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ASIPP’s Comprehensive Pain Medicine Board Review Course-2007

SECTION 5

Pharmacology

Directions: Choose the best answer


A. Acetazolamide
1267. With increasing concentrations of a local anesthetic, the
B. Furosemide
order of effect is
C. Hydrochlorothiazide
A. Pain fibers—sensory fibers—motor fibers
D. Mannitol
B. Sensory fibers—pain fibers—motor fibers
E. Spironolactone
C. Pain fibers—motor fibers—sensory fibers
D. Sensory fibers—motor fibers—pain fibers
1272. The following drug is not associated with enhancement
E. Sensory fibers—motor fibers—pain fibers
of the activity of g-aminobutyric acid (GABA)
A. Chlordiazepoxide
1268. Akathisia, Parkinson-like syndrome, galactorrhea, and
B. Phenobarbital
amenorrhea are side effects of perphenazine, caused
C. Diazepam
by
D. Valproic aicd
A. Blockade of muscarinic receptors
E. Chlorpromazine
B. Blockade of Alpha-adrenergic receptors
C. Blockade of dopamine receptors
1273. Which of the following is unlikely to be associated with
D. Supersensitivity of dopamine receptors
oral drug administration of an enteric-coated dosage
E. Stimulation of nicotinic receptors
form?
A. Irritation to the gastric mucosa with nausea and vomit-
1269. A patient on Lorazepam for fibromyalgia has been out
ing
of drug for four days. He presents with rhinorrhea,
B. Destruction of the drug by gastric acid or digestive en-
etc.Treatment of choice is:
zymes
A. Clonidine
C. Unpleasant taste of the drug
B. Gabapentin
D. Formation of nonabsorbable drug-food complexes
C. Diazepam
E. Variability in absorption caused by fluctuations in gastric
D. Oxycodone
emptying time
E. Methadone
1274. Tachyphylaxis to local anesthetics is most closely related
1270. Which of the following is a true labeled indication for
to the following
prescribing CNS stimulants?
A. Speed of injection
A. Narcolepsy
B. Dosing interval
B. Enhanced alertness for driving
C. Temperature of local anesthetic
C. Reversing opioid induced sedation
D. Volume of local anesthetic
D. Chronic pain associated with thalamic strokes
E. pH of solution
E. Fibromaylgia syndrome
1275. Which of the following is considered to be the most
1271. A 59-year-old woman with a 60 pack-year smoking
cardio-toxic?
history was diagnosed with lung cancer 2 months
A. Bupivacaine S-isomer
ago. She now enters the hospital in coma. Her serum
B. Bupivacaine racemic mixture
calcium is 16 mg/dL. Which of the following (given
C. Bupivacaine R-isomer
with IV fluids) would be most useful to reduce serum
D. Ropivacaine
calcium in this patient rapidly?
E. Lidocaine
246 Section 5 •Pharmacology

1276. Intrathecal baclofen may be indicated for B. Cefepime


A. Spasticity C. Ciprofloxacin
B. Neuropathic Pain D. Ticarcillin-clavulanate
C. nociceptive Pain E. Tobramycin
D. somatic Pain
E. Pelvic pain 1283. Which of the following is highly selective inhibitor of
cyclooxygenase II?
1277. The consumption of shellfish harvested during a “red A. Aspirin
tide” (due to a large population of a dinoflagellate B. Acetaminophen
species) is not recommended. This is because the C. Ibuprofen
shellfish are likely to contain D. Celecoxib
A. Arsenic E. Piroxicam
B. Botulinum toxins
C. Cyanide 1284. Regarding the thiazolidinediones used in diabetes
D. Saxitoxin mellitus, which one of the following statements is
E. Tetrodotoxin false?
A. They are inducers of liver drug-metabolizing enzymes
1278. A 23-year-old heroin addict was brought to a hospital B. They interact with peroxisome-proliferator-activated
suffering from marked bradykinesia, muscle rigidity, receptors
and tremor at rest. Unfortunately, the extrapyramidal C. Hypoglycemia is a major problem when they are used as
dysfunction was permanent in this patient, since he sole agents in type 2 diabetes
had self-administered this agent this is cytotoxic to D. They reduce both fasting and postprandial hyperglyce-
nigrostriatal dopaminergic neurons. mia
A. MDMA E. Though rare, troglitazone has caused liver failure
B. MPTP
C. Ma-huang 1285. Which best describes the mechanism of interaction of
D. Meperidine cimetidine with benzodiazepine?
E. Mescaline A. It decreases benzodiazepine’s metabolism
B. It decreases benzodiazepine’s sensitivity at the site of
1279. Which of the following local anesthetics may cause action
methemoglobinemia? C. It decreases benzodiazepine’s renal excretion
A. Prilocaine D. It decreases benzodiazepine’s plasma protein binding
B. Ropivacaine E. It decreases benzodiazepine’s intestinal absorption
C. Bupivacaine
D. Procaine 1286. The three scales of the Minnesota Multiphasic Personality
E. Chloroprocaine Inventory (MMPI) included in the “conversion V” are:
A. Hypochondriasis, psychasthenia, depression
1280. The pharmacologic effects of acetylsalicylic acid B. Hypochondriasis, depression, hysteria
(Aspirin®) include C. Paranoia, hysteria, depression
A. Reduction in elevated body temperature D. Social introversion, depression, hysteria
B. Promotion of platelet aggregation E. Hypochondriasis, anxiety, somatization
C. Alleviation of pain by stimulation of prostaglandin
synthesis 1287. The most likely cause of these signs and symptoms is
D. Efficacy equal to that of acetaminophen as an anti-in- overdosage of
flammatory agent A. Aspirin
E. Less gastric irritation than other salicylates B. Acetaminophen
C. Dextromethorphan
1281. If one patient is taking amitriptyline (Elavil®) and D. Diphenhydramine
another patient is taking chlorpromazine (Thorazine®), E. Ethanol
they are both likely to experience the following:
A. Excessive salivation 1288. The elimination half-life of which of the following
B. Extrapyramidal dysfunction tetracyclines remains unchanged when the drug is
C. Gynecomastia administered to an anuric patient?
D. Increased gastrointestinal motility A. Methacycline
E. Postural hypotension B. Oxytetracycline
C. Doxycycline
1282. If a single drug is to be administered to this patient the D. Tetracycline
most appropriate choice in terms of efficacy and safety E. None of the above
is
A. Ampicillin

ASIPP
Section 5 • Pharmacology 247

1289. Which of the following best describes the protein 1296. Which one of the following drugs mimics the activity of
binding properties of albumin for local anesthetics? metenkephalin in the dorsal horn of the spinal
A. Low affinity, low capacity A. Deprenyl (selegiline)
B. Low affinity, high capacity B. Trihexyphenidyl
C. High affinity, low capacity C. Baclofen
D. High affinity, high capacity D. Morphine
E. High affinity only E. Phenobarbital

1290. The phenothiazines have a variety of actions at different 1297. In the managemen of this patient, which one of the
receptor types. However, they do NOT appear to following procedures is not likely to have therapeutic
interact with receptors for value?
A. Dopamine A. Alkalinization of the urine
B. Histamine B. Correction of metabolic acidosis and electrolyte imbal-
C. Nicotine ance
D. Norepinephrine C. Gastric lavage with an endotracheal tube in place
E. Muscarine D. Hemodialysis, if pH or CNS signs are not readily con-
trolled
1291. A psychiatric patient taking medications develops a E. Treatment with acetylcysteine
tremor, thyroid enlargement, and leukocytosis. The
drug he is taking is most likely to be 1298. The first local anesthetic used clinically was
A. Clomipramine (Anafranil®) A. Cocaine
B. Haloperidol (Haldol®) B. Tetracaine
C. Imipramine(Tofranil®) C. Lidocaine
D. Lithium D. Bupivacaine
E. Sertraline( Zoloft®) E. Mepivacaine

1292. Inhibitors of serotonin (5-HT) uptake such as paroxetine 1299. The highest concentration of phenol clinically used in
(Paxil®) interact significantly with which of the neurolytic blocks is:
following drugs? A. 6%
A. Chlorpromazine B. 10%
B. Tranylcypromine C. 20%
C. Halothane D. 40%
D. Benztropine E. 100%
E. Digoxin
1300. In addition to its use in the treatment of schizophrenia,
1293. Which of the following agents does not act on chlorpromazine is effective
prostaglandins peripherally, and as such does not A. In reducing nausea and vomiting
block local inflammation? B. As an antihypertensive agent
A. Acetaminophen® C. As an antihistaminic
B. Ibuprofen® D. In the treatment of depression
C. Naproxen® E. For treating bipolar affective disorder
D. Celebrex®
E. Aspirin® 1301. Recreational use of drugs sometimes leads to
dependence. Which of the following is LEAST likely to
1294. The mechanism of action of benzodiazepines is cause physical dependence?
A. Activation of GABAb receptors A. Amphetamine
B. Antagonism of glycine receptors in the spinal cord B. Cocaine
C. Blockade of the action of glutamic acid C. Heroin
D. Increased GABA-mediated chloride ion conductance D. Mescaline
E. Inhibition of GABA aminotransferase E. Secobarbital

1295. Which one of the following statements about 1302. Which one of the following effects of the opioid
scopolamine is false? analgesics is most likely to be mediated via activation
A. It has depressant actions of the CNS of mu receptors?
B. It may cause hallucinations A. Cough suppression
C. It is poorly distributed across the placenta to the fetus B. Elevation of arterial PCO2
D. It may prevent motion sickness and vertigo when ap- C. Emesis
plied as a patch to the skin D. Sedation
E. It is similar to atropine in reducing gastrointestinal mo- E. Vasodilation
tility

ASIPP
248 Section 5 •Pharmacology

1303. A 38-year-old divorced woman who lived alone visited a B. It is a selective D2 receptor agonist
psychiatrist because she was depressed. Her symptoms C. Its mechanism of action is completely different from that
included low self-esteem, with frequent ruminations of chlorpromazine
on her worthlessness, and hypersomnia. She was D. It is more potent as an antipsychotic drug than is chlor-
hyperphagic and complained that her limbs felt heavy. promazine
An initial diagnosis was made of a major depressive E. It produces a lower incidence of extrapyramidal reac-
disorder with atypical symptoms. Treatment was tions than does chlorpromazine
initiated with amitriptyline, but after 2 months the
patient had not improved significantly. Which one of 1309. Of the following characteristics, which is unlikely to be
the following drugs is MOST likely to have therapeutic associated with the process of facilitated diffusion of
value in this depressed drugs?
A. Buprenorphine A. The transport mechanism becomes saturated at high
B. Diazepam drug concentrations
C. Paroxetine B. The process is selective for certain ionic or structural
D. Methylphenidate configurations of the drug
E. Risperidone C. If two compounds are transported by the same mecha-
nism, one will competitively inhibit the transport of
1304. Which of the following corticosteroids has the highest the other
anti-inflammatory potency? D. The drug crosses the membrane against concentration
A. Betamethasone gradient and the process requires cellular energy
B. Triamcinolone diacetate E. The transport process can be inhibited noncompetitively
C. Triamcinolone acetonide by substances that interfere with cellular metabolism
D. Depo-methylprednisolone
E. Hydrocortisone
1310. A young woman presents with a several-year history
1305. What is the maximum dose of lidocaine without of ulcerative colitis. Recently she has been treated
epinephrine? with alprazolam 0.5 mg Q 8 hrs. This pharmacologic
A. 2 mg/kg treatment can be expected to:
B. 3 mg/kg A. Reduce stress and anxiety
C. 4 mg/kg B. Result in long-term improvement
D. 5 mg/kg C. Reduce interpersonal dilemmas
E. 6 mg/kg D. Produce a mild stimulus
E. Be used without development of tolerance
1306. Psychiatric evaluation of a patient after 6 weeks of
treatment with a monoamine oxidase inhibitor 1311. Which one of the following statements about cocaine is
(MAOI) shows no improvement. The psychiatrist now false?
writes a prescription for fluoxetine which the patient A. Blocks sodium channels in axonal membranes
starts two days after her final dose of the MAOI. Since B. Blood pressure increase is due to its ability to release nor-
the MAOIs used as antidepressants continue to exert epinephrine from sympathetic nerve terminals
effects for 2 or more weeks after discontinuance, the C. Cardiac arrhythmias may occur at high doses
most likely result of the administration of fluoxetine D. Derived from a botanical source
now will be to cause E. Topical application can provide local anesthesia and re-
A. A rapid amelioration of her depressive symptoms strict bleeding
B. Electrocardiographic abnormalities
C. Extrapyramidal dysfunction 1312. The pKa of Lidocaine is:
D. The serotonin syndrome A. 7.4
E. Weight gain B. 7.6
C. 7.7
1307. After an intravenous bolus injection of lidocaine, D. 8.0
the major factors determining the initial plasma E. 8.2
concentration are
A. Dose and clearance 1313. Clinically significant methemoglobinemia may result
B. Dose and apparent volume of distribution from administration of large doses of
C. Apparent volume of distribution and clearance A. Chloroprocaine
D. Clearance and half-life B. Bupivacaine
E. Half-life and dose C. Etidocaine
D. Prilocaine
1308. Haloperidol may best be characterized by which of the E. Lidocaine
following statements?
A. It is classified as a phenothiazine

