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HYDROCHLOROTHIAZIDE

Indication Hypertension,oedema

Dose
Hypertension
Adult: Initially, 12.5 mg, may increase to 25-50 mg once daily as necessary either alone or
withother antihypertensives.
Child: <6 mth 1-3 mg/kg/day in 1-2 divided doses. Max: 37.5 mg daily; 6 mth to 2 yr 1-2
mg/kg/day in 1-2 divided doses. Max: 37.5 mg daily; >2-12 yr 1-2 mg/kg/day in 1-2 divided
doses Max: 100 mg daily.
Elderly: 12.5-25 mg once daily, titrate as necessary in increments of 12.5 mg.

Mechanism of action Hydrochlorothiazide inhibits the reabsorption of sodium and chloride in

the distal tubules causing increased excretion of sodium and water ,pottaium and hydrogen ions.

Contraindications Hypersensitivity to sulfonamide-derived drugs, anuria, severe renal

impairment.

Precautions Patients withelectrolyte disturbances, history of gout, allergy or bronchial asthma,

DM, parathyroid disease, hypercholesterolaemia. May exacerbate SLE. Hepatic and mild to
moderate renal impairment. Pregnancy and lactation.

Adverse Drug Reactions Electrolyte disturbances, weakness, hypotension, pancreatitis,

jaundice, diarrhoea, vomiting, sialadenitis, cramping, constipation, gastric irritation, nausea,
anorexia, aplastic anaemia, agranulocytosis, leukopenia, haemolytic anaemia, thrombocytopenia,
anaphylactic reactions, necrotising angiitis, resp distress, photosensitivity, fever, urticaria, rash,
purpura, hyperglycaemia, glycosuria, hyperuricaemia., muscle spasm, vertigo, paraesthesias,
dizziness, headache, restlessness, renal failure, renal dysfunction, interstitial nephritis, erythema
multiforme, exfoliative dermatitis, alopecia, transient blurred vision, xanthopsia, impotence.

Drug Interactions Increases toxicity of lithium. May potentiate orthostatic hypotension

withbarbiturates and narcotics. Enhanced neuromuscular blocking action of competitive
neuromuscular blockers (e.g. atracurium). Increased hypokalaemic effect withcorticosteroids,
corticotropin, β2 agonists (e.g. salbutamol). Additive effect withother antihypertensives.
Potentiation of orthostatic hypotension withbarbiturates or opioids. Reduced antihypertensive
effect by drugs that cause fluid retention (e.g. corticosteroids, NSAIDs, carbenoxolone).
Enhanced nephrotoxicity of NSAIDs. Reduced therapeutic effect of antidiabetics.

LOSARTAN

Indications Congestive heart failure, hypertension (myocardial infarction along with stroke
including reduction of stroke risk in hypertension) with left ventricular hypertrophy, diabetic
nephropathy in type II diabetes.
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Dose Hypertension and diabetic nephropathy:Adult- 50 mg once daily, increased to 100 mg daily
as single dose or in two divided doses, if needed.Child- 6 years, initially 700μg/kg, increased to a
max. of 50 mg once daily, if needed.Elderly over 75 years initially 25 mg daily. Maintenance
dose 25 to 100 mg orally in 1 to 2 divided doses.

Mechanism of action Losartan is an angiotensin II receptor antagonist. It selectively and

competitively blocks the vasoconstricting and aldosterone-secreting effects of angiotensin II by
selectively antagonising its binding to AT1 receptors.

Contraindications Hyperaldosteronism, hypersensitivity, pregnancy, lactation, not

recommended in children <6yrs of age or GFR <30 ml/min/1.73msq.

Precautions Pre-existing heart, liver or kidney diseases, diabetes, lactation, volume depleted
patients, renal artery stenosis, monitor serum potassium concentration, elderly.

Adverse effects Abdominal pain, edema, palpitation, back pain, dizziness, sinusitis, upper
respiratory tract infection, rash, gastrointestinal disturbances, transient elevation of liverenzymes,
impaired renal function, taste disturbances, hyperkalaemia, arthralgia, thrombocytopenia,
vasculitis.

AMLODIPINE

Indications: Oral: hypertension, stable angina, variant angina.

Dose: Initial, 5 mg once daily; maintenance 5-10 mg once daily.

Mechanism of action

Calcium channel blocker- Amlodipine relaxes peripheral and coronary vascular smooth
muscle. It produces coronary vasodilation by inhibiting the entry of Calcium ions into the slow
channels or select voltage-sensitive channels of the vascular smooth muscle and myocardium
during depolarisation

Contra indications: Sensitivity to amlodipine.

Precautions: Aortic stenosis, severe; symptomatic hypotension may occur ,hepatic impairment,
obstructive coronary artery disease, severe; increased risk of worsening angina or acute
myocardial infarction after initiating or increasing dose,

Adverse effects: Flushing, Palpitations, Peripheral edema, abdominal pain, Nausea, Dizziness,
Headache, Somnolence, Fatigue, Acute myocardial infarction, Angina, Angioedema.

Drug interactions: Clopidogrel, telaprevir, simvastatin, amiodarone, primidone.

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ATENOLOL

Indications. Angina pectoris; Migraine prophylaxis, Arrhythmias, Acute MI

Dose Adult: PO hypertension 25-100 mg/day. Angina pectoris; Migraine prophylaxis 50-100
mg/day. Max for angina pectoris: 200 mg/ day. IV Arrhythmias 2.5 mg at a rate of 1 mg/min.
May repeat every 5 mins if needed. Max: 10 mg. Switch to oral therapy 50-100 mg/day once
control is achieved. Acute MI 5-10 mg via slow inj w/in 12 hr of onset of chest pain, then an oral
dose of 50 mg 15 mins later.

