MODULE 4

PHARMACOLOGY AND BIOPHARMACEUTICS

1. A drug that causes significant delay in the absorption of acetaminophen by reducing the rate of gastric emptying:

a. Anticholinergicb. Digoxin

c. Levodopad. Propantheline

2. Histabloc® is a:

a. H1 agonistb. H1 antagonist

Histabloc is Famotidine (H2 antagonist)

c. H2 agonistd. H2 antagonist

3. Schilling test is used for the detection of:

a. Pernicious anemiab. Megaloblastic anemiac. Iron deficiency anemiad. Folate deficiency

Pernicious anemia is caused by loss of gastric parietal cells, and subsequent inability to absorb vitamin B12.

Megaloblastic anemia is an anemia (of macrocytic classification) that results from inhibition of DNA synthesis in red blood cell production.

4. Ambenonium, Neostigmine, and Pyridostigmine are most commonly used for which condition:

c. Bronchial asthmad. COPD

Tacrine, Donepezil, Rivastigmine and Galantamine, all of which are anticholinesterase are indicated for Alzheimer’s Disease

a. Atropine overdose

b. Myasthenia gravis

5. A new drug is currently being developed whose mechanism of action is stimulation of the beta-3 receptors. In which condition will this drug have most likely usefulness?

a. Obesity

b. Bronchial asthmaObesity as beta-3 receptor plays in lipolysis

c. shockd. Acute Renal failure

6. Among diabetic patients using insulin or oral hypoglycemic agents (OHAs), why are beta-blockers used with special caution if not totally avoided? a. Beta- blocker can induce hyperglycemiab. Beta-blocker can mask hypoglycemic

symptomsc. Beta-blocker can attenuate effect of

insulin and OHAsd. Beta-blocker can induce insulin or OHA

failure

7. The effects of muscarinic receptor activation in tissues like the exocrine glands and the extravascular smooth muscles have been linked with the generation of which second messenger molecule?

c. ATPd. cGMP

IP3, leading to an increase in intracellular calcium

a. IP3b. cAMP

8. In schizophrenic syndrome there is primarily:

a. Decreased cholinergic activityb. Decreased dopaminergic activityc. Increased dopaminergic activityd. Increased cholinergic activity

• psychosis and schizophrenia - abnormally high dopaminergic transmission

• Parkinson’s disease - decreased dopamine activity

9. Chloramphenicol can cause:

a. Diarrheab. Blindness

c. emesisd. bone marrow depression

10. A broad spectrum gram-negative cephalosporin:

a. Cefalexinb. Cefotaxime

Cefotaxime – 3rd generation cephalosporins have a broad spectrum of activity and further increased activity against Gram-negative organismsCefamandole – second generationCefalexin-first generation

c. Cefamandoled. AOTA

11. What is the most important mechanism of termination of effects of released Norepinephrine which is the target action of TCA’s and cocaine:

a. Degradation by COMTb. Sequestration into cellsc. Degradation by MAOd. Reuptake into the presynaptic terminal

12. A given adrenergic agent induces uterine relaxation and bronchial muscle relaxation and bronchial muscle relaxation. These effect can be attributed to:

a. Alpha-1 stimulationb. Alpha-2 stimulation

c. Beta-1 stimulationd. Beta-2 stimulation

13. In combination therapy for tuberculosis, the following are commonly administered orally EXCEPT:

a. Ethambutol

b. INH

Streptomycin - IM

c. Streptomycind. Rifampicin

14. Furosemide is useful for the treatment of all the following EXCEPT:

a. Acute pulmonary edemab. Hypertensive crisisc. Hypoglycemiad. Congestive heart failure

15. What is the dominant adrenergic receptor in the heart?

a. Alpha – 1b. Alpha – 2

c. Beta – 1 d. Beta – 2

16. In terms of mechanism of action, which of the following drugs most closely resembles that of clonidine:

a. Phenylephrineb. Reserpine

c. Methyldopad. Amlodipine

17. In the adrenal medulla, Norepinephrine is converted to epinephrine by the action of which enzyme?

a. DOPA decarboxylaseb. Phenylethylamine N-methyl transferasec. COMTd. MAO

18. At what dose should Dopamine be given as IV infusion to produce a predominantly dopaminergic effect?

a. 0.5 – 5 ug/kg/minb. 5-10 ug/kg/minc. 10-20 ug/kg/mind. 20-50 ug/kg/min

19. Prolonged therapeutic administration of cortisone induces:

a. Hypoglycemiab. Hypofunction of the adrenal cortexc. Hyperfunction of the pituitary glandd. Hypofunction of the adrenal medulla