ASIPP
Section 5 • Pharmacology 249

1314. Which of the following statements is most correct? C. Ropivacaine


A. Maximum efficacy of a drug is directly correlated with D. Mepivacaine
its potency E. Procaine
B. The therapeutic index if the LD50 (or TD50) divided by
the ED50 1321. Which of the following statements about antiplatelet
C. A partial agonist has no effect on its receptors unless drugs is false?
another drug is present A. Abciximab is a monoclonal antibody that binds to the
D. Graded dose-response data provide information about glycoprotein IIb/IIIa receptor
the standard deviation of sensitivity to the drug in the B. Decreased formation of thromboxane underlies the anti-
population studied platelet action of aspirin
E. Quantal dose-response curves provide information C. Ibuprofen reversibly inhibits cyclooxygenase in platelets
about the efficacy of a drug D. Ticlopidine is an inhibitor of the platelet thrombin
receptor
1315. The toxicity spectrum of aspirin does not include E. Dipyridamole is occasionally used with warfarin in pa-
A. Increased risk of encephalopathy in children with viral tients with artificial heart valves
infections
B. Increased risk of peptic ulcers 1322. Morphine 300 mg po is equivalent to:
C. Hyperprothrombinemia A. Morphine 10mg intrathecally
D. Metabolic acidosis B. Sufentanyl 100mcg intrathecally
E. Respiratory alkalosis C. Morphine 1mg intrathecally
D. Fentanyl 1mcg intrathecally
1316. In comparing the following possible routes, which is E. Codeine 60 mg orally
associated with the excretion of quantitatively small
amounts of drugs or their metabolic derivatives? 1323. A phase II clinical trials typically involve
A. Biliary tract A. Measurement of the pharmacokinetics of the new drug
B. Kidneys in normal volunteers
C. Lungs B. Double-blind evaluation of the new drug in thousands of
D. Feces patients with target disease
E. Milk C. Postmarketing surveillance of drug toxicities
D. Evaluation of the new drug in 50 to several hundred
1317. Although it does not act at any histamine receptor, patients with the target disease
epinephrine reverses many effects of histamine. E. Collection of data regarding late-appearing toxicities fro
Epinephrine is a patients previously studies in phase I trials
A. Competitive inhibitor of histamine
B. Noncompetitive antagonist of histamine 1324. Which one of the following drugs is used in the treatment
C. Physiologic antagonist of histamine of male impotence and activates prostaglandin E1
D. Chemical antagonist of histamine receptors?
E. Metabolic inhibitor of histamine A. Alprostadil
B. Fluoxetine
1318. Carbidopa is useful in the treatment of Parkinson’s C. Mifepristone
disease because it D. Sildenafil
A. Is a precursor of levodopa E. Zafirlukast
B. Is a dopaminergic receptor agonist
C. Prevents peripheral biotransformation of L-dopa 1325. A patient with Zollinger-Ellison syndrome has been
D. Prevents a breakdown of dopamine receiving high doses of cimetidine for 7 weeks. A
E. Promotes a decreased concentration of L-dopa in the frequent adverse effect of cimetidine is
nigrostriatum A. Agranulocytosis
B. Systemic lupus erythematosus
1319. Most drug receptors are C. Inhibition of hepatic metabolism of other drugs
A. Small molecules with a molecular weight between 100 D. Antiestrogenic effects
and 1000 E. Hypertension
B. Lipids arranged in a bilayer configuration
C. Proteins located on cell membranes or in the cytosol 1326. A 45-year-old patient is to have reconstructive surgery
D. DNA molecules on a hand that was recently injured in an accident. The
E. RNA molecules anesthesiologist plans to use regional anesthesia of the
arm for a fairly long procedure. The amide-type local
1320. Which of the following local anesthetics is the least anesthetic with the longest duration of action is
protein bound? A. Cocaine
A. Lidocaine B. Bupivacaine
B. Bupivacaine C. Lidocaine

ASIPP
250 Section 5 •Pharmacology

D. Procaine E. Etidocaine
E. Tetracaine
1333. Seizures occur at what serum concentration range for
1327. Which of the following local anesthetics is useful for lidocaine?
topical (surface) administration only? A. 10-12 µg/mL
A. Procaine B. 10-12 ng/mL
B. Bupivacaine C. 100-120µg/mL
C. Etidocaine D. 1-1.2 mg/mL
D. Benzocaine E. 10-12 mg/mL
E. Lidocaine
1334. The serum concentration of lidocaine would be highest
1328. Beta-lactamase production by strains of Haemophilus with which route of administration…..specifically at
influenzae, Moraxella catarrhalis, and Neisseria 60 minutes after administration?
gonorrhoeae confers resistance against penicillin G. A. Intravenous
Which one of the following antibiotics is most likely B. Epidural
to be effective against all strains of each of the above C. Brachial Plexus
organisms? D. Intercostal
A. Ampicillin E. Subarachnoid
B. Ceftriaxone
C. Clindamycin 1335. Which of the following corticosteroids has the highest
D. Gentamicin anti-inflammatory potency
E. Piperacillin A. Cortisone
B. Prednisone
1329. Which of the following drugs increase alprazolam’s half C. Triamcinolone
life? D. Methylprednisone
A. Fluoxetine (Prozac®) E. Dexamethasone
B. Fluvoxamine (Luvox®)
C. Paroxetine (Paxil®) 1336. The most common adverse effect associated with the
D. Sertraline (Zoloft®) tricyclic antidepressants is
E. Clozapine (Clozaril®) A. Anticholinergic effects
B. Seizures
1330. Of the following antiepileptic agents, which is associated C. Arrythmias
with causing psychosis? D. Hepatotoxicity
A. Phenobarbital E. Nephrotoxicity
B. Ethosuximide
C. Phenytoin 1337. Concomitant SSRI and TCA therapy can lead to which
D. Vigabatrin of the following:
E. Valproic acid A. Elevated TCA blood levels
B. Decreased TCA blood levels
1331. A patient with terminal cancer is suffering from pain that C. Increased SSRI blood levels
is gradually increasing in intensity. In the management D. Decreased SSRI blood levels
of pain in such a patient E. Increased TCA and SSRI blood levels
A. Physical dependency occurs universally in later stages of
the disease 1338. The serum concentration of lidocaine would be highest
B. To delay the development of dependency, opioid anal- with which route of administration…..specifically at 5
gesics should never be given for initial management of minutes after administration?
chronic pain A. Intravenous
C. Meperidine is more effective than morphine in cancer B. Intercostal
pain states C. Epidural
D. Nonsteroidal anti-inflammatory drugs may control D. Brachial Plexus
symptoms during a significant portion of the course E. Subcutaneous
of the disease
E. The placebo effect is absent 1339. Acetyl salicylic acid (aspirin) exerts its action by:
A. Prostaglandin synthesis
1332. Which of the following are hydrolyzed by plasma B. Inhibiting platelet aggregation
pseudocholinesterases? C. Antipyretic action at the hypothalamus
A. Lidocaine D. Inactivating cyclooxygenase
B. Ropivacaine E. All of the above
C. Bupivicaine
D. Tetracaine

ASIPP
Section 5 • Pharmacology 251

1340. Which of the following is most correct about modern brane-bound receptors increases the activity of an
psychopharmacology? intracellular second messenger
A. There is a one-diagnosis-one-drug approach E. Activation of membrane-bound receptors and subse-
B. Many variables affect the practice of psychopharmacol- quent intracellular events elicit a biologic response
ogy through the transcription of DNA
C. Medications must be given in large dosages for months
to work 1346. The antidepressant with the least sedation side effect is:
D. Monitoring is rarely necessary and dose adjustments are A. Desipramine
infrequently warranted B. Trazadone
E. Medications exert their effect with in hours. C. Nortriptyline
D. Maprotiline
1341. The earliest sign of lidocaine toxicity is: E. Amitriptiline
A. Shivering
B. Nystagmus 1347. The side effects of intravenous (IV) local anesthetics are
C. Lightheadedness and dizziness related to central nervous system (CNS) toxicity. Signs
D. Toxic-clonic seizures are all of the following EXCEPT
E. Nausea and vomiting A. Metallic taste
B. Tinnitus
1342. A 35-year-old female who has never been pregnant C. Agitation
suffers each month from pain, discomfort, and mood D. Increased appetite
depression at the time of menses. She may benefit E. Convolusions
from the use of this selective inhibitor of the reuptake
of serotonin. 1348. Which of the following statements is true?
A. Amitriptyline A. Acetaminophen leads to more toxicity annually than
B. Bupropion NSAIDs
C. Mirtazapine B. Aspirin is known to have a lower annual associated toxic-
D. Paroxetine ity cost compared to acetaminophen
E. Trazodone C. NSAIDs cause fewer GI toxicity events than acetamino-
phen and aspirin
1343. Efficacy with TCAs in treating depression is generally D. Acetaminophen use is associated with a lower annual
thought to be seen in____ toxicity cost
A. 1 to 3 days E. Aspirin produces a temporary effect on platelet aggrega-
B. 3 to 7 days tion
C. 3 to 7 weeks
D. 6 to 8 weeks 1349. Distribution of medication into the brain is most
E. After 2 months commonly governed by which of the following?
A. Regional cerebral blood flow
1344. Carisoprodol (Soma®) is associated with all of the B. Abnormalities in the blood-brain barrier
following EXCEPT: C. Percent of the drug that is protein bound
A. Potentially habituating, with potential for abuse D. Relative density of target receptors for binding
B. Hepatic impairment E. Gastric and intestinal motility
C. Excessive sedation
D. Direct central brain stem activity 1350. Norepinephrine will cause contraction of the smooth
E. Dizziness, vertigo, ataxia and tremor muscle in
A. Bronchioles
1345. Of the following, which is unlikely to be associated B. Pupils
with receptors bound to plasma membranes, their C. Intestine
interaction with ligands, and the biologic response to D. Arterioles
this interaction? E. Ciliary body
A. Structurally, these receptors have hydrophobic amino
acid domains, which are in contact with the membrane, 1351. When an inactive substance or condition induces a
and hydrophilic regions, which extend into the extracel- therapeutic change, the procedure (result) is called
lular fluid and the cytoplasm A. Nonpharmaceutical reaction
B. Chemical interactions of ligands with these receptors B. Modulated conditioning
may involve the formation of many types of bonds, in- C. Placebo effect
cluding ionic, hydrogen, van der Waals’, and covalent D. Reaction formation
C. Ligand-receptor interactions are often stereospecific E. Fantasy reaction
(i.e., one stereoisomer is usually more potent than the
other)
D. In some cases, a ligand that acts as an agonist at mem-

ASIPP
252 Section 5 •Pharmacology

1352. The drug of choice for the management of osteoporosis 1359. Which of the following is an antidepressant agent that
caused by high-dose use of glucocorticoids is selectively inhibits serotonin (5-HT) uptake with
A. Alendronate minimal effect on norepinephrine uptake
B. Calcitonin A. Protriptyline
C. Mestranol B. Maprotiline
D. Oxandrolone C. Fuoxetine
E. Vitamin D D. Desipramine
E. Amoxapine

1353. Catecholamines are all of the following, except 1360. The opioid which has been implicated in Torsade de
A. Drugs that contain a 3,4 dihydroxybenzene structure Pointes is:
B. Are produced by monoamine oxidase A. Morphine
C. Are inactivated by catechol-O-methyl transferase B. Meperidine
D. Are most effectively inactivated by synaptic re-uptake C. Buprenorphine
E. Broken down into byproducts, one of which is meta- D. Methadone
nephrine E. Propoxyphene

1361. Which of the following is false?


1354. Synaptic action of catecholamines is terminated by A. The rate of renal dose dopamine is 1-3mcg/kg/minute
A. Monoamine oxidase B. Renal dose dopamine promotes diuresis
B. Tyrosine hyroxylase C. Renal dose dopamine has been conclusively demon-
C. Norepinephrine transporter strated to prevent acute renal failure
D. Catechol-O-methyl transferase D. Renal dose dopamine may exacerbate bacterial translo-
E. Aromatic amino transferase cation in the presence of mesenteric ischemia
E. Metoclopramide may interfere with dopamine effects on
the kidney
1355. The primary determinant of local anesthetic potency is
A. pKa 1362. Which is true? Propanolol…
B. Molecular weight A. Does not decrease heart rate and cardiac contractility
C. Lipid solubility B. Is not subject to a significant hepatic first pass effect
D. Concentration C. Is not poorly protein bound
E. Protein binding D. Does not reduce the clearance of local anesthetics
E. Does not increase airway resistance

1356. Which of the following is a selective inhibitor of 1363. A patient has been taking aspirin for rheumatoid
monoamine oxidase type B (MAO-B) and, therefore, arthritis for 8 years. Exacerbations are becoming
useful in treating parkinsonism? worse and she asks the physician about drugs that
A. Bromocriptine might stop the progression of the disease. Which
B. Carbidopa one of the following is not a disease-modifying (slow-
C. Selegiline acting) antirheumatic drug?
D. Phenelzine A. Auranofin
E. Tranylcypromine B. Hydroxychloroquine
C. Methotrexate
1357. Two drugs may act on the same tissue or organ through D. Penicillamine
independent receptors, resulting in effects in opposite E. Rofecoxib
directions. This is known as
A. Physical antagonism 1364. A 24-year-old schizophrenic man has been treated for
B. Chemical antagonism several years with haloperidol but, since parkinsonism-
C. Competitive antagonism like effects are worsening, the drug is discontinued and
D. Irreversible antagonism treatment is started with olanzapine. Which one of
E. Dispositional antagonism the following statements about the new medication is
false?
1358. The intrathecal equivalent of the epidural administration A. Antipsychotic effects may take several weeks to develop
of 10 mg of morphine is: B. Alleviates some of the negative symptoms of schizo-
A. 0.1 mg phrenia
B. 1 mg C. Causes agranulocytosis
C. 5 mg D. Has a greater affinity for serotonin receptors than for
D. 10 mg dopamine receptors in the CNS
E. 0.5 mg E. Less effect on pituitary function than haloperidol

ASIPP
Section 5 • Pharmacology 253

1365. The main advantage of neurolytic nerve blockade with 1372. Which of the following local anesthetics has the lowest
phenol versus alcohol is ratio of dosage for cardiovascular collapse to dosage
A. Denser blockade required for central nervous system toxicity?
B. Blockade is permanent A. Lidocaine
C. The effects of the block can be evaluated immediately B. Etidocaine
D. The block is less painful C. Bupivacaine
E. Phenol is selective for sympathetic fibers D. Prilocaine
E. Chloroprocaine
1366. Of the following, which is a phase II biotransformation
reaction? 1373. The correct arrangement of local anesthetics in order
A. Sulfoxide formation of their ability to produce cardiotoxicity from most
B. Nitro reduction to least is:
C. Ester hydrolysis A. Bupivacaine, lidocaine, ropivacaine
D. Sulfate conjugation B. Bupivacaine, ropivacaine, lidocaine
E. Deamination C. Ropivacaine, bupivacaine, lidocaine
D. Lidocaine, ropivacaine, bupivacaine
1367. The concentration of epinephrine corresponding to a 1: E. Lidocaine, bupivacaine, ropivacaine
200,000 mixture is:
A. 0.5 µg/mL 1374. The antidepressant below with the highest risks of
B. 5 µg/mL inducing seizures is:
C. 50 µg/mL A. Doxepin
D. 0.5 µg/mL B. Trazadone
E. 0.1 mg/mL C. Amitriptyline
D. Maprotiline
1368. Damage to dopamine neurons in the midbrain is a E. Nortriptyline
central feature of the pathophysiology of Parkinsons
disease. The loss of midbrain dopamine in this disease 1375. The antidepressant below with the least anticholinergic
is accompanied by and least sedating effects is:
A. An increase in the dopamine transporter A. Amitriptyline
B. A decrease in dopamine 1 receptor density B. Imipramine
C. An increase in dopamine 2 receptor density C. Doxepin
D. A decrease in dopamine synthesis in remaining dopa- D. Trazadone
mine neurons E. Desipramine
E. An increase in both dopamine 1 and dopamine 2 recep-
tor density 1376. Adrenergic receptors are coupled to
A. G proteins
1369. What would be the most appropriate dose of ephedrine, B. Tyrosine kinase
for a patient that has a fall in blood pressure, following C. Sodium channels
epidural anesthesia? D. Cyclo-oxygenase
A. 10-25 mg E. Nerve growth factor
B. 100-250 micrograms
C. 10-25 micrograms 1377. All of the following medications can cause sexual
D. 1-2.5 micrograms dysfunction. However, the following drug does not
E. 100-250 mg inhibit desire or decrease arousal.
A. Amphetamines
1370. Clonidine B. Phenothiazines
A. Preferentially inhibits alpha 1 receptors C. alpha -Methyldopa
B. Only binds to alpha 2 receptors D. Guanethidine
C. Prolongs the sensory block of subarachnoid bupiva- E. Tricyclic Anti-Depressents
caine
D. Produce pruritis, epidurally 1378. Local anesthetic per spinal segment to patients between
E. Does not reduce shivering 20 and 40 years of age receiving an epidural is most
likely limited to
1371. Which of the following irreversibly inhibits alpha A. 0.5 mL
receptors? B. 1.0 mL
A. Phentolamine C. 1.5 mL
B. Prazosin D. 2.0 mL
C. Phenoxybenzamine E. 2.5 mL
D. Esmolol
E. Clonidine

