumab, Etanercept rheumatoid arthritis, other rheumatic disease hepatoxicity, hematotoxicity, cardiotoxicity Synergistic effects with methotrexate
Forms 6-thioguanine, suppressing inosinic acid Cannot give allopurinol with azathioprine
synthesis, B-cell and T-cell function, Immunoglobulin (allopurinol reduces xanthine oxidase
production and interleukin-2 secretion ; For Bone marrow supression, increased risk of catabolism of purine analogs, increasing 6-
rheumatoid arthritis, psoriatic arthritis, reactive infections, increased incidence of lymphoma, thioguanine nucleotides, leading to severe
iii. Azathioprine arthritis, polymyositis, SLE Fever, rash, hepatotoxicity, allergic reactions leukopenia)

Suppression of T-lymphocyte leading to decreased

leukocyte chemotaxis, stabilization of lysosomal
enzymes, inhibition of DNA and RNA synthesis, Ocular toxicity, Dyspepsia, Nausea, vomiting,
trapping of free radicals ; For rheumatiod arthritis, abdominal pain, rashes, nightmares, myopathy,
iv. Chloroquine, Hydroxychloroquine SLE, Sjogren's syndrome, Malaria neuropathy, ocular toxicity safe for pregnant women
 Forms phospharamide mustard, which cross links
DNA to prevent cell replication, Supresses T-cell and
B-cell function ; For Rheumatoid arthritis, SLE
vasculitis, Wegener's granulomatosis, severe Hemorrhagic cystitis, Rescue agent is
v. Cyclophosphamide rheumatic diseases Hemorrhagic cystitis Mesna
Inhibits interleukin-1 and iterleukin-2 receptor
production and secondarily inhibits macrophage-T-
cell interaction and T-cell responsiveness ; For Nephrotoxicity, hypertension, hyperkalemia,
vi. Cyclosporine rheumatoid arthritis, SLE, Tissue transplantation hepatoxicity, Gingival hyperplasia, hirsutism NONE
active product inhibits inosine monophosphate
dehydrogenase and inhibits T-cell lymphocyte
proliferation ; For SLE nephritis, vasculitis, Wegener's Gastrointestinal disturbances, headache,
vii. Mycophenolate Mofetil granulomatosis, rheumatoid arthritis hypertension, reversible myelosupression NONE
Nausea, vomiting headache,rash, hemolytic
active metabolite inhibits the release of anemia, methemoglobinemia, neutropenia,
inflammatory bowel cytokines; For rheumatoid leukopenia, thrombocytopenia, pulmonary
arthritis, inflammatory bowel disease, JRA, toxicity, autoantibody formation (anti dsDNA),
viii. Sulfasalazine ankylosing spondylitis Reversible infertility in men anti-IBD drugs
E. Antigout drugs
Diarrhea, nausea, vomiting, abdominal pain,
hepatic necrosis, acute renal failure, a general mitotic poison, may also be used
Inhibits microtubule assembly and LTB4 production disseminated intravascular coagulation, for Familial Mediterranean Fever ; diarrhea
i. Microtubule assembly inhibtor: leading to decreased macrophage migration and seizures, hair loss, bone marrow depression, is the adverse effect which signals toxicity
Colchicine phagocytosis ; For gout peripheral neuritis, myopathy from colchicine
May precipitate acute gout during early
phase of drug action (prevent by
coadministering with colchicine or
indomethacin) ; may be given together
with antimicrobial agents (particularly
are weak acids that compete with uric acid for Penicillins) to prolong therapeutic effect by
ii. Uricosuric agent: Probenecid, reabsorption in the PCT leading to increased uric acid Gastrointestinal irritation, rashes, nephrotic inhibiting renal tubular secretion of
Sulfinpyrazone excretion ; For gout syndrome, aplastic anemia ; sulfa allergy antibiotics
Inhibits metabolism of mercaptopurine and
azathioprine. Witheld for 1-2 wk after an
acute episode of gouty arthritis
(coadministered with colcichine or
Active metabolite (alloxanthine) irreversibly inhibits indomethacin to avoid an acute attack) ;
xanthine oxidase and lowers production of uric acid; Gastrointestinal upset, Rash, Peripheral neuritis, Feboxustat is a newer non-purine inhbitor
iii. Xanthine oxidase inhibitor: 1st line treatment of chronic gout, tumor lysis Vasculitis, bone marrow dysfunction, Aplastic of Xanthine Oxidase ; Febuxostat is more
Allopurinol, Febuxostat syndrome anemia, liver dysfunction (Febuxostat) effective than Allopurinol

6. ENDOCRINE DRUGS
Hypothalamic and Pituitary Hormones
 Recombinant Growth hormone, Increases release of
IGF-1 in the liver and carilage, stimulates skeletal
muscle growth, amino acid transport, protein
synthesis and cell proliferation ; For GH deficiency in
children and genetic disease associated with short
stature (Turner syndrome, Prader-Willi syndrome),
failure to thrive due to chronic renal failure or SGA, Peripheral edema, Myalgia, Arthralgia,
AIDS wasting, improve GI function in patients who Intracranial hypertension, pseudotumor cerebri,
underwent intestinal resection that led to slipped capital femoral epiphysis, progression of used as Performance enhancing drug since
i. Somatropin malabsorption syndrome scoliosis, hyperglycemia it increases muscle mass ; given SC
Recombinant IGF-1 ; For children unresponsive to remedy to hypoglycemia: give patient some
ii. Mecasermin GH therapy Hypoglycemia, increased LFT, intracranial HTN snacks prior to dose
Somatostatin analog, suppresses the release of
growth hormones, glucagon, insulin, gastrin, IGF-1,
serotonin and gastrointestinal peptides ; For regular release: given BID-QID SC, if slow
Acromegaly, pituitary adenoma, carcinoid, GI upset, gallstone, cardiac condution release: every 4wks IM ; are long-acting
iii. Octreotide, Lanreotide gastrinoma, glucagonoma, variceal bleeding abnormality synthetic analogs of somatostatin
Diarrhea, nausea, flu-like syndrome, elevated onset of action is expected within 2wks of
iv. Pegvisomant GH receptor antagonist ; For acromegaly LFTs, hypesensitivity reaction use
Headache, depression, edema, ovarian
Gonadotropin analog (FSH analog); activates FSH hyperstimulation syndrome (ovarian Follitropin alfa and beta are recombinant
receptors and mimics effects of endogenous FSH ; enlargement, ascites, hypovolemia, shock), FSH forms while Urofollitropin is a purified
v. Follitropin alfa, Follitropin beta, For Controlled ovarian hyperstimulation, infertility multiple pregnancies in women, gynecomastia preparation from urine of postmenopausal
Urofollitropin due to hypogonadism in men in men women
menotropins are mixtures of FSH and LH
Gonadotropin analog (LH analog); activates LH from postmenopausal women ;
vi. Menotropins, Human chorionic receptors and mimics effects of endogenous LH ; For Headache, depression, edema, ovarian Choriogondaotropin alfa is a recombinant
gonadotropin (HCG), Controlled ovarian hyperstimulation (ovulation hyperstimulation syndrome, multiple hCG while Lutropin is a recombinant LH ;
Choriogondaotropin alfa, Lutropin induction), hypogonadotripic hypogonadism pregnancies in women, gynecomastia in men hCG given IM

there is exacerbation of symptoms in males

GnRH analog, increased LH and FSH secretion with with prostate CA and children with
intermittent administration , reduced LH and FSH precocious puberty during the first few
secretion with prolonged continuous administration weeks of therapy (remedy: co-administer
(due to downregulation of GnRH receptors in the Flutamide, an androgen receptor
vii. Leuprolide, Gonadorelin, pituitary cells that normally release LH and FSH ; For Hot flushes, sweats, headaches, osteoporosis, antagonist) ; Gonadorelin is a synthetic
Goserelin, Histrelin, Nafarelin, Controlled ovarian hyperstimulation, endometriosis, gynecomastia, reduced libido, decreased human GnRH ; Leuprolide has a long
Triptorelin myoma uteri, precocious puberty, prostate CA hematocrit agonist activity
Does NOT cause tumor flare-up whe used
for treatment of advanced prostate cancer,
GnRH antagonist, blocks GnRH receptors, reduces also less likely to cause ovarian
endogenous production of LH and FSH ; For Nausea, headache, hypersensitivity, hot flushes, hyperstimulation syndrome ; Degarelix is
Controlled ovarian hyperstimulation (prevents gynecomastia, decreased libido, decreased used for prostate CA while Ganirelix
viii. Ganirelix, Cetrorelix, Degarelix premature LH surge), advanced prostate CA hematocrit, osteoporosis prevent LH surge in controlled ovulation
 Dopamine agonist, partial agonist at dopamine D2 Nausea, headache, lightheadedness, orthostatic
receptors in brain, inhibits prolactin release ; For hypotension, fatigue, behavioral changes, Slightly inhibits GH release if given in high
Hyperprolactinemia, Pituitary adenoma, acromegaly, erythromelalgia, Raynaud's phenomenon, doses ; CI in patients with history of
ix. Bromocriptine, Carbegoline Parkinson's disease pulmonary infiltrates psychotic illness
Activates oxytocin receptors, stimulates uterine
contraction and labor, stimulates mammary glands,
lactation and milk let-down ; For Labor induction, Fetal distress, placental abruption, uterine
labor augmentation, control of uterine hemorrhage rupture, fluid retention, hyponatremia, heart ATOSIBAN - an oxytocin antagonist used in
x. Oxytocin post-delivery failure, seizures, hypotension preterm labor

ADH agonist, Vasopressin V2 receptor agonist which

causes insertion of water channels in the collecting
duct leading to more water reabsoprtion, also
regulates the release of factor VIII and VWF ; For also contracts vascular smooth muscles via
Central DI, Hemophilia A, von Willebrand's disease, V1 receptor leading to vasoconstriction,
Variceal bleeding, colon diverticula, primary Headaches, flushing, nausea, hyponatremia, used as treatment for esophageal varices
xi. Desmopressin, Vasopressin nocturnal seizures seizures or colon diverticula
ADH antagonist, Antagonist at V1a and V2 receptors ;
For SIADH, Hyponatremia, offset fluid retention in Central pontine myelinolysis may occur
acute heart failure and SIADH which causes with rapid correction of hyponatremia,
xii. Conivaptan, Tolvaptan, Lixivaptan hyponatremia (dilutional) Infusion site reactions, hyperkalemia tolvaptan is more selective for V2 receptors
Thryoid & Antithyroid Drugs
T4 dose must be lowered in patients with
Thryoid hormone, activation of nuclear receptors cardiovascular disease or longstanding
results in gene expression with RNA formation and hypothyroidism (increased
i. Levothyroxine (T4), Liothyronine protein synthesis ; For Hypothyroidism, myxedema Dry skin, sweatng, tachycardia, nervousness, cardiosensitivity) ; Liothyronine has a faster
(T3) coma tremor, weight loss, weakness, heat intolerance onset but shorter half-life

Maculopapular pruritic rash, gastrointestinal

distress, fulminant hepatitis, agranulocytosis,
urticaria, vasculitis, lupus-like syndrome, Drug of choice for pregnant hyperthyroid
Inhibits thyroid peroxidase reactions, blocks iodine lymphadenopathy, hypoprothrombinemia, patients (does not eneter placenta and
organification, inhibits peripheral conversion of T4 Exfoliative dermatitis, polyserositis, arthralgia, breastmilk); slow onset of action (3-4
ii. Propylthiouracil (PTU) into T3 ; For Hyperthyroidism, thyroid storm hypothyroidism weeks for full effect)

Maculopapular pruritic rash, gastrointestinal

distress, fulminant hepatitis, dose-dependent,
agranulocytosis, urticaria, vasculitis, lupus-like
syndrome, lymphadenopathy, Methimazole and Carbimazole are
Inhibits thyroid peroxidase reactions, blocks iodine hypoprothrombinemia, Exfoliative dermatitis, teratogens (causes Aplasia Cutis Congenita)
iii. Methimazole, Carbimazole organification ; For Hyperthyroidism, thyroid storm polyserositis, arthralgia, hypothyroidism ; given as once daily dosing
onset is more rapid (2-7 days) but effect is
Inhibit iodine organification and hormone release transient (thyroid gland escapes iodide
leading to reduced size and vascularity of thyroid block after several weeks of treatment) ;
gland ; For Hyperthyroidism, thyroid storm, Iodism, acneiform rash, swollen salivary glands, Should not be used alone (escape in 2-8
preparation for surgical thyroidectomy to reduce the mucous membrane ulcerations, conjunctivitis, weeks); prevents radiation induced thryoid
iv. Lugol Solution (Iodine in Potssium size and vascularity of the thyroid gland, radiation rhinorrhea, drug fever, metallic taste, bleeding damage; prenatal exposure causes fetal
Iodide), Potassium Iodide prophylaxis disorders, anaphylactoid reactions goiter
 Beta blocker control HR and other cardiac
abnormalities of severe thyrotoxicosis, slows Esmolol may be used to treat
pacemaker activity; inhibits peripheral conversion of thyrotoxicosis-related arrhythmias; causes
v. Propranolol, Esmolol, Metoprolol, T4 into T3 ; For Hyperthyroidism, thyroid storm, post Bronchospasm, cardiac depression, AV block, clinical improvement WITHOUT altering
Atenolol MI prophylaxis, hypertension hypotension thyroid hormone levels
Preferred treatment for most patients due
Iodide, emits beta rays causing destruction of thyroid to ease of administration, effectiveness,
parenchyma ; For hyperthyroidism, permanent cure low expense and absence of pain;
of thyrotoxicosis without surgery and no effect on contraindicated in pregnant women or
vi. Radioactive Iodine other tissues Permanent hypothyroidism, sore throat nursing mothers
Adrenocorticosteroids & Adrenocortical Antagonists
Effects: stimulate gluconeogenesis,
increased fat deposition, muscle protein
and bone catabolism, lymphoid connective
tissue fat and skin wasting inhibit cell-
mediated immunologic functions,
lymphotoxic, increased neutrophils,
decreased lymphocytes eosinophils
Glucocorticoid, activates glucocorticoid receptors, basophils and monocytes, inhibit leukocyte
leading to altered gene transcription, Suppresses migration, inhibit PLA2, delay rejection in
inflammation, Replaces cortisol when deficient ; For transplant patients, increased GI acid
Acute adrenal insufficiency associated with life- secretion (ulcer) ; Biochemical effects:
threatening shock, chronic adrenal insufficiency induced synthesis of an inhibitor of PLA2,
(Addison's disease), congenital adrenal hyperplasia, Adrenal suppression, growth inhibition, DM, decreased mRNA for COX2, decrease in IL-2
insect bites, contact dermatitis, status asthmaticus, muscle wasting, osteoporosis, salt retention, and IL-3 and decrease in Platelet Activating
i. Low Potency: Desonide thyroid storm glucose intolerance, behavioral changes Factor (PAF)
ii. Med Potency: Fluticasone,
Mometasone
iii. High Potency: Desoximetasone,
Clobetasol

Glucocorticoid; For supressession of inflammation

and immune response, hematopoeitic cancers,
iv. Synthetic GCs: Prednisone, transplant rejection, collagen and rheumatic disease,
Prednisolone, Methylprednisolone, lung maturation in preterm labor (betamethasone prednisolone is the active metabolite of
Meprednisone, Dexamethasone, and dexamethasone), bronchial asthma, Adrenal suppression, growth inhibition, muscle prednisone ; this group has a long t1/2,
Betamethasone, Triamcinolone, chemotherapy-induced vomiting, hypercalcemia, wasting, osteoporosis, salt retention, glucose reduced salt-retaining effect and better
Beclomethasone, Budesonide mountain sickness intolerance, behavioral changes (psychosis) penetration of lipid barriers
Additive hypokalemia with loop diurectics
strong agonist of mineralocorticoid receptors and and thiazides ; Deoxycorticosterone is the
moderate activation of glucorticoid receptors, precursor of aldosterone ; Fludrocortisone
Increases Na reabsorption, K and H excretion ; For Salt and fluid retention, Hypokalemia, also has significant glucocorticoid activity ;
Chronic adrenal insufficiency (Addison's disease), Congestive heart failure, muscle wastng, Aldosterone is implicated in myocardial and
v. Mineralocorticoid: Congenital adrenal hyperplasia, adrenal replacement osteoporosis, glucose intolerance, behavioral vascular fibrosis and baroreceptor
Fludrocortisone, Deoxycorticosterone therapy post-adrenalectomy changes dysfunction
Corticosteroid Antagonists
 Glucorticoid synthesis inhibitor, inhibits desmolase
activity, blocking conversion of cholesterol to Also inhibits synthesis of all hormonally
vi. Aminoglutethimide pregnenolone ; For Breast CA, Cushing syndrome Skin rash, hepatotoxicity, hypothyroidism active steroids

