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. Anticholinergic b. Digoxin c. Levodopa d. Propantheline 2. Histabloc® is a: a. H1 agonist b. H1 antagonist c. H2 agonist d. H2 antagonist Histabloc is Famotidine (H2 antagonist) 3. Schilling test is used for the detection of: a. b. c. d. Pernicious anemia Megaloblastic anemia Iron deficiency anemia 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: a. Atropine overdose b. Myasthenia gravis c. Bronchial asthma d. COPD Tacrine, Donepezil, Rivastigmine and Galantamine, all of which are anticholinesterase are indicated for Alzheimer’s Disease 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 asthma c. shock d. Acute Renal failure Obesity as beta-3 receptor plays in lipolysis 6. Among diabetic patients using insulin or oral hypoglycemic agents (OHAs), why are betablockers used with special caution if not totally avoided? a. Beta- blocker can induce hyperglycemia b. Beta-blocker can mask hypoglycemic symptoms c. Beta-blocker can attenuate effect of insulin and OHAs d. 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? a. IP3 b. cAMP c. ATP d. cGMP IP3, leading to an increase in intracellular calcium 8. In schizophrenic syndrome there is primarily: a. b. c. d. Decreased cholinergic activity Decreased dopaminergic activity Increased dopaminergic activity Increased cholinergic activity •psychosis and schizophrenia - abnormally high dopaminergic transmission •Parkinson’s disease - decreased dopamine activity 9. Chloramphenicol can cause: a. Diarrhea b. Blindness c. emesis d. bone marrow depression 10. A broad spectrum gram-negative cephalosporin: a. Cefalexin b. Cefotaxime c. Cefamandole d. AOTA Cefotaxime – 3rd generation cephalosporins have a broad spectrum of activity and further increased activity against Gram-negative organisms Cefamandole – second generation Cefalexin-first generation 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. b. c. d. Degradation by COMT Sequestration into cells Degradation by MAO 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 stimulation b. Alpha-2 stimulation c. Beta-1 stimulation d. Beta-2 stimulation 13. In combination therapy for tuberculosis, the following are commonly administered orally EXCEPT: a. Ethambutol b. INH c. Streptomycin d. Rifampicin Streptomycin - IM 14. Furosemide is useful for the treatment of all the following EXCEPT: a. b. c. d. Acute pulmonary edema Hypertensive crisis Hypoglycemia Congestive heart failure 15. What is the dominant adrenergic receptor in the heart? a. Alpha – 1 b. 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. Phenylephrine b. Reserpine c. Methyldopa d. Amlodipine 17. In the adrenal medulla, Norepinephrine is converted to epinephrine by the action of which enzyme? a. b. c. d. DOPA decarboxylase Phenylethylamine N-methyl transferase COMT MAO 18. At what dose should Dopamine be given as IV infusion to produce a predominantly dopaminergic effect? a. b. c. d. 0.5 – 5 ug/kg/min 5-10 ug/kg/min 10-20 ug/kg/min 20-50 ug/kg/min 19. Prolonged therapeutic administration of cortisone induces: a. b. c. d. Hypoglycemia Hypofunction of the adrenal cortex Hyperfunction of the pituitary gland 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. Isoflurane b. Sevoflurane c. Halothane d. Desflurane 22. Anaphylactoid reaction may be seen as a side effect with which of the following neuromuscular blockers? a. Pancuronium b. Vecuronium c. Tubocurarine d. Rocuronium Tubocurarine induces a non-immune mediated histamine release by mast cells which can manifest as an anaphylaxis like reaction 23. This can decrease gastric emptying time: a. Stress b. Metoclopramide c. None of these d. Vigorous exercise Stress – increase stomach contractions and emptying rate Metoclopramide – gastroprokinetic agent 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/ml b. >150 ng/ml c. >10 ng/ml d. >2 ng/ml 26. The drug of choice in the treatment of arrhythmia caused by digitalis intoxication: a. Methyldopa b. Phenytoin c. Hydralazine d. Phenylephrine 27. Inotropic activity of the heart in congestive heart failure can be increased by which of the following agents? I. Bipyridines II. ACE inhibitors III. Beta-1 Agonist a. b. c. d. e. I only II only I and III II and III I, II and III 28. Which of the following anti-arrhythmic agents has been associated with lupus-like side effect? a. Quinidine b. Lidocaine c. Amiodarone d. Procainamide 29. Which of the following calcium channel blocker is most useful in arrhythmia therapy? a. Verapamil b. Diltiazem c. Nifedipine d. Lidocaine Verapamil is the ONLY CCB with proven clinical role in arrhythmia therapy 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. Prazosin b. Amlodipine c. Metoprolol d. HCTZ Chinese patients are most likely to be more sensitive to the effects of beta blocker 31. Which of the following benzodiazepines has the shortest half-life and a rapid onset of action? a. Lorazepam b. Triazolam c. Oxazepam d. Diazepam Triazolam and Midazolam have the shortest halflives with a rapid onset of action 32. Which of the following findings in a patient taking Phenytoin would warrant reduction in the dose? a. Gingival hyperplasia b. Nystagmus c. Osteomalacia d. Ataxia Ataxia and diplopia are early manifestations of toxicity 33. Which of the following drugs for seizure is metabolized to yield Phenobarbital? a. Lamotrigine b. Vigabatrin c. Primidone d. Topiramate Phenobarbital is one of the two active metabolites of Primidone 34. When Phenytoin is given intravenously, what is the maximum rate by which the drug can be administered? a. 10mg/min b. 20mg/min c. 30mg/min d. 