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254 Section 5 •Pharmacology

1379. The maximum dose of lidocaine containing 1:200,000 C. Nystatin, for a yeast infection
epinephrine that can be administered to a 70-kg D. Phentermine, used for weight reduction
patient for regional anesthesia is E. Triazolam, used as a sleeping pill
A. 50 mg
B. 100 mg 1386. Accidental poisonings are common with both aspirin
C. 200 mg and ibuprofen, two OTC drugs available in tasty
D. 500 mg chewable tablets. In cases of overdose, aspirin is more
E. 1000 mg likely than ibuprofen to cause
A. Autonomic instability
1380. Which of the following is described as a competitive B. Hepatic necrosis
benzodiazepine receptor antagonist? C. Metabolic acidosis
A. Ketamine D. Thrombocytopenia
B. Chlordiazepoxide E. Ventricular arrhythmias
C. Flumazenil
D. Midazolam
E. Triazolam
Directions: Each question below contains four suggested
1381. Among the local anesthetics used for intravenous responses of which one or more is correct. Select
regional anesthesia (Bier block) the most rapidly A if 1, 2 and 3 are correct
metabolized and thus least toxic accentis: B if 1 and 3 are correct
A. Etidocaine C if 2 and 4 are correct
B. Lidocaine
D if 4 is correct
C. Ropivacaine
D. Prilocaine
E if All (1, 2, 3 and 4) are correct
E. Mepivacaine

1382. Intractable itching is best treated with:


1387. Newer COX-2 selective NSAIDs were believed to be
A. Chlorpromazine
preferred agents based on which of the following
B. Pimozide
criteria:
C. Haloperidol
1. Diminished renal toxicity
D. Risperidone
2. Diminished hepatic toxicity
E. Clozapine
3. Diminished platelet effects
4. Diminished gastrointestinal toxicity
1383. The polyethylene glycol in depot steroids
A. Does not cause degenerative lesions in nerves of experi-
mental animals
1388. Which one of the following best describes the
B. Is present in methylprednisolone but not triamcinolone
implications of aging on the activity of psychoactive
C. Is not concentrated enough in the commercial prepara-
medications?
tion to block nerve transmission
1. Absorption is increased due to decreased surface villi,
D. Does not cause arachnoiditis when injected intrathe-
gastric motility, intestinal perfusion & delayed gastric
cally
emptying
E. All of the above
2. Increased albumin lessens the amount of free medica-
tion carried in the blood
1384. Acetaminophen is a proven analgesic and anti-pyretic
3. Changes in liver & kidney function along with drug-
through action at:
drug interactions lead to increased metabolism, short-
A. Hypothalamus
ened half-lives, and less likely toxicity
B. Dorsal horn of the spinal cord
4. Distribution is altered due to decrease in total body
C. Modulation of neurotransmitter activity at the locus
water & lean body mass
ceruleus
D. By cholinergic enhancement of the GABA-B receptor
complex
1389. Which of the following antidepressant classes maintains
E. Acetaminophen is superior to aspirin in providing anal-
the best evidence for treating neuropathic pain?
gesia.
1. Selective Serotonin Reuptake Inhibitors
2. Heterocyclic Antidepressants
1385. A young mother is breast-feeding her 2-month-old
3. Serotonin Norepinephrine reuptake inhibitors
infant. Which one of the following drug situations
4. Tricyclic Antidepressants
involving the mother is MOST likely to be safe for the
nursing infant?
A. Doxycycline, for Lyme disease
B. Metronidazole, for trichomoniasis

ASIPP
Section 5 • Pharmacology 255

1390. Of the following agents is/are effective topical anesthetics 1397. Concomitant use of a COX-2 selective NSAID with
when applied to mucous membranes an ACE inhibitor potentially produces which of the
1. Lidocaine following adverse effects:
2. Cocaine 1. Hypotension via an additive pharmacodynamic effect
3. Tetracaine 2. Hypertension via an additive pharmacokinetic effect
4. Procaine 3. Hypotension via an opposing pharmacokinetic effect
4. Hypertension via an opposing pharmacodynamic ef-
1391. Which of the following best describes the receptor effects fect
of psychoactive medications?
1. Some agents are agonists for receptors and stimulate the 1398. Gabapentin is labeled by the Food and Drug
specific biological activity of the receptor Administration for use in:
2. Some agents are antagonists for receptors and inhibit 1. Epilepsy
biological activity 2. Myofascial pain syndrome.
3. Some agents are partial agonists because they cannot 3. Post herpetic neuralgia.
fully activate a specific receptor 4. Bi-polar disease
4. All antagonists stimulate receptor activity
1399. The seizure threshold for local anesthetics is raised by
1392. Most commonly observed side effects in adults who use 1. Hypokalemia
Gabapentin include: 2. Hyperoxia
1. Somnolence 3. Hypocarbia
2. Peripheral edema. 4. Acidosis
3. Dizziness.
4. Amnesia. 1400. Dopamine agonists include
1. Bromocriptine (Parlodel)
1393. Epidurally administered opioids encompass the 2. Pergolide (Permax)
following true statements. 3. Ropinirole (Requip)
1. Posterior radicular arteries transfer opioids to the dorsal 4. Prochlorperazine (Compazine)
horn
2. The epidural venous system carries opioids through the 1401. The triptan class of drugs are selective
systemic circulation 1. Muscarinic agonists
3. Epidural fat and opioids bind 2. Dopamine agonists
4. Opioids are carried through the dura by diffusing across 3. Cholinergic agonists
arachnoid granulations and enter the cerebrospinal 4. Serotonin agonists
fluid (CSF)

1394. Traditional NSAIDs (e.g. Ibuprofen) are now known to 1402. Local anesthetic metabolized by ester hydrolysis include
effect their pharmacodynamic activity via inhibition 1. Lidocaine
of: 2. Cocaine
1. Cyclooxygenase 1 3. Mepivacaine
2. Prostaglandin synthetase 4. Tetracain
3. Thromboxane synthetase
4. Cyclooxygenase 2 1403. Which of the following local anesthetic concentrations
is(are) isobaric?
1. 2% Lidocaine
1395. Which of the following local anesthetics depend on 2. 0.5% Tetracaine
hepatic blood flow for plasma clearance? 3. 0.5% Bupivacaine
1. Procaine 4. 0.75% Bupivacaine
2. Prilocaine
3. Tetracaine 1404. Which is true about the lumbar epidural instillation of
4. Lidocaine local anesthetics?
1. Ropivacaine and bupivacaine at identical concentra-
tions will provide identical depths and durations of
1396. Which of the following drugs have sodium channel motor block
blocking properties? 2. Local anesthetics diffuse across the dura and act on the
1. Lidocaine spinal cord and exiting nerve roots
2. Ziconotide 3. Hypotension, bradycardia, and high thoracic levels of
3. Quinidine sensor-motor block that occurs 10-15 minutes after an
4. Strychnine epidural test dose, suggest a subarachnoid block
4. Local anesthetics exit the intervertebral foramina and
cause multilevel paravertebral nerve blocks

ASIPP
256 Section 5 •Pharmacology

1405. Risk factors for induction of gastropathy and induction 1411. Plasma monitoring should be considered with a tricyclic
of gastroduodenal ulcers include: antidepressant in the following situation:
1. Age over 60 1. Lack of efficacy
2. Alcohol use 2. Suspected Non-compliance
3. Steroid use 3. Dosing in excess of 50 mg
4. Multiple NSAID use 4. Concurrent therapies with potential cardiac toxicity

1406. Which of the following statements about routes of 1412. Which of the following statements about alcoholics
administration of opioids is/are true: withdrawing from alcohol are true?
1. The rectal route may be used safely in patients with 1. Overhydration more likely than dehydration
thrombocytopenia. 2. Well-nourished patients should receive vitamins
2. The intravenous route is more effective than the subcu- 3. Often dependent also on other CNS depressants
taneous route. 4. Withdrawal syndrome followed by insomnia
3. The transdermal route yields predictable and stable
blood levels.
4. The transmucosal route may be effective in certain situ- 1413. Factor(s) that antagonize local anesthetics include
ations but it is expensive. 1. Tissue acidosis
2. Presence of myelin
3. Increasing fiber diameter
1407. True statements concerning local anesthetics include the 4. Rapid firing rate
following:
1. The un-ionized form of a local anesthetic binds to the
nerve membrane to actually block conduction 1414. Local anesthetic blockade is
2. If one node of Ranvier is blocked, conduction will be 1. Ionic
reliably interrupted 2. Reversible
3. The ability of a local anesthetic to block nerve conduc- 3. Frequency-dependant
tion is directly proportional to the diameter of the 4. Depolarizing
fiber
4. The presence of myelin enhances the ability of a local
anesthetic to block nerve conduction 1415. Which of the following are metabolized by monoamine
oxidase?
1. Norepinephrine
1408. Non Steroidal Anti Inflammatory medicines should be 2. Dopamine
used with caution with the following cotherapeutic 3. Epinephrine
agents: 4. Serotonin
1. Coumadin
2. Methotrexate
3. Lithium Carbonate 1416. Side effect/s of corticosteroids is/are:
4. H2 Antagonists 1. Hypoglycemia
2. Hyperkalemia
3. Decreased intraocular pressure
1409. Hepatic toxicity and NSAID is related to: 4. Psychosis
1. Class of NSAID
2. Pharmacokinetics of drug
3. Dose of drug 1417. A 29-year-old male requires suturing for a deep laceration
4. Cholestatic activity in his palm. He is allergic to benzocaine. Which of the
following local anesthetics could safely be used?
1. Cocaine
1410. Factor(s) that influence systemic absorption of local 2. Tetracaine
anesthetics include 3. Procaine
1. Site of injection of the local anesthetic 4. Bupivacaine
2. Lipid solubility of the local anesthetic
3. Addition of vasoconstrictor substances to the local
anesthetic 1418. Hypercalcemia can occur in the following:
4. Concentration of the local anesthetic 1. Renal cell carcinoma
2. Cushing’s syndrome
3. Hyperparathyroidism
4. Pituitary Adenoma

ASIPP
Section 5 • Pharmacology 257

1426. Which best describes the mechanism of interaction of


1419. Tricyclic toxicities are best described by which of the nonsteroidal anti-inflammatory drugs (NSAIDs) with
following? lithium salts?
1. Diarrhea and urinary frequency 1. They increase lithium intestinal absorption
2. Adverse effect on cardiac rhythm 2. They increase lithium plasma protein binding
3. No effect on other mental disorders other than relief of 3. They increase lithium sensitivity at its site of action
Major Depression 4. They increase lithium renal reabsorption
4. Delirium may result from central cholinergic blockade

1427. The elimination half-life of an amide local anesthetic is


1420. Symptoms of salicylate toxicity include: prolonged in which of the following the conditions?
1. Tinnitus 1. Liver disease
2. Acid-Base disturbances. 2. Term pregnancy
3. Dehydration 3. Heart failure
4. Mydriasis 4. Kidney disease

1421. Non-selective NSAID agents inhibit both: 1428. Epinephrine is effective in increasing the clinical
1. Cyclooxygenase-I Constitutive Pathway duration of action of
2. Leukotrienes Pathway 1. Procaine
3. Cyclooxygenase-II Inducible Pathway 2. Lidocaine
4. Arachidonic Acid Lipid Membrane Cascade 3. Tetracaine
4. Etidocaine

1422. Which of the following would indicate alcohol


dependence? 1429. Drugs that will decrease the plasma clearance of ester-
1. Persistent drinking, even though worsens gastric ulcers type local anesthetics include
2. Job efficiency impaired due to repeated hangovers 1. Echothiophate
3. Several unsuccessful attempts to cut down on drinking 2. N2O
4. Family history of alcoholism 3. Neostigmine
4. Phenytoin

1423. Pharmacokinetic properties and toxicity of NSAIDs


appear to be related to: 1430. True statements regarding additives to local anesthetics
1. Plasma half life for neuraxial blocks include
2. Protein binding 1. Intrathecal clonidine has analgesic properties
3. Dose of the drug 2. Intrathecal phenylephrine has analgesic properties
4. Hepatic function 3. Intrathecal epinephrine has analgesic properties
4. Addition of epinephrine to epidural local anesthetics
increases the incidence of hypotension
1424. Which of the following is true about local anesthetics?
1. They pass through the nerve membrane as in their base
form 1431. Anti Inflammatory medications exert their action at the
2. Once in the axoplasm, the ionized form that binds to tissue level by blocking:
the Na+ channel 1. Phospholipase A2
3. Those local anesthetics with PKa of 7.6 would be ex- 2. Arachidonic Acid Liberation at the Lipid Membrane
pected to have a faster onset of action compared to 3. Functional Leukotrienes
those with a PKa of 8.0 4. Lipoxygenase
4. The benzene ring is an important moiety in determing
the lipid solubility of ester local anesthetics
1432. Clonidine has been found to be a useful drug for
1. Nociceptive Pain
1425. Indentify accurate statements of central nervous system 2. Somatic Pain
effects of anti-inflammatory drugs? 3. Psychogenic pain
1. Reduction of hyperalgesia at the spinal level 4. Neuropathic Pain
2. Decreasing prostanoid production
3. Action at the central opioid mechanisms responsible
for analgesia
4. Inhibition of magnesium activation at the N-Methyl D
Aspartate Receptor

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258 Section 5 •Pharmacology

1433. Frequency-dependant anesthetic blockade is 1441. Pharmacogenetic variability in drug effects occur by:
characterized by 1. Differences in drug metabolism
1. Enhanced binding in open state 2. Altered levels of normal receptor protein
2. Reduced release in resting state 3. Variations in drug receptor binding
3. State-dependent phasic block 4. Acquired variations due to mutations
4. Deeper blockade at higher frequency

1442. Para-aminobenzoic acid is a metabolite of


1434. Receptors involved in opioid activity include: 1. Mepivacaine
1. Mu 2. Benzocaine
2. Delta 3. Bupivacaine
3. Kappa 4. Tetracaine
4. Gamma

1443. Which of the following classes of pharmacologic agents


1435. The following agents are Alpha-2 agonists, is(are) useful for nausea?
1. Clonidine 1. Butyrophenones (Haloperidol and droperidol)
2. Dexmedetomidine 2. Benzodiazepines (midazolam, Diazepam)
3. Tizanidine 3. Antiserotonergic agents (ondansetron)
4. Antipamezole 4. Opioids (fentanyl, Sufentanyl, Demerol)