Glucorticoid synthesis inhibitor; azole antifungal;

inhibits cholesterol side chain cleavage, cytochrome
P450 enzymes and other enzymes necessary for
synthesis of all steroids ; For Adrenal CA, Hirsutism,
Breast CA, steroid-responsive metastatic Prostate CA, Hepatotoxicity, many drug interactions,
vii. Ketoconazole Cushing's syndrome, Fungal infections, hirsutism androgenic effect Potent inhibitor of CYP450 enzymes
Glucorticoid synthesis inhibitor, selective inhibitor of
viii. Metyrapone steroid-11 hydroxylation, interfering with cortisol
and corticosterone synthesis ; As diagnostic test for DOC for pregnant patients with Cushing's
adrenal function Dizziness, GI disturbances syndrome
abdominal pain and cramping, uterine cramping, also used as an approved abortifacient for
ix. Mifepristone (RU486) competitive inhibitor at the GC receptor as well as nausea, headache, vomiting, diarrhea, dizziness, medical abortion (usually together with
progesterone receptor ; For Cushing's syndrome vaginal bleeding misoprostol)
Aldoesterone antagonist ; For hypokalemia due to
x. Spironolactone, Eplerenone other diuretics, for post-MI, hyperaldoteronism- see Hyperkalemia, gynecomastia (spironolactone) - also with weak antagonist effect at the
entry - see entry - androgen receptor
Gonadal Hormones and Inhbitors
A. Estrogen compounds
Increases risk of endometrial cancer and
breast cancer ; Ethinyl Estradiol has low
bioavailability, PO/TD/IM/Intravaginal ;
Estradiol cypionate is IM with longer t1/2 ;
Premarin is a mixture of conjugated
estrogen used in HRT ; Ethinyl estradiol
undergoes enterohepatic recirculation ;
i. Ethinyl Estradiol, Mestranol,
Effects of Estrogen: growth of genital
Estradiol cypionate, Premarin
breakthrough bleeding, nausea, breast structures and secondary sexual
Activates etrogen receptors, leads to changes in rates tenderness, migraine, thromboembolism (DVTs), characteristics, modifies serum protein
of trasncription of estrogen-regulated genes ; For gallbladder disease, hypertriglyceridemia, levels and decrease bone resorption,
Primary hypogonadism, Postmenopausal hormonal hypertension, premature closure of the enhances coagulability of blood, increases
replacement therapy, Osteoporosis and prevention epiphysis in young females, increased risk of TG and HDL levels while decreasing LDL
of bone loss, Contraception, Intractable breast and endometrial cancer (remedy: add levels, if given as continuous infusion will
dysmenorrhea progesterone to the preparation) inhibt FSH and LH release
 breakthrough bleeding, nausea, breast
tenderness, migraine, thromboembolism (DVTs),
Synthetic estrogen (nonsteroid); activates estrogen gallbladder disease, hypertriglyceridemia,
ii. Diethylstilbestrol receptors; leads to changes in rates of transcription hypertension, premature closure of the associated with Infertility, ectopic
of estrogen-regulated genes ; For Atrophic vaginitis, epiphysis in young females, increased risk of pregnancy, clear cell vaginal
hormone replacement therapy, prevention of breast and endometrial cancer (remedy: add adenocarcinoma in daughters of women
adverse pregnancy outcomes, metastatic prostate CA progesterone to the preparation) treated with DES
B. Progestins
Prevents estrogen induced endometrial
cancer when used in combination with
estrogens; Megesterol is used as an
appetite stimulant ; given PO or as vaginal
cream ; Medroxyprogesterone has a better
oral bioavilability ; L-Norgestrel and
i. Norgestrel, Medroxyprogesterone,
Norethindrone has more androgenic effect
Norethindrone, Norgestimate,
activates progesterone receptors, changes rate of ; Norgestrel undergoes enterohepatic
Desogestrel, Megestrol
transcription of progesterone-regulated genes ; For recirculation ; Effects of progesterone:
Hormone replacement therapy (given together with induces secretory changes in the
Estrogen, to prevent estrogen-induced endometrial endometrium, stabilize the endometrium,
cancer), contraception, assisted reproduction (for Hypertension, decreased HDL, weight gain, affect carbohydrate metabolism and
maintenance of pregnancy), anovulation induction reversible decrease in bone mineral density, stimulate deposition of fat, high doses
(given in high doses to suppress FSH and LH) delayed resumption of ovulation after use suppress FSH and LH secretion
C. Combined Hormonal
Contraceptives maybe PO/IM/TD/vaginal rings/IUD
Lifetime risk of breast cancer is NOT
changed; Norethindrone is a testosterone
Combined oral contraceptive, activates estrogen and derivative while Drospirenone is a
progesterone receptors, inhibits ovulation, effects on spironolactone derivative that is
cervical mucus gland, uterine tubes and breakthrough bleeding, nausea, breast antiandrogenic ; Norgestimate and
endometrium lead to decreased fertility, inhibit tenderness, migraine, thromboembolism (DVTs), Desogestrel are newer progestins ;
ovulation when given before the LH surge ; For breast cancer (earlier onset), headache, skin combined OCPs may be used for androgen-
Contraception, hypogonadism, acne, hirsutism, pigmentation, depression, weight gain acne and induced hirsutism ; Mestranol (Estrogen)
i. Estradiol + Norethindrone dysmenorrhea, endometriosis hirsutism for older OCPs may also be used in OCPs
ii. Ethinyl Estradiol + Desogestrel
iii. Ethinyl Estradiol + Drospirenone
iv. Ethinyl Estradiol + Noregistmate
Progestin-only contraceptive, activates
progresterone receptors, Prevents conception by
altering cervical mucus and creating a hostile
endometrium ; For Contraception, hormone Breakthrough bleeding, hair loss, dysmenorrhea,
v. Medroxyprogesterone Acetate replacement therapy delayed return of fertility, osteoporosis IM depot preparation
Severe nausea, vomiting, breast tenderness,
Postcoital contraceptive, activates estrogen and/or irregular bleeding, headache, dizziness (fewer SE
progesterone receptors, thickens cervical mucus, compared to estrogen alone and combi Must be taken within 72 hours of
vi. Levonorgestrel inhibits ovulation ; For Emergency contraception contraceptives) unprotected sexual intercourse
D. Selective Estrogen Receptor
Modulators (SERMs)

Estrogen antagonist actions in breast tissue and CNS,

Estrogen agonist effects in uterus, liver and bone ; prevent osteoporosis in post-menopausal
For Hormone responsive breast CA, prophylaxis of Hot flushes, thromboembolism, endometrial women ; Torimefene is structurally related
i. Tamoxifen, Torimefene breast CA esp. in those with high risk hyperplasia, endometrial cancer to Tamoxifen
Estrogen antagonist actions in breast tissue, uterus,
and CNS, Estrogen agonist effects in liver and bone.
Increases bone mineral density ; For Osteoporosis
esp on post menopausal women, breast CA No estrogenic effect on endometrial tissue
ii. Raloxifene prevention Hot flushes, thromboembolism unlike tamoxifen
Partial agonist in pituitary, reduces negative feedback may cause multiple pregnancies ;
by estradiol, increases FSH and LH output ; For Hot flushes, afterimages, headache, FULVESTRANT: pure estrogen receptor
Induction of ovulation in women who want to constipation, reversible hair loss, ovarian anatgonist in all tissues used in breast CA
iii. Clomiphene become pregnant enlargement resistant to tamoxifen
Effective against brest CA that have
iv. Anastrozole, Letrozole, Reduces estrogen synthesis by inhibiting aromatase ; Hot flushes, musculoskeletal disorders, become tamoxifen-resistant ; Exemestane
Exemestane For breast CA, precocious puberty osteoporosis, joint pains is an IRREVERSIBLE inhibitor
Ovarian inhibitor, weak cytochrome P450 inhibitor
and partial agonist of progestin and androgen
receptors ; For Endometriosis, Fibrocystic disease, Acne, hirsutism, weight gain, menstrual
v. Danazol Hemophilia, Angioneurotic edema disturbances, hepatic dysfunction May also act on Glucocorticoid receptors
Combined with misoprostol results in
abortion of 95% of early pregnancies ; as
abortifacient in early pregnancy (may be
Glucocorticoid receptor antagonist, progesterone Vaginal bleeding, abdominal pain, GI upset used up to 49days after menses) ;
receptor antagonist ; For Medical abortion, Cushing's (vomiting, diarrhea), uterine cramping, nausea, complication: failure to induce complete
vi. Mifepristone (RU486) syndrome vomiting, headache, dizziness, diarrhea abortion
vii. Leuprolide and Ganirelix see entry see entry see entry
E. Androgens may be given IV or as TD
Effects of androgen: secondary sexual
characteristics, fertility and libido, male
Activates androgen receptors, promotes pattern baldness, increases muscle mass,
development of male characteristics, increases body increased RBC production, decreased urea
muscle bulk and RBC production ; For Male Virilization and menstrual irregularities in nitrogen excretion, maintains normal bone
i. Testosterone, Fluoxymesterone, hypogonadism, delayed puberty, wasting syndromes females, paradoxical feminization in males, density ; used illegally by atheletes as
Methyltestosterone (for weight gain), certain types of anemias cholestatic jaundice, elevated LFTs performance enhancer

Activates androgen receptors, promotes

development of male characteristics, increases body Virilization in females, paradoxical feminization
ii. Oxandrolone, Stanozolol, muscle bulk and RBC production; increased ratio of in males; cholestatic jaundice, elevated liver
Nandrolone anabolic-to-androgenic activity in animals enzymes, hepatocellular CA this group is called "anabolic steroids"
For benign and malignant prostate disease,
F. Anti-androgens precocious puberty, hair loss and hirsutism
 GnRH analogs must be coadministered with
flutamide to prevent acute flareups of
i. Flutamide, Bicalutamide, Competitive antagonist at androgen receptor ; For Gynecomastia, hot flushes, impotence, prostate CA ; Bicalutamide and Nilutamide
Nilutamide Prostate CA, surgical castration hepatotoxicity have less heaptotoxicity
Antagonist at androgen receptor. Marked
progestational effect that suppresses the feedback
enhancement of LH and FSH ; for Hirsutism, Hepatotoxicity, Adrenal suppression,
component of combined oral contraceptives, depression, gynecomastia, galactorrhea,
ii. Cyproterone decreased sexual drive in men thromboembolism Orphan drug status
Androgen synthesis inhibitor, inhibits 5a reducase
enzyme that converts testosterone to Dutasteride is newer with longer t1/2 ; this
dihydrotestosterone ; For BPH, Male pattern group is less likely to cause impotence,
iii. Finasteride, Dutasteride baldness. Hirsutism Impotence, gynecomastia, depression infertility and decreased libido
iv. GnRH agonist and antagonists see entry see entry see entry
v. Spironolactone for treatment of hirsutism in women
vi. Ketoconazole inhibit gonadal and adrenal steroid synthesis see entry see entry
P ancreatic Hormones & Antidiabetic Drugs
A. Insulins
Effects of insulin: increased glycogen and
protein synthesis, decreased protein
catabolism, increased TG storage ; rapid
acting insulins are injected a few mins prior
to meals and they are the preferred insulin
Activates insulin receptors leading to a reducting of for continuous SC infusion devices ; short-
circulating glucose: promotes glucose transport and acting insulins are injected more than an
oxidation; glycogen, lipid, protein synthesis and hour before a meal ; intermediate acting
regulation of gene expression ; For Diabetes mellitus, Hypoglycemia (antidote: sugar or candy, IV insulins are often combined with regular
i. Rapid Acting Insulin: Lispro, Aspart, diabetic emergencies like DKA, HHS (rapid-acting), glucose, IM glucagon), insulin allergy, immune and rapid acting insulins ; long acting
Glulisine Hyperkalemia insulin resistance, lipodystrophy at injection site insulins are called "peakless" insulins
ii. Short Acting Insulin: Regular
iii. Intermediate Acting: NPH, Lente
iv. Long Acting Insulin: Detemir,
Glargine, Ultralente, Lantus
B. Sulfonylureas
2nd generation sulfonylurea, acts as an insulin
secretagogue, increases insulin secretion from
pancreatic beta cells by closing ATP sensitive K+ Less hypoglycemia, weight gain,
i. Glipizide, Glibenclamide, channels leading to depolarization of the B cell; For photosensitivity, cholestatic jaundice Not effective in patients with functional B
Glimepiride, Gliclazide, Glyburide Type 2 Diabetes Mellitus (glibenclamide) cells
 1st generation sulfonylurea, acts as an insulin
secretagogue; increases insulin secretion from Hypoglycemia, weight gain, disulfiram reaction, tolbutamide and chlorpropamide are highly
ii. Tolazamide, Tolbutamide, pancreatic beta cells by losing ATP sensitive K+ hyperemic flush, dilutional hyponatremia, protein bound drugs, which may also cause
Chlorpropamide channels ; for Type 2 Diabetes Mellitus hematologic toxicity allergic reactions and rash
C. Meglitinides
Insulin Secretagogue, similar to sulfonylureas with
some overlap in binding sites, reduces circulating
glucose, increases glycogen, fat and protein
formation and gene regulation ; For Type 2 Diabetes Least Hypoglycemia, rapid onset and short
i. Repaglinide Mellitus Least hypoglycemia, headache, URTI DOA
Insulin Secretagogue, similar to sulfonylureas with
some overlap in binding sites, reduces circulating
glucose, increases glycogen, fat and protein Has least incidence of hypoglycemia, may
formation and gene regulation ; For Type 2 Diabetes be used in CKD patients ; rapid onset and
ii. Nateglinide Mellitus Least hypoglycemia, headache, URTI short DOA
D. Biguanides
DOC for obese diabetics ; may also cause
slowing of glucose absorption from GIT,
decreased plasma glucagon ; causes a
Reduced hepatic and renal gluconeogenesis with decrease in endogenous insulin production
decreased endogenous glucose production, activates by increasing insulin sensitivity of tissues
AMP-stimulated protein kinase leading to inhibition GI disturbance, weight loss, lactic acidosis (esp "Insulin Sparing Effect" therefore does not
of gluconeogenesis ; For Type 2 DM, Diabetes in renally and hepatically impaired patients), Vit have weight gain as a SE ; do NOT cause
i. Metformin prevention, PCOS B12 malabsorption hypoglycemia
E. Alpha Glucosidase Inhibitors

Inhibits intestinal alpha-glucosidases , reduces

conversion of starch and disacchardies to relatively minor glucose lowering effects ;
monosaccharidea, reduces post prandial GI disturbance, hypoglycemia, increased liver impaired absoprtion of sucrose ; taken
i. Acarbose, Miglitol hyperglycemia ; For Type 2 DM, Diabetes prevention enzymes, flatulence, diarrhea, abdominal pain immediately before a meal
F. Thiazolidinediones

Regulates gene expression by binding to PPAR-

gamma and PPAR-alpha which increases tissue
sensitivity, increases glucose uptake in muscle and
adipose tissue, inhibits hepatic gluconeogenesis, Fluid retention, weight gain, congestive heart binds to PPAR-gamma and PPAR-alpha ;
effects on lipid metabolism and distribution of body failure, fractures esp in women, cardiovascular PPAR regulates transcription of genes
fat, control of fasting and postprandial glucose, events, hepatotoxicity (Troglitazone), macular encoding proteins involved in carbohydrate
decreased risk of DM in high-risk patients ; For Type 2 edema, dyslipidemia, increased risk of MI and lipid metabolism ; may increase risk for
i. Pioglitazone DM, Diabetes prevention (Rosiglitazone) developing Bladder Cancer
Regulates gene expression by binding to PPAR-
ii. Rosiglitazone gamma ONLY ; for Type 2 DM, Diabetes prevention binds to PPAR-gamma ONLY
G. Novel Antidiabetic Agents
 Analog of GLP-1, Binds to GLP-1 receptors which
leads to reducetion of post-meal glucose excursions,
increases glucose-mediated insulin release, lowers
glucagon levels, slows gastric emptying time, Hypoglycemia, acute pancreatitis, GI upset, usually combined with SU or metformin ;
i. Exenatide produces satiety ; For Type 2 DM nausea, vomiting long-acting injectables

Dipeptidyl Peptidase-4 Inhibitors, blocks degradation

of GLP-1, raises circulating GLP-1 levels, reduces
post-meal glucose excursions, increases glucose
mediated insulin release, lowers glucagon levels,
slows gastric emptying time, decreases appetite ; For
ii. Sitagliptin, Linagliptin Type 2 DM Headache, nasopharyngitis, URTI often combined with metformin
Analog of amylin, Binds to amylin receptors, reduce
post-meal glucose excursions, lowers glucagon levels,
slows gastric emptying, decreases appetite ; For Type used with insulin to control post-prandial
iii. Pramlintide 2 DM Hypoglycemia, GI disturbances glucose
Bile acid binder, lowers glucose through unknown
iv. Colesevelam hydrochloride mechanisms ; For Type 2 DM constipation, dyspepsia, myalgia, asthenia None
Agents That Affect Bone Mineral Homeostasis
A. Vitamin D Metabolites and Analogs