20. What is the mechanism of skeletal muscle paralysis produced by succinylcholine?

a. Competitively inhibits binding of acetylcholine to the NM receptor

b. Increase the inward chloride conductance leading to hyperpolarization of the neuromuscular endplate membrane

c. Sustained depolarization of the motor end plate making it unresponsive to other impulses and upon repolarization cannot easily be depolarized

d. Repeated short depolarization of the motor end plate leading to a prolonged state of sodium channel inactivation

e. Irreversible and non-competitive inhibition of the NN receptor in both the ganglia and motor end plate with attenuation of depolarization impulse

21. Which of the following inhalational anesthetics produces the greatest augmentation of the effect of neuromuscular blockers?

a. Isofluraneb. Sevoflurane

c. Halothaned. Desflurane

22. Anaphylactoid reaction may be seen as a side effect with which of the following neuromuscular blockers?

a. Pancuroniumb. Vecuronium

Tubocurarine induces a non-immune mediated histamine release by mast cells which can manifest as an anaphylaxis like reaction

c. Tubocurarined. Rocuronium

23. This can decrease gastric emptying time:

a. Stress

b. Metoclopramide

Stress – increase stomach contractions and emptying rate

Metoclopramide – gastroprokinetic agent

c. None of thesed. Vigorous exercise

24. What is the primary mechanism of action of the drug Indapamine?

a. Inhibition of the 2Cl-Na-K contransporter in the distal convoluted tubule

b. Inhibition of the Na-Cl cotransporter at the distal convoluted tubule

c. Inhibition of the Na-Cl cotransporter at the collecting duct

d. Competitive inhibition of Aldosterone binding to its receptor

e. Competitive inhibition of Vasopressin binding to V2 receptor

25. What is considered as the toxic plasma concentration of Digoxin?

a. >0.5 mg/mlb. >150 ng/ml

c. >10 ng/mld. >2 ng/ml

26. The drug of choice in the treatment of arrhythmia caused by digitalis intoxication:

a. Methyldopab. Phenytoin

c. Hydralazined. Phenylephrine

27. Inotropic activity of the heart in congestive heart failure can be increased by which of the following agents?

I. BipyridinesII. ACE inhibitorsIII. Beta-1 Agonist

a. I onlyb. II onlyc. I and IIId. II and IIIe. I, II and III

28. Which of the following anti-arrhythmic agents has been associated with lupus-like side effect?

a. Quinidineb. Lidocaine

c. Amiodaroned. Procainamide

29. Which of the following calcium channel blocker is most useful in arrhythmia therapy?

a. Verapamilb. Diltiazem

Verapamil is the ONLY CCB with proven clinical role in arrhythmia therapy

c. Nifedipined. Lidocaine

30. Chinese patients are most likely to be more sensitive to the effects of which of the following drugs for hypertension that lower doses may have to be used?

a. Prazosinb. Amlodipine

Chinese patients are most likely to be more sensitive to the effects of beta blocker

c. Metoprolold. HCTZ

31. Which of the following benzodiazepines has the shortest half-life and a rapid onset of action?

a. Lorazepamb. Triazolam

Triazolam and Midazolam have the shortest half-lives with a rapid onset of action

c. Oxazepamd. Diazepam

32. Which of the following findings in a patient taking Phenytoin would warrant reduction in the dose?

a. Gingival hyperplasiab. Nystagmus

Ataxia and diplopia are early manifestations of toxicity

c. Osteomalaciad. Ataxia

33. Which of the following drugs for seizure is metabolized to yield Phenobarbital?

a. Lamotrigine

b. Vigabatrin

Phenobarbital is one of the two active metabolites of Primidone

c. Primidoned. Topiramate

34. When Phenytoin is given intravenously, what is the maximum rate by which the drug can be administered?

a. 10mg/minb. 20mg/min

c. 30mg/mind. 50mg/min

When Phenytoin is given intravenously, the maximum rate by which the drug can be administered is 50mg/min