1436. Glycerin is 1444. The duration of epidural anesthesia is affected by


1. Weakly neurolytic 1. Height of patient
2. Hyperbaric relative to CSF 2. Age of patient
3. Used for trigeminal neuralgia 3. Weight of patient
4. Usually mixed with ethyl alcohol 4. Addition of epinephrine (1:200,000) to the local anes-
thetic

1437. Which of the following drugs will decrease the plasma


clearance of amide-type local anesthetics? 1445. Adverse effects of traditional NSAIDs (e.g. Ibuprofen)
1. Propranolol may include:
2. Cimetidine 1. Renal
3. Halothane 2. Cutaneous
4. Phenytoin 3. Gastrointestinal
4. Central nervous system

1438. Glucocorticoids enhance


1. Phospholipase A2 1446. The following statements about drug therapy for
2. Gluconeogenesis insomnia are accurate.
3. Cytokines 1. Barbiturates gradually lead to an increase in the activity
4. Lipolysis of hepatic enzymes
2. Patients develop tolerance for benzodiazepines much
more rapidly than for pentobarbital
1439. Methemoglobin associated with prilocaine 3. Barbiturates suppress REM sleep
1. Requires liver metabolism of local anesthetic 4. There is no cross-tolerance to other hypnotics
2. Is of little clinical consequence
3. Is treated with methylene blue
4. Arises from oxidation of hemoglobin 1447. COX II selectivity of NSAIDs:
1. Is associated with prostaglandin inhibition that is as-
sociated with pain and hyperalgesia
1440. As compared to adults, which of the following typify 2. Preserves normal function of the GI mucosa
pediatric osseous development? 3. Is characterized by the ability to decrease sensitization in
1. Lower energy absorption the central nervous system by inhibition of prostanoid
2. Greater mineral content formation, and action of substance P at the NMDA
3. Thinner periosteum receptor
4. Greater porosity 4. Related to sexual dysfunction in males over age 60

ASIPP
Section 5 • Pharmacology 259

1448. Ziconotide 1455. Which of the following drugs produce sodium channel
1. Is a N-type voltage sensitive calcium channel antago- blockade?
nist. 1. Lidocaine
2. Has been reported to be beneficial in spinal cord injury. 2. Phenytoin
3. Has side effects including nystagmus, ataxa, hallucina- 3. Quinidine
tions etc. 4. Amitritpyline
4. Is a L-type voltage sensitive calcium channel antago-
nist.
1456. The following statements are true regarding fentanyl as a
good agent for transdermal use:
1449. Phenol is 1. Low molecular weihjt
1. Hyperbaric relative to CSF 2. Adequate lipid solubility
2. Produces selective coagulation of proteins 3. High analgesic potency
3. Has a local anesthetic effect 4. Low abuse potential
4. Causes selective small fiber destruction

1457. Pharmacodynamics is concerned with:


1450. Local anesthetics are added to an infusion to treat 1. Absorption
following type(s) of pain. 2. Signaling pathways coupled to receptors
1. Nociceptive Pain 3. Distribution
2. visceral Pain 4. Receptor binding
3. somatic pain
4. neuropathic pain
1458. The mechanism of action for the neurolytic effects of
alcohol is/are?
1451. Hypercalcemia may lead to the following: 1. Dehydration of proteins
1. Delirium and confusion 2. Extraction of cholesterol
2. Fatigue 3. Precipitation of mucoproteins
3. Anorexia 4. Protein coagulation
4. Constipation
1459. Opioid peptides are derived from larger prohormones
that include:
1. Proenkephalin A
1452. Which of the following local anesthetic/s has/have 2. Proopiomelanocortin
inherent vasoconstriction activity? 3. Proenkephalin B
1. Ropivacaine 4. Alpha neoendorphin
2. Cocaine
3. Mepivacaine
4. Lidocaine 1460. Prototypic kappa-receptor agonists include:
1. Dynorphin
2. N-allyl normetazocaine
1453. Duration of action of local anesthetics may be increased 3. Ketocyclazocaine
by 4. DADL
1. Adding vasoconstrictors
2. Adding bicarbonate
3. Increasing the dose 1461. Enkephalins are found in the:
4. Use of carbonated solutions 1. Sympathetic nervous system
2. Gastrointestinal tract
3. Periaqueductal gray
4. Adrenal Medulla
1454. Tramadol might be considered a medication to use with
caution in those taking:
1. Monoamine oxidase inhibitors. 1462. Ethyl alcohol
2. Serotonin reuptake inhibitors. 1. Causes selective small fiber destruction
3. Concomitant use of tricyclic anti-depressants. 2. Produces a more profound block than phenol
4. Benzodiazepines. 3. Has a local anesthetic effect
4. Hypobaric relative to CSF

ASIPP
260 Section 5 •Pharmacology

1463. The following are true choices which may lead to 1471. The following drugs are effective in a treatment of
decreased opioid requirements: pruritus from administration of neuraxial opiates:
1. Combined treatment with local anesthetics 1. Nalbuphine 5mg IV
2. Advance age 2. Diphenhydramine 50mg IV
3. Decreased renal function 3. Hydroxyzine 20mg IM
4. Combined treatment with gabapentin 4. Propofol 10mg IV

1464. Beta-endorphin is found in the: 1472. Which of the following drugs are serotonin antagonists?
1. Locus ceruleus 1. Ondansetron (Zofran)
2. Hypothalamus 2. Granisotron (Kytril)
3. Periaqueductal gray 3. Dolasetron (Anzemet)
4. Pituitary 4. Metoclopramide (Reglan)

1465. Examples of phenanthrene class of opioid include all 1473. Serious drug interactions may occur with MAO
except: inhibitors and which of the following drugs?
1. Morphine 1. Fluoxetine
2. Fentanyl 2. Amitriptyline
3. Codeine 3. Sumatriptan
4. Meperidine 4. Meperidine

1466. 30mg of MS04 orally are equivalent to:


1. 10mg MS04 IV 1474. The common side effects of clonidine may include the
2. 20mg of oral oxycodone following:
3. 1.5mg hydromorphone IV 1. Orthostatic hypotension
4. 20mg methadone 2. Dry mouth
3. Bradycardia
1467. A patient in the intensive care unit is receiving an 4. Sedation
infusion of epinephrine, after exsanguinating
significantly following a total hip replacement. The 1475. Tricyclic antidepressant toxicities include which of the
order states that epinephrine should be titrated, but following?
kept in the range of 10-20 micrograms/minute. The 1. Delirium
ICU nurse, however, accidentally writes for 1-2 mcg/ 2. Weight gain
minute. One would expect: 3. Urinary retention
1. An increase in the systolic blood pressure 4. Prolongation of QT interval
2. A reduction in mean arterial blood pressure
3. An increase in blood flow to the muscles 1476. Which of the following factors must be true for two
4. An increase in blood flow to the skin drugs to be considered
1. Identical Area Under the Curve data for both drugs
1468. Which of the following can be administered orally? 2. Drugs given by the same route of administration
1. Albuterol 3. Time to peak plasma concentrations the same
2. Epinephrine 4. Equal peak plasma concentrations
3. Ephedrine
4. Dopamine 1477. Phase II reactions
1. Are oxidative processes
1469. Epinephrine causes which of the following? 2. Increase water solubility
1. Relaxation of gastrointestinal smooth muscle 3. Are typically microsomal
2. Relaxation of the trigone 4. Occur in the kidney
3. Contraction of the urinary sphincter
4. Contraction of the detrusor muscle 1478. Dose-response curves of drugs describe
1. Activity
1470. The volume of distribution for a particular 2. Potency
pharmacologic agent is influenced by its: 3. Affinity
1. Ionization state 4. Slope
2. Polarity
3. Lipophilicity 1479. High risk factors for NSAID-induced renal insufficiency
4. Molecular weight include:
1. Significant hypovolemia
2. Sever congestive heart failure
3. Hepatic cirrhosis
4. Older age

ASIPP
Section 5 • Pharmacology 261

1480. Which of the following are correct regarding drugs 3. Phenytoin


bound to plasma proteins? 4. Fluoxetine
1. Have large volumes of distribution
2. Are typically biologically active 1489. Therapy with acetylsalicylic acid needs to be carefully
3. Displaced by other drugs evaluated in patients with “Franklin’s triad” which
4. Filtered by the glomerulus includes:
1. Nasal polyps
2. Athsma
1481. Medications used for the pharmacologic treatment of 3. Urticaria
mania include: 4. Rhinorrhea
1. Carbamazepine
2. Gabapentin 1490. True statement regarding alpha 1-acid glycoprotein
3. Valproate include that it:
4. Verapamil 1. Has high capacity and low affinity
2. Has a high affinity for basic drugs
1482. Ergot alkaloid drugs include: 3. Remains unaffected by recent trauma
1. Ergonovine 4. Is an acute-phase reactant
2. Lysergic acid
3. Methysergide 1491. The antidepressant(s) which is/are secondary amine(s)
4. Bromocriptine TCA:
1. Desipramine
1483. Dopamine effects include regulation of 2. Doxepin
1. Memory 3. Nortriptyline
2. Cognition 4. Imipramine
3. Motivation
4. Emotion
1492. Which of the following are true statements concerning
1484. Factor(s) that determine the proportion of local NSAIDs?
anesthetic that exists in the un-ionized (freebase) and 1. Do not produce pharmacological dependence
ionized (cation) forms include 2. May be opioid sparing
1. Local anesthetic concentration 3. Are extensively protein bound
2. Tissue pH 4. Do not maintain an analgesic ceiling
3. Local anesthetic volume
4. pKa of the local anesthetic
1493. Medical conditions and/or factors which may affect the
1485. Local anesthetics are organic amount of free circulating drug include:
1. Amines 1. Hepatic Cirrhosis
2. Aromatic 2. Burns
3. Alkaloids 3. Renal sufficiency
4. Acids 4. Trauma

1486. The adverse effects of L-dopa therapy improved by


adding carbidopa include: 1494. NSAIDs which are considered “prodrugs” include:
1. Mydriasis 1. Piroxicam
2. Cardiac arrhythmia 2. Nabumetone
3. Nausea 3. Diflunisal
4. Depression 4. Sulindac
1495. Glucocorticoids enhance:
1487. Choose the true statement: 1. Phopholipase A2
1. Alpha - 1 acid glycoprotein predominantly binds basic 2. Gluconeogenesis
drugs 3. Cytokines
2. Local pH may affect the volume of distribution 4. Lypolysis
3. the volume of distribution is inversely related to protein
binding
4. Morphine is mostly bound to albumin 1496. Which of the following is/are amino ester local
anesthetic/s?
1488. Which of the following drugs induces the activity of CYP 1. Lidocaine
3A4? 2. Bupivacaine
1. Carbamazepine 3. Mepivacaine
2. Phenobarbital 4. Tetracaine

ASIPP
262 Section 5 •Pharmacology

Tables
Definitions of Opioids
Definition
Term
Opiate A drug derived from alkaloids of the opium poppy

Opioid The class of drugs that includes opiates, opiopeptins, and all synthetic and semisynthetic
drugs that mimic the actions of the opiates
Opioid peptides Endogenous peptides that act on opioid receptors

Opioid agonist A drug that activates some or all opioid receptor subtypes and does not block any

Partial agonist A drug that can activate an opioid receptor to effect a submaximal response

Opioid antagonist A drug that blocks some or all opioid receptor subtypes

Mixed agonist antagonist A drug that activates some opioid receptor subtypes and blocks other subtypes

Source: Katzung & Trevor’s Pharmacology, Examination and Board Review, 6th Ed., McGraw Hill, New York, 1998.

List of Opioids Agonists and Antagonists

Subclass Prototype Major Variants Other Significant Agents


Strong agonists Morphine Heroin, meperidine, Fentanyl, levorphanol
methadone

Moderate agonists Codeine Oxycodone, hydrocodone

Weak agonists Propoxyphene

Partial agonists Buprenorphine

Mixed agonist-antagonists Pentazocine Nalbuphine Butorphanol

Antagonists Naloxone Naltrexone

Antitussive Dextromethorphan Codeine

Antidiarrheal Diphenoxylate Loperamide

Source: Katzung & Trevor’s Pharmacology, Examination and Board Review, 6th Ed., McGraw Hill, New York, 1998.

ASIPP
Section 5 • Pharmacology 263

Definitions

Term Definition

Tolerance A decreased response to a drug, necessitating larger doses to achieve the same effect. This can
result from increased disposition of the drug (metabolic tolerance), an ability to compensate
for the effects of a drug (behavioral tolerance), or changes in receptor or effector systems
involved in drug actions (functional tolerance)

Psychologic Compulsive drug-using behavior in which the individual uses the drug for personal
dependence satisfaction, often despite known health risks

Physiologic A state characterized by signs and symptoms, frequently the opposite of those caused
dependence by a drug, when it is withdrawn from chronic use or when the does is abruptly lowered.
Psychologic dependence usually precedes physiologic dependence

Abstinence A term used to describe the signs and symptoms that occur on withdrawal of a drug in a
syndrome physiologically dependent person

Controlled A drug deemed to have abuse liability that is listed on governmental Schedules of Controlled
substance Drugs. Such schedules categorize illicit drugs, control prescribing practices, and mandate
penalties for illegal possession, manufacture, and sale of listed drugs. Controlled substance
schedules are presumed to reflect current attitudes toward substance abuse; therefore, which
drugs are regulated depends on a social judgment

Designer drug A synthetic derivative of a drug, with slightly modified structure but no major change
in pharmacodynamic action. Circumvention of the Schedules of Controlled drugs is a
motivation for the illicit synthesis of designer drugs.

Source: Katzung & Trevor’s Pharmacology, Examination and Board Review, 6th Ed., McGraw Hill, New
York, 1998.

Schedules of Controlled Drugs

Schedule Criteria Examples


I No medical use; high addiction Flunitrazepam, heroin, LSD, marijuana,
potential mescaline, methaqualone, PCP, DOM,
MDMA
II Medical use; high addition potential Strong opioid agonists, cocaine, short half-life
barbiturates, amphetamines, methylphenidate
III Medical use; moderate potential for Anabolic steroids, codeine and moderate
dependence opioid agonists, dronabinol, thiopental
IV Medical use; low abuse potential Benzodiazepines, chloral hydrate,
meprobamate, weak opioid agonists,
zolpidem, zaleplon

Source: Katzung & Trevor’s Pharmacology, Examination and Board Review, 6th Ed., McGraw Hill, New
York, 1998.

ASIPP
264 Section 5 •Pharmacology

Signs and symptoms of overdose and withdrawal

Overdose Effects Withdrawal Symptoms


Amphetamines • Agitation • Apathy
methylphenidate • hypertension • irritability
cocaine1 • tachycardia • increased sleep time
• delusions • disorientation
• hallucinations • depression
• hyperthermia
• seizures
• death

Barbiturates Slurred speech, “drunken” Anxiety, insomnia, delirium,


benzodiazepines behavior, tremors, seizures, death
ethanol2 dilated pupils, weak and rapid
pulse, clammy skin, shallow
respiration, coma, death

Heroin; other opioid Constricted pupils, clammy skin, Nausea, chills, sweats, cramps,
analgesics nausea, drowsiness, respiratory lacrimation, rhinorrhea, yawning,
depression, coma, death hyperpnea, tremor

1
Cardiac arrhythmias, myocardial infarction, and stroke occur more frequently in cocaine overdose than
with other CNS stimulants.
2
Ethanol withdrawal includes the excited hallucinatory state of delirium tremens.