Mechanism of action Atenolol is a competitive cardioselective β1-blocker It reduces resting

and exercise-induced heart rate as well as myocardial contractility.

Contraindications: Hypersensitivity. Sinus bradycardia, sinus node dysfunction, heart block

>1stdegree, compensated cardiac failure, cardiogenic shock, bronchospastic diseases, peripheral
vascular diseases. Pregnancy.

Precautions: Compensated heart failure. Variant angina, acute MI, DM; peripheral vascular
disorders; hepatic and renal dysfunction; elderly patients, children. Lactation. If atenolol and
clonidine are co-administered, then gradual withdrawal of clonidine should take place a few days
after withdrawal of atenolol.

Drug interaction Decreased effect with aluminum and calcium salts, barbiturates,
cholestyramine, NSAIDs, ampicillin, rifampicin.May increase effects of drugs which slow AV
conduction (digoxin, verapamil, diltiazem).

Adverse effects: Bronchospasm; cold extremities, fatigue, dizziness, insomnia, lethargy,

confusion, headache, depression, nightmares, nausea, diarrhoea, constipation, impotence and
paraesthesia.Heart failure, 2nd or 3rd degree AV block.

DILTIAZEM

Indications Angina pectoris ,hypertension , Cardiac arrhythmias

Dose Adult: PO Angina pectoris Initial: 60 mg 3 times/day, up to 480 mg/ day if needed.
Hypertension Initial: 60-120 mg twice daily. Max: 360 mg/day. IV Cardiac arrhythmias Initial:
250 mcg/kg, may repeat another dose at 350 mcg/kg 15 mins later if needed.

Mechanism of action Calcium channel blocker -Diltiazem relaxes coronary vascular smooth
muscles by inhibiting influx of calcium ions during depolarisation of the vascular smooth
muscles and myocardium.

Contraindications: Sick-sinus syndrome; 2nd or 3rd ° AV block; porphyria. Severe congestive

cardiac failure; marked bradycardia. Pregnancy and lactation.
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Precautions: Elderly. Hepatic or renal impairment; impaired left ventricular function; prolonged
AV periods; DM; hypotension. Avoid abrupt withdrawal and long-term use. Patients with sick-
sinus syndrome, preexisting AV block, bradycardia and those taking beta-blockersor digitalis are
at risk of developing AV block, bradycardia, asystole or sinus arrest.

Adverse effects: Headache, ankle oedema, hypotension, dizziness, fatigue, flushing, nausea, GI
discomfort, gingival hyperplasia, rashes, erythema multiforme, exfoliative dermatitis,
photosensitivity, occasionally hepatitis.: AV block, bradycardia, asystole, sinus arrest.

Drug interaction Increases serum theophylline levels. Cimetidine may increase plasma
concentrations of diltiazem. Concurrent use may lead to increased blood ciclosporin
levels.Increased depression of cardiac conduction with amiodarone, β-blockers, digoxin and
mefloquine. May potentiate risk of bradycardia and conduction disturbance of propranolol and
risk of neurotoxicity of lithium.

ENALAPRIL

Indications Hypertension

Dose Adult: PO Hypertension Initial: 5 mg/day at bedtime. Maintenance: 10-20 mg once daily.
Severe: Up to 40 mg/day in divided doses. Max: 40 mg/day. Heart failureInitial: 2.5 mg/day.
Maintenance: 20 mg once daily, up to 40 mg/day in 2 divided doses. IVHypertension1.25 mg via
slow inj, repeat 6 hrly if needed.

Mechanism of action Angiotensin converting enzyme(ACE inhibitor). Enalapril, a prodrug of

enalaprilat, competitively inhibits ACE from converting angiotensin I to angiotensin II (a potent
vasoconstrictor) resulting in increased plasma renin activity and reduced aldosterone (a hormone
that causes water and Na retention) secretion. This promotes vasodilation and BP reduction

Contraindications: Hypersensitivity. History of angioedema due to previous treatment

with ACE inhibitors; bilateral renal artery stenosis. Pregnancy.

Precautions: Impaired renal function. Hyperkalaemia, hypovolaemia, collagen vascular disease,

valvular stenosis, during or immediately before or after anaesthesia, unilateral renal artery
stenosis. Hypotension due to volume depletion, diuretic therapy. Monitor WBC count. Lactation,
children.

Adverse effects: Initial hypotension may be severe and prolonged. Dizziness, headache, fatigue,
persistent dry cough, abnormal tasterash, neutropenia, renal impairment or failure, Angioedema..

Drug interaction Diuretics potentiate hypotensive action. May increase lithium levels. Other
antihypertensives potentiate enalapril action.Increased risk of bone marrow suppression when
used with immunosuppressive drugs. Hyperkalaemia with potassium-sparing diuretics or
potassium supplements especially in the presence of renal failure. Probenecid delays excretion.
Potentiates analgesia and respiratory depression produced by morphine. NSAIDs may result in
further deterioration of renal function
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METOPROLOL

Indications Supraventricular arrhythmia, angina pectoris, hypertension, myocardial

infarction;migraine prophylaxis; hyperthyroidism, heart failure.

Dose Oral Heart failure: Initiating dose 12.5 - 25 mg once a day, Maximum dose: 200 mg oncea
day; Hypertension: initially 100 mg daily, increase if required to 200 mg in two divided doses
(max 400 mg daily). Angina: 50 mg daily, up to 300 mg daily in 2 to 3 divided doses if
necessary.
Intravenous injection Arrhythmia: up to 5 mg at a rate of 1 to 2 mg per min, repeated after
5 min if necessary (max dose 10 to 15 mg). Arrythmia developing during anaesthesia: 2 to 4 mg
during induction.