INACTIVE Vitamin D; Regulates gene tanscription via

the vitamin D receptor; stimulates intestinal calcium
absorption, bone resorption, renal calcium and
phosphate reabsorption, decreases PTH, promote
innate immunity ; For Vitamin D deficiency states
(intestinal osteodystrophy, CKD, chronic liver disease,
hypoparathyroidism, nephrotic syndrome) Hypercalcemia, hyperphosphatemia, given topically for psoriasis ; given with
i. Cholecalciferol, Ergocalciferol osteoporosis, psoriasis hypercalciuria calcium supplements for osteoporosis
The active form Calcitriol is preferred in
patients with CKD, chronic liver disease and
ACTIVE Vitamin D; Regulates gene tanscription via hypoparathyroidism ; Doxercalciferol is a
the vitamin D receptor; stimulates intestinal calcium prodrug that is converted in the liver to
absorption, bone resorption, rena calcium and 1,25-dihydroxyvitaminD ; Paricalcitol,
phosphate reabsorption, decreases PTH, promote Hypercalcemia, hyperphosphatemia, Calcipotriene are analogs of calcitriol and
innate immunity ; For Secondary hypercalciuria ; Doxercalciferol, Paricalcitol and are used topically for psoriasis and are
ii. Calcitriol, Doxercalciferol, hyperparathyroidism in CKD, hypocalcemia in Calcipotriene cause less hypercalcemia and being investigated for malignancies and
Paricalcitol, Calcipotriene hypoparathyroidism, psoriasis hypercalciuria inflammatory disorders
B. Bisphosphonates

Pamidronate, Zoledronic acid and

Suppress the activity of osteoclasts in part via Etidronate are used IV for hypercalcemia in
inhibition of farnesyl pyrophosphate synthesis, Paget's disease and cancer ; all other
i. Alendronate, Risedronate, inhibit resorption and formation of bone by acting on Adynamic bone, Esophagitis, Osteonecrosis of preparations and Etidronate can be given
Ibandronate, Pamidronate, the basic hydroxyapatite crystal structure ; For the Jaw, renal impairment, GI irritation (remedy: PO but with low bioavailability (<10%) ;
Zoledronate, Etidronate, Tiludronate, Paget's disease of the bone, Hypercalcemia esp in take lots of water and keep patient in an upright Treatment regimen: oral OD (alendronate,
Zoledronic acid malignancies, Osteoporosis position for 30mins after intake of drug) risedronate, ibandronate), weekly PO
 (alendronate, risedronate), monthly PO
(ibandronate), quarterly injection
(ibandronate), annual IV (zoledronate)

C. Hormones
Recombinant PTH, Acts via cognate G protein
coupled receptors, stimulates bone formation when hypercalcemia, arthralgia, rhinitis, nausea,
i. Teriparatide given in low intermittent doses weakness, dizziness, pharyngitis, dyspepsia, rash used IV for osteoporosis
Acts via cognate G protein coupled receptors;
suppresses bone resorption ; For Paget's disease of given as injection or as nasal spray ; used
the bone, hypercalcemia, osteoporosis, tumor for osteoporosis but is less effective than
ii. Calcitonin marker for thyroid CA Rhinitis, Nausea, vomiting, facial flushing bisphosphonates and teriparatide
D. Selective Estrogen Receptor
Modulators (SERMs)
Interacts selectively with estrogen receptors, inhibits
PTH-stimulated bone resorption without stimulating
breast or endometrial hyperplasia, delay bone loss in
i. Raloxifene post-menopausal women see entry see entry
E. Rank Ligand (RANKL) Inhibitor
Monoclonal antibody, binds to RANKL and prevents it
from stimulating osteoclast differentiation and
function, blocks bone resorption ; For as potent as bisphosphonates ; given SC
i. Denosumab postmenopausal osteoporosis increased risk of infection every 6months which avoid the GI SE
F. Calcium Receptor Antagonist
Activates the calcium sensing receptors in the
parathyroid gland, inhibits PTH secretion ; For
secondary hyperparathyroidism in CKD, hypocalcemia, adynamic bone disease
i. Cinacalcet hypercalcemia in patients with parathyroid CA (profound decreae in bone cell activity) considered a Calcimimetic (decreases PTH)

7. CHEMOTHERAPEUTIC DRUGS
Beta-Lactam & Other Cell Wall-Active & Membrane-Active Antibiotics
Bactericidal ; excreted unchanged in the
A. Penicillin urine ; capable of entering the blood brain
barrier
Inactivated by beta-lactamase
i. Natural Penicillins: Penicillin G, Binds to penicillin-binding proteins, inhibits (penicillinase) ; given IM but Pen V can be
Penicillin V (narrow spectrum transpeptidation in bacterial cell walls ; DOC for given PO ; increased activity against
penicillin) syphillis, for streptococcal, meningococcal, G+ bacilli, enterococci when given together with
spirochete infection hypersensitivity, GI disturbances aminoglycosides
 Resistant to inactivation by beta-lactamase
ii. Anti-Staphylococcal Penicillins:
Binds to penicillin-binding proteins, inhibits (penicillinase) ; all penicillins are excreted
Methicillin, nafcillin, oxacillin,
transpeptidation in bacterial cell walls; For hypersensitivity, GI disturbances, interstitial unchanged in the urine EXCEPT for Nafcillin
cloxacillin (very narrow spectrum)
staphylococcal infections nephritis (methicillin), neutropenia (nafcillin) which is excreted in the bile
Inactivated by beta-lactamase
(penicillinase), enhanced effect when used
iii. Extended Spectrum Penicillin: Binds to penicillin-binding proteins, inhibits with beta-lactamase inhibitors (clavulanic
Ampicillin, Amoxicillin transpeptidation in bacterial cell walls ; For hypersensitivity, GI disturbances, acid, sulbactam) ; ampicillin undergoes
enterococci, Listeria, E. coli, Proteus, H. influenza, pseudomembranous colitis (ampicillin), rash enterohepatic recirculation ; synergistic
Moraxella (ampicillin) effect with aminoglycosides
Inactivated by beta-lactamase
iv. Antipseudomonal Penicillin: Binds to penicillin-binding proteins, inhibits (penicillinase), enhanced effect when used
Piperacillin, ticarcillin, carbenicillin transpeptidation in bacterial cell walls ; For with beta-lactamase inhibitors (clavulanic
Pseudomonas, Enterobacter, Klebsiella hypersensitivity, GI disturbances acid, tazobactam)
Bactericidal ; mostly IV ; all have renal
B. Cephalosporins excretion EXCEPT Cefoperazone and
Ceftriaxone

i.First Generation: Cefazolin, Binds to penicillin-binding proteins, inhibits Increases nephrotoxicity of

cefadroxil, cephalothin, cephapirin, transpeptidation in bacterial cell walls ; For surgical aminoglycosides ; do not cross the BBB ;
cephradine, cephalexin prophylaxis, bone infections, infections due to staph hypersensitivity, injection site reactions, minimal activity against G- cocci,
and strep, E. coli, Klebsiella, G+ cocci phlebitis, GI upset enterococci, MRSA and most G- rods
Increases nephrotoxicity of
aminoglycosides ; do not cross the BBB ;
ii. Second Generation: Cefamandole, Binds to penicillin-binding proteins, inhibits slight less activity against G+ but extended
cefaclor, cefonicid, cefuroxime, transpeptidation in bacterial cell walls ; For surgical G- activity ; Cefuroxime has improved
cefprozil, loracarbef, ceforanide, prophylaxis, bone infections, infections due to staph action against pneumococcus and H.
cefoxitin, cefmetazole, cefotetan strep and E. coli, Enterobacter, Neisseria, infections hypersensitivity, injection site reactions, influenzae ; Cefotetan and Cefoxitin have
against anaerobes (Bacteroides), sinus ear and phlebitis, GI upset, Hypoprothrombinemia and good activity against B. fragilis and thus are
respiratory infections by Klebsiella andHemophilus Disulfiram rection (cefamandole, cefotetan) used for abdominal and pelvic infections
Synergistic effect with aminoglycosides ; all
have renal excretion EXCEPT Cefoperazone
and Ceftriaxone ; all can penetrate the BBB
EXCEPT Cefoperazone and Cefixime ;
Ceftriaxone and Cefotaxime are the most
iii. Third Generation: Cefoperazone,
active Cephs against Penicillin resistant
cefotaxime, ceftizoxime, ceftriaxone,
Streptococcus pneumoniae ; Ceftizoxime is
cefixime, cefpodoxime proxetil,
Binds to penicillin-binding proteins, inhibits commonly used against Bacteroides ;
cefdinir, ceftibuten
transpeptidation in bacterial cell walls ; decreased should be reserved against serious
gram + coverage, increased gram – activity infection EXCEPT ceftriaxone and cefixime ;
(pseudomonas, bacteroides), against Providencia, hypersensitivity, GI upset, Ceftriaxone has very good CNS penetration
Serratia, Neiserria, Haemophilus ; DOC for gonorrhea Hypoprothrombinemia and Disulfiram rection ; Ceftazidime has very good action on
(Ceftriaxone and Cefixime) (cefoperazone) Pseudomonas
More resistant to beta-lactamase produced
by Enterobacter, Haemophilus, Neisseria
iv. Fourth Generation: Cefipime,
Binds to penicillin-binding proteins, inhibits and Pneumococcal ; Has improved stability
Ceftaroline
transpeptidation in bacterial cell walls ; wide to chromosomal lactamase ; Ceftaroline
coverage against gram + and gram - bacteria hypersensitivity, GI upset used for MRSA
C. Other Beta-Lactams
Reserved for serious ife-threatening
infections; cilastatin inhibits renal
metabolism of imipenem ; given IV ; low
susceptibility to B-lactamases ; active
against Pseudomonas and Acinetobacter
i. Carbapenems: Imipenem-cilastatin
Binds to penicillin-binding proteins, inhibits EXCEPT Ertapenem ; Imipenem given with
, ertapenem, meropenem
transpeptidation in bacterial cell walls, wide Cilastatin which acts as Dehydropeptidase
coverage against gram + gram - bacteria and enzyme inhibitor ; Partial cross-allergenicity
anaerobes ; For infections resistant to other with Penicillins ; Ertapenem has longer t1/2
antibiotics EXCEPT MRSA, DOC for Enterobacter, hypersensitivity, GI upset, CNS toxicity but less active against Enterococci and
Citrobacter and Serratia (confusion, encephalopathy, seizures) Pseudomonas
Resistant to beta-lactamase, no activity
ii.Monobactam: Aztreonam Binds to penicillin-binding proteins, inhibits against gram + bacteria or anaerobes ;
transpeptidation in bacterial cell walls ; used against GI upset, superinfection, vertigo, headache, skin given IV ; synergistic with AG ; renal
Gram – like klebsiella, pseudomonas and Serratia rash and hepatotoxicity excretion ; No cross-allergenicity with Pens
Most active against plasmid encoded B
iii. Beta-Lactamase Inhibitors: Inhibits inactivation of penicillins by bacterial beta- lactamases (Gonococci, Streptococci, E coli
Clavulanic acid , sulbactam, lactamase (penicillinase); used against beta- and H. Influenzae ; not good inhibitor of
tazobactam lactamase producing gonococci, streptococci, E. coli inducible chromosomal B lactamases
and H. influenza hypersensitivity and cholestatic jaundice (Enterobacter,Pseudomonas, Serratia)
D. Other Cell Wall Synthesis Inhibitors
Narrow spectrum Treat red man syndrome
by slowing the rate of infusion ; VRSA and
VRE are due to D-Ala-D-Lactate formation ;
teicoplanin and telavancin are not
absorbed in the GIT thus used for bacterial
i. Glycopeptides: Vancomycin,
enterocolitis, they are also eliminated
teicoplanin, telavancin, dalbavancin
Inhibits cell wall synthesis by binding to the D-Ala-D- unchanged in the urine ; decrease dose for
Ala terminus of nascent peptidoglycan --> inhibit renally impaired patients ; Dalbavancin has
transglycosylation --> prevent elongation and cross- very long t1/2 (6-11 days) which permits
linking of peptidoglycan chain ; For MRSA, PRSP, as red man syndrome, nephrotoxicity, ototoxicity, once-weekly dosing and is more active than
alternative for pseudomembranous colitis chills, fever, phlebitis Vancomycin

ii. Peptide Antibiotic: Bacitracin Interferes with a late stage oin cell wall synthesis in Reserved for topical use only due to
gram + organisms ; For gram + bacteria nephrotoxicity marked nephrotoxicity
Blocks incorporation of D-Ala into the pentapeptide
iii. Antimetabolite: Cycloserine side chain of the peptidoglycan ; For drug-resistant
TB neurotoxicity (tremors, seizures and psychosis) only used as a second-line agent in TB
inhibits cytosolic enolpyruvate transferase --> renal excretion ; resistance emerges rapidly
iv. Antimetabolite: Fosfomycin prevents formation of N-acetylmuramic acid (a ; synergistic with Beta lactam and
peptidoglycan precursor molecule) Diarrhea quinolones
monitoring of CPK is needed, NOT
v. Cyclic lipopeptide: Daptomycin same spectrum of activity as Vancomycin ; For VRE, Bactericidal (only destabilizes bacterial cell
VRSA, for G+ acitivity, against endocarditis and sepsis myopathy membrane)
Tetracyclines, Macrolides, Clindamycin, Chloramphenicol, Streptogramins & Oxazolidinones

Inhibits transpeptidation (catalyzed by peptidyl given PO and IV ; able to cross the placenta
transferase) by blocking the binding of aminoacyl and BBB ; Inhibits hepatic drug-
moiety of the charged tRNA to the acceptor site o metabolizing enzymes causing many drug
mRNA at 50S subunit, basteriostatic ; For meningitis interactions ; resistance is due to the
(Strep pneumonia, H influenza, Neisseria formation of acetyltransferase that
A. Chloramphenicol (broad spectrum meningitides), back up for Salmonella, Rickettsia, GI disturbance, aplastic anemia, gray baby inactivates drug ; usually used as topical
protein synthesis inhibitor) Bacteroides, Wide spectrum antibiotic syndrome agent

Binds 30s ribosomal subunit thus preveting the

binding of tRNA to mRNA, bacteriostatic ;
Broad/Wide Spectrum (G+ and G-), For infections Tigecycline has the broadest spectrum and
caused by Mycoplasma pneumonia, Chlamydia, has the longest t1/2 (30-36hrs); do not
Rickettsia, Vibrio, Spirochetes such as Leptospira, drink with milk (decreased absorption with
Peptic ulcer disease, Lyme disease, Malaria divalent cations like calcium) ; high Vd,
prophylaxis, Amoebiasis, Acne, Doxycycline is an cross the placenta, enterohepatic recycling
alternative to macrolides as initial treatment of CAP, ; all are excreted renally EXCEPT
Alternative in syphilis, treatment of respiratory Doxycycline (bile) ; Resistance is due to
infection caused by susceptible organism, development of efflux pumps for active
prophylaxis against infection in chronic bronchitis ; GI disturbances (enetrocolitis, nausea, diarrhea, extrusion of tetracyclines and the
Selective uses: Tetracycline (H. Pylori PUD), vomiting), teratogen (tooth enamel formation of ribosomal protection proteins
Doxycycline (Lyme disease and malaria prevention), dysplasia/discoloration), hepatotoxicity, that interfere with tetracycline binding (but
Minocycline (Meningococcal carrier state), nephrotoxicity, photosensitivity n(esp. not present with Tigecycline EXCEPT in
B. Tetracyclines: Tetracycline, Demeclocycline (SIADH), Tigecycline (more broad demeclocycline), vestibulotoxicity, candidiasis, Proteus and Pseudomonas) ; Tigecycline is
doxycycline, minocycline, tigecycline, spectrum - MRSA, VRE, B-lactamase producing G- bacterial superinfection with S. aureus and C. given IV only and is unaffected by common
demeclocycline bacteria, anaerobes, Chlamydiae, Mycobacteria) difficile, Fanconi syndrome tetracyclie resistace mechanisms
C. Macrolides

good oral bioavilability but azithromycin

Binds 30s ribosomal subunit, inhibit transpeptidation, absoprtion is impeded by food ; All
bacteriostatic ; For community-acquired pneumonia, macrolides inhibit CYP450 except
pertussis, diphtheria, chlamydial infections ; azithromycin; azithromycin has highest Vd
Eryhthromycin (Campylobacter, Chlamydia, and slowest elimination; telithromycin is
Mycoplasma, Legionella, Corynebacterium, used for macrolide-resistance ; Half-lives:
Chlamydophila, Legionella, Ureaplasma, Bordetella, Erythromycin (2hrs), Clarithromycin (6hrs),
G+ cocci, some G-), Clarithromycin and Azithromycin Azithromycin (24-48hrs) ; Resistance is due
(coverage of Erythromycin plus greater activity to development of efflux pumps and
against Chlamydia, Mycobacterium avium, production of methylase enzyme ; Cross-
Toxoplasma, Helicobacter, Haemophilus, Moraxella, resistance among macrolides: complete or
i. Erythromycin, azithromycin, Neiserria) ; Azithromycin is used as an alternative GI disturbance, cholestatic hepatitis, QT partial resistance with drugs acting on the
clarithromycin, telithromycin Ceftriaxone in Gonorrhea and to Pen G in syphilis prolongation, drug interaction 50S
 a narrow spectrum macrolide, for G+ and anaerobe, GI upset, rashes, eosinophilia, acute cholestatic as effective as Vancomycin as treatment for
ii. Fidaxomicin low oral bioavailability hepatitis, enzyme inhibitor C. difficile possibly with lower relapse rate
Ketolide, structurally related to macrolide, same
MOA and spectrum as erythromycin but macrolide- For CAP including multi-drug resistant
resistant organisms are susceptible to telithromycin ; QT prolongation, enzyme inhibitor, hepatic organisms, A ketolide not a macrolide in
iii. Telithromycin For CAP dysfunction chemical structure