Source: Katzung & Trevor’s Pharmacology, Examination and Board Review, 6th Ed., McGraw Hill, New York, 1998.

Drugs of Abuse

Subclass Prototype Major Variants Other Significant Agents


Sedative- Secobarbital, benzodiazepines, Pentobarbital, alprazolam, Methaqualone,
hypnotics ethanol diazepam meprobamate
Opioids Heroin
Stimulants Amphetamine Methamphetamine, DOM, MDA, MDMA
phenmetrazine
Cocaine, caffeine, nicotine

Hallucinogens LSD, phencyclidine Mescaline Scopolamine


Marijuana “Grass” Hashish Dronabinol
Inhalants Nitrous oxide, toluene Ether Chloroform, benzene
Amyl nitrite Isobutyl nitrite
Source: Katzung & Trevor’s Pharmacology, Examination and Board Review, 6th Ed., McGraw Hill, New York, 1998.

ASIPP
Section 5 • Pharmacology 265

Benzodiazepine Indications

Drug and Half-life Primary Indications

Short-acting (t1/2 < 5 hr)

Midazolam [Versed] Preanesthetic

Triazolam [Halcion] Hypnotic, preanesthetic

Intermediate-acting (t1/2 5-24 hr)

Alprazolam [Xanax] Anxiolytic, antidepressant *

Clonazepam [Klonopin] Anticonvulsant

Estazolam [ProSom] Hypnotic

Lorazepam [Ativan} Anxiolytic, hypnotic, preanesthetic

Oxazepam [Serax] Anxiolytic

Temazepam [Restoril] Hypnotic

Long-lasting (t1/2 > 24 hr)

Chlordiazepoxide [Librium] † Anxiolytic, preanesthetic

Clorazepate [Tranxene] † ‡ Anxiolytic

Diazepam [Valium] † Anxiolytic, preanesthetic, anticonvulsant

Flurazepam [Dalmane] Hypnotic

Prazepam [Centrax] † ‡ Anxiolytic

Quazepam [Doral] Hypnotic

* For panic disorders.


† Converted to the long-acting, active metabolite.
‡ Pro-drug.

Source: Katzung & Trevor’s Pharmacology, Examination and Board Review, 6th Ed., McGraw Hill, New York, 1998.

ASIPP
266 Section 5 •Pharmacology

Classification, Potency, and Adverse Effects of Antipsychotic Drugs

Oral Dosage Extrapyramidal Autonomic Sedation


Drugs and Classifications Range (mg/day) Effects* Effects
Aliphatic phenothiazines
Chlorpromazine 100-1000 ++ +++ +++
[Thorazine, generic]
Triflupromazine [Vesprin] 50-150 ++ +++ +++
Piperidine phenothiazines
Thioridazine [Mellaril, 100-800 + +++ +++
generic]
Mesoridazine [Serentil] † 50-400 + +++ +++
Piperazine phenothiazines
Trifluoperazine [Stelazine, 10-60 +++ ++ ++
generic]
Fluphenazine [Prolixin, 5-20 ++++ ++ ++
Permitil] ‡
Perphenazine [Trilafon] 16-64 +++ ++ ++
Acetophenazine [Tindal] 80-120 +++ + ++
Aliphatic thioxanthene
Chlorprothixene [Taractan] 100-600 ++ +++ +++
Piperazine thioxanthene
Thiothixene [Navane, 2-120 +++ ++ ++
generic]
Butyrophenone
Haloperidol [Haldol, 2-20 ++++ + +
generic]
Other heterocyclic drugs
Molindone [Moban] † 20-200 +++ ++ ++
Loxapine [Loxitane] 20-250 +++ ++ ++
Clozapine [Clozaril] ‡** 25-400 + +++ +++
* Excluding tardive dyskinesia.
† No antiemetic action.
‡ Esterification (enanthate or decanoate) results in depot form.
** Agranulocytosis I up to 3% of patients.

Source: Katzung & Trevor’s Pharmacology, Examination and Board Review, 6th Ed., McGraw Hill, New York, 1998.

ASIPP
Section 5 • Pharmacology 267

Relative Activity of Antidepressant Drugs on Norepinephrine and Serotonin Prejunctional Neuronal


Uptake.

Drug and Classification Inhibition of Norepinephrine Uptake Inhibition of Serotonin Uptake

Tricyclic antidepressants

Tertiary amines

Amitriptyline [Elavil, others] +/- ++

Imipramine [Tofranil, others] + +

Trimipramine [Surmontil] + 0

Doxepin [Sinequan, others] ++ +

Clomipramine [Anafranil] + +++

Secondary amines

Desipramine [Norpramin, +++ 0


Petofrane, generic]
Nortriptyline [Aventyl, Pamelor] ++ +/-

Protriptyline [Vivactil] ++ 0

Dibenzoxazepines

Amoxapine [Asendin]* ++ 0

Selective serotonin reuptake inhibitors

Fluoxetine [Prozac] + +++

Paroxetine [Paxil] 0 +++

Sertraline [Zoloft] 0 +++

Atypical antidepressants

Trazodone [Desyrel, generic] 0 +

Maprotiline [Ludiomil] ++ 0

Bupropion [Wellbutrin] + 0

Venlafaxine [Effexor] + +

Nefazodone [Serzone] ‡ + +

* Has dopamine-receptor antagonist activity.


† Has serotonin-receptor agonist and antagonist activity.
‡ Has serotonin-receptor antagonist activity.
Source: Katzung & Trevor’s Pharmacology, Examination and Board Review, 6th Ed., McGraw Hill, New York, 1998.

ASIPP
268 Section 5 •Pharmacology

Relationship between Blockade of Neurotransmitter Receptors and Anti-Depressant-induced


Side Effects
Receptor Subtype Side Effects
Histamine H1-receptors Sedation
Weight gain
Hypotension
Potentiation of CNS depressants

Muscarinic receptors Dry mouth


Blurred vision
Urinary retention
Constipation
Memory dysfunction
Tachycardia

α1-adrenoceptors Postural hypotension


Reflex tachycardia
Potentiation of antihypertensive effects of prazosin

α2-adrenoceptors Blockade of antihypertensive effects of clonidine


alpha-methyldopa

Serotonin 5-HT2-receptors Ejaculatory dysfunction


Hypotension
Alleviation of migraine

Source: Katzung & Trevor’s Pharmacology, Examination and Board Review, 6th Ed., McGraw Hill, New York, 1998.

Relative Development of Tolerance to Opioid Actions.

Substantial Minimal
Analgesia Constipation
Respiratory depression Seizures
Euphoria and dysphoria Antagonist activity
Sedation
Nausea and vomiting
Cough suppression

Source: Katzung & Trevor’s Pharmacology, Examination and Board Review, 6th Ed., McGraw Hill, New York, 1998.

ASIPP
Section 5 • Pharmacology 269

Answers

1267. Answer: A B. Barbiturates also act on the Cl¯ channel to increase the
Explanation: opening frequency of the channel.
Reference: Katzung, pp 439-441. D. Valproic acid elevates brain levels of GABA by
The primary effect of local anesthetics is blockade of inhibiting GABA metabolism.
voltage channel-gated Na channels. E. Chlorpromazine blocks the activity of dopamine
Progressively increasing concentrations of local receptors and has little or no effect on the GABA system.
anesthetics results in an increased threshold of excitation, a Source: Stern - 2004
slowing of impulse conduction, a decline in the rate of rise
of the action potential, a decrease in the height of the 1273. Answer: E
action potential, and eventual obliteration of the action Explanation:
potential. Reference: Katzung, p 602.
Tasteless enteric-coated tablets and capsules are
Local anesthetics first block small unmyelinated or lightly formulated to resist the acidic pH found in the stomach.
myelinated fibers (pain), followed by heavily myelinated Once the preparation has passed into the intestine, the
but small-diameter fibers (sensory) and then larger- coating dissolves in the alkaline milieu and releases the
diameter fibers (proprioception, pressure, motor). drug. Therefore, gastric irritation, drug destruction by
Source: Stern - 2004 gastric acid, and the forming of complexes of the drug
with
1268. Answer: C food constituents will be avoided.
Explanation: Source: Stern-2004
Reference: Hardman, pp 414-416.
Unwanted pharmacologic side effects produced by 1274. Answer: B
phenothiazine antipsychotic drugs (e.g., perphenazine)
include Parkinson-like syndrome, akathisia, dystonias,
galactorrhea, amenorrhea, and infertility. These side effects 1275. Answer: C
are due to the ability of these agents to block dopamine Explanation:
receptors. (Raj, Practical Mgmt of Pain, 3rd Ed, page 566, Stoelting,
The phenothiazines also block muscarinic and a- Pharmacology and Physiology of Anesthetic Practice, 3rd
adrenergic receptors, which are responsible for other Ed., page 170-171)
effects.
Source: Stern - 2004 All local anesthetics can produce a dose dependent
depression of cardiac conduction velocity, including intra-
1269. Answer: C atrial, AV nodal, His-Purkinje, and intraventricular
pathways. Part of local anesthetic cardiac toxicity is due to
1270. Answer: A blockade of cardiac sodium channels. Accidentally
Source: Cole EB, Board Review 2003 administered bupivacaine can lead to precipitous
hypotension, dysrhythmias, and A-V heart block. The
1271. Answer: B dissociation of highly lipid soluble bupivacaine from Na+
channels is slow.

1272. Answer: E Bupivacaine is a racemic mixture, wherein the R


Explanation: enantiomer is more toxic than the S-enantiomer.
Reference: Hardman, pp 280-281. Ropivacaine is a pure S-enantiomer which is intermediate
in toxicity between lidocaine and bupivacaine
A, C. Benzodiazepines (e.g., chlordiazepoxide, diazepam) Source: Shah RV, Board Review 2004
bind to receptors on the Cl¯ channel and enhance the
binding of GABA to its receptor. 1276. Answer: A
* g-aminobutyric acid is an inhibitory neurotransmitter Source: Lou Etal. Pain Practice: march 2001
that activates the Cl¯ channel.
1277. Answer: D

ASIPP
270 Section 5 •Pharmacology

1278. Answer: B 1286. Answer: B


Explanation:
1279. Answer: A Many patients with prolonged chronic pain have elevation
Explanation: of the hypochondriasis, depression, and hysteria scores of
(Stoelting, 3rd Ed, pa 164-5) 2 or more standard deviations above the mean. This is
considered clinically significant. Patients with acute pain
Prilocaine is an amide local anesthetic that is metabolized frequently have slightly elevated hypochondriasis,
to orthotoluidine. Orthotoluidine is an oxidizing depression, and hysteria scores, but not to a clinically
compound that is capable of converting hemoglobin to significant degree. Once the pain resolves, the mild
methemoglobin. If the dose of prilocaine exceeds 600mg, elevation returns closer to or within the normal range.
there may be enough methemoglobin (3-5 g/dl) to cause Source: Kahn CH, DeSio JM. PreTest Self Assessment and
the patient to appear cyanotic. Methemoglobinemia is Review. Pain Management. New York, McGraw-Hill, Inc.,
readily reversed by the administration of methylene blue, 1996.
1-2 mg/kg intravenously over 5 minutes. This effect,
however, may be short lived, since the methylene blue may 1287. Answer: A
be cleared before converting all of the methemoglobin to
hemoglobin. 1288. Answer: C
Source: Shah RV, Board Review 2004 Explanation:
Reference: Hardman, pp 1129-1131.
1280. Answer: A All teracyclines can produce negative nitrogen balance and
Explanation: increased blood urea nitrogen (BUN) levels. This is of
Reference: Katzung, pp 599-603 clinical importance in patients with impaired renal
Aspirin (acetylsalicylic acid) is the most extensively used function. With the exception of doxycycline, tetracyclines
analgesic, antipyretic, and anti inflammatory agent of the should not be used in patients that are anuric. Doxycycline
group of compounds known as NSAIDs, or nonopiod is excreted by the GI tract under these conditions, and it
analgesics. Most of its therapeutic and adverse effects will not accumulate in the serum of patients with renal
appear to be related to the inhibition of prostaglandin insufficiency.
synthesis. Nonsteroidal anti-inflammatory drugs inhibit Source: Stern-2004
the activity of the enzyme cyclooxygenase, which mediates
the conversion of arachidonic acid to prostaglandins that 1289. Answer: B
are involved in pain, fever, and inflammation. Aspirin may Source: Day MR, Board Review 2004
produce irritation and ulceration of the gastrointestinal
(GI) tract, an adverse effect that is about equal to other 1290. Answer: A
salicylates. It also inhibits platelet aggregation.
Acetaminophen, like aspirin, has analgesic and antipyretic 1291. Answer: D
properties, but it does not have clinically significant anti-
inflmmatory activity and is not irritating to the GI tract. 1292. Answer: B
Source: Stern - 2004 Explanation:
Reference: Katzung, p 1130.
1281. Answer: E
Fatalities have been reported when fluoxetine and MAO
1282. Answer: E inhibitors (MAOIs) such as tranylcypromine have been
given simultaneously.
1283. Answer: D
Explanation: The MAOIs should be stopped at least two weeks before
Reference: Katzung, p 603. the administration of fluoxetine or paroxetine.
Celocoxib is a cyclooxygenase II inhibitor. Aspirin, Source: Stern - 2004
ibuprofen, and piroxicam are relatively nonselective
inhibitors of cyclooxygenases. Acetaminophen has no 1293. Answer: A
effect on cyclooxygenases Source: Jackson KC. Board Review 2003
Source: Stern - 2004

1284. Answer: C 1294. Answer: D

1285. Answer: A 1295. Answer: C


Explanation:
Reference: Hardman, p 906. Katzung, p 1127. 1296. Answer: D
Cimetidine inhibits the activity of cytochrome P450, Explanation:
slowing benzodiazepam metabolism. Reference: Hardman, pp 521-522.
Source: Stern - 2004

ASIPP
Section 5 • Pharmacology 271

* The enkephalins are endogenous agonists of the opioid of 25.


receptors. Source: Day MR
- The enkephalins are located in areas of the brain and
spinal cord related to the perception of pain. These areas 1305. Answer: C
include the laminae I and II of the spinal cord, the spinal Explanation:
trigeminal nucleus, and the periaqueductal gray. Explanation: Maximum dose is 4 mg/kg. Maximum dose
of lidocaine with epinephrine is 7 mg/kg.
* Selegiline and trihexyphenidyl are anti-Parkinsonism
drugs. Source: Hahn, McQuillan, Sheplock: Regional Anesthesia:
An Atlas of Anatomy and Techniques. Mosby 1996.
* Baclofen is a skeletal muscle relaxant agonist for the Source: Day MR
GABA receptor.
Source: Stern - 2004 1306. Answer: D