Mechanism of action β1-adrenergic receptor antagonist Metoprolol selectively inhibits β1-

adrenergic receptors

Contraindications Asthma , Prinzmetal’s angina, marked bradycardia, hypotension, sick sinus

syndrome, secondor third- degree AV block, cardiogenic shock, metabolic acidosis, severe
peripheral arterial disease;pheochromocytoma (apart from specific use with alpha-blockers).
Beta-blockers, including those considered to be cardioselective, should not be given to patients
with a history of asthma or bronchospasm. However, in rare situations where there is no
alternative a cardioselective beta-blocker is given to these patients with extreme caution and
under specialist supervision.

Precautions Avoid abrupt withdrawal especially in ischaemic heart disease, firstdegree AV

block, portal hypertension (risk of deterioration in liver function); diabetes; history of obstructive
airways disease (introduce cautiously and monitor lung function); myastheniagravis; symptoms
of hypoglycaemia and thyrotoxicosis may be masked; history of hypersensitivity-may increase
sensitivity to allergens and result in more serious hypersensitivity response; also may reduce
response to adrenaline (epinephrine); reduce dose of oral propranolol in hepatic impairment;
renal impairment; lactation; pregnancy

Adverse Effects Gastro-intestinal disturbances; bradycardia, heart failure, hypotension,

conduction disorders; peripheral vasoconstriction (including exacerbation of intermittent
claudication and Raynaud’s phenomenon); bronchospasm; dyspnoea; headache; fatigue; sleep
disturbances; paraesthesia; dizziness; vertigo; psychosis; sexual dysfunction; purpura;
thrombocytopenia; visual disturbances; exacerbation of psoriasis; alopecia; rarely, rashes and dry
eyes (reversible on withdrawal); on infusion venous irritation and thrombophlebitis;
agranulocytosis; hyperglycemia; myocardial depression.

TELMISARTAN

Indications Hypertension
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Dose Oral Hypertension

Adult: Initially, 40 mg once daily. Max: 80 mg/day.
Renal impairment: Severe impairment/ Haemodialysis: Initial dose 20 mg/day.
Hepatic impairment: Mild to moderate: Max 40 mg/day. Severe: Contra-indicated

Mechanism of action Telmisartan is a nonpeptide AT1 angiotensin II receptor antagonist. It

exerts antihypertensive activity by preventing angiotensin II from binding to AT1 receptors thus
inhibiting the vasoconstricting and aldosterone-secreting effects of angiotensin II.

Contraindications Severe hepatic impairment, biliary obstructive disorders. Pregnancy.

Lactation.

Precautions Hepatic insufficiency, biliary obstruction, renal impairment, renaly artery stenosis.
Correct volume depletion before initiating treatment. Monitor serum potassium levels regularly,
especially in elderly and renally-impaired patients.

Adverse effects URTI, dizziness, back pain, sinusitis, pharyngitis and diarrhoea. Slight
elevations in liver enzymes.Rarely angioedema, rash, pruritus and urticaria.

Drug Interactions Concurrent use increases digoxin concentration; increases risk of lithium
toxicity; increases risk of hyperkalaemia with potassium sparing diuretics, heparin.

ISOSORBIDE MONONITRATE

Indication Management of angina, Heart failure

Dose Adult: 20 mg 2-3 times daily. Dose may range from 20-120 mg daily.
Elderly: Intiate at lower doses.

Administration Should be taken on an empty stomach (i.e. At least one hour before food or two
hours after food).

Mechanism of action Isosorbide mononitrate relaxes vascular smooth muscles. It decreases

left ventricular pressure (preload) and arterial resistance (afterload).

Contraindication Severe hypotension or anaemia, hypovolaemia, heart failure due to

obstruction, or raised intracranial pressure due to head trauma or cerebral haemorrhage.

Precautions Severe renal or severe hepatic impairment, hypothyroidism, malnutrition, or

hypothermia. Caution in patients who are already hypotensive. May aggravate angina caused by
hypertrophic cardiomyopathy. Tolerance may develop after long-term treatment. Lactation.

Adverse Drug Reactions Hypotension, tachycardia, flushing, headache, dizziness, palpitation,

syncope, confusion. Nausea, vomiting, abdominal pain. Restlessness, weakness and vertigo. Dry
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mouth, chest pain, back pain, oedema, fatigue, abdominal pain, constipation, diarrhoea,
dyspepsia and flatulence.Severe hypotension and cardiac failure.

Drug Interactions Hypotensive effects may be increased when used with alcohol or
vasodilators. Concurrent use with calcium channel blockers may lead to marked orthostatic
hypotension.

ATORVASTATIN

Indications: Mixed dyslipidaemia, Nonfamilial hypercholestrolaemia, Heterozygous

familial hypercholestrolaemia

Dose: Initially 10-20mg daily,may increase at 4-weekly intervals. Max dose- 80mg/day

Mechanism of action HMG-CoA reductase inhibitor -Atorvastatin competitively inhibits

HMG-CoA reductase, the enzyme that catalyses the conversion of HMG-CoA to mevalonate.
This results in the induction of the LDL receptors and stimulation of LDL catabolism, leading to
lowered LDL-cholesterol levels.

Contra indications: Hypersensitivity,active liver disease/unexplained persistent elevations of

serum transaminase, porphyria,pregnancy, lactation

Precautions: Use with caution in patients who consume substantial quantities of alcohol,with
history of liver disease,with risk factor for myopathy & rhabdomyolysis.Hypothyroidism should
be properly managed before starting statin therapy.Use with caution in case of children<10 yr
&in pre menarcheal female

Adverse effects: Headache, flatulence, diarrhoea,nausea, vomiting, anorexia, xerostomia,

angioedema,myalgia,rash/pruritis, alopecia, allergy, infection, chestpain, rhabdomyolysis

Drug interaction : Increased AUC for norethindrone&ethinyl estradiol. Concomittent multiple

doses of atoirvastatin&digoxin increases steady-state digoxin level.Increased risk of
rhabdomyolysis when used with fibrates. Co- admnistration with antacid suspension&colestipol
decreases atorvaststin levels.

