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Organic Pharmaceutical Chemistry

B 1. The ratio of disinfectant to the dilution of phenol required to kill a given strain of the bacterium Salmonella
typhi:
a. Phenol number b. Phenol coefficient c. Phenol value d. None of the above

C 2. The generic name of Nizoral:


a. Meconazole b. Clotrimazole c. Ketoconazole d. Potassium sorbate

C 3. Sulfonamides used for burn therapy:


a. Mafenide b. Silver sulfadiazine c. both a and b d. none of the preceeding

A 4. The following are preservatives except:


a. undecylenic acid b. Methyl paraben c. benzoic acid d. potassium sorbate

C 5. The combination of trimethoprim and sulfamethoxazole is also known as:


a. clotrimazole b. miconazole c. co-trimoxazole d. cotrimazine

B 6. A polyene anti-fungal antibiotic:


a. Griseofulvin b. Nystatin c. Salicylic acid d. Econazole

A 7. Benzyl penicillin is also known as:


a. Penicillin G b. Penicillin V c. Oxacillin d. Ampicillin

D 8. First generation urinary tract anti-infective:


a. salicylic acid b. Griseofulvin c. Norfloxacin d. Nalidixic acid

A 9. A fluoroquinolone:
a. Norfloxacin b. Pipemedic acid c. Methenamine d. none of the above

D 10. Combination therapy in the treatment of tuberculosis contain the following drugs, except:
a. Ethambutol b. Rifampin c. Isoniazid d. Streptomycin

B 11. These drugs are used in treatment of amoebic dysentery, except:


a. Tinidazole b. Chloroquine c. Etofamide d. Metronidazole

B 12. A fourth generation cephalosphorins:


a. Cefaloxin b. Cefepime c. Cefamandole d. Cefuroxime

C 13. This drug is used in the treatment of chicken pox:


a. Zidovudine b. Chloroquine c. Acyclovir d. Metronidazole

A 14. The drug of choice for typhoid fever:


a. Chloramphenicol b. Lincomycin c. Penicillin d. Cephalosporins

D 15. The generic name of Dalacin C which is often used to treat pimples:
a. Erythromycin b. Tetracycline c. Lincomycin d. Clindamycin

B 16. The study of chemical agents which are selectively more toxic to the invading organisms than the host:
a. therapeutics b. chemotherapy c. organic chemistry d. biochemistry

C 17. Compounds that kill or prevent the growth of microorganisms when applied to living tissues:
a. disinfectant b. fungicides c. antiseptics d. systemic anti-infectives

A 18. A combination of non-ionic and cationic surfactants with iodine:


a. Povidone-Ioduine b. Strong I2 solution c. Iodine Tincture d. I2 in KI solution

D 19. The generic name of new Merthiolate is:


a. Chorhexidine gluconate c. Mexachlorophene
b. Thimerosal d. Benzalkonium chloride

B 20. Mechanism of action of quinolones:


a. injury to plasma membrane c. protein synthesis inhibition
b. inhibition of DNA gyrase d. production of toxic free radicals

B 21. Prodrugs of active anti-malarial metabolites, the dihydrotriazines:


a. quinolines b. biguanides c. beta-lactams d. quinolones

A 22. 7 chloro-7-deoxy lincomycin:


a. clindamycin b. roxithromycin c. spectinomycin d. ilotycin

D 23. The drug is effective against both exoerythrocytic and erythrocytic forms of malaria:
a. chloroquine b. quinine c. amodiaquine d. cycloguanil

B 24. Newest and most potent quinoline derivative for malaria:


a. amodiaquine b. mefloquine c. atabrine d. daraprim

B 25. An aromatic diamide derivative used for sleeping sickness:


a. suramin b. pentamidine c. efflornithine d. stibophen

A 26. Methylated erythromycin:


a. clarithromycin b. azithromycin c. lincomycin d. ilotycin

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Organic Pharmaceutical Chemistry
B 27. A semi-synthetic aminoglycoside whose structural prototype is kanamycin:
a. Kantrex b. Amikin c. Garamycin d. Nebcin

A 28. Structural congener of Symmetrel which is used for viral influenza:


a. ribavirin b. rimantadine c. gancyclovir d. foscarnet

A 29. More potent optical isomer of ofloxacin:


a. levo b. dextro c. cis isomer d. trans isomer

B 30. These group of drugs share the same mechanism of action as that of sulfanilamide but are less effective:
a. trimethoprim b. sulfones c. quinolones d. none of the above

B 31. Mechanism of action of thiabendazole:


a. paralysis due to GABA receptor occupation c. phagocytic attack on worms
b. inhibition of cell division d. decreased glucose uptake

B 32. This anti-burn therapy causes systemic acidosis:


a. silvadene b. sulfamylon c. whitfield d. vandol

C 33. Drug of choice for filarial infections:


a. ivermectin c. diethylcarbamazine
b. praziquantel d. Stibophen

B 34. Active form of the sulfonamide:


a. non-ionized b. ionized c. amphoteric d. oxo ring

B 35. Use of crotamiton:


a. pediculicide b. scabicide c.anthelmintic d. antibacterial

C 36. Mechanism of action of mebendazole:


a. paralysis due to excessive loss of calcium c. decreased glucose uptake
b. unknown mechanism of action d. phagocytic attack on worms