1297. Answer: E 1307. Answer: B

1298. Answer: A 1308. Answer: D


Explanation:
1299. Answer: B Reference: Hardman, pp 407-412.
Source: Day MR, Board Review 2004 Haloperidol is a butyrophenone derivative with the same
mechanism of action as the phenothiazines, that is,
blockade of dopaminergic receptors.
1300. Answer: A It is more selective for D2 receptors.
Explanation: Haloperidol is more potent on a weight basis than the
Reference: Hardman, pp 418-419, 930. phenothiazines, but produces a higher incidence of
Chlorpromazine is the prototype compound of the extrapyramidal reactions than does chlorpromazine
phenothiazine class of antipsychotic drugs. It is indicated Source: Stern - 2004
for use in the treatment of a variety of psychoses, which
includes schizophrenia, and in the treatment of nausea
and vomiting, in both adults and children, from a number 1309. Answer: D
of causes. The drug can be administered orally, rectally, or Explanation:
intramuscularly for this purpose. It is believed that the Reference: Hardman, pp 3-4.
effectiveness of the compound is based on the inhibition Drugs can be transferred across biologic membranes by
of dopaminergic receptors in the chemoreceptor trigger passive processes (i.e., filtration and simple diffusion) and
zone of the medulla. Other phenothiazine derivatives by specialized processes (i.e., active transport, facilitated
are also used for emesis, including thiethylperazine, diffusion, and pinocytosis). Active transport is a carrier-
prochlorperazine and perphenazine. mediated process that shows all of the characteristics listed
Although chlorpromazine may cause orthostatic in the question. Facilitated diffusion is similar to active
hypotension and has mild H1-histamine receptor blocking transport except that the drug is not transported against a
activity, the drug is never used as an antihypertensive or as concentration gradient and no energy is required for this
an antihistaminic. carrier-mediated system to function. Pinocytosis usually
Chlorpromazine is not an effective antidepressant drug, involves transport of proteins and macromolecules by a
and lithium salts are used for treating the mania that is complex process in which a cell engulfs the compound
associated with bipolar affective disorder. within a membrane-bound vesicle.
Source: Stern - 2004 Source: Stern-2004

1301. Answer: D 1310. Answer: A


Explanation:
1302. Answer: B (Baum, pp 224.)
· Traditionally, minor tranquilizers have been used as a
1303. Answer: C standard approach to the treatment of psychophysiologic
disorders. However, they fail to deal with the underlying
psychological, social, or physiologic problem, especially
1304. Answer: A on a long-term basis. They are effective in providing
Explanation: short-term relief for high levels of stress or anxiety and
Explanation: Hydrocortisone has an anti-inflammatory can be more effective if combined with behavior therapy
potency of 1. Triamcinolone diacetate, triamcinolone or psychotherapy.
acetonide, and depo-methylprednisolone all have an anti- · Interpersonal dilemmas are not affected, though they
inflammatory potency of 5. Betamethasone and may seem to be temporarily dulled with minor
dexamethasone both have an anti-inflammatory potency tranquilizers.

ASIPP
272 Section 5 •Pharmacology

· Minor tranquilizers often have the side effect of 1324. Answer: A


drowsiness, can lead to tolerance with the need for
increased dosages, and can produce withdrawal symptoms 1325. Answer: C
of insomnia, tremors, and even hallucinations.
Source: Ebert 2004 1326. Answer: B

1311. Answer: B
1327. Answer: D
1312. Answer: C Explanation:
Source: Day MR, Board Review 2004 Reference: Katzung, p 437.
Local anesthetics are agents that, when applied locally,
block nerve conduction; they also prevent generation of a
1313. Answer: D nerve impulse. All contain a lipophilic (benzene)
Explanation: functional group and most a hydrophilic (amine) group.
Large doses of prilocaine, usually greater than 600 mg
epidurally, can result in clinically significant
methemoglobinemia. Prilocaine is metabolized by the Benzocaine does not contain the therminal hydrophilic
liver to o-toluidine, which is responsible for the oxidation amine group; thus, it is only slightly soluble in water and is
of hemoglobin to methemoglobin. Methemoglobinemia slowly absorbed with a prolonged duration. It is,
can be treated with IV methylene blue, or it will resolve therefore, only useful as a surface anesthetic.
spontaneously. Source: Stern -2004
Source: Hall and Chantigan.
1328. Answer: B
1314. Answer: B
1329. Answer: B
1315. Answer: C Explanation:
Among the SSRIs, fluvoxamine appears to present the
1316. Answer: E greatest risk of drug-drug interactions. Fluvoxamine is
Source: Smith H, Board Review 2005 metabolized by CYP 3A4. Fluvoxamine may increase the
half-lives of alprazolam and diazepam and should not be
1317. Answer: C coadministered with these agents. Fluvoxamine may
increase theophylline concentrations 3-fold and warfarin
1318. Answer: C concentrations 2-fold, with important clinical
Explanation: consequences. Fluvoxamine raises concentrations and may
Reference: Hardman, pp 510 increase the activity of clozapine, carbamazepine,
Carbidopa is an inhibitor of aromatic L-amino acid methadone, propranolol, and diltiazem.
decarboxylase. It cannot readily penetrate the central Source: Laxmaiah Manchikanti, MD
nervous system (CNS) and, thus, decreases the
decarboxylation of L-dopa in the peripheral tissues. This 1330. Answer: D
promotes an increased concentration of L-dopa in the Explanation:
nigrostriatum, where it is converted to dopamine. In Reference: Katzung, pp 404-405.
addition, the effective dose of L-dopa can be reduced.
Source: Stern - 2004 Vigabatrin can induce psychosis. It is recommended that it
not be used in patients with preexisting depression and
psychosis.
1319. Answer: C Source: Stern - 2004

1320. Answer: E 1331. Answer: D


Source: Day MR, Board Review 2004

1321. Answer: D 1332. Answer: D


Explanation:
1322. Answer: C (Raj, Practical Mgmt of Pain, 3rd Ed. Page 558)
Explanation: Plasma pseudocholinesterases hydrolyze the ester linkage
MSO4 300mg po is equivalent to 100mg IV, 10mg of ester local anesthetics. Amide local anesthetics undergo
epidurally, or 1mg intrathecally. Sufentanyl is 20 times as biotransformation in the liver.
potent as MSO4, and fentanyl is 3 times as potent. Source: Shah RV, Board Review 2004
Source: Trescot AM, Board Review 2004
1333. Answer: A
1323. Answer: D Explanation:

ASIPP
Section 5 • Pharmacology 273

(Raj, Practical Mgmt of Pain 3rd Ed., pag 565) 1345. Answer: E
Explanation:
As the serum levels of lidocaine rise, the patient may be at Reference: Hardman, pp 31-34.
increased risk for seizures. At 10 to 12 micrograms/ml.,
inhibitory pathways in the brain are selectively inhibited, * Based upon the molecular mechanisms with which
but facilitatory neurons are unopposed. receptors transduce signals, four major classes of
receptors have been identified:
Seizures originate in the amygdale and hippocampus. - ion channel receptors,
- receptors that interact with G proteins,
Lidocaine toxicity presents with prodromal symptoms, - receptors with tyrosine kinase activity, and
before seizures: slow speech, jerky movements, tremors, - nuclear receptors.
and hallucinations
Source: Shah RV, Board Review 2004 * The first three types of receptors are complex membrane
bound proteins with hydrophilic regions located within
1334. Answer: D the lipoid cell membrane and hydrophilic regions located
Explanation: within the lipoid cell membrane and hydrophilic portions
(Raj, Practical Mgmt of Pain, 3rd Ed., page 565)Similarly found protruding into the cytoplasm of the cell and the
the peak concentrations would be extracellular milieu; when activated, all of these receptors
Intercostal > Epidural > Intravenous = Brachial Plexus > transmit (or transduce) information presented at the
Subcutaneous extracellular surface into ionic or biochemical signals
Source: Shah RV, Board Review 2004 within the cell (i.e., second messengers). Nuclear receptors
are found in the nucleus of the cell, not bound to plasma
1335. Answer: E membranes. In addition, these receptors do not transduce
Source: Smith H, Board Review 2005 information by second-messenger systems; rather, they
bind to nuclear chromatin and elicit a biologic response
1336. Answer: A through the transcription of DNA and alterations in the
Source: Smith H, Board Review 2005 formation of cellular proteins. Ligand binding to all types
of receptors may involve the formation of ionic, hydrogen,
1337. Answer: A hydrophobic, van der Waals’, and covalent bonds. In most
Source: Smith H, Board Review 2005 cases, ligand-receptor interactions are stereospecific; for
example, natural (-)-epinephrine is 1000 times more
potent than (+)-epinephrine.
1338. Answer: A Source: Stern-2004
Explanation:
(Raj, Practical Mgmt of Pain, 3rd Ed., page 565, figure 39- 1346. Answer: A
6) Ok, a trick question. Explanation:
Tricyclic antidepressants (TCA) have been known to be
The actual peak concentrations of these routes at 5 effective in managing chronic pain. Unfortunately, their
minutes would be on the order of micrograms per side effect profile very often limits their clinical use. Some
milliliter IV> Intercostal> Epidural> Brachial Plexus > of the major side effects include orthostatic hypotension,
Subcutaneous anticholinergic effects, weight gain, sedation, cardiac
Source: Shah RV, Board Review 2004 conduction disturbances, sexual dysfunction and
restlessness.
1339. Answer: E
Source: Hansen HC, Board Review 2004 TCA’s with lower sedating effects include Protriptyline,
amoxapine, desipramine and imipramine. Trazadone is an
1340. Answer: B atypical antidepressant. It inhibits serotonin uptake, blocks
Source: Cole EB, Board Review 2003 serotonin 5-HT2 receptors, a1 receptor antagonist. Its
most common side effects are sedation and orthostatic
1341. Answer: B hypotension. At low doses it is used an adjunct for
Source: Smith H, Board Review 2005 insomnia.
Source: Chopra P, 2004
1342. Answer: D
1343. Answer: C 1347. Answer: D
Source: Smith H, Board Review 2005 Source: Raj P, Pain medicine - A comprehensive Review -
Second Edition
1344. Answer: D
Source: Hansen HC, Board Review 2004 1348. Answer: D
Source: Jackson KC. Board Review 2003

ASIPP
274 Section 5 •Pharmacology

1349. Answer: A 1355. Answer: C


Source: Cole EB, Board Review 2003

1350. Answer: D 1356. Answer: C


Explanation: Explanation:
(Guyton, pp 701-703.) The catecholamines nor, * Two types of MAO have been found:
epinephrine and epinephrine will activate both alpha and - MAO-A, which metabolizes norepinephrine and
ß-adrenergic receptors. When the a1-adrenergic receptors serotonin, and
are stimulated, they activate a G protein, which in turn - MAO-B, which metabolizes dopamine.
activates phospholipase C that hydrolyzes PIP2 and
produces IP3 and DAG. The IP3 causes the release of Ca2+
from the sarcoplasmic reticulum, which in turn increases A. Bromocriptine is a dopamine receptor agonist.
muscle contraction. alpha1 adrenergic receptors
predominate on arteriolar smooth muscle, so theses B. Carbidopa inhibits the peripheral metabolism of L-
muscles contract when stimulated with norepinephrine. dopa.
The bronchi, pupillary, and ciliary smooth muscles all - It is also useful in the treatment of parkinsonism.
contain beta receptors, which cause smooth muscle
relaxation. The intestinal smooth muscle relaxation is C. Selegiline is a selective inhibitor of MAO-B. It
initiated by an alpha2-aradrenergic receptor. therefore inhibits the breakdown of dopamine and
prolongs the therapeutic effectiveness of L-dopa in
1351. Answer: C parkinsonism.
Explanation:
(Carlson, pp 352-359.) D. Phenelzine and tranylcypromine are nonselective
· Testosterone administered postpubertally to castrated MAOIs.
rats can restore aggressiveness to almost normal levels. Source: Katzung
Similarly, neonatal female mice develop masculine
aggressive behavior on receiving androgens. Androgens
also promote aggression in humans. 1357. Answer: A
· Boys are more aggressive than girls at ages 3 to 10, as Explanation:
has been demonstrated in studies of children. Reference: Hardman, p 68.
Source: Ebert 2004 Physiologic, or functional, antagonism occurs when two
drugs produce opposite effects on the same physiologic
function, often by interacting with different types of
1352. Answer: A receptors. A practical example of this is the use of
epinephrine as a bronchodilator to counteract the
1353. Answer: B bronchoconstriction that occurs following histamine
Explanation: release from mast cells in the respiratory tract during a
(Stoelting, 3rd Ed., Chapter 12) severe allergic reaction. Histamine constricts the
bronchioles by stimulating histamine H1 receptors in the
In order for a drug to be classified as a catechol, hydroxyl tissue; epinephrine relaxes this tissue through its agonistic
groups must be present on the 3 and 4 carbon positions of activity on b2-adrenergic receptors.
the benzene ring. Catecholamines are rapidly inactivated Chemical antagonism results when two drugs
by monoamine oxidase and catechol-O-methyl transferase. combine with each other chemically and the activity
MAO is found in the GI tract, liver, and kidneys and of one or both is blocked. For example, dimercaprol
catalyzes oxidative deamination. COMT methylates the chelates lead and reduces the toxicity of this heavy
hydroxyl group of catecholamines and these inactive metal. Competitive antagonism, or inactivation,
methylated metabolites are conjugated with glucuronic occurs when two compounds compete for
acid and appear in the urine as breakdown products. the same receptor site; this is a reversible
These byproducts include metanephrine, nometanephrine interaction. Thus, atropine blocks the effects of
, and 3-methoxy-4-hydroxymandelic acid. acetylcholine on the heart by competing with the
neurotransmitter for binding to cardiac muscarinic
Despite the importance of enzymatic breakdown, the receptors. Irreversible antagonism generally results from
actions of catecholamines are principally stopped by the binding of an antagonist to the same receptor site as
uptake back into the post-ganglionic sympathetic nerve the agonist by covalent interaction or by a very slowly
endings. The synapse is between the post-ganglionic nerve dissociating noncovalent interaction. An example of this
terminal and the effector tissue. antagonism is the blockade produced by
Source: Shah RV, Board Review 2005 for Smith phenoxybenzamine on a-adrenergic receptors, resulting in
a long-lasting reduction in the activity of
1354. Answer: B norepinephrine.
Dispositional antagonism occurs when one drug

ASIPP
Section 5 • Pharmacology 275

alters the pharmacokinetics (absorption, distribution, 1364. Answer: C


biotransformation, or excretion) of a second drug so that
less of the active compound reaches the target tissue. For 1365. Answer: D
example, Phenobarbital induces the biotransformation of Explanation:
warfarin, reducing its anticoagulant activity. A. At concentrations less than 5% phenol produces
Source: Stern-2004 protein denaturation whereas greater than 5% cause
protein coagulation and non-specific segmental
demyelination
1358. Answer: B - Density of blockade is similar with phenol and alcohol
Explanation:
* The site of action of spinally administered opiates is the
substantia gelatinosa of the spinal cord. B. The initial block wears off over a 24-hour period,
during which time neurolysis occurs.
* Epidural administration is complicated by factors
related to dural penetration, absorption in fat, and C. One must wait a day to determine effectiveness of the
systemic uptake; therefore, the quantity of intrathecally neurolytic block.
administered opioid required to achieve effective analgesia
is typically much smaller. D. Neurolytic blockade with phenol (6% to 10% in
glycerine) is painless because phenol has a dual action as
* The ratio of epidural to intrathecal dose of morphine is both a local anesthetic and a neurolytic agent.
approximately 10:1. - Alcohol (100% ethanol) is painful on injection and
should be preceded by local anesthetic injection.
* Morphine is typically given in doses of 3 to 10mg in the
lumbar epidural space. 5) Intrathecal morphine dosage is E. None of the neurolytic agents affect only sympathetic
0.2 to 1.0 mg. fibers.