ROSUVASTATIN

Indications: Hyperlipidaemias

Dose: 5-10mg daily, may increase dose at 4-weekly intervals to20mg daily.
Max dose-40mg daily

Mechanism of action HMG-CoA reductase inhibitor -Rosuvastatin is a selective and

competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis.
It increases the number of hepatic LDL receptors on the cell surface, enhancing uptake and
catabolism of LDL. It also decreases apolipoprotein B, triglycerides and increases HDL
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Contraindications: Severe renal impairment,active liver disease,unexplained persistent

elevations of serum transaminases, hypersensitivity, pregnancy,lactation

Precautions: Not to be used in patients with myopathy/ renal failure, sepsis, hypotension, major
surgery, trauma, severe metabolic, endocrine & electrolyte disorders/uncontrolled seizures.Use
with caution in patients with history of liver disease&alcoholism.Discontinue treatment if an
increase in concentration of serum aminotransferase/ creatinine phosphokinase is seen

Adverse effects: Headache, dizziness, constipation, nausea, vomiting, abdominal

pain,myalgia,chest pain, peripheraloedema, depression, insomnia, rash, paraesthesia,
proteinuria&asthenia. Rhabdomyolysis withacute renal failure

Drug interaction: Increased risk of myopathy when used with gemfibrozil. May increase serum
level of warfarin&oral contraceptives. Concurrent admn with Al/Mg OH decreases
bioavailability of rosuvastatin .Serum level is increased by fluconazole.Increased risk of
myopathy & renal failure when used with ciclosporin

FENOFIBRATE

Indications: Hypertriglyceridemia, type IV or V, hypercholesterolemia, mixed dyslipidemia

Dose: PO Dose depends on the formulation used. For standard micronized formulations: Initial:
67 mg 3 times/day, may adjust to 67 mg 2-4 times/day. For non-micronised formulations: Initial:
200-300 mg/ day in divided doses. Usual range: 200-400 mg/day.

Mechanism of action Fenofibrate, a fibric acid derivative, lowers plasma triglyceride by

activating lipoprotein lipase thus increasing catabolism of VLDL with consequent increase in
HDL levels.

Contraindications: Hypersensitivity,sever hepatic& renal impairment, unexplained persistent

liver function abnormality &primary biliary cirrhosis, preexisting gallbladder
disease,pregnancy,lactation

Precautions: Renal/hepatic impairment.Monitor LFTs&blood counts regularly.Increased risk of

cholelithiasis,pancreatitis ,skeletal muscle effects. With draw treatment if no result is observed
within 2 months of therapy

Adverse effects: Headache, dizziness, asthaenia, fatigue, arrhythmia, photosensitivity, eczema,

vaginitis, paraaesthesia, rhinitis, cough, sinusitis, allergic pulmonary alveolitis, polyuria,
myopathy, myositis, arthralgia, myalgia, myasthenia, hepatitis, cholecystitis

Drug interaction: Resins impede the absorption of fenofibrate. May increase cyclosporine
concentration &associated nephrotoxicity when used together. Statins increase risk of
rhabdomyolysis&myopathy with renal failure.May increase the effect of oral anticoagulants
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CLOPIDOGREL

Indication: Prophylaxis of thromboembolic events, myocardial infarction, unstable angina

Dose: Adult: PO Prophylaxis of thromboembolic events 75 mg once daily. Acute coronary

syndrome For ST-elevation myocardial infarction: with aspirin: 75 mg once daily. Continue
treatment for up to 28 days. For unstable angina, non-ST-elevation myocardial infarction: Initial:
300 mg loading dose, followed by 75 mg once daily (with aspirin 75- 325 mg once daily).

Mechanism of action Antiplatelet drug action .Clopidogrel inhibits adenosine diphosphate

(ADP) from binding to its receptor sites on the platelets and subsequent activation of
glycoprotein GP IIb/IIIa complex thus preventing fibrinogen binding, platelet adhesion and
aggregation.

Contraindications Hypersensitivity. Active pathological bleeding. admin within 7 days

after MI and ischaemic stroke, coagulation disorders. Lactation.

Precautions Patients at risk of increased bleeding from trauma, surgery, or other pathological
conditions; ulcer; renal and hepatic impairment; history of bleeding or haemostatic disorders.
Pregnancy.

Adverse Reactions Dyspepsia, abdominal pain, nausea, vomiting, flatulence, constipation,

gastritis, gastric and duodenal ulcers. GI upset, diarrhoea, paraesthesia, vertigo, headache,
dizziness, pruritus and rashes.Potentially Fatal: Bleeding disorders including GI and intracranial
haemorrhage. Blood dyscrasias.

Drug Interactions Co-administartion with NSAIDs may increase the risk of stomach and
intestinal bleeding. High-dose clopidogrel may lead to increased warfarin levels thus increasing
the risk of bleeding. High-dose clopidogrel may also inhibit P450 (2C9), thus interfering with the
metabolism of phenytoin, tamoxifen, torasemide, fluvastatin and some NSAIDs. Avoid
concurrent use of drugs that inhibit CYP2C19, including omeprazole, esomeprazole, cimetidine,
fluconazole, ketoconazole, voriconazole, etravirine, felbamate, fluoxetine, fluvoxamine and
ticlopidine.

ASPIRIN

Indication Prophylaxis of myocardial infarction, Stent implantation

Dose Adult: 75-325 mg once daily. Lower doses should be used in patients receiving ACE
inhibitors.
Adult: 325 mg 2 hr before procedure followed by 160-325 mg/day thereafter.

Mechanism of action It also inhibits platelet aggregation.