Binds 30s ribosomal subunit, inhibit transpeptidation, Cross-resistance between clindamycin and
bacteriostatic ; For anaerobic infections macrolides is common ; Resistance is due
(Bacteroides), alternative against gram + cocci GI disturbance, skin rash, neutropenia, hepatic to methylation of binding sites and
(MRSA), endocarditis prophylaxis esp in those allergic dysfunction, possible superinfection enzymatic inactivation ; G- aerobes are
D. Lincosamides: Clindamycin, to Pens, PCP pneumonia, toxoplasmosis (+ (Pseudomembranous colitis - C. difficile resistant because of poor penetration
lincomycin Pyrimethamine), skin and soft tissue infection overgrowth) through th eouter membrane

Binds 50s ribosomal subunit, constricting the channel

where polypeptides are extruded thus tRNA
synthetase is also inhibited --> decreased free tRNA ;
E. Streptogramin: Quinupristin- For infections caused by drug-resistant gram + cocci Injection site reaction, anthralgia-myalgia Inhibits CYP450 enzymes causing multiple
Dalfopristin (MRSA, VRSA, PRSP, resistant E. faecium) syndrome drug interactions ; BACTERICIDAL

Binds 23S rRNA of 50s ribosomal subunit, inhibit

initiation by blockin formation of the tRNA-ribosome-
mRNA ternary complex, bacteriostatic ; Reserved for Inhibits CYP450 enzymes causing multiple
infections caused by drug-resistant gram + cocci Thrombocytopenia, neutropenia, serotonin drug interactions ; Resistance is due to
F. Oxazolidinone: Linezolid (MRSA, VRE, PRSP), Listeria, Corynebacteria syndrome, neuropathy, optic neuritis decreasedaffinity of drug to binding site
Aminoglycosides & Spectinomycin
AG are given IM or IV only, have
concentration dependent killing, is not
capabale of penetrating the blood brain
barrier, low tissue penetration,
SYNERGISTIC effect with cell wall synthesis
inhibitors due to enhancement of transport
General MOA of all aminoglycosides (AG) is by to the inside of the bacterial cell ;
inhibiting protein synthesis by binding to 30s subunit: nephrotoxicity (reversible - Acute Tubular mechanism of resistance of AG: plasmid-
(1) block formation of the initiation complex (2) Necrosis esp in elderly, if given with mediated formation of inactivating
cause misreading of the code on the mRNA template Amphotericin B, Cephalosporin and enzymes "group transferase" --> catalyze
(3) inhibit translocation, bactericidal ; For serious Vancomycin)), ototoxicity (irreversible), the acetylation of amine functions and the
infections caused by aerobic gram – bacteria (E.coli, neuromuscular blockade (Curare-like block --> transfer of phosphoryl or adenylyl groups
Enterobacter, Klebsiella, Proteus, Providencia, respiratory paralysis. Remedy: Calcium, to the oxygen atoms of the hydroxyl groups
Pseudomonas, Serratia, Haemophilus, Moraxella, Neostigmine and Mechanical Ventilator) ; S. of AG, For Streptomycin, resistance is due
Shigella), endocarditis, ocular infections ; If given pneumoniae is resistant to Gentamicin, to changes in the ribosomal binding site ;
together with Pens, may be used for Listeria, Enterococci is resistant to amikacin, gentamicin, Gentamicin and tobramycin are the most
A. Gentamycin, tobramycin Enterococcus and G+ cocci tobramycin but NOT streptomycin vestibulotoxic and nephrotoxic
 Inhibits protein synthesis by binding to 30s subunit,
bactericidal ; For serious infections caused by aerobic
gram – bacteria (E.coli, Enterobacter, Klebsiella,
Proteus, Providencia, Pseudomonas, Serratia,
Haemophilus, Moraxella, Shigella), endocarditis,
ocular infections, multidrug resistant TB (2nd line) ; Least resistance and narrowest therapeutic
If given together with Pens, may be used for Listeria, nephrotoxicity (reversible), ototoxicity window ; used for streptomycin-resistant
B. Amikacin Enterococcus and G+ cocci (irreversible), neuromuscular blockade TB
hypersensitivity, nephrotoxicity (reversible), Administered intramuscularly ; if given
Inhibits protein synthesis by binding to 30s subunit, ototoxicity (irreversible), neuromuscular together with Pens can be used for
bactericidal ; For TB, tularaemia, bubonic plague, blockade, teratogen (congenital deafness), enterococcal endocarditis, TB plague and
C. Streptomycin brucellosis injection site reactions tularemia

Inhibits protein synthesis by binding to 30s subunit, Limited to topical and oral use due to
bactericidal ; For skin infections, bowel preparations hypersensitivity, nephrotoxicity (reversible), nephrotoxicity, kanamycin is most ototoxic
D. Neomycin, kanamycin, for elective surgeries, hepatic encephalopathy, ototoxicity (irreversible), neuromuscular ; Neomycin has the most skin reactions
paromomycin visceral leishmaniasis (paromomycin) blockade (allergic reactions, contact dermatitis)

Inhibits protein synthesis by binding to 30s subunit,

bactericidal ; For drug-resistant gonorrhoea, nephrotoxicity (reversible), ototoxicity Ototoxcity of AG's can be increased by loop
E. Spectinomycin gonorrhoea in penicillin allergic patients (irreversible), neuromuscular blockade diuretics
Inhibits protein synthesis by binding to 30s subunit, hypersensitivity, nephrotoxicity (reversible), For Treatment of serious infections caused
bactericidal ; For serious infections caused by aerobic ototoxicity (irreversible), neuromuscular by organisms resistant to other
F. Netilmicin gram – bacteria blockade aminoglycosides
Sulfonamides, Trimethoprim & Quinolones
GI upset, mild hepatic dysfunction, acute low solubility in acidic urine causing
hemolysis in G6PD deficiency, nephrotoxicity formation of stones ; Resistance is due to
(precipitate in the urine at acidic pH --> plasmin-mediated (decreased intracellular
Inhibits dihydropteroate synthase, bacteriostatic ; crystalluria, hematuria), hypersensitivity (cross- accumulation of the drug, increased
For burn infections, for G=, G-, Chlamydia and allergenicity with other related drugs such OHAs production of PABA by bacteria, decreased
Nocardia, Simple oral sulfas (UTI), Sulfacetamide and diurectics), exfoliative dermatitis, sensitivity of dihydropteroate synthetase to
(ocular infection, topical), Mafenide and Silver polyarteritis nodosa, SJS, hematotoxicity sulfas and production of dihydrofolate
sulfadiazine (burn infection, topical), Sulfasalazine (granulocytopenia, thrombocytopenia, aplactis reductase that has decreased affnity for
A. Sulfonamides: Silver sulfadiazine, (Ulcerative colitis and RA, oral), Sulfadizaine + anemia), kernicterus ; Drug Interactions: the drug ; sulfonamides are formulated in a
mafenide acetate Pyrimethamine + Folinic acid (Toxoplasmosis, oral) warfarin, methotrexate, bilirubin 5:1 ratio with trimethoprim
i. Short acting: Sulfisoxazole
ii. Intermediate acting:
Sulfamethoxazole
iii. Long acting: Sulfadoxine
 Sequential blockade of dihydropteroate synthase
(sulfamethoxazole) and dihydrofolate reductase
(trimethoprim), bactericidal ; For UTI, respiratory, ear GI upset, acute hemolysis in G6PD deficiency,
and sinus infections (Hemophilus, Moraxella, nephrotoxicity, hypersensitivity, hematotoxicity,
Aeromonas), DOC for P. jiroveci pneumonia and kernicterus ; trimethoprim toxicity: antifolate Sulfonamides are weakly acidic while
B. Combination: Co-trimoxazole Nocardiosis, toxoplasmosis, Back-up for cholera effects (megaloblastic anemia, leukopenia, Trimethroprim is a weak base ; remedy for
(Sulfamethoxazole + Trimethoprim) typhoid fever shigellosis, G- sepsis, MRSA, Listeria granulocytopenia) antifolate effects: Folinic acid supplement
C. Fluoroquinolones Avoid in pregnancy due to absence of safety data

General SE: GI distress, skin rashes, HA,

Inhibits DNA replication by binding to DNA gyrase dizziness, insomnia, increased LFT,
and topoisomerase IV (G+) and Topoisomerase II (G-), phototoxicity, CNS effects (dizziness, headache),
bactericidal, inhibition of Topoisomerase II results in tendinitis and tendon rupture, opportunistic
blockade of relaxation of supercoiled DNA that is infection by Candida and Streptococci ; CI in
catalyzed by DNA gyrase while inhibition of pregnancy and in children (damage growing
Topoisomerase IV interferes with the separation of cartilage --> arthropathy), enhance toxicity of
replicated chromosomal DNA during cell division ; methylxanthines (theophylline) ; Mechanism of General properties of quinolones: good
General use of FQs: For infections of the urogenital resistance for Quinolones: decreased oral bioavailability, high Vd, t1/2 3-8hrs,
and GI tract by G- (gonococci, E. coli, Klebsiela, intracellular accumulation via efflux pumps, absorption is impeded by antacids,
Campylobacter, Enterobacter, Pseudomonas, change in porin structure, chnages in sensitivity elimination is via kidneys by tubular
Salmonella, Shigella), respiratory tract, skin and soft of target enzyme svia point mutations in the secretion (may compete with probenecid
tissue infection ; may be used against meningococcal antibiotic binding region, mutations in the for excretion) EXCEPT for MOXIFLOXACIN ;
i. First Generation Fluoroquinolones: carrier state, for treatment of TB and prophylaxis in quinolone resistance determining region of the Norfloxacin does not achieve adequte
Norfloxacin, Nalidixic acid neutropenic patients gyrA gene that encodes for DNA gyrase plasma levels for use in systemic infections

Inhibits DNA replication by binding to DNA gyrase GI distress, skin rashes, HA, dizziness, insomnia, high resistance esp for C. jejuni, gonococci,
and topoisomerase IV (G+) and Topoisomerase II (G-), increased LFT, phototoxicity, CNS effects G+ cocci like MRSA, Pseudomonas and
bactericidal, bactericidal ; For UTI and GIT infections (dizziness, headache), tendinitis and tendon Serratia ; are used as alternative to
ii. Second Generation (gram – rods, gonococci, gram + cocci), atypical rupture, opportunistic infection by Candida and Ceftriaxone and Cefixime in gonorrhea ;
Fluoroquinolones: Ciprofloxacin, pneumonia (Mycoplasma, Chlamydophila), Streptococci ; CI in pregnancy and in children Ofloxacin can be used against C.
ofloxacin, Enoxacin Norfloxacin Mycobacteria ; increased activity against G- (damage growing cartilage --> arthropathy) trachomatis
 "Respiratory Quinolones" ; Moxifloxacin
and Gemifloxacin are the newest members
of this family and are condisered to have
the broadest spectrum of activity with
increased activity aginst anaerobes ang
atypical agents ; FQ elimination is via
kidneys by tubular secretion (may compete
with probenecid for excretion) EXCEPT
Moxifloxacin ; NEVER use moxifloxacin in
UTI ; Levofloxacin is used in CAP caused by
Chlamydia, Mycoplasma and Legionella ;
Gemifloxacin, Levofloxacin and
Moxifloxacin can prolong QT ; Levofloxacin
has superior activity against G(+) bacteria
Inhibits DNA replication by binding to DNA gyrase including S. pneumoniae ; All have
and topoisomerase IV (G+) and Topoisomerase II (G-), GI distress, skin rashes, HA, dizziness, insomnia, relatively long t1/2 permitting once daily
bactericidal, bactericidal ; For lung infections caused increased LFT, phototoxicity, CNS effects dosing ; Oral absorption is impaired by
iii. Third Generation by gram + cocci, atypical pneumonia (Chlamydia, (dizziness, headache), tendinitis and tendon cations ; Gatifloxacin can cause
Fluoroquinolones: Levofloxacin, mycoplasma) ; less G- activity compared to 2nd gen rupture, opportunistic infection by Candida and hyperglycemia in DM Px and hypoglycemia
Gemifloxacin, Moxifloxacin, but increased activity against G+ cocci, enterococci, Streptococci ; CI in pregnancy and in children in patients also receiving OHA and was
Sparfloxacin MRSA (damage growing cartilage --> arthropathy) withdrawn from the market in 2006 (USA)
GI distress, skin rashes, HA, dizziness, insomnia,
increased LFT, phototoxicity, CNS effects
Inhibits DNA replication by binding to DNA gyrase (dizziness, headache), tendinitis and tendon
and topoisomerase IV (G+) and Topoisomerase II (G-), rupture, opportunistic infection by Candida and
iv. Fourth Generation bactericidal, bactericidal ; has broad spectrum Streptococci ; CI in pregnancy and in children
Fluoroquinolones: Trovafloxacin, activity (gram – and gram +), enhanced activity (damage growing cartilage --> arthropathy) QT additional SE: diabetes (gatifloxacin),
Alatrofloxacin against anaerobes prolongation hepatotoxicity (trovafloxacin)
D. Miscellaneous agents

Reactive reduction by ferredoxin forming free

radicals that disrupt electron transport chain,
bactericidal ; For anaerobic or mixed intra-abdominal
infections, vaginitis (trichomonas, gardnerella), GI irritation, metallic taste, headache, dark
pseudomembranous colitis, brain abscess, protozoal urine, leukopenia, dizziness, ataxia, neuropathy, DOC for amoebiasis, giardiasis and
i. Metronidazole, tinidazole infections seizures and disulfiram reaction Pseudomembranous colitis

Forms multiple reactive intermediates when acted GI irritation, skin rashes, pulmonary infiltrates, single OD dose can prevent recurrent UTI ;
upon by bacterial nitrofuran reductase, bactericidal ; phototoxicity, neuropathies, hemolysis in acidification of urine enhances activity ;
ii. Nitrofurantoin For UTI (except Proteus and Pseudomonas) patients with G6PD deficiency adjust dose in renal patients
Antimycobacterial Drugs
 Most impt drug in TB, prevent
neurotoxicity by giving pyridoxine (vit B6) ;
structural congener of pyridoxine ; high
level resistance due to deletion of KatG
gene whichh codes for catalase-peroxidase
enzyme involved in bioactivation of INH,
hepatotoxicity, neurotoxicity (seizures, low level resistance due to deletion og inhA
Inhibits mycolic acid synthesis, bactericidal ; For TB, peripheral neuritis, insomnia, restlessness, gene which encodes the target enzyme
for latent infection, given as a sole drug for muscle twitching), acute hemolysis in G6PD which is an acyl protein reductase ; Potent
A. Isoniazid (nicotinic acid derivative) prophylaxis of close contacts and skin test converters deficiency, drug-induced lupus CYP450 inhibitor
Potent CYP450 inducer ; rapid development
of resistance if used alone ; resistance is
due to changes of drug sensitivity of the
polymerase enzyme; undergoes
Inhibits DNA-dependent RNA polymerase, enterohepatic recirculation ; orange-
bactericidal ; For TB, leprosy, prophylaxis for colored metabolites ; delay emergence of
meningococcal and staphylococcal carrier states, resistance to dapsone ; Rifabutin is equally
drug-resistant infections (MRSA, PRSP) when given effective as anti-mycobacterial agent with
together with Vancomycin, can be used as sole drug red-orange urine, light chain proteinuria, skin less drug interaction and it is the preferred
in the treatment of latent TB in INH-intolerant rash, thrombocytopenia, nephritis, anti-TB for AIDS patients ; Rifamixin is not
B. Rifamycin derivatives: Rifampicin, patient or in close contact of patients with INH- hepatotoxicity, flulike syndrome, anemia, impair absorbed in the GIT and is used for
rifabutin, rifapentine, rifamixin resistant strains of the organism antibody response traveler's diarrhea
dose-dependent visual disturbances (decreased
visual acuity, red green color blindness, Resistance is due to mutation in emb gene ;
Inhibits arabinosyl transferases involved in the retrobulbar neuritis, retinal damage, optic dose adjustment id needed in renal
synthesis of arabinogalactan in mycobacterial cell neuritis), headache, confusion, hyperuricemia, patients ; always used in combination with
C. Ethambutol (butanol derivative) wall, bacteriostatic ; For TB peripheral neuritis other drugs for TB
Most hepatotoxic anti-TB drug, also known
as sterilizing agent ; require metabolic
conversion via pyrazinamidases in MTb ;
Unknow MOA, bacteriostatic but can be bactericidal hepatotoxicity, nongouty polyarhtralgia, resistance is via mutation in pncA gene
on actively dividing mycobacteria, is metabolozed to asymptomatic hyperuricemia, myalgia, GIT which codes for pyrazinamidases and
pyrazinoic acid, t 1/2 is increased in liver and kidney irritation, maculopapular rash, porphyria, increased efflux systems ; decrease dose in
D. Pyrazinamide (pyrazine derivative) disease ; For TB photosensitivity ; CI in pregnancy hepatic and renal patients
for MDRTB (TB meningitis, miliary TB, severe organ
E. Streptomycin (aminoglycoside) TB) see entry see entry
Drugs for Leprosy
Most active drug against M. leprae ; used in
combination with rifampicin and
GI irritation, fever, skin rashes, clofazimine ; Acedapsone is a repository
Inhibition of folic acid synthesis, bacteriostatic ; For methemoglobinemia, acute hemolysis in G6PD form of dapsone which has drug action that
A. Sulfones: Dapsone, acedapsone leprosy, alternative for PCP pneumonia deficiency patients can last for several months
Binds to guanine bases in bacterial DNA, bactericidal
B. Clofazimine ; For leprosy GI irritation, skin discoloration a phenazine dye
Antifungal Agents
 Control infusion reactions by slowing the
rate of infusion and premedication with
antihistamines, additive nephrotoxicity
with other nephrotoxic drugs
Binds to ergosterol in fungal cell membranes, (aminoglycosides) ; highly lipid soluble,
forming artificial pores, fungicidal, WIDEST antifungal infusion reactions (chills, fever, muscle spasms, poorly absorbed in the GIT ; high Vd except
spectrum ; For systemic fungal infections vomiting, hypotension), dose limiting in the CNS with a t1/2 of 2weeks ;
(aspergillus, blastomyces, candida, Cryptococcus, nephrotoxicity (decreased GFR, ATN with resistance is due to decreased level of
histoplasma, mucor), for initial induction before magnesium and potassium wasting, decreased ergosterol or change in membrane
followup treatment with azoles, can be used topically erythropoietin), neurotoxicity (seizure, neuronal structure ; has the WIDEST antifungal
A. Polyene antifungal: Amphotericin B in mycotic corneal ulcers and keratitis damage) spectrum