* Onset time for epidural administration is 30 to 60 1366. Answer: D


minutes with a peak effect in 90 to 120 minutes. Source: Smith H, Board Review 2005

1359. Answer: C
Source: Smith H, Board Review 2005 1367. Answer: B
Explanation:
1360. Answer: D Epinephrine is commonly packaged as followos:
Source: Smith H, Board Review 2005
1:1000 1000 mg per 1,000 mL = 1 mg/mL
1361. Answer: C
Explanation: 1:10,000 1000 mg per 10,000 mL = 0.1 mg/mL
(Stoelting 3rd Ed., Chapter 12)
1:200,000 means 1 g = 1000mg = 1,000,000 µg per
Renal dose dopamine may promote diuresis, but it is not 200,000mL
conclusive whether it may protect against acute renal
failure. Dopamine antagonists, such as metoclopramide or 1,000,000 µg /200,000 mL = 5 mg/mL
droperidol, interfere with dopamine effects on the kidney.
Low dose dopamine may exacerbate GI mucosal ischemia Source: Hall and Chantigan
and contribute to multiple organ dysfunction syndrome.
Source: Shah RV, Board Review 2005 for Smith 1368. Answer: E
Explanation:
1362. Answer: C (Cooper, pp 317-322.)
Explanation: · Although there are hypotheses and models of
(Stoelting, 3rd Ed., Chapter 14) neurotransmitter dysfunction for many psychiatric and
Nonselective Beta Blockers do reduce heart rate and neurologic diseases, Parkinson’s disease remains the
cardiac contractility. They are highly absorbed by the gut, model disorder in which damage to a specific neural
but are subject to a significant first pass effect. They are pathway characterized by a particular neurotransmitter
highly protein bound. They do reduce the clearance of can explain most or all of the pathophysiology of the
local anesthetics, by affecting hepatic blood flow. They do disease.
increase airway resistance.
Source: Shah RV, Board Review 2005 for Smith · Patients with Parkinson’s disease have biochemical
evidence of greatly decreased dopamine function in the
1363. Answer: E brain because of degeneration of the nigrostriatal tract. A
neurotoxic model of the disease, produced in primates by

ASIPP
276 Section 5 •Pharmacology

administration of a derivative of meperidine (MPTP), Phentolamine and prazosin are reversible alpha blockers.
demonstrated that severe damage to dopaminecontaining Phenoxybenzamine is an irreversible alpha blocker.
nigrostriatal neurons produced nearly all of the signs and Esmolol is a selective Beta-1 blocker. Clonidine is a
symptoms of Parkinsons disease. selective partial alpha 2 agonist.
· As dopamine neurons in the nigrostriatal tract Source: Shah RV, Board Review 2005 for Smith
degenerate, compensatory changes occur that also
contribute to the pathophysiology. These changes include
a matching loss of the dopamine transporter and a 1372. Answer: C
compensatory rise in both dopamine 1 and dopamine 2 Explanation:
postsynaptic receptor density. The remaining dopamine In general, there is an overall direct correlation between
neurons synthesize and release more dopamine as a anesthetic’s potency and its direct depressant effect on
compensatory mechanism. These secondary physiologic myocardial contractility.
changes probably explain some of the signs and symptoms
seen in patients with advanced Parkinson’s disease who are A. Ratio for lidocaine and mepivacaine is 7.1.
being treated with agents that augment dopamine B. Ratio for etidocaine is 4.4
production. One example is the “on-off’ phenomenon in C. The ratio of dosage required for cardiovascular
which patients have abnormal increases in movement after collapse in animal models compared with that required to
administration of dopamine-augmenting agents, probably produce neurologic symptoms is the lowest for
because of hypersensitive dopamine receptors in bupivacaine and levo-bupivacaine (2.0)
remaining neurons of the nigrostriatal tract. - Ratio for ropivacaine is 2.2
Source: Ebert 2004 D. Ratio for prilocaine is 3.1;
E. Ratio for procaine and chloroprocaine is 3.7

1369. Answer: A 1373. Answer: A


Explanation: Source: Smith H, Board Review 2005
(Stoelting, 3rd Ed., Chapter 12)
1374. Answer: D
Ephedrine 10-25 mg is administered to adults that drop Source: Smith H, Board Review 2005
their BP following regional anesthesia. Ephedrine is an
indirect acting synthetic non-catecholamine that 1375. Answer: E
stimulates alpha and beta receptors. Ephedrine is more Source: Smith H, Board Review 2005
effective in correcting non-cardiac circulatory changes
as compared to selective alpha and beta agonists. 1376. Answer: A
The doses of ephedrine are1/250th that of epinephrine.
Tachyphylaxis may occur.
Source: Shah RV, Board Review 2005 for Smith 1377. Answer: A
Explanation:
1370. Answer: C (Sierles, pp 393-397.)
Explanation: - Side effects on sexual function are frequently
(Stoelting 3rd Ed., chapter 15) produced by antihypertensives, other cardiovascular
compounds, and psychotropic medications.
Clonidine preferentially activates alpha 2 receptors over - Sexual dysfunctions can be produced through
alpha 1 by 220:1. Hence it does not inhibit alpha 1 anticholinergic parasympathetic and sympathetic
receptors and it does not only bind to alpha 2 receptors. ganglionic-blocking, antiandrogenic, ß-adrenergic,
Clonidine is often used to prolong the effects of progestational, antihistaminic, and dopamine antagonist
subarachnoid bupivacaine and tetracaine…specifically, actions.
motor and sensory blockade. Intravenous fluids may be - Tricyclics, phenothiazines,lpha-methyldopa, and
needed to prevent hypotension. Oral clonidine, 150-200 guanethidine all have the effect of decreasing sexual
mcg, may prolong spinal anesthesia, but may increase the arousal. They can also inhibit desire and produce orgasmic
risk of hypotension and bradycardia. Clonidine does not difficulties.
cause the side effects associated with spinal or epidural - Amphetamines can produce orgasmic difficulties, but
opioids: pruritis, nausea and vomiting, delayed gastric do not appear to inhibit desire or decrease arousal.
emptying. Clonidine does stop shivering, when given IV - The physician must always consider that drug
(75 mcgs), by inhibiting central thermoregulatory control. combinations can create untoward effects on sexual
Source: Shah RV, Board Review 2005 for Smith function.
Source: Ebert 2004
1371. Answer: C
Explanation: 1378. Answer: B
(Stoelting, 3rd Ed.) Explanation:
Each milliliter of local anesthetic will anesthetize about

ASIPP
Section 5 • Pharmacology 277

one spinal segment. Two thirds of these would be above is not useful as a topical agent.
the epidural entry side and one third would be below.
1391. Answer: A (1, 2, & 3 )
1379. Answer: D Source: Cole EB, Board Review 2003
Explanation:
The maximum dose of local anesthetics containing 1392. Answer: A (1,2, & 3)
1:200,000 epinephrine that can be used for major nerve Source: Hansen HC, Board Review 2004
blocks is:
Lidocaine, 500mg 1393. Answer: E (All)
Mepivacaine, 500mg Explanation:
Prilocaine, 600mg When an opioid is delivered to the epidural space, all the
Bupivacaine, 225mg listed actions occur. These characteristics affect the
Etidocaine, 400mg clinical effects of various opioids in the following way:
Tetracaine, 200mg. Lipid-soluble agents (e.g., fentanyl) have rapid onset of
analgesia, short duration, and early respiratory depression
1380. Answer: C associated with the degree of systemic uptake. Hydrophilic
Explanation: agents (e.g., morphine) have slow onset of analgesia,
Reference: Katzung, pp 373-374. prolonged duration, and late respiratory depression
antagonist. The drug reverses the CNS sedative effects of associated with rostral spread via the CSF to the
benzodiazepines and is indicated where general anesthesia brainstem.
has been induced by or maintained with benzodiazepines Source: Kahn CH, DeSio JM. PreTest Self Assessment and
such as diazepam, lorazepam, or midazolam. Review. Pain Management. New York, McGraw-Hill, Inc.,
Source: Stern - 2004 1996.

1394. Answer: D (4 Only)


1381. Answer: B Source: Jackson KC. Board Review 2003
Source: Smith H, Board Review 2005

1382. Answer: A 1395. Answer: C (2 & 4)

1383. Answer: C 1396. Answer: B (1 & 3)


Source: Raj P, Pain medicine - A comprehensive Review -
Second Edition 1397. Answer: D (4 Only)
Source: Jackson KC. Board Review 2003
1384. Answer: A
Source: Hansen HC, Board Review 2004 1398. Answer: B (1 & 3)
Source: Hansen HC, Board Review 2004
1385. Answer: C
1399. Answer: B (1 & 3)
1386. Answer: C Explanation:
* Hyperventilation of the lungs and hypocarbia decrease
1387. Answer: D (4 Only) cerebral blood flow, thus reducing delivery of local
Source: Jackson KC. Board Review 2003 anesthetic to the brain.

1388. Answer: D (4 Only) * The alkalosis and hypokalemia that occur as a result of
Source: Cole EB, Board Review 2003 hyper-ventilation lead to hyperpolarization of the resting
transmembrane potential of neurons, thus increasing the
seizure threshold for local anesthetics.
1389. Answer: D (4 Only)
Source: Jackson KC. Board Review 2003 * Acidosis and hypercarbia decrease the seizure threshold
for local anesthetics.
1390. Answer: A (1, 2, & 3)
Explanation: * Hyperoxia does nothing to prevent seizures.
* Lidocaine, tetracaine, and cocaine are all effective topical
anesthetics when applied to mucous membranes. 1400. Answer: A (1, 2, & 3 )

* Cocaine is unique among local anesthetics in that it is a 1401. Answer: D (4 Only)


vasoconstrictor.

* Procaine penetrates the mucous membranes poorly and 1402. Answer: C (2 & 4)

ASIPP
278 Section 5 •Pharmacology

1403. Answer: E (All) 1409. Answer: A (1,2, & 3)


Explanation: Source: Hansen HC, Board Review 2004
All of these local anesthetic concentrations are isobaric.
Tetracaine 0.5% is prepared by mixing equal volumes of 1410. Answer: E (All)
1% tetracaine and preservative-free saline. Hyperbaric Explanation:
solutions can be prepared by mixing equal volumes of 1% The amount of systemic absorption of a local anesthetic
tetracaine and 10% dextrose, resulting in 0.5% tetracaine depends on the total dose injected, the vascularity of the
in 5% dextrose, or by mixing equal volumes of 0,75% injection site, the speed of injection, whether or not a
bupivacaine with 10% dextrose, yielding a 0.375% vasoconstrictor is added to the local anesthetic solution,
solution of bupivacaine in 5% dextrose. Alternatively, and the physicochemical properties of the local anesthetic,
factory-mixed preparations of 0.75% bupivacaine in 8.25% such as protein and tissue binding, lipid solubility, and the
dextrose and 5% lidocaine in 7.5% dextrose are available. degree of ionization at physiologic pH. For all local
To prepare hypobaric tetracaine, 10mg (1 mL of 1% anesthetics, systemic absorption is greatest after injection
tetracaine) are mixed with 9 mL of sterile H2O to yield 10 for intercostal nerve and caudal blocks, intermediate for
mL of 0.1% tetracaine. This has a baricity of 1.0. epidural blocks, and least for brachial plexus and sciatic
nerve blocks.
1404. Answer: C (2 & 4)
Explanation: 1411. Answer: A (1, 2, & 3)
(Raj, Practical Mgmt of Pain 3rd Ed. Chapter 39 Source: Jackson KC. Board Review 2003
,Stoelting, 3rd Ed., page 174-5.)
1412. Answer: E (All)
There are 2 prevailing theories of how epidural local Explanation:
anesthetics work. These are choices 2 and 4. Ropivacaine is Physical symptoms of withdrawal from alcohol usually
thought to produce a less dense and less prolonged motor occur 6-48 hours after last drink, subside in 5-7 days
block compared to bupivacaine. Additionally, ropivacaine without treatment, but irritability nd insomnia may last 10
is less cardiotoxic and is thus advantageous in the obstetric days or longer. Nutritional and vitamin deficiences are
population. Delayed onset of hypotension, bradycardia, common even if the individual appears well nourished.
and a high motor-sensory block, suggests a subdural block. The patient must be watced for overhydration especially
A test dose, by definition, is a small volume of local during IV fluid replacement.
anesthetic (with/without an admixture of epinephrine [to Source: Psychiatry specialty Board Review By William M.
check for vascular uptake]) that is used to exclude an Easson, MD and Nicholas L. Rock, MD
subarachnoid injection. The delay in presentation suggests
a subdural block. 1413. Answer: B (1 & 3)
Explanation:
The hypotension is due to sympatholysis. The bradycardia * The presence of myelin and a rapid neuronal firing rate
is due to interruption of the cardiac accelerator fibers and actually enhance the ability of local anesthetics to block the
the Bezold-Jarisch reflex. neuron.
Source: Shah RV, Board Review 2004
* Local anesthetics gain access to receptors when the
1405. Answer: E (All) sodium channels are open, as occurs during an action
Source: Hansen HC, Board Review 2004 potential.

1406. Answer: D (4 Only) * Larger-diameter fibers are more difficult to block than
Source: Reddy Etal. Pain Practice: Dec 2001, march 2002 smaller-diameter fibers.

1407. Answer: D (4 Only) * Tissue acidosis results in formation of the ionized form
Explanation: of the local anesthetics. This form does not readily
1. The un-ionized form of the local anesthetic traverses the transverse the lipophilic cell membrane.
nerve membrane whereas the ionized form actually blocks
conduction. About three nodes of Ranvier must be 1414. Answer: A (1, 2, & 3 )
blocked to achieve anesthesia.
1415. Answer: E (All)
2. The ability of a local anesthetic to block conduction is
inversely proportional to the diameter of the fiber. 1416. Answer: D (4 Only)
Source: Day MR, Board Review 2004
3. The presence of myelin enhances the ability of a local
anesthetic to block conduction, as does rapid firing. 1417. Answer: D (4 Only)
Explanation:
1408. Answer: A (1,2, & 3) Reference: Hardman, p 340. Katzung, p 437.
Source: Hansen HC, Board Review 2004

ASIPP
Section 5 • Pharmacology 279

Of the listed agents, only bupivacaine is an amide. Allergy 1428. Answer: A (1, 2, & 3)
to amide-type local anesthetics is much less frequent than Explanation:
with ester-type local anesthetics, such as benzocaine; 1. Epinephrine or phenylephrine is frequently added to
patients who demonstrate an allergy to one such drug will local anesthetic solutions to produce vasoconstriction.
be allergic to all of them. This decrease systemic absorption of the local anesthetic
Source: Stern - 2004 and prolongs the duration of action of the local anesthetic.