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. b. c. d. A selective MAO-A inhibitor A selective MAO-B inhibitor A Dopamine-3 receptor agonist 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. Levodopa b. Bromocriptine c. Selegeline d. Entacapone 37. What type of protein is primarily targeted by Digitalis glycosides when they exert their effect on the heart? a. Receptor b. Ion channels c. transporters d. 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. b. c. d. Enterohepatic recirculation Gastric emptying First pass effect Enzyme induction 39. What neurotransmitter is released by the preganglionic fibers as a response to sympathetic stimulation? a. Acetylcholine b. Norepinephrine c. Serotonin d. 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. Furosemide b. HCTZ c. Spironolactone d. 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. Losartan b. Nifedipine c. Prazosin d. 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. Phenylalanine b. Glycine c. Tyrosine d. Tryptamine Tryptamine for 5HT/Serotonin 43. Which of the following beta-blockers is cardioselective? a. Labetalol b. Propranolol c. Pindolol d. Esmolol BEAM = Bisoprolol, Esmolol, Atenolol, Metoprolol 44. Bethanechol is clinically used for which of the following conditions? a. b. c. d. Urinary retention in neurogenic bladder Intestinal obstruction Chronic glaucoma 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. Constipation b. Mydriasis c. Emesis d. 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. b. c. d. Mydriatics Cycloplegic agents Relaxant of bronchial smooth muscles Inhibitors of involuntary muscle contractions e. 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. Prazosin b. Metoprolol c. HCTZ d. 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. Indomethacin b. Ibuprofen c. Mefenamic acid d. 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. b. c. d. INH Bacillus calmette guerine vaccine Ethambutol Streptomycin 50. Which of the following agents is a strong full agonist of opioid receptors? a. Hydromorphone b. Propoxyphene c. Hydrocodone d. 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. b. c. d. Protime Platelet count Activated Partial thromboplastin time Bleeding time 52. Which of the following benzodiazepines has the shortest half-life and a rapid onset of action? a. Lorazepam b. Triazolam c. Oxazepam d. 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 hyperplasia b. Nystagmus c. Ataxia d. 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 overdoses b. Hyperkalemia c. Cocaine intoxication d. 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. Carbenicillin b. Ticarcillin c. Piperacillin d. Pivampicin Piperacillin and Mezlocillin are ureidopenicillins. 56. Methotrexate is an/a: a. Antimetabolite b. Nitrourea c. alkylating agent d. antibiotic 57. Which of the following antibiotics reversibly binds to the 50S subunit of the bacterial ribosome? a. Orimed b. Gerafen c. Zyvox d. 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. Lantus b. Humalog c. Apidra d. Novomix 70/30 Lantus is Insulin Glargine “peakless insulin” 59. What is considered as the most common cause of air pollution? a. Sulfur oxide b. Nitrogen oxide c. Hydrocarbons d. 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 effect b. Chloramphenicol increases the absorption of chlorpropamide c. Chloramphenicol inhibits the metabolism of chlorpropamide d. Chloramphenicol causes release of insulin 61. Use of Yerba buena: a. Antiseptic b. Mouthwash c. Analgesic d. Diuretic 62. Use of Quisqualis indica: a. b. c. d. Intestinal worm Lowers blood pressure Arthritis Antifungal 63. Which of the following is not employed in the treatment of depression? a. Venlafaxine b. Sertraline c. Paroxetine d. Zolpidem Zolpidem is used as a sedative hypnotic 64. Lioresal® is used primarily as a/an: a. Sympathomimetic c. muscle relaxant b. Anti-anxiety d. 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. b. c. d. e. Propranolol Ipratropium Metaproterenol Finasteride Prazosin 66. Which agent and use could worsen or cause an acute asthma attack? a. Propranolol b. Ipratropium c. Metaproterenol d. Finasteride e. 