Accumulated in fungal cells by the action of

permease and converted by cytosine deaminase to 5- decrease dose in renal patients ; resistance
FU, which inhibits thimidylate synthase, pyrimidine is due to decreased activity of fungal
antimetabolite, fungistatic ; given together with permease and deaminase ; has synergistic
ampho B and Triazoles - For cryptococcal infection, reversible myelosuppresion, alopecia, effect when given with ampho B and
B. Flucytosine systemic candidal infections, chromoblastomycosis hepatotoxicity Triazoles.
C. Azole Antifungals
Limited to topical use because of systemic
toxicity ; narrow antifungal spectrum ;
Inhibit 14α-demethylase --> decreased ergosterol resistance is due to chnages in the
production --> increased permeability of cell sensitivity of target enzyme ; Potent
membrane, Inhibits fungal P450-dependent enzymes GI disturbances (vomiting, diarrhea), rash, CYP450 inhibitor ; Ketoconazole is rarely
blocking ergosterol synthesis, fungistatic ; For chronic hepatotoxicity, drug interaction, gynecomastia, used due to drug interactions and narrow
i. Ketoconazole (Imidazole) mucocutaneous candidiasis, dermatophytosis menstrual irregularities and infertility spectrum

Inhibit 14α-demethylase --> decreased ergosterol

production --> increased permeability of cell
membrane, Inhibits fungal P450-dependent enzymes
blocking ergosterol synthesis, fungistatic ; DOC for
candidiasis (esophageal, oropharyngeal, alternative to Ampho B in the treatment of
vulvovaginitis), coccidioidomycosis, cryptococcal GI disturbances (vomiting, diarrhea), rash, C. neoformans, as effective as Ampho B in
ii. Fluconazole (Triazole) meningitis (treatment and prophylaxis) hepatotoxicity candidemia

Inhibit 14α-demethylase --> decreased ergosterol

production --> increased permeability of cell
membrane, Inhibits fungal P450-dependent enzymes
blocking ergosterol synthesis, fungistatic ; DOC for
blastomycosis, sporotrichosis, dermatophytosis esp
onchomycosis, chromoblastomycosis ; alternative for
infections due to Aspergillus, Coccidioides,
Cryptococcus and Histoplasma , for esophageal GI disturbances (vomiting, diarrhea), rash, may also be used for subcutaneous
iii. Itraconazole (Triazole) candidiasis resistant to fluconazole hepatotoxicity chromoblastomycosis
 Inhibit 14α-demethylase --> decreased ergosterol
production --> increased permeability of cell
membrane, Inhibits fungal P450-dependent enzymes
blocking ergosterol synthesis, fungistatic ; co-DOC for
invasive aspergillosis, alternative in candidemia, for GI disturbances (vomiting, diarrhea), rash,
fluconazole-resistant organisms, for candidal hepatotoxicity, blurring of vision in 30% of
iv. Voriconazole (Triazole) esophagitis and stomatitis in AIDS patients patients, CI in pregnancy wider specturm azole

Inhibit 14α-demethylase --> decreased ergosterol

production --> increased permeability of cell
membrane, Inhibits fungal P450-dependent enzymes
blocking ergosterol synthesis, fungistatic ; For
Candida and Aspergillus, as prophylaxis of fungal BROADEST spectrum triazole ; the only
infection during cancer chemotherapy, salvage GI disturbances (vomiting, diarrhea), rash, azole with activity against Rhizopus sp.
v. Posaconazole (Triazole) therapy in invasive aspergillosis hepatotoxicity (mucormycosis) ; Potent CYP450 inhibitor

Inhibit 14α-demethylase --> decreased ergosterol

production --> increased permeability of cell
membrane, Inhibits fungal P450-dependent enzymes
blocking ergosterol synthesis, fungistatic ; For
vi. Clotrimazole, miconazole, mucocutaneous candidiasis, dermatophytosis, Limited to topical use because of systemic
ketoconazole seborrheic dermatitis, pityriasis versicolor None when administered topically toxicity

Inhibit beta-glucan synthase which produces β(1-->2)

glycan which is a cellwall component, thus
decreasing fungal cell wall synthesis, fungostatic ; For
disseminated and mucocutaneous candidiasis who
D: Echinocandins: Caspofungin, fail to respond to amphoB, for mucormycosis, headache, GI distress, rash, fever, flushing all are given IV ; micafungin can increase
anidulafungin, micafungin salvage therapy for invasive aspergillosis (histamine release), elevated liver enzymes levels of cyclosporine and tacrolimus
headache, mental confusion, GI irritation, given PO ; Accumulates in keratin ; potent
photosensitivity, hepatotoxicity, disulfiram CYP450 inducer ; absorption is increased by
Interferes with microtubule function in reaction, drug interactions (decreases intake of fatty meal ; resistance is due to
dermatophytes, inhibits synthesis and polymerization bioavialability of warfarin) ; contraindicated in decreased transport of drug into the fungal
E. Griseofulvin of nucleic acids, fungistatic ; For dermatophytosis porphyria cell wall

Inhibits withg ergosterol synthesis by inhibiting

fungal squalene oxidase leading to increased given PO and topical, also accumulates in
squalene which interferes with ergosterol synthesis, keratin, more effective than griseofulvin in
F. Terbinafine fungicidal ; For dermatophytosis, onchomycosis GI upset, rash, headache, taste disturbances onchomycosis
 Binds to ergosterol in fungal cell membranes,
forming artificial pores, fungicidal ; For candidiasis
((oropharyngeal, esophageal and vaginal), for GI
fungal infections in patients with impaired defense Minimal mucocutaneous absorption,
G. Nystatin (polyene) mechanisms nephrotoxicity (severe) available as swish and swallow preparation
Antiviral Agents
A. Anti-Herpes
given PO, topical and IV ; dose adjustment
in renal patients ; No activity against strains
Activated by viral thymidine kinase (TK) to forms that of HSV with absent thymidine kinase
inhibit viral DNA polymerase, guanosine analog, activity ; resistance is due to changes in
competitive substrate for DNA polymerase, causes viral DNA polymerase ; Valacyclovir is a
chain termination after its incorporation into the viral prodrug that is converted to Acyclovir and
DNA ; For infections due to HSV1, HSV2, VZV reached plams levels 3-5x (longer t1/2)
(mucocutaneous and genital herpes, prophylaxis in more than acyclovir ; Penciclovir does not
AIDS and in other Immunocompromised states such cause chain termination ; Famciclovir is a
i. Acyclovir, valacyclovir, penciclovir, as organ transplant patients, herpes encephalitis, nausea, diarrhea, headache, delirium, tremor, prodrug which is converted to Penciclovir
famciclovir, docosanol neonatal HSV infection etc. seizures, hypotension, nephrotoxicity in vivo
Inhibits fusion between the HSV envelope and
plasma membrane, prevents viral entry and nausea, diarrhea, headache, delirium, tremor,
ii. Docosanol subsequent replication seizures, hypotension, nephrotoxicity topical preparation shortens healing time
given as IV or intraocular implant (for CMV
retinitis) ; No activity against strains of HSV
with absent thymidine kinase activity ; CMV
Inhibits viral DNA polymerase causing chain resistance is due to mutation in viral DNA
termination, guanosine derivative ; For infections due polymerase and in the genes that code for
to CMV, HSV1, HSV2, VZV ; For prohylaxis and the activating viral phosphotransferase ;
iii. Ganciclovir, valganciclovir (anti- treatment of CMV retinitis and other CMV infections leukopenia, thrombocytopenia, mucositis, Valganciclovir is a prodrug of ganciclovir
CMV) in the immunocompromised patients hepatotoxicity, seizures, neutropenia with increased oral bioavialability
Inhibits viral DNA polymerase causing chain
termination ; For CMV retinitis, mucocutaneous HSV Active against strains of HSV with absent
infections, acyclovir-resistance, ganciclovir- thymidine kinase activity ; resistance is due
resistance, genital warts and molluscum to mutation in DNA polymerase ; dose
iv. Cifodovir (anti-CMV) contangiosum nephrotoxicity adjustment in renal patients

Inhibits viral RNA polymerase, DNA polymerase, and Active against strains of HSV with absent
HIV reverse transcriptase, binds to pyrophosphate thymidine kinase activity ; does not require
binding site ; as alternative for prophylaxis and phosphorylation for antiviral activity ;
treatment of CMV retinitis, gancyclovir-resistant nephrotoxicity, electrolyte abnormalities resistance is due to mutations in DNA
strains of CMV, HSV infection in patients with AIDS, (hypocalcemia), GU ulcerations, CNS effects polymerase gene ; dose adjusment in renal
v. Foscarnet (anti-CMV) also used in organ transplantation (headache, hallucination, seizures) patients
used topically only because it is rapidly
GI irritation, paresthesia, tremor, convulsion, metabolized into the inactive form and
vi. Vidarabine adenine analog ; For HSV, VZV, CMV hepatic dysfunction, CI in pregnancy because it has a toxic potential
 topical only because it is too toxic fo
vii. Idoxuridine, trifluridine pyrimidine analogs ; For herpes keratitis (HSV-1) irritation, blurred vision, photophobia systemic use
injected intravitreally ; concurrent systemic
use of anti-CMV in threapy is
antisense oligonucleotide that binds to mRNA of recommended to protect against
CMV causing inhibition of early protein synthesis ; extraocular and contralateral retinal CMV
viii. Fomivirsen For CMV retinitis iritis, vitritis, increased IOP, changes in vision disease
B. Drugs for HIV
these are prodrugs converted by host cell
Inhibit HIV reverse transcriptase after kinases tp triphosphates causing
phosphorylation by cellular enzymes, acts as chain competitive binding of natural nulecotides
terminators via insertion into the growing DNA chain to the dNTP-binding site of Reverse
; For HIV infection, prevention of maternal-fetal HIV Transcriptase ; resistance is due to
i. NRTI: transmission see specific drugs below mutation in pol gene
good oral bioavailability, T1/2 is 12-24hrs,
a. Abacavir guanosine analog hypersensitivity reaction resistance is slow
acute pancreatitis, peripheral neuropathy, oral bioavailability is decreased by food and
diarrhea, hepatic dysfunction, hyperuricemia, chelating agents ; dose adjustment in renal
b. Didanosine (ddI) NRTI CNS effects patients
aesthenia, GI upset, headache,
hyperpigmentation of palms of soles, CI in
pregnancy, children, renal and hepatic and per orem once a day treatment, dose
c. Emtricitabine NRTI patients adjustment in renal patients
80% oral bioavailability ;may also be used
for Hepa B infection ; HAART, dose
d. Lamivudine (3TC) NRTI GI upset, headache, fatigue, insomnia adjustment in renal patients
peripheral neuropathy esp if given together with good oral bioavailability, dose adjustment
e. Stavudine (d4T) NRTI Zalcitabine, lactic acidosis with hepatic steatosis in renal patients
a nucleotide but acts as NRTI, competitively inhibits
RT, cause chain termination after incorporation into GI upset, asthenia, headache, Fanconi oral bioavailabilty is 25-40% ; halflife is
f. Tenofovir DNA syndrome, AKI 60hours ; also used against HBV
peripheral neuropathy, pancreatitis, esophageal increased oral bioavailability, dose
g. Zalcitabine (ddC) NRTI ulceration, stomatitis, arthralgias adjustment in renal patients
BM suppression (anemia, neutropenia, dose adjustment in uremic patients and
thrombocytopenia), acute cholestatic hepatitis, cirrhosis ; affected by enzymes inducers
h. Zidovudine (ZDV) Azidothymidine or AZT agitation, insomnia, myalgia, headache, GI upset and inhibitors
Inhibits HIV reverse transcriptase, no Delavirdine and Nevirapine (rash, increased
ii. NNRTI: Delavirdine, efavirenz, phosphorylation required, do not compete with AST/ALT, Efavirenz (teratogenicity), Etravirine binds to a different binding site ; resistance
etravirine, nevirapine nucleoside triphosphate ; For HIV infection (increased cholesterol and triglycerides) is due to mutations in pol gene
metabolized by CYP3A4 and CYP2D6,
a. Delavirdine NNRTI rashes, teratogenic affected by enzyme inducer and inhibitor
CNS dysfunction, skin rash, increased plasma enhanced absorption by fatty meals, drug
b. Efavirenz NNRTI cholesterol, teratogenic interactions are common
nausea, vomiting, diarrhea, increased
c. Etravirine NNRTI, for drug-resistant HIV cholesterol, triglycerides and LFTs NEWEST NNRTI
 used as a singledose to prevent HIV vertical
transmission at the onset of labor and also given to
d. Nevirapine the neonate rash, SJS, TEN good oral bioavailability,t1/2 is >24hours
General SE: hyperglycemia, insulin resistance,
hyperlipidemia, altered body fat distribution
(buffalo hump, gynecomastia, truncal obesity,
iii. Protease Inhibitor: Atrazanavir, facial and peripheral lipodystrophy) due to the
Darunavir, Fosamprenavir, Indinavir, cleaves precursor polyprotein to form the final inhibition of lipid-regulating proteins which have
Nelfinavir, Lopinavir-Ritonavir, structural protein of the mature virion core, inhibits active sites with structural homology to that of Resistance is due to mutation in pol gene ;
Saquinavir, Tipranavir viral protein processing ; For HIV infection HIV protease are potent CYP3A4 inhibitor esp Ritonavir
per orem absorption requires acidic
environment ; can penetrate CSF and
seminal fluid ; is not associated with
peripheral neuropathy, skin rash, dyslipidemia, fat deposition or metabolic
a. Atazanavir Protease Inhibitor hyperbilirubinemia, QT prolongation syndrome ; CYP3A4 and 2C9 inhibitor
rash, hepatotoxicity, hypersensitivity ; CI in Given together with Ritonavir in patients
b. Darunavir Protease Inhibitor patients with sulfa allergy resistant to other PIs
GI upset, paresthesia, rash, CI in pregnant
patients and children if drug uses propylene
glycol as solvent ; does not have risk for a prodrug that is converted to the active
hyperlipidemia, fat maldistribution, drug Amprenavir ; absorption is impaired
c. Fosamprenavir Protease Inhibitor hyperglycaemia and insulin resistance by fatty food ; used with lowdose Ritonavir
nausea, vomiting, diarrhea, thrombocytopenia, decreased bioavailability in the presence of
hyperbilirubinemia, nephrolithiasis, insulin food ; affected by enzyme inhibitors and
d. Indinavir Protease Inhibitor resistance inducers
used as a combination drug: uses subtherapeutic there is increased compliance with this
dose of ritonavir which inhibits CYP3A4 mediated drug ; Ritonavir has “boosting effect” on
e. Lopinavir-Ritonavir metabolism of lopinavir GI upset (well-tolerated side effects) other PI due to enzyme inhibitory effect
absorption is increased by food, short half-
life ; has the most favorable safety profile
f. Nelfinavir Protease Inhibitor Diarrhea for pregnancy
Protease Inhibitor ; subtherapeutic doses inhibit
CYP3A4-mediated metabolism of other Pis (Indnavir, good oral bioavailability esp when taken
Lopinavir, Saquinavir) which permits lower dose of GI upset, bitter taste, paresthesia, increased with meals ; affected by enzyme inducer
g. Ritonavir the other PI LFT's and inhibitors
Protease Inhibitor ; given together with low dose
Ritonavir to improve compliance and decrease GI
h. Saquinavir upset nausea, vomiting, diarrhea, dyspepsia, rhinitis affected by enzyme inducers and inhibitors
newer drug ; induces P-glycoprotein
Protease Inhibitor ; given with Ritonavir for PI- transporters which leads to alteration of GI
i. Tipranavir resistant HIV GI upset, rash, hepatotoxicity absorption of other drugs
iv. Entry inhibitors:
 Binds to gp41 subunit of viral envelope glycoprotein,
preventing fusion of viral and cellular membranes ;
a. Fusion Inhibitor: Enfuvirtide, For previously drug-treated patients with persistent injection site reaction, hypersensitivity reaction, subcutaneous and usually given together
Docosanol HIV replication despite ongoing therapy increased incidence of bacterial pneumonia with other HIV agents
Blocks viral attachment by blocking CCR5, a
b. CCR5 receptor antagonist: transmembrane protein involved in the attachment cough, diarrhea, muscle and joint pains, good tissue penetration ; affected by
Maraviroc of HIV to host cell ; For HIV infection increased LFTs enzyme inhibitors and inducers
C. Drugs for Influenza
Amantadine is also used in treating
parkinsonism ; should be given within
48hrs of exposure ; Rimantadine has longer
Inhibit early step replication and prevent uncoating halflife and doe snot need dose-adjustment
i. Uncoating inhibitors: Amantadine, by binding to M2 proton channels ; For influenza A GI irritation, dizziness, cerebellar dysfunction for renally-impaired Px ; there is increased
rimantadine and rubella (ataxia, dysarthria), livedo reticularis resistance observed with amantadine
DOC for influenza (including H1N1) ;
Oseltamivir is PO while Zanamivir is
Inhibits neuraminidase which cleaves sialic acid intranasal ; Peramivir has been given
residues from viral proteins and surface proteins of GI effects (Oseltamivir), bronchospasm in temporary emergency use authorization by
ii. Neuraminidase inhibitors: infected cells , decrease release of progeny virus ; For asthmatics and cough with throat discomfort US FDA for H1N1 in 2009 but has not yet
Oseltamivir, Zanamivir, Peramivir influenza A and B, shortens duration of symptoms (Zanamivir ) been licensed by the US FDA
D. Drug for HBV and HCV