35. What is Entacapone?

a. A selective MAO-A inhibitorb. A selective MAO-B inhibitorc. A Dopamine-3 receptor agonistd. COMT inhibitor

Entacapone is an inhibitor of COMT which can convert levodopa to 3-O-methyldopa, a metabolite which can interfere with the transport of Levodopa across the blood brain barrier

36. Which of the following drug is most useful in controlling the bradykinesia of Parkinsonism?

a. Levodopab. Bromocriptine

c. Selegelined. Entacapone

37. What type of protein is primarily targeted by Digitalis glycosides when they exert their effect on the heart?

a. Receptorb. Ion channels

c. transportersd. structural proteins

Cardiac glycosides inhibit Na+/K+ ATPase, the membrane bound transporter often called the sodium pump.

38. Biotransformation of orally administered drugs occurring primarily in the liver that reduces the amount of drug finally entering the systemic circulation is often referred to as:

a. Enterohepatic recirculationb. Gastric emptyingc. First pass effectd. Enzyme induction

39. What neurotransmitter is released by the preganglionic fibers as a response to sympathetic stimulation?

a. Acetylcholineb. Norepinephrine

c. Serotonind. Dopamine

Acetylcholine is the preganglionic neurotransmitter in both the sympathetic and parasympathetic nervous system

40. A 55 year old male with kidney stones has been placed on a diuretic to decrease calcium excretion. However, after a few weeks, he develops an attack of gout. Which diuretic was he taking?

a. Furosemideb. HCTZ

c. Spironolactoned. d. Triamterene

HCTZ can also inhibit the excretion of uric acid and cause its accumulation, leading to an attack of gout

41. A 45-year-old man has recently been diagnosed with hypertension and started on monotherapy designed to reduce peripheral resistance and prevent NaCl and water retention. He has developed a persistent cough. Which of the following drugs would have the same benefits but would not cause cough?

a. Losartanb. Nifedipine

c. Prazosind. Propranolol

Losartan is an ARB that will have the same beneficial effects but will not produce cough.

42. What is the amino acid precursor in the synthesis of catecholamines?

a. Phenylalanineb. Glycine

c. Tyrosined. Tryptamine

Tryptamine for 5HT/Serotonin

43. Which of the following beta-blockers is cardioselective?

a. Labetalolb. Propranolol

c. Pindolold. Esmolol

BEAM = Bisoprolol, Esmolol, Atenolol, Metoprolol

44. Bethanechol is clinically used for which of the following conditions?

a. Urinary retention in neurogenic bladderb. Intestinal obstructionc. Chronic glaucomad. Supraventricular tachycardia

Due to its acetylcholine-like effect on the genitourinary tract

45. Which of the following findings may be consistent with an overdose of or accidental exposure to an organophosphate?

a. Constipationb. Mydriasisc. Emesisd. Peripheral vasodilation

DUMBBELSS ( diarrhea, urination, miosis, bradycardia, bronchoconstriction, emesis,

lacrimation, sweating, salivation)

46. Ipratropium, Oxytopium, and Tiotropium are antimuscarinic agents that are most useful as:

a. Mydriaticsb. Cycloplegic agentsc. Relaxant of bronchial smooth musclesd. Inhibitors of involuntary muscle

contractionse. Inhibitors of bronchial gland secretions

47. Which of the following anti hypertensive agents is most appropriate for elderly male patients with benign prostatic hyperplasia?

a. Prazosinb. Metoprolol

c. HCTZd. Enalapril

- alpha blocker, which can also relax the prostatic smooth muscles providing relief of urinary retention

48. Which of the following drugs classified as NSAIDs inhibit/s the COX-2 more than the COX-1 isozymes?

a. Indomethacinb. Ibuprofen

c. Mefenamic acidd. Celecoxib

Coxibs and Meloxicam inhibit the COX 2 more than the COX 1 isozymes

49. The most common prophylactic measure used worldwide to prevent tuberculosis:

a. INHb. Bacillus calmette guerine vaccinec. Ethambutold. Streptomycin

50. Which of the following agents is a strong full agonist of opioid receptors?

a. Hydromorphoneb. Propoxyphene

c. Hydrocodoned. Pentazocin

Hydromorphone, Oxymorphone, Methadone and Morphine are the strong full agonist of opioid receptor