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. b. c. d. e. Propranolol Ipratropium Metaproterenol Finasteride 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. II. III. IV. V. Metoprolol Pilocarpine gel Epinephrine drops Isoflurophate Timolol a. b. c. d. e. III only I and V only II and V only IV only 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. II. III. IV. V. Metoprolol Pilocarpine gel Epinephrine drops Isoflurophate Timolol a. b. c. d. e. III only I and V only II and IV only IV only II and V only 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) . 70. Which two glaucoma agents could lessen the effects of the other? I. II. III. IV. V. Metoprolol Pilocarpine gel Epinephrine drops Isoflurophate Timolol a. b. c. d. e. III only I and V only II and IV only IV only 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. Increase b. Decrease c. remain unchanged d. 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. Amitriptyline b. Cocaine c. Haloperidol d. Heroin 73. Contraindications to the administration of syrup of ipecac include which of the following? a. an unconscious patient b. a patient who is experiencing a generalized tonicclonic seizure c. a patient who has ingested a caustic substance d. Al l of the above e. 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. Calcium b. Potassium c. Uric acid d. 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. Drugs b. Poisons c. hormones d. Xenobiotics 77. Symbol for bioavailability a. F b. f c. AUC d. 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. b. c. d. Relative bioavailability Absolute bioavailability Peak concentration Max AUC 79. When tissue concentration high, plasma concentration is: a. Increase b. Decrease c. Unchange d. 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 – gaseous c. Nicotine - liquid b. Nitric oxide – solid d. 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 size b. Physical nature c. Drug reactivity d. AOTA e. NOTA 82. Reaction of drug to the body. a. Pharmacodynamics c. Biopharmaceutics b. Pharmacokinetics d. Pharmacology 83. Reaction of body to drug a. Pharmacodynamics c. Biopharmaceutics b. Pharmacokinetics d. Pharmacology 84. Drugs bound to receptors should bear the following to exert pharmacologic action a. Affinity b. Intrinsic action c. AOTA d. 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. Exocytosis b. Endocytosis c. Membrane permeation d. Transmembrane transport 86. The passive flux of molecule down a concentration gradient is given by which equation? a. b. c. d. Fick’s law Henderson-Hasslebach Equation Charles’ law Michealis-Menten Equation 87. Rate of diffusion is inversely proportional to which of the following? a. Surface area b. membrane thickness c. Concentration d. NOTA 88. Which of the following is the membrane receptor for cardioactive digitalis glycosides? a. Na+/K+ ATPase b. Na+/ Cl- ATPase c. K+ ATPase d. PO4 ATPase 89. Time to achieve maximum plasma concentration a. Tmax b. Cmax c. Half-life d. Shelf-life 90. Transduction process that links drug occupancy of receptor and pharmacologic response is termed: a. Binding b. Coupling c. Drug activity d. Drug attachment 91. Volume of distribution is used to: a. Relate drug amount and plasma concentration b. Guide to know if the drug is free or bound to plasma proteins c. AOTA d. 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. Onset b. Duration c. MEC d. MTC 93. All exist in the gastric gland, except; a. Mucous secreting cells b. Chief cells c. Parietal cells d. 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. Cephalexin b. K+ ion c. Propranolol d. Acetaminophen Food increases propranolol absorption 95. Which of the following can be done if dissolution is slow, except; a. b. c. d. Use salts Use pH control use crystalline solids use rapidly dissolving polymorph Instead of crystalline use AMORPHOUS solids 96. Which of the following is given with food to reduce irritation? a. Iron salts b. NSAIDS c. AOTA d. NOTA Both and erythromycin as well are given with food to reduce irritation 97. Drugs that interact with solvents forming crystals. a. Solvates b. Solvates c. Liquid Crystals d. Poly morphs 98. The equation which was developed from the observation of dissolution behaviour of solids in solvents systems a. b. c. d. Noyes-Whitmann equation Noyes-Whatmann equation Noyles-Whitney equation Noyes-Whitney equation Definition of Noyes-Whitney equation Dc/dt = KDS/ h (Cs-C) Where: K =disso constant D=diffusion rate S= surface area h=thickness of diffusion stagnant layer Cs= conc at diffusion/stagnant layer C=conc at bulk solvent 99. In dissolution systems, increase agitation result to? a. b. c. d. Reduce thickness of stagnant layer Decrease dissolution No effect Either A or B Increase dissolution and decrease thickness of stagnant layer 100. Measured by comparing AUC of oral and IV administration a. b. c. d. Relative bioavailability Absolute bioavailability Peak concentration Max AUC €$