cytokine, increased activity of JAKS leading to

phosphorylation of signal transducers and activation
of transcription (STATS) which causes increased
formation of antiviral proteins , also increases NK
cells that destroy infected liver cells, Degrades viral
RNA via activation of host cell RNAse (ribonuclease) ; alopecia, myalgia, severe depression, flu-like
For chronic HBV, HCV infection, Kaposi sarcoma, syndrome, thyroid dysfunction, reversible slow absorption, given IM or SC once a day
genital warts, prevents dissemination of HZV in hearing loss, neutropenia ; Contraindications 3x week but the PEG-form is only given
cancer patients and decreased CMV shedding after include autoimmune disease, history of cardiac once a week, given topically for genital
i. Interferon-α renal transplantation arrhythmia and pregnancy warts
Dipiroxil is a prodrug of Adefovir ;
Telbivudine is a newer drug (nucleoside
Inhibits HBV DNA polymerase causing chain analog) but develpoment of resistance is
termination after incorporation into the viral DNA ; rapid, it is as effective as lamivudine ;
For lamivudine-resistant Hepatitis B infection, Tenofovir is an anti-RT drug that is also
ii. Adefovir, Dipivoxil, Telbivudine, suppresses HBV replication and improves liver Lactic acidosis, renal toxicity, severe effective in chronic HBV, it is active against
Tenofovir histology and fibrosis hepatomegaly with steatosis lamivudine and entecavir-resistant strains
is as effective as lamivudine, longer t1/2 of
iii. Entecavir guanosine nucleoside, inhibits DNA polymerase headache, dizziness, fatigue, nausea 12hrs
Coinfection between HBV and HIV may
see entry, also active for HBV, rapidly suppresses increase the risk of pancreatitis with
iii. Lamivudine (3TC) HBV replication see entry lamivudine use ; longer t1/2 in HBV
 infected cells than in HIV (lower dose
required in HBV than in HIV)

Inhibits guanosine triphosphate formation, prevents

capping of viral mRNA, blocks RNA-dependent RNA
polymerase, inhibit replication of many DNA and RNA given PO, IV or aerosol, avoid concomitant
viruses like Influenza A and B, parainfluenza, administration of anatcids ; Early IV
paramyxo viruses, HCV and HIV ; For HCV infection administration of ribavirin decreases
(with IFN-α) and RSV infection, decreases mortality in haemolytic anemia, conjunctival and bronchial mortality in viral hemorrhagic fevers ;
iii. Ribavirin viral hemorrhagic fevers irritation, teratogen monotherapy is NOT effective
Antiprotozoal Drugs
A. Antimalarial drugs

accumulates in the food vacuole of plasmodia —>

Prevents polymerization of heme into hemozoin —> May precipitate porphyria ; Chloroquine is
inc heme concentration which is toxic to the parasite, 4-aminoquinoline derivative, can be given
Blood schizonticide ; For malaria (non-falciparum, PO and has high Vd, absorption is decrease
chloroquine-sensitive), DOC for acute attacks of non- by antacids ; resistance is due to dec.
Falciparum and sensitive Falciparum malaria, used as GI irritation, skin rash, headache, severe skin intracellular accumulation via inc activation
chemoprophylaxis except in regions where P. lesions, peripheral neuropathies, myocardial of membrane pumps, dec intravacuolar
falciparum is resistant, for autoimmune diseases such depression, retinal damage, auditory accumulation via transporter encoded by
i. Chloroquine, hydroxychloroquine as rheumatoid arthritis, amoebic liver abscess impairment, psychosis pfcrt gene

Complexes with double stranded DNA to prevent

strand separation —> blocks DNA replication and
transcription to RNA, blood schizonticide ; For
malaria (chloroquine-resistant) and severe cinchonism (headache, tinnitus, vertigo), Quinine is commonly used with doxycycline
falciparum malaria (quinidine), given together with hemolysis in G6PD deficiency, blackwater fever, or clindamycin to limit toxicities, PO and IV
Doxycycline and or Clindamycin to shorten duration blurring of vision, GI upset, disturbance n (in severe infection) ; NEVER use as
ii. Quinine, Quinidine gluconate of disease cardiac conduction ; CI in pregnancy prophylaxis

Unknown MOA, blood schizonticide ; For

chemoprophylaxis (chloroquine-resistant areas) ; 1st
line drug (weekly administration) for prophylaxis in
all areas with Chloroquine resistance), alternative to GI distress, skin rash, headache, dizziness,
quinine in acute attacks and uncomplicated cardiac conduction defects, psychiatric disorders
iii. Mefloquine infections from falciparum malaria (psychosis), neurologic symptoms, seziures is a 4-quinoline derivatives, PO
 8-aminoquinoline, Forms quinoline-quinone
metabolites which are electron-transferring redox
compounds that act as cellular oxidants, tissue
schizonticides, gametocides ; For malaria, eradicates
liver stages of P. vivax and P. ovale (radical cure of P. Eradicates hypnozoites in the liver,
vivax and P. ovale), alternative as primary GI distress, pruritus, headaches, preventing malarial relapse, PO , should be
prevention, terminal prophylaxis (vivax, ovale), PCP methemoglobinemia, hemolysis in G6PD used with a blood schizonticide, 14-day
iv. Primaquine pneumonia deficient patients ; CI in pregnancy course of Tx after Tx with choloroquine

Atovaquone disrupts mitochondrial electron

transport, blood and tissue schizonticide, proguanil
inhibits folate synthesis, sporonticide ; For treatment also effective against Mefloquine-resistant
and chemoprophylaxis of chloroquine-resistant Falciparum infection ; Proguanil has a t1/2
falciparum, protective vs. Mefloquine-resistant abdominal pain, nausea, vomiting, diarrhea, 12-16h ; Atovaquone is an alternative for P.
v. Atovaquone-proguanil falciparum headache, rash, increased liver enzymes jiroveci infection
Sequential blockade of folic acid synthesis
(sulfadoxine blocks Dihyrodpteroate synthetase, GI disturbances, teratogen (enamel dysplasia
Pyrimethamine blocks Dihydrofolate reductase, and discoloration), hepatotoxicity,
vi. Sulfadoxine-pyrimethamine blood schizonticide and sporonticide ; For malaria nephrotoxicity, photosensitivity, t1/2 is usually >100h, PO, highly protein
(Fansidar) (for Chloroquine-resistant) vestibulotoxicity, hemolysis bound ; pyrimethamine is a sporonticide
Impairs progeny of malarial apicoplast genes, GI disturbances, teratogen (enamel dysplasia
resulting in abnormal cell division, blood and discoloration), hepatotoxicity,
schizonticide ; For chemoprophylaxis in multi-drug nephrotoxicity, photosensitivity, Do not drink with milk (decreased
vii. Doxycycline resistant strains vestibulotoxicity absorption), PO
Lumefantrine used in combination with
artemether (Co-arthem) for uncomplicated
Unknown MOA, active vs the erythrocytic stage of all falciparum infection ; Halofantrine is never
4 strains including Chloroquine-resistant, blood abdominal pain, diarrhea, vomiting, cough, rash, used for prophylaxis because of
schizonticide ; For chloroquine-resistant malaria and headache, pruritus, elevated liver enzymes, cardiotoxicity and embryogenecity,
viii. Halofantrine , lumefantrine severe falciparum malaria cardiotoxicity, teratogen Lumefantrine has minimal cardiotoxicity
Co-artem is the DOC for uncomplicated
falciparum malaria in the Philippines ;
Combination therapy of artemesinins with
one or two long-acting antimalarial drugs
(amodiaquine, mefloquine,
sulfadoxine/pyrimethamine or
lumefantrine) is favored to retard the
development and progression of drug
is metabolized in the food vacuole of protozoa —> resistance in P. falciparum ; not given as
Forms toxic free radicals in malarial food vacuole, Prophylaxis due to short t1/2 (1-3h) ; the
ix. Artemsinin, artesunate, blood schizonticide ; For malaria (falciparum and only reliably effective meds vs Quinine-
artemether, dihydroartemsinin MDR strains) nausea, vomiting, diarrhea ; SAFE in pregnancy resistant strains

MOA same as chloroquine (inhibits the digestion of low-cost, given as combination with
x. Amiodaquine hemoglobin) ; For chloroquine-resistant falciparum agranulocytosis, aplastic anemia Artesunate
B. Anti-amoebiasis
 Unknown MOA, converted to Diloxanide freebase
(active amobecide), luminal amebicide ; DOC for converted in vivo into Diloxanide freebase
i. Diloxanide Furoate asymptomatic cyst carrier of E. histolytica flatulence, nausea, abdominal cramps which is the amoebicide
Inhibits protein synthesis by blocking ribosomal Reserved only for situations where
movement along messenger RNA, tissue amebicide ; metronidazole can’t be used , given SC or
back up drug for severe intestinal, hepatic and GI distress, muscle weakness, CV dysfunction IM , usually given together with luminal
ii. Emetine, dehydroemetine extraintestinal amebiasis (arrhythmias and CHF) amebicides
halogenated hydroxyquinoline, Unknown MOA, GI distress, thyroid enlargement, skin reactions
luminal amebicide ; Alternative to Diloxanide for mild due to iodine toxicity, neurotoxicity (peripheral Usually used in combination with
ii. Iodoquinol to severe intestinal amebiasis neuropathy, visual dysfunction) metronidazole, PO

given PO, IV or topical, Metronidazole t1/2

Reactive reduction by ferredoxin forming free is 6-8h, Tinidazole t1/2 is 12-14h; dose
radicals that disrupt electron transport chain, tissue adjustment in renal patients, well
amebicide ; DOC for severe intestinal wall disease distributed even in CSF ; active against
and in hepatic abscess and other extra intestinal GI irritation, metallic taste, headache, dark protozoan and bacteria (Bacteroides and
amebic disease, DOC for trichomoniasis, also used for urine, leukopenia, dizziness, ataxia, neuropathy, Clostridium, DOC for Pseudomembranous
iii. Metronidazole, Tinidazole, giardiasis, bacterial vaginosis (Gardnerella vaginalis), seizures, disulfiram reaction, opportunistic colitis) ; causes potentiation of warfarin
Secnidazole anaerobic infections, H. pylori PUD infections, parestheisa, CI in pregnancy action ; bets taken with meals
may be given together with tetracycline in
An aminoglycoside, Inhibits protein synthesis, binds mild intestinal disease ; superior to
to 16S ribosomal subunit, luminal amebicide ; For Diloxanide in asymptomatic carries but SE
iv. Paromomycin intestinal amebiasis, cryptosporidiosis headaches, dizziness, rashes, arthralgia limits its use
Reactive reductions by ferredoxin forming free
radicals that disrupt electron transport chain, tissue
amebicide ; For metronidazole-resistant amebiasis,
v. Nitazoxanide giardiasis, cryptosporidiosis (DOC) GI distress may also be used in helminthic infections
C.Drugs for Pneumocystis and
Toxoplasmosis
Sequential blockade of dihydropteroate synthase
(sulfamethoxazole) and dihydrofolate reductase
(trimethoprim), bactericidal ; DOC for prophylaxis GI upset, acute hemolysis in G6PD deficiency,
and treatment of Pneumocystosis, prophylaxis (T. nephrotoxicity, hypersensitivity, hematotoxicity, Recommended at CD4 count < 200, given
i. Co-trimoxazole gondii, I. belli) kernicterus daily, PO or IV

Unknown MOA but may involve inhibition of respiratory stimulation followed by depression,
glycolysis or interference with NA metabolism of hypotension, hypoglycaemia, anemia, Administered by nasal spray/aerosol, given
Protozoans and Fungi ; For prophylaxis and neutropenia, hepatitis, pancreatitis, inhalant once a month if used for prophylaxis, IV or
ii. Pentamidine treatment of pneumocystosis and trypanosomiasis route has minimal SE IM for 21 days if for Tx of active disease
gastric irritation, glossitis, neurologic symptoms an alternative drug for Toxoplasmosis is
Sequential blockade of dihydropteroate synthase (headache, insomnia, tremors, seizures), Clindamycin ,give daily for 3-4 weeks if for
(sulfadiazine) and dihydrofolate reductase hematotoxicity (megaloblastic anemia, Tx of active toxoplasmosis , if for
(pyrimethamine) ; DOC for prophylaxis and thrombocytopenia), pseudomembranous colitis Toxoplasma encephalitis, give for at least 6
iii. Pyrimethamine-sulfadiazine treatment of toxoplasmosis (clindamycin) weeks
 Atovaquone disrupts mitochondrial electron
transport ; For mild to moderate PCP, as
chemoprophylaxis for Chloroquine resistant malaria abdominal pain, nausea, vomiting, diarrhea, has increased absorption in the presence of
iv. Atovaquone (with Proguanil) fever, increased liver enzymes food, PO
D. Drugs for Trypanosomiasis
Unknown MOA but may involve inhibition of
glycolysis or interference with NA metabolism of respiratory stimulation followed by depression,
Protozoans and Fungi ; For hemolymphatic stage of hypotension, hypoglycaemia, anemia, do not use for latter stages because it does
T. gambiense and T. rhodiense, For prophylaxis and neutropenia, hepatitis, pancreatitis, inhalant not cross the BBB, also used for Kala-azar
i. Pentamidine treatment of pneumocystosis route has minimal SE and PCP
fatigue, nausea, vomiting, seizures, shock fever,
Polyanionic compound, Unknown MOA ; DOC for rash, headache, paresthesia, neuropathies, renal
early hemolymphatic stages of African sleeping abnormalities (proteinuria), chronic diarrhea, Do not cross blood brain barrier , Used in
ii. Suramin sickness, Alternative to Ivermectin in onchocerciasis haemolytic anemia and agranulocytosis combination with melarsoprol
Suicide inhibitor of ornithine decarboxylase ; DOC for diarrhea, vomiting, anemia, thrombocytopenia,
iii. Eflornithine advanced west African sleeping sickness leukopenia, seizures Crosses blood brain barrier, PO, IV
Organic arsenical, inhibits enzyme sulfhydryl (-SH)
groups in trypanosomes ; DOC for African sleeping Crosses BBB, administered parenterally
iv. Melarsoprol sickness GI irritation, reactive encephalopathy because it causes GI upset