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Contraindications Hypersensitivity (attacks of asthma, angioedema, urticaria or rhinitis), active

peptic ulceration; pregnancy (3rd trimester), children <12 yr, patients with haemophilia or
haemorrhagic disorders, gout, severe renal or hepatic impairment, lactation.

Precautions History of peptic ulcer or those prone to dyspepsia and those with gastric mucosal
lesion, asthma or allergic disorders, dehydrated patients, uncontrolled hypertension, impaired
renal or hepatic function, elderly.

Adverse Drug Reactions GI disturbances; prolonged bleeding time, rhinitis, urticaria and
epigastric discomfort; angioedema, salicylism, tinnitus; bronchospasm.Gastric erosion,
ulceration and bleeding; severe, occasionally fatal exacerbation of airway obstruction in asthma;
Reye's syndrome (children <12 yr). Hepatotoxicity; CNS depression which may lead to coma;
CV collapse and resp failure; paroxysmal bronchospasm and dyspnoea.

Drug Interactions Alcohol, corticosteroids, analgin, phenylbutazone and oxyphenbutazone may

increase risk of GI ulceration. Aspirin increases phenytoin levels. May antagonize actions of
uricosurics andspironolactone.May potentiate effects of anticoagulants, methotrexate and oral
hypoglycaemics

VOGLIBOSE

Indication: Diabetes mellitus type1, diabetes mellitus type 2, glycogen storage disease,
hyperinsulinism (non-diabetic), steroid induced diabetes.

Dose: In adult, 0.2mg 3 times daily in NIDDM, 0.2 or 0.3mg 3 times daily in IDDM, 0.2mg 3
times daily in non-diabetic hyperinsulinemia and steroid induced diabetes. In paediatric, 0.1mg
daily in glycogen storage disease.

Mechanism of action Voligbose selectively inhibits α-glucosidase in the enteric canal,

delaying the digestion and absorption of carbohydrate, there by suppressing sharp increase in
post-prandial plasma glucose.

Contraindication: Hypersensitivity to voglibose.

Precaution: GI disorders with diarrheal component, potential hepatotoxicity.

Adverse effects : Hypoglycemia, GI tract finding (stools/diarrhea, flatulence, bloating,

abdominal pain or discomfort, abdominal fullness, and nausea), hepatotoxicity, CNS finding
(dizziness, nausea, vomiting).

Drug interaction: May enhance effects of other antidiabetics including insulin.

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GLIBENCLAMIDE

Indication: Diabetes mellitus type 2

Dose: PO Initial: 2.5-5 mg/day, up to 15 mg/day. Max: 20 mg/day.

Mechanism of action Glibenclamide lowers blood glucose concentration principally by

stimulating secretion of endogenous insulin from the pancreatic β-cells. Hypoglycaemic
action associated with short-term therapy appears to include reduction of basal hepatic glucose
production and enhancement of peripheral insulin action at target sites

Contraindication: Concomitant use of bosentan, diabetic ketoacidosis, with or without coma;

should be treated with insulin, known hypersensitivity to glyburide or any component of the
product, type 1 diabetes mellitus; should be treated with insulin.

Precaution: Increased risk of hypoglycemia, allergy to other sulfonamide derivatives, autonomic

neuropathy, cardiovascular mortality has been reported with tolbutamide, Elderly, debilitated or
malnourished patients, glucose 6-phosphate dehydrogenase (G6PD) deficiency; can lead to
hemolytic anemia, hepatic insufficiency, renal insufficiency, stress.

Adverse effects : Epigastric fullness, Heartburn, Nausea, Hypoglycemia, Hemolytic anemia,

Cholestatic jaundice syndrome, Hepatitis.

GLICLAZIDE

Indication: Type 2 diabetes mellitus.

Dose: Initially, 40-80 mg daily gradually increased to 320 mg daily if necessary. Doses >160 mg
daily may be given in 2 divided doses.

Mechanism of action Gliclazide stimulates insulin secretion from pancreatic β-cells, reduces
insulin uptake and glucose output by the liver, and increases insulin sensitivity at peripheral
target sites. It decreases microthrombosis by partial inhibition of platelet aggregation and
adhesion, and by restoring fibrinolysis with an increase in tissue plasminogen activator (t-PA)
activity.

Contraindication: Type 1 DM, diabetes complicated with ketoacidosis; hypersensitivity; severe

renal and hepatic impairment. Pregnancy and lactation.

Precaution: Monitor blood glucose concentration. May require insulin during metabolic stress.
Care when transferring from combination therapy. Increased risk of severe hypoglycemia in
elderly, debilitated patients, patients with hepatic or renal impairment. Risk of hypoglycemia
when caloric intake is deficient, after strenuous exercise, when taken with ethanol or when >1
anti diabetic drug is used.
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Adverse effects : GI disturbances, skin reaction, leucopenia, thrombocytopenia, agranulocytosis,

hemolytic anemia, cholestatic jaundice, vomiting, diarrhea, gastritis, increased transaminases

Drug interaction: Nausea and flushing with alcohol. Hypoglycemic effect increased by
salicylates, phenylbutazone, clofibrate, sulphonamides, oral anticoagulants and MAOIs.
Hypoglycemic effect diminished by rifampicin, barbiturates, alcohol, diuretics, diazoxide,
corticosteroids, beta-blockers, estrogens and sympathomimetic drugs; dose adjustment may be
required.

GLIMEPIRIDE

Indication: oral: diabetes mellitus, type 2

Dose: Adult: Initially, 1-2 mg daily. Maintenance: 4 mg daily. Max: 6 mg daily.

Renal impairment: Initiate at 1 mg daily; subsequent increments
should be based on fasting blood glucose levels

Mechanism of action Glimepiride stimulates the insulin release from pancreatic β-cells and
reduces glucose output from the liver. It also increases insulin sensitivity at peripheral target sites

Contraindication: hypersens. to drug, diabetic ketoacidosis, caution if hypersens.

tosulfonamides, caution if G6PD deficiency, caution if hypoglycemia risk, caution if autonomic
neuropathy, caution in elderly or debilitated pts.