1418. Answer: B (1 & 3)


Source: Reddy Etal. Pain Practice: Dec 2001, march 2002 2. The extent to which epinephrine prolongs the block
depends on both the site of injection and the specific local
1419. Answer: C (2 & 4) anesthetic. These beneficial effects are limited when
Source: Cole EB, Board Review 2003 vasoconstrictors are used with epidural etidocaine and
bupivacaine.
1420. Answer: A (1,2, & 3)
Source: Hansen HC, Board Review 2004
1429. Answer: B (1 & 3)
1421. Answer: B (1 & 3) Explanation:
Source: Hansen HC, Board Review 2004 * Ester-type local anesthetics are broken down partly in the
blood by pseudocholinesterase and red cell esterase and
1422. Answer: A (1, 2, & 3) partly in the liver.
Explanation:
Alcohol dependence is characterized by the inability to cut * Anticholinesterase drugs, such as echothiophate,
down and stop drinking, despite repeated efforts to control neostigmine, pyridostigmine, and edrophonium, inhibit
drinking (“going on the wagon”), binges, and amnesia pseudocholinesterase and thus slow the plasma clearance
periods, and continued drinking while knowing a serious of ester-type local anesthetics.
physical condition is being exacerbated by alcohol.
Source: Psychiatry specialty Board Review By William M. * Phenytoin is an enzyme inducer that may hasten the
Easson, MD and Nicholas L. Rock, MD metabolism of amide-type local anesthetics, such as
lidocaine but would have little, if any, effect on ester-type
1423. Answer: A (1,2, & 3) local anesthetics and would certainly not impede their
Source: Hansen HC, Board Review 2004 plasma clearance.

1430. Answer: E (All)


1424. Answer: E (All) Explanation:
Explanation: Clonidine alone, when administered neuraxially, is an
( Raj, Practical Mgmt of Pain, 3rd E. , Chapter 39) effective analgesic. Intrathecal drugs possessing alpha-
agonist (phenylephrine/epinephrine) properties will also
The benzene ring is an aromatic moiety that is a major produce analgesia. Intrathecal epinephrine will reduce
contributor to the lipid solubility of a local anesthetic. systemic/vascular uptake of local anesthetics, thereby
Local anesthetics need to be lipid soluble, i.e., unionized or enhancing their effects, including hypotension.
in their base form, in order to cross the neural membrane
and enter the axoplasm. Once in the axoplasm, the local 1431. Answer: D (4 Only)
anesthetic can acquire a proton and become ionized. The Source: Hansen HC, Board Review 2004
ionized form will bind to the active portion of the Na+
channel 1432. Answer: D (4 Only)
Source: Shah RV, Board Review 2004 Source: Lou Etal. Pain Practice: march 2001

1425. Answer: A (1, 2, & 3) 1433. Answer: E (All)


Source: Hansen HC, Board Review 2004
1434. Answer: A (1, 2, & 3)
1426. Answer: D (4 Only) Source: Trescot A, Board Review 2003
Explanation:
Reference: Hardman, p 448. Katzung, p 493, 1130.
Some NSAIDs can increase proximal tubular reabsorption 1435. Answer: A (1, 2, & 3)
of lithium salts, which can create toxic levels of lithium in Explanation:
the plasma. Clonidine, Tizanidine and Dexmedetomidine are a2 (alpha
Source: Stern - 2004 -2) agonists. Antipamazole is an a2-antagonist. a2 agonists
have been used in the management of hypertension for
1427. Answer: B (1 & 3) many years. Their role has now expanded to chronic pain
management and as muscle relaxants. One proposed

ASIPP
280 Section 5 •Pharmacology

mechanism of analgesic action of a2 agonists is by


reducing sympathetic outflow by a direct action on the * Para-aminobenzoic acid is a metabolic breakdown
preganglionic outflow at the spinal level. product of ester anesthetic and is responsible for allergic
reactions in some individuals.
Clonidine is available in oral, transdermal and epidural or
intrathecal use form. It is used for the treatment of 1443. Answer: B (1 & 3)
Complex Regional Pain Syndromes, cancer pain, Source: Reddy Etal. Pain Practice: Dec 2001, march 2002
headaches, post herpetic neuralgia and peripheral
neuropathy. 1444. Answer: D (4 Only)

Tizanidine has been used for painful conditions involving


spasticity. Dexmedetomidine is currently used as sedative 1445. Answer: E (All)
in the Intensive Care Unit. Source: Smith H, Board Review 2005
Source: Chopra P, 2004
1446. Answer: B (1 & 3)
1436. Answer: A (1, 2, & 3 ) Explanation:
(Kandel, pp 498-959.)
1437. Answer: A (1, 2, & 3) · Even though many sleeping pills are initially helpful,
Explanation: they lose their effectiveness within 2 weeks.
Sympathomimetics, ß(beta)-adrenergic receptor · The repeated administration of barbiturates (e.g.,
antagonist, volatile anesthetics, and the H2 - receptor pentobarbital or phenobarbital) results in a gradual
antagonist cimetidine reduce hepatic blood flow, thereby increase in hepatic enzymes, which normally are
reducing plasma clearance of amide-type local anesthetics. responsible for the degradation of the barbiturates. Not
There is also evidence that propranolol directly inhibits only is their pharmacologic action decreased, but since the
mixed-function oxidase activity of hepatocytes. Phenytoin liver enzymes are relatively nonspecific, the result is often
increases clearance of lidocaine by enzyme induction. a broad cross-tolerance to other hypnotics. Barbiturates
are known to suppress REM sleep, so when the drug is
1438. Answer: C (2 & 4) withdrawn, a marked REM rebound results, often
aggravating insomnia.
1439. Answer: E (All) · The benzodiazepines are addictive. Flurazepam
increases
hepatic enzymes at a much slower rate; hence patients
1440. Answer: D (4 Only) develop a tolerance much more slowly than for
Source: Boswell MV, Board Review 2004 pentobarbital. However, an active metabolite of
flurazepam remains in the body for a longer period of
1441. Answer: E (All) time (more than 24 h), which results in a gradual increase
Explanation: of these breakdown substances in the blood. Thus, the
Important variations in drug response occur in effects of the drug are often felt during the daytime as
microorganisms, such as HIV and bacteria, which diminished alertness and hand-eye coordination. These
accounts for resistance to drugs symptoms are also aggravated by alcohol.
Source: Ebert 2004
1442. Answer: C (2 & 4)
Explanation: 1447. Answer: A (1,2, & 3)
* Para-aminobenzoic acid is a metabolite of the ester-type Source: Hansen HC, Board Review 2004
local anesthetics.
1448. Answer: A (1, 2, & 3)
* Local anesthetics may be placed into two distinct Source: Lou Etal. Pain Practice: march 2001
categories based on their chemical structure: ester or
amide. 1449. Answer: B (1 & 3)

* All of the amides contain the letter “i” twice, once in


“caine” and once elsewhere in the name (e.g., lidocaine, 1450. Answer: D (4 Only)
etidocaine, prilocaine, mepivacaine, and bupivacaine). Source: Lou Etal. Pain Practice: march 2001
These are metabolized in the liver.
1451. Answer: E (All)
* The ester local anesthetics are cocaine, procaine, Source: Reddy Etal. Pain Practice: Dec 2001, march 2002
chloroprocaine, tetracaine, and benzocaine. These drugs
are metabolized by the enzyme pseudocholinesterase 1452. Answer: A ( 1, 2, & 3)
found in the blood. Their half-lives in blood are very short Source: Day MR, Board Review 2004
, about 60 seconds.

ASIPP
Section 5 • Pharmacology 281

1453. Answer: B (1 & 3) 1467. Answer: C (2 & 4)


Explanation: Explanation:
Addition of CO2 or HCO3¯ to local anesthetic solutions (Stoelting, 3rd Ed., Chapter 12)
hastens the onset of the anesthetic block but does not
increase its duration. Vasoconstrictors decrease Epinephrine demonstrates:
absorption (and metabolism) of local anesthetics. A larger - Beta-2 receptor agonism at 1-2 mcg/minute
dose results in longer anesthetic duration, as well as denser - Beta-1 receptor agonism at 4-6 mcg/minute
blockade. - Alpha and Beta agonism at 10-20 mcg/minute

1454. Answer: A (1,2, & 3) Thus, at


Source: Hansen HC, Board Review 2004 - High doses: Beta 1 will increase systolic
BP/HR/Cardiac Output Beta 2 will reduce diastolic BP
1455. Answer: E (All)
Hence, mean arterial pressure will marginally increase,
1456. Answer: A ( 1, 2, & 3) and pulse pressure will increase—reflex bradycardia will
Source: Smith H, Board Review 2005 not occur High to Low doses: reduced alpha agonism
implies increased perfusion to the skin. Since Beta-2
1457. Answer: C (2 & 4) agonism is preserved at low doses, then skeletal muscle
Source: Smith H, Board Review 2005 perfusion will be preserved
Source: Shah RV, Board Review 2005 for Smith

1458. Answer: A (1, 2 & 3) 1468. Answer: B (1 & 3)


Explanation: Explanation:
Explanation: Neurolytic action is by dehydration, with (Stoelting, 3rd Ed., chater 12)
extraction of cholesterol, phospholipids, and cerebrosides,
and precipitation of mucoproteins. This results in Albuterol is a selective beta 2 agonist that is given for the
sclerosis of nerve fibers and myelin sheath (demyelination treatment of acute bronchospasm due to asthma.
and subsequent wallerian degeneration). The basal lamina Although it can be given orally, it is usually given via
of the Schwann cell is often spared and the axon often nebulization or as a metered dose inhaler.
regenerates.
Ephedrine is resistant to MAO in the gut and is absorbed
Source: Warfield C, Bajwa Z. Principles and Practice of unchanged into the circulation after oral administration.
Pain Medicine 2nd Ed., McGraw-Hill 2004.
Source: Day MR Endogenous catecholamine can be broken down by GI
mucosal and hepatic enzymes
1459. Answer: A ( 1, 2, & 3) Source: Shah RV, Board Review 2005 for Smith
Source: Smith H, Board Review 2005

1460. Answer: B ( 1 & 3) 1469. Answer: B (1 & 3)


Source: Smith H, Board Review 2005 Explanation:
(Stoelting, 3rd Ed., chapter 12)
1461. Answer: E (All)
Source: Smith H, Board Review 2005 Epinephrine relaxes the detrusor and the gastrointestinal
smooth muscle. Epinephrine contracts the trigone and
1462. Answer: C (2 & 4) urinary sphincter. During a ‘fight or flight’ resoponse, one
Source: Smith H, Board Review 2005 does not want to pee or defecate.
Source: Shah RV, Board Review 2005 for Smith
1463. Answer: E (All)
Source: Smith H, Board Review 2005 1470. Answer: E (All)
Source: Smith H, Board Review 2005
1464. Answer: E (All)
Source: Smith H, Board Review 2005 1471. Answer: E (All)
Source: Smith H, Board Review 2005

1465. Answer: B ( 1 & 3) 1472. Answer: E (All)


Source: Smith H, Board Review 2005
1473. Answer: E (All)
1466. Answer: E (All) Source: Boswell MV, Board Review 2004
Source: Smith H, Board Review 2005
1474. Answer: E (All)

ASIPP
282 Section 5 •Pharmacology

Source: Smith H, Board Review 2005 effects of L-dopa are mediated by CNS dopamine, so
adding carbidopa does not make them less likely. The
1475. Answer: E (All) combination of L-dopa and carbidopa reduces the
Source: Boswell MV, Board Review 2004 extracerebral metabolism of L-dopa, resulting in decreased
peripheral adverse effects.
1476. Answer: E (All) Source: Stern - 2004
Source: Boswell MV, Board Review 2004
1487. Answer: A ( 1, 2, & 3)
Source: Smith H, Board Review 2005
1477. Answer: C (2 & 4)
Explanation: 1488. Answer: A ( 1, 2, & 3)
Metabolism of drugs occurs in the liver (most important) Explanation:
as well as the kidneys, lungs and gastrointestinal tract. Fluoxetine is an inhibitor of CYP 2D6
Phase II reactions are conjugation reactions, which involve Source: Boswell MV, Board Review 2004
covalent binding of adducts to drugs to increase water
solubility and enhance renal excretion. Most conjugation 1489. Answer: A ( 1, 2, & 3)
reactions occur in the cytosol (except for glucuronidation, Source: Smith H, Board Review 2005
which is microsomal).
Source: Boswell MV, Board Review 2004
1490. Answer: C (2 & 4)
1478. Answer: E (All) Source: Smith H, Board Review 2005
Source: Boswell MV, Board Review 2004
1491. Answer: B ( 1 & 3)
1479. Answer: A ( 1, 2, & 3) Source: Smith H, Board Review 2005
Source: Smith H, Board Review 2005
1492. Answer: A ( 1, 2, & 3)
1480. Answer: B (1 & 3) Source: Smith H, Board Review 2005
Source: Boswell MV, Board Review 2004
1493. Answer: E (All)
1481. Answer: E (All) Source: Smith H, Board Review 2005
Explanation:
Anticonvulsants are effective more quickly than lithium, 1494. Answer: C (2 & 4)
and potentiate the effect. Centrally acting L type calcium Source: Smith H, Board Review 2005
channel blockers are also helpful.
Source: Boswell MV, Board Review 2004 1495. Answer: C (2 & 4)
Source: Smith H, Board Review 2005
1482. Answer: E (All)
1496. Answer: D (4 only)
1483. Answer: E (All) Explanation:
1484. Answer: C (2 & 4) Explanation: Amino ester local anesthetics include
Explanation: tetracaine, cocaine, prilocaine, and chloroprocaine. Amino
* Local anesthetics are weak bases with pKas ranging from amide local anesthetics include: lidocaine, etidocaine,
7.6 to 8.9. bupivacaine, ropivacaine, mepivacaine, prilocaine, and
levobupivacaine.
* A low pH will result in the formation of the ionized
species because more protons (hydrogen ions) are Source: Hahn, McQuillan, Sheplock: Regional Anesthesia:
available to bind to the nitrogen atoms in the local An Atlas of Anatomy and Techniques. Mosby 1996.
anesthetics. Source: Day MR

* Local anesthetic concentration and volume have nothing


to do with the fraction of anesthetics in the ionized form.

1485. Answer: A (1, 2, & 3 )

1486. Answer: A (1, 2, & 3)


Explanation:
Reference: Katzung, pp 464-467.
Adding carbidopa decreases the amount of dopamine that
is formed peripherally from dopa by dopa decarboxylase.
Depression, psychosis, and other psychiatric adverse

ASIPP

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