Nitrofurazone derivative, Inhibits trypanothione

reductase which is unique to the parasite ; DOC for
Chagas disease / American Sleeping sickness
(Trypanosoma cruzi), alternative for African sleeping nausea, vomiting, fever, rash, restlessness,
v. Nifurtimox sickness, also for mucocutaneous leishmaniasis insomnia, neuropathies, seizures Does not cross BBB
Drugs for Leishmaniasis
IV ; alternative for leishmaniasis are as
follows: Pentamidine or Miltefosine (for
visceral leishmaniasis), Fluconazole or
Metronidazole (for cutaneous
Pentavalent antimony, Inhibits glycolysis or effects GI symptoms, fever, rash, arthralgia, healdache, leishmaniasis) and Amphotericin B (for
vi. Sodium Stibogluconate on NA metabolism ; DOC for Leishmaniasis myalgia, sterile abscesses, cardiotoxicity mucocutaneous leishmaniasis)
Anthelmintics

Selectively inhibits microtubule synthesis and glucose

uptake in nematodes, ovicidal ; Whipworm infections Greatly affected by enzyme inducers and
(drug of choice), Also a primary drug (together with inhibitors ; Contraindicated in pregnancy,
albendazole) for ascariasis, pinworm, Trichinosis, GI irritation, agranulocytosis, alopecia, Elevated Use cautiously in patients with Cirrhosis
A. Mebendazole Visceral larval migrans (backup) liver enzymes and children <2y.o.
 primary drug for ascariasis,
ancylostomiasis, trichuriasis ; safety in
Inhibits microtubule assembly, larvicidal and ovicidal pregnant and children is not yet
; DOC for Ascariasis, Hookworm, Pinworm, Hydatid established ; Improved penetration (>
disease ; Also used for Whipworm infections, Praziquantel) of the subarachnoid space in
Cutaneous & Visceral Larva migrans, Cysticercosis Neurocysticersosis
(larval stages of T. solium), Angiostrongylus reversible leukopenia, alopecia, elevation of Should not be given to patients with
B. Albendazole cantonensis, Capillaria philippinensis liver function tests, bone marrow suppression Cirrhosis

Immobilizes microfilariae by an unknown mechanism headache, malaise, weakness, anorexia, filarial

—> inc susceptibility to host defense mechanism ; fever (fever, rashes, ocular damage, joint and May cause mazzotti reaction when used for
C. Diethylcarbamazine DOC for filariasis and eye worm disease (Loa-Loa) muscle pain, lymphangitis) onchocerciasis
Intensifies GABA-mediated neurotransmission in Antidote for Mazzoti reaction:
nematodes —> immobilizes parasites —> removal by Mazzotti reaction (fever, headache, dizziness, antihistamine and NSAIDs ; CI in pregnancy,
reticuloendothelial system ; Used for Strongyloidiasis rashes, pruritus, tachycardia, hypotension, pain children 5 y.o. and Avoid concomitant use
(drug of choice), Onchocerciasis, Cutaneous larva in muscles and joints and lymph glands), corneal with other drugs that enhance GABA
D. Ivermectin migrans, Filariasis (back up) opacities activity (Barbituraates, BZDs etc)

Stimulates nicotinic receptors at NMJ of nematodes

—> depolarization-induced paralysis, Causes release
of ACh and inhibition of Cholinesterase, Kills adult
worms not eggs ; DOC for pinworm, may be used also Contraindicated in patients with hepatic
for Hookworm, Trichostrongylus and Ascaris GI distress headache, weakness, dizziness, dysfunction (may cause an increase in LFT) ;
E. Pyrantel pamoate infections insomia, rash, fever, No study on pregnant and children <2y.o.

Structural congener of Mebendazole, same MOA as

Mebendazole, Selectively inhibits microtubule Gastrointestinal irritation, Headache, Dizziness,
synthesis and glucose uptake in nematodes, Inhibits Drowsiness, Leukopenia, Hematuria,
fumarate reductase. Ovicidal, has anti-inflammatory Hypersensitivity reactions (SJS), Hepatotoxicity
and immunosuppressive action in the host ; Used for (intrahepatic cholestasis, liver failure), Reactions CI in renal and liver disease and in
F. Thiabendazole Trichinosis (drug of choice), Strongyloidiasis (backup) caused by dying parasites pregnancy

Increases membrane permeability to calcium —>

contraction of trematode and cestode muscle —>
muscle paralysis, vacualization and death ; DOC for
trematodes (schistosoma, paragonimus, clonorchis, Used with steroid when treating
opistorchis, Fasciolopsis, Heterophyes) and cestodes neurocysticercosis to dec swelling ,
(taenia, diphyllobothrium, Hymenopelsis) together contraindicated in ocular cysticercosis (may
with Niclosamide ; for infection by small and large cause irreparable eye damage) ; May be
intestinal flukes ; alternative to Albendazole in headache, dizziness, nausea, malaise, Inc ICP, used as an adjunct to Albendazole in
G. Praziquantel Cysticerci seizure (neurocystecercosis) ; CI in pregnancy Hydatid disease
 Uncouples oxidative phosphorylation or by activating
ATPases, scoleces and segments are killed but NOT
Ova ; alternative drug to Praziquantel for cestode
infection (Taenia, Diphyllobotrium), not effective in
cystecercosis (use Albendazole or Praziquantel
instead) or Hydatid disease (use Albendazole), Avoid ethanol consumption for 48 hours
effective in the Tx of infections from small and large upon drug consumption ; Safety in children
H. Niclosamide intestinal flukes GI distress, headache, rash, fever <2y.o. and pregnanct not yet established
GABA agonist —> paralyze ascaris —> expelled by
normal peristalsis , block ACh at the myoneural Contraindicated in pregnancy, impaired
junction --> expulsion via normal peristalsis ; As renal or hepatic function or with a history
I. Piperazine alternative for ascariasis GI upset of epilepsy or chronic neurologic disease
Unknown MOA ; co-DOC (with Triclabendazole) for
Tx of Fascioliasis (sheep liver fluke), as alternative for Nausea,vomiting, diarrhea, abdominal cramps,
J. Bithionol paragonimiasis phototoxicity, rash do not use in Px <8y.o.
an organophosphate prodrug —> Dichlorvos (AchE
inhibitor) -> muscle contraction —> paralysis ; Active
K. Metrifonate vs Schistosoma haemoatobium Excess cholinergic stimulation (DUMBBELSS) CI in pregnancy
GI upset, pruritus, eosinophilia, urticaria,
pulmonary infiltrates, fever, orange-red
effective solely in Schistosoma mansion (intestinal discoloration of urine ; CI in pregnancy and
bilharziasis) - on male immature forms and adult seizure disorder, proteinuria, microscopic Px is not allowed to drive within 24hrs after
L. Oxamniquine schistosomal forms ; MOA is unknown hematuria, intake of Oxamniquine
Cancer Chemotherapy

all are Cell-cycle non-specific ; Universal MOA: form

reactive molecular species that alkylate nucleophilic
groups on DNA bases, particularly the N-7 of guanine Resistance is due to increased DNA repair,
leading to cross-linking of bases, abnormal base decreased drug permeability and
A. Alkylating agents pairing and DNA strand breakage production of trapping agents such as thiols

Forms DNA cross-links, resulting in inhibition of DNA

synthesis and function, Cell-cycle nonspecific, bone marrow suppression, hemorrhagic cystitis,
Mechlorethamine has additional MOA: converts to a hepatotoxicity, alopecia, SIADH, pulmonary Rescue therapy is MESNA and hydration;
i. Nitrogen Mustards: reactive cytotoxic product ; For non-hodgkin’s toxicity, cardiac dysfunction ; Mechorethamine metabolite is acrolein which is important
Cyclophosphamide, Chlorambucil, lymphoma, breast cancer, ovarian cancer, SE include marked vesicant action, sterility, for Cyclophosphamide’s anti-cancer effect
Mechlorethamine neuroblastoma, CLL myelosuppresion, alopecia and also its toxicity

Forms DNA cross-links, resulting in inhibition of DNA IV, Rescue therapy is Amifostine, decreased
synthesis and function, Cell-cycle nonspecific ; nephrotoxicity by giving mannitol with
component of regimen For testicular cancer, ovarian nausea, vomiting, nephrotoxicity, neurotoxicity forced hydration ; Carboplatin is less
ii. Platinum Analogs: Cisplatin, cancer, bladder cancer and lung cancer ; Oxaliplatin (peripheral neuritis), ototoxicity (acoustic nerve nephrotoxic but has more
Carboplatin, oxaliplatin is used also for advanced colon CA damage), hematotoxicity myelosuppression
 Forms DNA cross-links, resulting in inhibition of DNA
synthesis and function, Cell-cycle nonspecific ; For pulmonary fibrosis, adrenal insufficiency, skin
iii. Alkyl sulfonate: Busulfan CML pigmentation Spares the bone marrow

Forms DNA cross-links, resulting in inhibition of DNA CNS toxicity (dizziness, ataxia), nausea and
iv. Nirtosoureas: Carmustine, synthesis and function, Cell-cycle nonspecific ; For vomiting, bone marrow suppression, skin Highly lipophilic allowing ease of passage
lomustine brain tumors, melanoma, skin cancer flushing through BBB into the CNS
a reactive agent which forms hydrogen peroxide,
which generates free radicals that cause DNA strand
scission, cell cycle non-specific ; component of bone marrow suppression, pulmonary toxicity, PO, can pemetrate the CSF,
reigned For Hodgkin’s lymphoma, non-hodgkin’s hemolysis, disulfiram reaction,skin reactions, LEUKEMOGENIC, CPY450 inhibitor,
v. Others: Procarbazine, Dacarbazine lymphoma, brain tumors peripheral neuropathy, CNS dysfunction Dacarbazine is phototoxic
all are cell-cycle specific , they also have
B. Antimetabolites immunosuppressant action
PO, IV, Rescue therapy is Leucovorin
(Folinic acid) ; cytotoxic due to formation of
polyglutamate derivatives ; resistance is
Inhibits dihydrofolate reductase, decreases synthesis due to decreased drug accumulation,
of thymidylate, amino acids, purine nucleotides —> changes in drug sensitivity or activity of
interfere with NA and CHON metabolism ; cell cycle DHF reductase and decreased formation of
specific ; For choriocarcinoma, acute leukemia, non- polyglutamates ; clearance is dependent on
hodgkin, primary CNS lymphoma, breast cancer, renal function therefore adequate
head and neck cancer, bladder cancer ; also for bone marrow suppression, pulmonary infiltrates hydration is important to prevent
i. Folate antagonist: Methotrexate psoriasis, rheumatoid arthritis, ectopic pregnancy and fibrosis, mucositis, crystalluria, hepatotoxic crystallization into stones

are activated by hypoxanthie-guanine 6-MP metabolism inhibited by allopurinol

phosphoribosyltransferase (HGPRT) to toxic and febuxostat , Resistance is due to
nucleotides which inhibit enzymes in purine decreased activity of HGPRT, increased
ii. Purine antagonist: 6- metabolism —> Inhibits de novo purine nucleotide alkaline phosphatase activity (which
Mercaptopurine, 6-thioguanine, synthesis , cell cycle specific ; For acute leukemia bone marrow suppression, hepatic dysfunction inactivates the toxic nucleotide) , undergo
fludarabine, cladribine (AML, ALL), CML (necrosis, jaundice, cholestasis) significant FPE (by xanthine oxidase)
IV, can distribute to CSF, causes
converted to 5-fluoro-2’-deoxyuridine-5’- “thymineless” death of cells, Resistance is
monophosphate (5-FdUMP) which Inhibits due to decreased activation of 5-FU,
thymidylate synthase, incorporation inhibits DNA increase thymidylate synthase activity and
synthesis and function, cell cycle specific ; For decreased sensitivity of this enzyme ;
bladder cancer, breast cancer, colorectal cancer, anal another metabolite is 5-florouridine-
cancer, head and neck cancer, liver cancer and 5’triphosphate (FUTP) which incorporates
iii. Pyrimidine antagonist: 5- ovarian cancer, topically for keratoses and superficial into RNA —> interfere with RNA processing
Fluorouracil basal cell skin cancer bone marrow suppression, GI irritation, alopecia and function

a cytosine arabinoside, activated by kinases to Ara-

Cytidine Triphosphate (AraCTP) which Inhibits DNA
polymerase —> inhibition of DNA synthesis and Most specific for the S-phase of the cell
repair, inhibits ribonucleotide reductase with cycle, Resistance is due to decreased
iv. Pyrimidine antagonist: Cytarabine reduced formation of dNTPs, cell cycle specific ; For GI irritation, bone marrow suppression, uptake and decreased conversion to
(ARA-C) AML, ALL, CML neurotoxicity AraCTP, a cytosine arabinoside
 a deoxycytidine analog, converted to Gemcitabine
diphosphate which inhibits ribonucleotide reductase
with reduced formation of deoxyribonucleotide
triphosphate required for DNA synthesis,
Gemcitabine triphosphate is incorporated into DNA
causing chain termination, cell cycle specific ; For
v. Pyrimidine antagonist: pancreatic cancer, bladder cancer, non-small cell lung bone marrow suppression, neutropenia,
Gemcitabine cancer, non-Hodgkins lymphoma pulmonary toxicity a deoxycytidine analog
C. Natural Anticancer Drugs all are cell-cycle specific

Prevents assembly of tubulin dimers into microtubule

assembly blocking the formation of mitotic spindles,
causes cell arrest at metaphase, cell cycle specific ;
For acute leukemias, lymphomas, wilms tumor and
neuroblastoma ; Vinblastine For lymphomas, IV, highly distributed except in CSF, Acts
neuroblastomas, testicular carcinoma and Kaposi primarily in M phase of cancer cell cycle,
i. Vinca alkaloid: Vincristine, sarcoma ; Vinorelbine For non-small cell lung cancer Neurotixicity (areflexia, peripheral neuritis, Resistance is due to increased efflux of
Vinblastine, Vinorelbine and breast cancer paralytic ileus) drugs via membrane drug transporter

Induces DNA breakage by inhibiting DNA

topoisomerase II, inhibits mitochondrial electron
transport, cell cycle specific ; Combination regimen
For lung cancer, prostate cancer, testicular cancer, PO, high Vd ; dose adjustment in renal
ii. Podophyllotoxin: Etoposide, non-hodgkin’s lymphoma, germ cell and gastric patients ; Act on the Late S and early G2
Teniposide cancer bone marrow suppression, alopecia, GI distress phase
Inhibits DNA topoisomerase I which cute and
relegates single DNA strands during normal DNA
repair, cell cycle specific; For advanced ovarian
iii. Camptothecins: Topotecan, cancer (2nd line), small cell lung cancer, Irinotecan Irinotecan can be used for metastatic
Irinotecan For metastatic colorectal cancer bone marrow suppression, diarrhea colorectal cancer

Interferes with mitotic spindle synthesis by

preventing microtubule disassembly into tubulin
monomers, cell cycle specific ; For solid tumors - Paclitaxel (neutropenia, thrombocytopenia,
advanced breast and ovarian cancer, lung cancer, peripheral neuropathy, hypersensitivity),
gastroesophageal cancer, prostate cancer, bladder Docetaxel (neurotoxicity, bone marrow
iv. Taxanes: Paclitaxel, Docetaxel cancer, head and neck cancer suppression) Act on M phase
D. Antitumor antibiotics
 Intercalates between base pairs, inhibits
topoisomerase II, generates free radicals, blocks
synthesis of RNA and DNA causing DNA strand
scission, causes membrane disruption, cell cycle non-
specific ; Doxorubicin For Hodgkins and Non-
Hodgkins lumphoma, myelomas, sarcomas, breast
cancer, endometrial cancer, lung cancer, ovarian
cancer and thyroid cancer ; Daunorubicin For acute
leukemias Idarubicin For AML, Epirubicin For breast
i. Anthracycline: Doxorubicin, cancer and gastroesophageal ; Mitoxantrine For
Daunorubicin, Idarubicin, Epirubicin, acute myeloid leukemias, Non-Hodgkins lymphoma, alopecia, nausea, vomiting, Cardiotoxicity Rescue therapy is Dexrazoxane and
Mitoxantrone breast and gastroesophageal cancer (dilated cardiomyopathy, CHF) liposomal formulation of the drug

Generated free radicals which bind to DNA and

causes DNA strand breaks leading to inhibition of
DNA synthesis, intercalates with DNA, cell cycle
specific ; Component of regimens in Hodgkins
lymphoma and testicular cancer, lymphomas and pneumonitis, pulmonary fibrosis, alopecia, IV, inactivated by tissue aminopeptidases,
squamous cell cancer, head and neck cancer, skin mucocutaneous reactions, hypersensitivity Most specific for the G2 phase of cell cycle,
ii. Bleomycin cancer reactions a glycopeptide
Binds to double stranded DNA, inhibits DNA-
dependent RNA synthesis, cell cycle non-specific ; For
melanoma, wilm’s tumor, choriocarcinoma, Kaposi bone marrow suppression, skin reactions, GI
iii. Actinomycin D sarcoma irritation None