Precaution: Increased risk of mortality, elderly, hepatic& renal impairment, moniter blood
glucose concentration, pregnancy, lactation.

Adverse effects : hypoglycemia, anemia, hemolytic, Thrombocytopenia, pancytopenia,

agranulocytosis, hypersensitivity reaction, Stevens- Johnson syndrome, hepatotoxicity
Hypoglycemia, dizziness, asthenia, headache, nausea, photosensitivity.

Drug interaction: bosentan, lopinavir/ritonavir, tipranavir, aminolevulinic acid topical, ethanol,

hydroquinone/ retinoid combos, nateglinide.

GLIPIZIDE
Indication: oral: diabetes mellitus type 2

Dose: Adult: PO Initial: 2.5-5 mg/day as a single dose, may increase slowly.
Doses >15 mg may be given in 2 divided doses. Max: 40 mg/day.

Mechanism of action Glipizide stimulates insulin release from pancreatic β-cells and reduces
glucose output from the liver. It also increases insulin sensitivity at peripheral target sites
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Precaution: Hypoglycemia, stress, elderly, thyroid, hepatic, renal impairment. Monitor blood
glucose concentration.

Contraindication: hypersens. to drug, diabetic ketoacidosis, pregnancy near-term, caution if

hypersens. to sulfonamides, caution if renal impairment, caution if hepatic impairment, caution
in elderly pts, caution if adrenal insufficiency, caution if malnutrition, caution if G6PD
deficiency.

Adverse effects : hypoglycemia, agranulocytosis,anemia, thrombocytopenia, Leucopenia,

pancytopenia, cholestatic jaundice, hepatitis, hepatic failure, hepatic porphyria, disulfiram-like
reaction, hyponatremia, SIADH, hypersensitivity reaction, Diarrhea, nausea, hypoglycemia,
dizziness, nervousness, tremor, flatulence, headache, drowsiness, rash, pruritus,photosensitivity

METFORMIN
Indication: Diabetes mellitus, type 2, polycystic ovary syndrome.

Dose Adult: PO Type 2 DM Initial: 500 mg 2-3 times/day, may increase slowly. Max:2.25 g/day.
Polycystic ovary syndrome Initial: 500 mg/ day in the morning for 1 wk, then 500 mg twice daily
for 1 wk, then 1.5-1.7 g/day in 2-3 divided doses.

Mechanism of action Metformin decreases hepatic glucose production by inhibiting

gluconeogenesis and glycogenolysis; delays intestinal absorption of glucose; and enhances
insulin sensitivity by increasing peripheral glucose uptake and utilization

Contraindication: Hypersensitivity to drug, Renal dysfunction, metabolic acidosis, diabetic

ketoacidosis, lactic acidosis, iodinated contrast, hypoxemia, dehydration, sepsis, surgery, hepatic
disease, caution if CHF, elderly patients alcohol abuse, if hypoglycemia risk.

Adverse effects : lactic acidosis, anemia, megaloblastic, diarrhea, nausea/vomiting, flatulence,

asthenia, indigestion, abdominal discomfort, anorexia, headache, metallic taste, rash, ovulation
induction.

Precaution: pregnancy, lactation.

Drug interaction: cimetidine, ethanol, linagliptin, sulfonylurea combos,pioglitazone ,

repaglinide, rosiglitazone, sitagliptin

PIOGLITAZONE
Indication
Type 2 diabetes mellitus

Dose Adult: 15 or 30 mg once daily, increased gradually if necessary. Max: 45 mg/day.

Elderly: No dosage adjustment needed.
Hepatic impairment: Moderate to severe: Avoid.
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Mechanism of action Pioglitazone is as a potent and highly selective agonist for the
peroxisome proliferator activated receptor-γ (PPAR-γ). Activation of these receptors
promotes the production of gene products involved in lipid and glucose metabolism. It also
improves insulin response to target cells with increasing the pancreatic secretion of insulin.

Contraindications Type 1 DM or diabetic ketoacidosis. Severe heart failure (NYHA class III or
IV). Active or history of bladder cancer. Moderate to severe hepatic impairment. Patients
withuninvestigated macroscopic haematuria.

Precautions Symptomatic and congestive heart failure (NYHA class I or II). Mild hepatic
impairment. Pregnancy and lactation. Monitoring Parameters Monitor for signs and symptoms
of heart failure (e.g. dyspnoea, rapid weight. gain, unexplained fatigue or cough), bladder cancer
(e.g. blood in urine, urinary urgency, pain on urination, or back or abdominal pain), and fluid
retention. Periodically monitor fasting plasma glucose levels. LFT should be performed prior to
treatment and monitor periodically. Patient Counselling Adequate contraception is recommended
in premenopausal anovulatory women as pioglitazone may cause resumption of ovulation.

Adverse Drug Reactions Oedema, weight gain, sinusitis, upper resp tract infections, hepatic
dysfunction (e.g. vomiting, unexplained nausea, anorexia, dark urine, abdominal pain, fatigue),
bone loss and fracture, myalgia, visual disturbances; decreased haemoglobin and haematocrit
counts (dose related); decreased serum triglycerides, increased HDL-cholesterol; abnormal LFT.
Mixed hepatocellular-cholestatic liver injury and liver failure; hepatitis.

Drug Interactions Increased risk of oedema withinsulin, metformin and sulfonylureas.

Increased plasma levels withgemfibrozil and ketoconazole. Decreased plasma levels
withrifampicin.

DEFLAZACORT

Indication: Allergic and inflammatory disorders

Dose: Up to 120mg daily orally in adults initially. Maintenance dose of 3- 18mg/day

Mechanism of action Deflazacort, derived from prednisolone, is a corticosteroid with mainly

glucocorticoid activity.