51. The activity of regular heparin when given intravenously is best monitored at least every 6 hours for the first 24 hours of therapy using what parameter?

a. Protimeb. Platelet countc. Activated Partial thromboplastin timed. Bleeding time

52. Which of the following benzodiazepines has the shortest half-life and a rapid onset of action?

a. Lorazepamb. Triazolam

c. Oxazepamd. Diazepam

Triazolam and Midazolam have the shortest half lives with rapid onset of action

53. Which of the following findings in a patient taking Phenytoin would warrant reduction in dose?

a. Gingival hyperplasiab. Nystagmus

c. Ataxiad. Hirsutism

Ataxia and diplopia are early manifestations of toxicity.

54. Parenteral calcium is used as an antidote for which of the following situations? a. Verapamil overdosesb. Hyperkalemiac. Cocaine intoxicationd. Verapamil overdoses and hyperkalemia

Parenteral calcium is used to reverse the cardiac effects of calcium channel blocker overuse and hyperkalemia.

55. Which of the following antibiotics belong to the ureidopenicillin class of agents?

a. Carbenicillinb. Ticarcillin

c. Piperacillind. Pivampicin

Piperacillin and Mezlocillin are ureidopenicillins.

56. Methotrexate is an/a:

a. Antimetaboliteb. Nitrourea

c. alkylating agentd. antibiotic

57. Which of the following antibiotics reversibly binds to the 50S subunit of the bacterial ribosome?

a. Orimedb. Gerafen

c. Zyvoxd. Inoflox

50S (Macrolide, Chloramphenicol, Clindamycin)• Gerafen is Chloramphenicol • Orimed is Gentamycin(Aminoglycoside)• Zyvox is Linezolid• Inoflox is Ofloxacin (Quinolones)

58. Which of the following new Insulin preparations has a characteristic release pattern that shows no peak and a plateau serum Insulin level that is maintained for about 24 hours?

a. Lantusb. Humalog

c. Apidrad. Novomix 70/30

Lantus is Insulin Glargine “peakless insulin”

59. What is considered as the most common cause of air pollution?

a. Sulfur oxideb. Nitrogen oxide

c. Hydrocarbonsd. Carbon monoxide

60. A diabetic on oral hypoglycemic drug, chlorpropamide, suffered from enteric fever and was prescribed chloramphenicol. He developed severe hypoglycemia. This is because:

a. Chloramphenicol itself has mild hypoglycemic effectb. Chloramphenicol increases the absorption of

chlorpropamidec. Chloramphenicol inhibits the metabolism of

chlorpropamided. Chloramphenicol causes release of insulin

61. Use of Yerba buena:

a. Antisepticb. Mouthwash

c. Analgesicd. Diuretic

62. Use of Quisqualis indica:

a. Intestinal wormb. Lowers blood pressurec. Arthritisd. Antifungal

63. Which of the following is not employed in the treatment of depression?

a. Venlafaxineb. Sertraline

c. Paroxetined. Zolpidem

Zolpidem is used as a sedative hypnotic

64. Lioresal® is used primarily as a/an:

a. Sympathomimeticb. Anti-anxiety

c. muscle relaxantd. Anti-spasmodic

LIORESAL is baclofen

For questions 65-67: A 58-year –old white male who has a history of essential hyper tension and bronchial asthma has recently been diagnosed with prostatic hypertrophy. His medication history includes the following drugs:

65. Which of these agents and uses could worsen the urinary retention he is experiencing as a result of his prostate problems?

a. Propranololb. Ipratropiumc. Metaproterenold. Finasteridee. Prazosin

66. Which agent and use could worsen or cause an acute asthma attack?

a. Propranololb. Ipratropiumc. Metaproterenold. Finasteridee. Prazosin

Because this is a nonselective β-blocker , there could be some inhibit ion of β2 -receptors in the bronchial tree, causing bronchoconstriction and possible complication of the patient 's asthma.