Metabolized into an alkylating agent that cross-links

DNA ; In combination regimens for adenocarcinoma severe myelosuppression, toxic the heart, liver,
iv. Mitomycin C of the cervix, stomach, pancreas and lungs lungs and kidneys IV, used for hypoxic tumor cells
E. Miscellaneous Anticancer Drugs
i. TK inhibitor: Imatinib, Dasatinib, Tyrosine kinase inhibitor of the protein product of Resistance is due to mutation is bcr-abl
Nilotinib bcr-abl oncogene in CML ; For CML, GIST diarrhea, myalgia, fluid retention, CHF gene
ii. Growth Factor Receptor Inhibitor
recognizes a surface protein in breast CA cells that
overexpress Her-2-neu receptors for epidermal nausea, vomiting, chills, fever, headache,
a. Her-2-neu inhibitor: Trastuzumab growth factor cardiotoxicity (CHF) None
 EGFR (Epidermal Growth Factor Receptor) regulate
signaling involved in cellular proliferation, invasion
and metastasis and angiogenesis, it also inhibits
cytotoxic activity of some anti-cancer and radiation
treatment, Gefitinib and Erlotinib are capable of
inhibiting EGFR’s Tyrosine Kinase domain ; Cetuximab
(+ Irinotecan and Oxalipatin) For metastatic colon
cancer and Head and Neck cancer ; Panitumumab For
b. EGFR inhibitor: Cetuximab, refractory colorectal cancer ; Gefitinib and Erlotinib Erlotinib can also be used for advanced
Panitumumab, Gefitinib, Erlotinib as second-line agents for non-small cell lung cancer folliculitis, diffuse hair loss, dry skin, paronychia pancreatic cancer

VEGF (Vascular Endothelial Growth Factor) has a role

in angiogenesis required for metastasis, Inhibits
binding of VEGF to VEGFR leading to inhibition of
VEGF signalling, inhibits tumor vascular permeability
but enhances tumor blood flow and drug delivery ;
Sorefenib Sunitinib and Pazopanib inhibits multiple
receptor Tyrosine Kinase including those associated
c. VEGF Inhibitor: Bevacizumab, to VEGF ; For metastatic colorectal cancer, breast hypertension, arterial thrombosis, impaired may also be used in non-small cell lung CA
Sorafenib, Sunitinib, Pazopanib cancer, diabetic retinopathy wound healing, proteinuria, GI perforation and renal CA
Binds to a surface protein in NHL cells, induces
complement-mediated lysis, direct cytotoxicity and
induction of apoptosis ; For Non-Hodgkin’s hypersensitivity reaction, bone marrow
iv. Rituximab lymphoma and other lymphomas suppression None
Endogenous glycoproteins with antineoplastic, alopecia, myalgia, depression, thyroid
immunosuppressive and antiviral actions ; For hairy dysfunction, hearing loss, bone marrow
v. Interferon alpha cell leukemia, early CML, T-cell lymphoma suppression None
Depletes serum asparagine ; For ALL, T-cell
auxotrophic CA (leukemia and lymphomas) that acute pancreatitis, bleeding, severe
vi. Asparaginase require asparagine for growth hypersensitivity reaction None
Allows DNA transcription and differentiation of Only vitamin that can cure cancer, treat
immature leukemic promyelocytes into mature retinoic acid syndrome (dyspnea, fever, weight retinoic acid syndrome with
vii. All-Trans retinoic acid granulocytes ; For acute promyelocytic leukemia gain, peripheral edema) dexamethasone
a reversible inhibitor of 26s proteasome in
viii. Protease Inhibitor: Bortezomib mammalian cell ; For multiple myeloma peripheral neuropathy, thrombocytoppenia
F. Hormonal Anticancer Agents
Suppresses inflammation and immune response, may
trigger apoptosis and work on nondividing cancer
cells ; For CLL, Hodgkin’s lymphoma, leukemia, adrenal suppression, growth inhibition, muscle
i. Prednisone lymphoma wasting, osteoporosis, salt retention see entry
 Estrogen antagonist actions in breasts tissue and
CNS, estrogen agonist effects in uterus, liver and
bone ; For hormone-responsive breast cancer, hot flushes, thromboembolism, endometrial Prevents osteoporosis and decrease risk of
ii. SERM: Tamoxifen, Toremifene Toremifene For advanced breast cancer hyperplasia, endometrial cancer atherosclerosis
GnRH analogs (leuprolide) must be co-
administered to prevent acute flare-up of
iii. Androgen antagonist: Flutamide Androgen antagonist ; For prostate cancer gynecomastia, hot flushes, impotence prostate cancer
Increased LH, FSH secretion with intermittent
administration, reduced LH and FSH secretion with hot flushes, sweats, headache, osteoporosis,
iv. GnRH analog: Leuprolide, prolonged continuous administration ; For prostate gynecomastia, gynecomastia, testicular atrophy,
Goserelin Nafarelin cancer impotence, bone pain see entry
v. Aromatase inhibitor: Anastrazole, Reduces estrogen synthesis by inhibiting aromatase; nausea, diarrhea, hot flushes, bone and back Effective againsts breast cancer that have
Letrozole For advanced breast cancer pain, dyspnea, peripheral edema become resistant to tamoxifen

Drugs Used in the Treatment of Gastrointestinal Diseases [Divided into 2 classes: agents that reduce intragastric acidity and agents that promote mucosal defense
Impairs absorption of tetracyclines,
flouroquinolones,itraconazole and iron -->
should not be given within 2 hours with
these drugs ; When used regularly in large
doses needed to significantly raise the
stomach pH, antacids, decrease recurrence
Sodium bicarbonate: Belching, metabolic rate of peptic ulcers ; Aluminum and
alkalosis. Calcium carbonate: hypercalcemia, Magnesium are always given together to
A. Antacids: Magnesium-Aluminum Neutralize stomach acid by reacting with protons in renal insufficiency, metabolic alkalosis (milk- cancel out each other's adverse effects ;
Hydroxide, Calcium carbonate, Sodium the lumen ; For peptic ulcer disease, Gastroesophagal alkali syndrome) exc for Aluminum Magnesium Avoid in renally impaired patients ; DOA: 1-
bicarbonate reflux Hydroxide 2 hours
Cimetidine is a potent inhibitor of CYP450.
Highly effective in suppressing nocturnal
acid secretion but only modest effect on
meal- stimulated secretion ; avoid in renally
and hepatically (severe) impaired patients ;
Gynecomastia (cimetidine only), Diarrhea, are highly selective and does not affect H1
Competitive pharmacologic block of H2 receptors ; headache, fatigue, Myalgias, constipation, and H3 receptors, may also reduce
B. H2 receptor antagonist: Cimetidine, For peptic ulcer disease, Zollinger-Ellison syndrome, Nosocomial pneumonia, Mental status changes, seceretion of pepsin ; DOA: 6-10hrs ;
Ranitidine, Famotidine, Nizatidine Gastroesophagal reflux, dyspepsia Bradycardia, Hypotension, Blood dyscrasias Reduces acid secretion by 60-70%
usually enetric coated, t1/2 is 1-2hrs but
DOA of is around 24hrs, needs 3-4 days
treatment to achieve full effectiveness ;
decreases bioavailability drugs that require
acidity for GI absorption ; when used for
Irreversible blockade of H/K ATPase in active gastric PUD together with 2 antibiotics, achieve
C. Proton Pump Inhibitor: parietal cells, Long lasting reduction of meal Diarrhea, headache, abdominal pain, 90% cure ; Reduces acid secretion by 90-
Omeprazole, Lansopraole, stimulated and nocturnal acid secretion ; For Peptic Malabsorption syndrome (Vit B12, Ca, Fe, Zn, 98% ; should be taken on an empty
Rabeprazole, Pantoprazole, ulcer disease(DOC), Zollinger-Ellison syndrome, Digoxin, Ketoconazole), Infections (respiratory, stomach since food decreases its
Esomeprazole Gastroesophageal reflux, dyspepsia enteric), Hypergastrinemia, Atrophic gastritis bioavailability by 50%
D. Mucosal Protective Agent:
 polymerizes in acidic environmet —> polymers bind
to injured tissue and forms a protective covering over Highly insoluble, requiring frequent dosing
ulcer bed, Accelerates healing of peptic ulcers and (QID) ; chemically: Aluminum Sucrose
i. Sucralfate reduces recurrence rate ; For Peptic ulcer disease constipation, dizziness, flatulence, dry mouth Sulfate
forms a protective coating on ulcerated tissue,
stimulates mucosal protective mechanisms, direct
antimicrobial effects and sequestration of Black stools, darkening of tongue,
enterotoxins ; For Peptic ulcer disease, Dyspepsia, Encephalopathy (Atraxia, headaches, confusion, Reduces stool frequency and liquidity in
ii. Bismuth Salicylate Infectious diarrhea seizures) infectious diarrhea

PGE1 analog, Activates EP receptors, causes

increased HCO3 and mucus secretion and inhibits
acid secretion in the stomach, causes uterine
contraction ; For Peptic ulcer disease, Prevention of Abdominal pain, Diarrhea, Uterine cramping, see entry, decreases ulcer in NSAIDs
iii. Misoprostol NSAID-induced gastric mucosal injury, Abortifacient Miscarriage induced ulceration
E. Prokinetics

Metoclopramide and domperidone block D2

receptors, Erythromycin stimulates motilin receptor,
Increases gastric emptying and intestinal motility ; As
Antiemetic for post operative/chemotherapy Domperidone does not cross the BBB (less
i. Metoclopramide, Domperidone, vomiting, Diabetic gastroparesis (drug of choice), Parkinsonism, Extrapyramidal effects, toxic) ; Increases LES pressure (helpful in
Erythromycin, Neostigmine Neostigmine for acute large bowel distention Hyperprolactinemia GERD)
F. Laxatives

Indigestible, hydrophilic colloids that absorb water,

i. Bulk-forming: Psyllium, forming a bulky emollient gel that distends the colon
Methylcellulose, Polycarbophil and promotes peristasis ; For constipation Diarrhea None
Diarrhea, Aspiration,(Lipid pneumonitis),
ii. Stool-softener: Docusate, Soften stool material, Permitting water and lipids to Malaabsorption of fat-soluble vitamins (A, D, E,
Glycerine, Mineral oil penetrate the stool ; For constipation K) None
Soluble but nonabsorbable compound that result in
iii. Osmotic: Lactulose, Magnesium increased stool liquidity due to an obligate increase Diarrhea, Flatus, Abominal cramps, Electrolyte
oxide, Magnesium hydroxide, Sorbitol, in fecal fluid ; For Constipation, Hepatic abnormalities (hyperphosphatemia,
Magnesium citrate, Sodium encephalopathy (lactulose), Preparation for hypocalcemia, hypernatremia, hypokalemia,
phosphate, Polyethylene Glycol endoscopy (polyethylene glycol) hypermagnesemia) None
iv. Stimulant: Bisacodyl, Aloe, Senna, Unknown. Directly stimulate enteric nervous system
Cascara, Castor oil and colonic electrolyte and fluid secretion Diarrhea can cause melanosis coli
 Lubiprostone is a Chloride channel activator which
stimulates Cl secretion into the intestines leading to
increased fecal fluid content, Methylnaltrexone and
v. Miscellaneous: Lubiprostone, Alvimopan are Opioid receptor antagonist that block mild nausea, stomach pain, mild diarrhoea,
Methylnaltrexone, Alvimopan intestinal mu receptors, but not the CNS bloating, headache NONE
Activates opioid receptors in enteric nervous system. Do not use in children less than 4 years of
Slows motility with negligible CNS effects, Kaolin age (increased chance of causing paralytic
G. Anti-diarrheals: Diphenoxylate, (+pectin) absorbs bacterial toxin and fluid leading to ileus), Reverse ileus by administering
Loperamide, Kaolin+Pectin, Colloidal decreased stool liquidity ; for Diarrhea (nonspecific, Drowsiness, Nausea, Paralytic ileus, interfere Betanechol. Direct m-agonist, Kaolin is
Bismuth noninfectious) with absorption of other drugs hydrated Magnesium Aluminum Silicate
H. Drugs for IBS
i. laxatives, antidiarrheals and low-
dose TCA see entry see entry see entry
ii. Anticholinergics: Dicylomine, see entry ; antispasmodic for abdominal pain, for IBS
Hyoscyamine with prominent diarrhoea see entry see entry
iii. 5HT3 antagonist: Alosteron see entry ; For IBS with severe diarrhoea severe constipation, ischemic colitis see entry

see entry ; activate type2 chloride channels in small

iv. Lubiprostone intestines ; For IBS with predominant constipation see entry see entry
I. Anti-emetics
Blocks chemoreceptor trigger zone and enteric
i. Ondansetron, Granisetron, nervous system 5-HT3 receptors ; For Vomiting (Post Headache, Dizziness, Constipation, QRS and QT
Dolasetron, Palonosetron chemothereaphy, postoperative) prolongation (Dolasetron only) see entry
antagonist of the Neurokinin-1 receptor in the areas
postrema that is activated by substance P and other
tackykinins ; For post-chemotherapy nausea and
ii. Aprepitant vomiting fatigue, dizziness, diarrhea an enzyme inhibitor
iii. Scopoloamine see entry ; For motion sickness emesis see entry see entry
J. Drugs for IBD
Unknown. Probably inhibits production of eicosanoid
inflammatory mediators (PG and LT) and interfering Gastrointestinal upset,Headaches, Arthralgias,
i. Aminosalicylates: Mesalamine, with cytokines ; For Inflammatory bowel disease Myalgias, Bone marrow suppression, Malaise, Not useful for treating active flare ups of
Balsalazine, Olsalazine, Sulfasalazine (mild to moderate) Hypersensitivity reactions ( severe) disease
ii. Other agents: Antibiotics,
Immunosuppressibe antimetabolites see entry ; Natalizumab is a Mab that blocks
(Azathioprine, 6-MP, Methotrexate), intergrins in circulating leukocytes, restricted to
anti-TNF (Infliximab), Natalizumab severe refractory Crohn’s disease multifocal leukoencephalopathy see entry
K. Miscellaneous Agents
 For pancreatic enzyme replacement, improve
digestion of fats proteins and carbohydrates ; For
i. Pancreatic lipase: Pancreatin or pancreatic insufficiency due to Cystic Fibrosis,
Pancrealipase pancreatitis and pancreatectomy hyperuricemia Taken with every meal
a bile acid derivative that decreases cholesterol
content of bile by decreasing hepatic cholesterol
secretion and other effects on hepatocyte canalicular
ii. Drugs that inhibit formation of membrane ; For gallstone in patients refusing or not headache, dizziness, mild stomach pain,
Gallstones: Ursodiol eligible for surgery rhinorrhea, sore throat, rash hair loss None

Drugs Used For Cough

decrease sputum activity ; Usually derivatives of

cysteine; reduce disulfide bridges that bind
glycoproteins to other proteins such as albumin ; Chest tightness, Disagreeable odor, Drowsiness,
Also act as antioxidants & may reduce airway Fever, Hemoptysis, Increased volume of
inflammation ; Orally available drugs are well- bronchial secretions, Irritation of tracheal or
A. Mucolytics : N-acetylcysteine, tolerated; but of little benefit in acute respiratory bronchial tract, Nausea, Rhinorrhea, Stomatitis, available as IV, PO, IM and inhalational
Carbocysteine, Ambroxol condition Vomiting forms
Drowsiness, Incomplete or Infrequent Bowel
may act as an irritant to gastric vagal receptors, and Movements, Inducing of a Relaxed Easy State,
recruit efferent parasympathetic reflexes that cause Stomach Cramps, dizziness or headache, a rash,
B. Expectorants: Guiafenesin glandular exocytosis of a less viscous mucus mixture. or. nausea, vomiting, or stomach upset Are often emetics (ipecac, guaifenesin)
DO NOT suppress in bacterial lung
infections, asthma, bronchiectasis
(suppurating bronchial inflammation) or
Used for dry painful cough of neoplasia or pleural chronic bronchitis where antitussives can
disease ; Irritative cough in inflammation of the cause harmful sputum thickening &
C. Antitussives respiratory tract (epiglottitis); in hemoptysis retention
Morphine may be effective but indicated
only in intractable cough from bronchial
Decreases secretions in the bronchioles, carcinoma ; Dextromethorphan has no
i. Centrally-acting: Opioid decreased sensitivity of the medullary/ CNS cough thickens sputum & inhibits ciliary activity, addictive potential, no analgesic effect,
antitussives (codeine, centers to peripheral stimuli and decreased mucosal reducing clearance of thickened sputum, produces less constipation and inhibition of
dextromethorphan) secretion Constipation mucociliary clearance
Centrally acting antitussive but is neither
ii. Centrally-acting: Non-opioid act through receptors in the brainstem to inhibit Somnolence, nausea, vomiting, diarrhea, chemically or pharmacologically related to
(butamirate citrate) cough dizziness and hypotension opioids
does not cause side effects such as
Non-opoid drug with a peripheral action by inhibiting Nausea, vomiting, heartburn, diarrhea, fatigue, constipation or respiratory depression
iii. Peripherally-acting: the afferent pathways that generate the cough reflex weakness, drowsiness, dizziness, headache, which can be produced by opioid
Levodropropizine (modulates C-fibre activity) palpitations antitussives