Contraindication: Systemic infection, live virus vaccines in those receiving immunosuppressive

doses.

Precaution : Adrenal suppression and infection, child, adolescent, elderly, history of TB, and
steroid myopathy, hypertension, recent MI, CHF, liver failure, renal impairment , DM and
glaucoma, osteoporosis, corneal perforation, severe affective disorders, epilepsy, peptic ulcer,
 15

hypothyroidism, pregnancy, lactation.

Adverse effects : GI disturbances, musculoskeletal, endocrine, neuropsychiatric, ophthalmic,

fluid and electrolyte disturbances, susceptible to infection, impaired healing, hypersensitivity,
skin atrophy, striae, telangiectasia, acne, myocardial rupture following recent MI,
thromboembolism

Drug interaction : antacids, ACE inhibitors , acetazolamide, adrenergic neuron blockers, ant
diabetics, aspirin, barbiturate, beta blockers, calcium channel blockers, carbamezepine,
carbanoxolone, cardiac glycosides, clonidine, coumarins, diazoxide, diuretics, erythromycin,
hydralazine, ketoconazole, methotrexate, methyldopa, mifepristone, minoxidil, moxonidine,
nitrates , nitroprusside, NSAIDs, estrogens, phenytoin, primidone, rifamycins, ritonavir,
somatropin, beta2 sympathomimetics, theophylline, vaccines

PANTOPRAZOLE
Indication GERD, Peptic ulcer , H. pylori infection, Prevention of NSAID-induced ulcers ,
Zollinger-Ellison syndrome and other hypersecretory states

Dose
Adult: PO GERD 20-40 mg /day in the morning for 4 wk, up to 8 week if needed. Maintenance:
20-40 mg/day. Peptic ulcer 40 mg/day in the morning. Duration: Duodenal ulceration: 2-4 week;
Benign gastric ulceration: 4-8 week. H. pylori infection 40 mg twice daily
with clarithromycin and either amoxicillin or metronidazole. Prevention of NSAID-induced
ulcers 20 mg/day. Zollinger- Ellison syndrome and other hypersecretory states Initial: 80 mg/
day. Max: 240 mg/day. IV Zollinger-Ellison syndrome and other hypersecretory statesAs Na
salt: 80 mg/day. Max: 240 mg/day in divided doses if rapid control required. GERD; Peptic ulcer
As Na salt: 40 mg/day until PO can be resumed

Mechanism of action Pantoprazole also known as PPI(proton pump inhibitor) due to its
property to block the final step of acid secretion by inhibiting H+/K+ ATPase enzyme system
in gastric parietal cell. Both basal and stimulated acid are inhibited

Precaution Long-term therapy may lead to bacterial overgroweighth in the GI tract. Hepatic
impairment; monitor liver function regularly (if enzymes increase, discontinue); pregnancy; not
recommended in children <18 yr; long term use may lead to atrophic gastritis.

Adverse effects Diarrhoea, dizziness, pruritus, skin rashes, GI tract infections, chest pain,
headache, nausea, pain, anxiety, hyperglycaemia; malaise or lassitude; myalgia; oedema;
insomnia; hyperlipidaemia; flatulence, abdominal pain, constipation, eructation, dyspepsia, rectal
disorder; urinary frequency, UTI; abnormalities in liver function; local site reaction; hypertonia,
neck pain, weakness; bronchitis, cough, dyspnoea, pharyngitis, rhinitis, sinusitis, upper
respiratory tract infection, flu syndrome.
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Drug interaction Decreased absorption of ketoconazole and itraconazole; may slightly increase
digoxin plasma concentration; may reduce plasma concentration of atazanavir, avoid
concomitant use; may enhance anticoagulant effect of coumarins; may cause gastric mucosal
irritation with alcohol; may increase levels or effects of: bosentan, dapsone, fluoxetine,
glimepiride, glipizide, losartan, montelukast, nateglinide, paclitaxel, phenytoin, warfarin, and
zafirlukast; may decrease levels or effects of aminoglutethimide, carbamazepine, phenytoin, and
rifampicin.

Contraindication Lactation.

PREGABALIN

Indication; Neuropathic pain, Fibromyalgia

Dose : Neuropathic pain Initial: 150 mg/day, may increase to 300 mg/day after 3-7 days. Max:
600 mg/day after a 7-day interval. Fibromyalgia Initial: 150 mg/day, may increase to 300 mg/day
after a wk. Max: 450 mg/day, if needed. All doses to be given in 2 or 3 divided doses

Mechanism of action Pregabalin is an analog of the neurotransmitter GABA. It binds

potently to the alpha 2 delta subunit of the voltage-dependent calcium channel in the central
nervous system resulting in modulation of Ca channels and reduction in the release of several
neurotransmitters, including glutamate, norepinephrine, serotonin, dopamine, calcitonin gene-
related peptide and substance P.

Contraindication Hypersensitivity, pregnancy, lactation. Driving or working with machines or

do other dangerous activities.

Precaution Discontinue treatment if patients develop severe angioedema. Withdraw treatment

gradually over at least one week. May cause peripheral edema. Regular vision check is
recommended. May decrease platelet count and prolong PR interval

Adverese effects : Dizziness, drowsiness, visual disturbance, ataxia, dysarthria, tremor, lethargy,
memory impairment, euphoria, constipation, dry mouth, depression, confusion, agitation,
hallucinations, excessive salivation, sweating, flushing, rash, muscle cramp, myalgia,
thrombocytopenia, hypotension, hypertension.

Drug interaction Concurrent use with oxycodone, Lorazepam and ethanol may increase the
CNS effect.