67. Which agent acts selectively at β2 - receptors?

a. Propranololb. Ipratropiumc. Metaproterenold. Finasteridee. Prazosin

• Propranolol is a nonselective β-blocker• Prazosin is a selective α1 -blocker • Neither ipratropium nor Proscar works through the

adrenergic system.

For quest ions 68-70: A 55-year –old black female has a history of moderate hyper tension, glaucoma, and mild osteoarthritis. Her medication history includes the following drugs:

68. Which of her glaucoma medicines acts via an indirect mechanism?

I. MetoprololII. Pilocarpine gelIII. Epinephrine drops

IV. IsoflurophateV. Timolol

a. III onlyb. I and V only c. II and V onlyd. IV onlye. II and IV only

- Pilocarpine acts directly at the muscarinic receptor- Epinephrine and timolol both act directly at β- receptors- Isoflurophate inhibits the metabolism of acetylcholine,

indirectly increasing levels of the endogenous neurotransmitter .

69. Which two agents could have an additive effect to produce excessive bradycardia?

I. MetoprololII. Pilocarpine gelIII. Epinephrine dropsIV. IsoflurophateV. Timolol

Metoprolol , a β1 -selective agent, can cause bradycardia.The addition of topical timolol , while limiting systemic absorption, could have an additive β-blocking effect to decrease hear t rate (negative chronotropy) .

a. III onlyb. I and V onlyc. II and IV onlyd. IV only e. II and V only

70. Which two glaucoma agents could lessen the effects of the other?

I. MetoprololII. Pilocarpine gelIII. Epinephrine dropsIV. IsoflurophateV. Timolol

a. III onlyb. I and V onlyc. II and IV onlyd. IV only e. II and V only

- Pilocarpine and isoflurophate both act via cholinergic receptors- Pilocarpine - acts directly on the receptor- Isoflurophate – indirectly increases acetylcholine levels - Epinephrine - β-agonists- Timolol - β-antagonists

71. A patient on oral anticoagulant therapy is commenced on sulfamethoxaole-trimethoprim, double-strength twice daily. One may expect to see the international normalized ratio:

a. Increaseb. Decrease

c. remain unchangedd. AOTA

72. An unconscious patient is brought into the emergency department. The patient is given 50 mL of 50% dextrose in water, thiamine 100 mg IV, followed by naloxone 1 mg, at which point he awakens. This patient most likely has overdosed on which of the following substances?

a. Amitriptylineb. Cocaine

c. Haloperidold. Heroin

73. Contraindications to the administration of syrup of ipecac include which of the following?a. an unconscious patientb. a patient who is experiencing a generalized tonic-

clonic seizurec. a patient who has ingested a caustic substanced. Al l of the abovee. none of the above

74. Ethyl alcohol (EtOH) is administered to patients who have ingested ei ther ethylene glycol or methanol because EtOH:

a. helps sedate patients.b. increases the metabolism of ethylene glycol and methanol.c. blocks the format ion of the toxic metabolites of ethylene

glycol and methanol.d. increases the renal clearance of ethylene glycol and

methanol .e. is not an antidote for ethylene glycol or methanol overdoses.

75. A 75 year old woman with hypertension is being treated with a thiazide. Her blood pressure responds and reads at 120/76mmHg. After several months on the medication, she complains of being tired and weak. An analysis of the blood indicates low values for which of the following?

a. Calciumb. Potassium

c. Uric acidd. Sodium

Hypokalemia is a common adverse effect of the thiazides and causes fatigue and lethargy in the patient. Calcium, uric acid and glucose are usually elevated by thiazide. The sodium loss does not weaken the patient.

76. Drugs may be considered as chemicals which are not synthesized in the body.

a. Drugsb. Poisons

c. hormonesd. Xenobiotics

77. Symbol for bioavailability

a. Fb. f

c. AUCd. BA

F is the Symbol for bioavailability. BA is abbreviation for it.