METHYLCOBALAMIN

Indications To prevent neurological disorder in patients with neuropathy due to diabetes,

alcohol or other drug induced neuropathies.
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Dose Initially 1000 μg 3 times a day for 2 weeks, thereafter 1000μg every 3 months by
intramuscular injection in case of pernicious anaemia and other macrocytic anaemia. Incase with
neurological involvement, initially 1μg on alternate days. Until non further improvement,
thereafter 1000μg every 2 to 3 months. Prophylaxis: 1000 μg every 2 to 3 months.

Mechanism of action Mecobalamin is the neurologically active form of vitamin B12 and
occurs as a water-soluble vitamin in the body. It is a cofactor in the enzyme methionine synthase,
which functions to transfer methyl groups for the regeneration of methionine from homocysteine.
In anaemia, it increases erythrocyte production by promoting nucleic acid synthesis in the
bone marrow and by promoting maturation and division of erythrocytes.

Contraindications Hypersensitivity.

Precautions Allergies; pregnancy

Adverse Effects Itching; anaphylactic shock with parenterals, pulmonary oedema;CHF;

polycythemiavera

PYRIDOXINE

Indications Treatment of pyridoxine deficiency due to metabolic disorders; isoniazid

neuropathy; sideroblastic anaemia.

Dose Oral Adult- Deficiency states: 25 to 50 mg up to 3 times daily. Isoniazid neuropathy,

prophylaxis: 10 mg daily. Isoniazid neuropathy, treatment: 50 mg, 3 times daily. Sideroblastic
anaemia: 100 to 400 mg daily in divided doses.

Mechanism of action Pyridoxine is a water-soluble vitamin which functions in the

metabolism of carbohydrates, proteins and fats. It is essential in Hb formation and GABA
synthesis within the CNS. It also aids in the release of glycogen stored in the liver and muscles

Precautions Interactions pregnancy

Adverse Effects Generally well tolerated, but chronic administration of high doses may cause
peripheral neuropathies; paresthesia; neurotoxicity; muscular weakness.

THIAMINE
Indications Prevention and treatment of vitamin B1 deficiency, acute alcohol intoxication.

Dose OralAdult- Mild chronic thiamine deficiency: 10 to 25 mg daily.Acute alcohol

intoxication: 50-100 mg daily.Wernicke-Korsakoff syndrome: 50-100 mg daily.
 18

Mechanism of action Thiamine, a water soluble vitamin, combines with ATP to form
thiamine pyrophosphate, an essential coenzyme in carbohydrate metabolism.

Precautions Parenteral administration, lactation; pregnancy

Adverse Effects Nausea; urticaria; gastrointestinal bleeding; oedema; pruritus; dizziness;

anorexia

BENFOTIAMINE
Indication Alcoholic neuropathy, Diabetic neuropathy

Dose Adult: 100 mg 4 times daily.

Mechanism of action Benfotiamine is an allithiamine that boosts Advanced Glycation

Endproduct (AGE)-inhibiting thiamine pyrophosphate and cell-shielding transketolase activity

Contraindications Hypersentivity.

FOLIC ACID

Indications& Dose Adult: PO Folate-deficient megaloblastic anaemia 5 mg/day for 4 mth, up to

15 mg/day in malabsorption states. Prophylaxis of megaloblastic anaemia in pregnancy 0.2-0.5
mg/day.Prophylaxis of neural tube defect in pregnancy 4 or 5 mg/day. Supplement for women of
child-bearing potential 0.4 mg/day.

Mechanism of action Folic acid is essential for the production of certain coenzymes in many
metabolic systems such as purine and pyrimidine synthesis. It is also essential in the
synthesis and maintenance of nucleoprotein in erythropoesis. It also promotes WBC and platelet
production in folate-deficiency anaemia.

Contraindications Undiagnosed megaloblastic anaemia; pernicious, aplastic or normocytic

anaemias.

Precautions Treatment resistance may occur in patients with depressed haematopoiesis,

alcoholism, deficiencies of other vitamins. Neonates.

Adverse Drug Reactions GI disturbances, hypersensitivity reactions; bronchospasm.

Drug Interactions Antiepileptics, oral contraceptives, anti-TB drugs, alcohol, aminopterin,

methotrexate, pyrimethamine, trimethoprim and sulphonamides may result to decrease in serum
folate contrations. Decreases serum phenytoin concentrations.
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NICOTINAMIDE

Indication Treatment and prophylaxis of nicotinic acid deficiency

Dose Adult: Up to 500 mg daily in divided doses. May also be given via IM or by slow IV inj.

Mechanism of action Nicotinamide is a vitamin B3 derivative. It is incorporated into

coenzymes nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine
dinucleotide phosphate (NADP), which are involved in multiple cellular metabolic pathways.

Precautions Peptic ulcer; liver disease; gall bladder disease, DM; gout; bleeding problems.
Pregnancy, lactation.

Adverse Drug Reactions Elevated LFT values, liver damage e.g. jaundice, parenchymal liver
cell injury; orthostatic hypotension; tachycardia, irregular heartbeat; nausea, vomiting, diarrhoea,
abdominal pain; headache, dizziness, fever. Inj: skin rash, itching, wheezing. Topical: Dry skin,
pruritus, erythema; burning sensation, irritation.

Drug Interactions May decrease clearance of carbamazepine and primidone.

CALCIUM PANTOTHENATE

Indications Calcium Pantothenate is primarily indicated in conditions like Vitamin deficiency,

and can also be given in adjunctive therapy as an alternative drug of choice in Hyperlipidemia,
Nephropathic cystinosis, Paralytic ileus.

Dose Adult 50 to 100 mg ,24 hourly PO,IM

Mechanism of action Pantothenic acid is a precursor of coenzyme A and is required for various
metabolic functions, including metabolism of carbohydrates, proteins, and lipids. Pantothenic
acid may also be necessary for normal epithelial function

Contraindications Hypersensitivity