78. Extent of absorption of oral drugs as compared to the absorption of a marketed drug product

a. Relative bioavailabilityb. Absolute bioavailabilityc. Peak concentrationd. Max AUC

79. When tissue concentration high, plasma concentration is:

a. Increaseb. Decrease

c. Unchanged. Either A or B

Tissue and plasma concentration are inversely proportional

80. Which of the following pairs is correct in reference to the physical nature of drugs at room temperature?

a. Aspirin – gaseousb. Nitric oxide – solid

c. Nicotine - liquidd. Atropine - liquid

Nicotine is liquid a room temperature. (A) & (D) is solid and (D) is gaseous.

81. Which of the following affects drug activity?

a. Drug sizeb. Physical naturec. Drug reactivity

d. AOTAe. NOTA

82. Reaction of drug to the body.

a. Pharmacodynamicsb. Pharmacokinetics

c. Biopharmaceuticsd. Pharmacology

83. Reaction of body to drug

a. Pharmacodynamicsb. Pharmacokinetics

c. Biopharmaceuticsd. Pharmacology

84. Drugs bound to receptors should bear the following to exert pharmacologic action

a. Affinityb. Intrinsic action

c. AOTAd. A only

(A) & (B) are required for drugs to exert effect. Affinity is for attachment to the receptor and intrinsic affinity is for signaling the intended effect of drug.

85. The process by which the drug is engulfed by the cell membrane and carried into the cell by pinching off the newly formed vesicle inside the membrane.

a. Exocytosisb. Endocytosis

c. Membrane permeation

d. Transmembrane transport

86. The passive flux of molecule down a concentration gradient is given by which equation?

a. Fick’s lawb. Henderson-Hasslebach Equationc. Charles’ lawd. Michealis-Menten Equation

87. Rate of diffusion is inversely proportional to which of the following?

a. Surface areab. membrane

thickness

c. Concentrationd. NOTA

88. Which of the following is the membrane receptor for cardioactive digitalis glycosides?

a. Na+/K+ ATPaseb. Na+/ Cl- ATPase

c. K+ ATPased. PO4 ATPase

89. Time to achieve maximum plasma concentration

a. Tmaxb. Cmax

c. Half-lifed. Shelf-life

90. Transduction process that links drug occupancy of receptor and pharmacologic response is termed:

a. Bindingb. Coupling

c. Drug activityd. Drug attachment

91. Volume of distribution is used to:

a. Relate drug amount and plasma concentrationb. Guide to know if the drug is free or bound to

plasma proteinsc. AOTAd. B Only

Both are possible areas where volume of distribution is used

92. Time it takes for a drug to exert its first observable effect.

a. Onsetb. Duration

c. MECd. MTC

93. All exist in the gastric gland, except;

a. Mucous secreting cellsb. Chief cells

c. Parietal cellsd. NOTA

All exist in the gastric glands and aids in the possible metabolism of drugs

94. Metabolism of the following drugs is delayed with food, except;

a. Cephalexinb. K+ ion

c. Propranolold. Acetaminophen

Food increases propranolol absorption

95. Which of the following can be done if dissolution is slow, except;

a. Use saltsb. Use pH controlc. use crystalline solidsd. use rapidly dissolving polymorph

Instead of crystalline use AMORPHOUS solids

96. Which of the following is given with food to reduce irritation?

a. Iron saltsb. NSAIDS

c. AOTAd. NOTA

Both and erythromycin as well are given with food to reduce irritation

97. Drugs that interact with solvents forming crystals.

a. Solvatesb. Solvates

c. Liquid Crystalsd. Poly morphs

98. The equation which was developed from the observation of dissolution behaviour of solids in solvents systems

a. Noyes-Whitmann equation b. Noyes-Whatmann equationc. Noyles-Whitney equationd. Noyes-Whitney equation

Definition of Noyes-Whitney equationDc/dt = KDS/ h (Cs-C)

Where: K =disso constantD=diffusion rateS= surface areah=thickness of diffusion stagnant layerCs= conc at diffusion/stagnant layerC=conc at bulk solvent

99. In dissolution systems, increase agitation result to?a. Reduce thickness of stagnant layerb. Decrease dissolutionc. No effectd. Either A or B

Increase dissolution and decrease thickness of stagnant layer

100. Measured by comparing AUC of oral and IV administration

a. Relative bioavailabilityb. Absolute bioavailabilityc. Peak concentrationd. Max AUC

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