D 37. A sympathomimetic agent that bind to alpha receptors found centrally that cause suppression of appetite:
a. Xenical b. Gas-X c. Apokinon d. Adifax

B 38. An example of a glycine conjugation pathway:


a. phenol to phenolsulfate c. noradrenaline to epinephrine
b. benzoic acid to hippuric acid d. antabuse to dithiocarbamic acid

B 39. The following are characteristics of active transport, except:


a. follow saturation kinetics c. carrier mediated
b. expenditure of energy d. higher to lower concentration gradient

B 40. These anti-diarrheals tend to decrease pore sizes of GIT epithelial to prevent formation of watery stools:
a. adsorbents b. astringents c. anti-motility d. oresols

C 41. This anti-histamine possesses the same indications as that of diphenhydramine:


a. meclizine b. hyoscine c. dimenhydrinate d. celestamine

A 42. The metabolism of warfarin is induced by the following except:


a. tolbutamide b. haloperidol c. nitroglycerine d. DDT

C 43. Fertility vitamins:


a. retinoic acid b. riboflavin c. alpha tocopherol d. biotin

C 44. Calcitriol, a hormone responsible for enhanced absorption of calcium from the intestines, is synthesized
from:
a. calcitonin b. vitamin D2 c. vitamin D3 d. caltrate

A 45. A metabolite of chloral hydrate:


a. trichloroacetic acid b. acetaldehyde c. carbapenem ring d. phenacetone

A 46. A sample drug excreted via the saliva:


a. lidocaine b. sulfonamide c. sulfonamide d. thiamine

B 47. A vitamin A derivative used in the management of psoriasis:


a. Retin-A b. Tegison c. Accutane d. Oilatum

B 48. Structurally specific drugs are those whose activity depends on:
a. physical characteristics c. both a and c
b. ability to bind on a specific receptor d. none of the above

A 49. The most potent anti-bacterial alcohol:


a. primary b. secondary c. tertiary d. quaternary

A 50. Product of acid hydrolysis of penicillins:


a. penicillenic acid b. penicilloic acid c. penicilloate Cl d. pinecillic acid

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Organic Pharmaceutical Chemistry
B 51. Cidex:
a. gammabenzenehexachloride c. hexachlorophene
b. glutarol d. carbamoyl phosphate

B 52. Presence of electron withdrawing groups attached to the alpha carbon of the amide side chain in penicillins
render:
a. activity against Pseudomonas c. activity against Gram (-) bacteria
b. acid stability d. penicillinase resistance

D 53. Attachment of bulky groups to the alpha carbon of the amide side chain in penicillins render:
a. activity against Pseudomonas c. activity against Gram (-) bacteria
b. acid stability d. penicillinase resistance

B 54. A glycopeptide antibiotic:


a. beta-lactam b. vancomycin c. polymyxin d. probenecid

C 55. A tumor is benign if:


a. metastasis is evident
b. cell originating from the tumor may invade other tissues and cause damage
c. tumor mass may be removed by surgery and regression of remaining cells occur
d. cause damage to surrounding structures

B 56. 1 gram mass of tumor is equivalent to:


a. 100,000 cancer cells b. 1 billion cancer cells c. 1 million cancer cells d. none of the above

C 57. The following are mucolytics, except:


a. bromhexine b. acetylcysteine c. caramiphen d. none of the above

C 58. The side effects of steroids used for asthma are minimized when the drug is given:
a. orally b. intravenously c. via inhalation d. rectally

B 59. A progesterone derivative which is used for the treatment of endometrial cancer:
a. tamoxifen b. depo-provera c. flutamide d. goserelin

B 60. Drug of choice for absence seizures:


a. carbamazepine b. ethosuximide c. phenytoin d. primidone

C 61. An anti-oxidant added in food products which are potent carcinogens:


a. aspartame b. PCP c. BHT d. EDTA

A 62. Pentavalent antimony in the presence hydrochloric acid gives a violet precipitate with this pink dye:
a. rhodomine B c. p-nitrobenzene azo-resorcinol
b. aluminum reagent d. dimethylglyoxime

C 63. Expectorant obtained from the phenol volatile oil of Fagus grandiflora:
a. potassium iodide b. tyloxapol c. guaiafenesin d. emetine

B 64. Mescaline is a _________ derivative:


a. indolethylamine b. phenylethylamine c. steroidal d. xanthine

D 65. Anesthetic of choice for labor:


a. halothane b. enflurance c. nitrous oxide d. methoxyflurane

B 66. The drug of choice for the acute attack of migraine:


a. Codeine b. Avamigran c. Litec d. Inderal

C 67. Anesthetic of choice for patients with asthma:


a. ketamine b. thiopental c. enflurane d. none of the above

D 68. Propionic acid derivative:


a. paracetamol b. dipyrone c. piroxicam d. naproxen

B 69. An example of iodophor:


a. iodine tincture b. povidone-iodine c. Lugol’s solution d. all of the above

B 70. Phenylmethanol:
a. chloretone b. benzyl alcohol c. phenylalcohol d. carvacrol

A 71. A characteristic of cancer cells:


a. lack of normal growth controls c. G0 phase is the resting phase for all cell types
b. synthesis of DNA occurs in the M phase d. None of the above

A 72. Carcinogenic substances obtained from paper products:


a. polychlorinated biphenyls c. butylatedhydroxyanisole
b. acesulfame d. none of the above

C 73. Prostaglandins are also known as:


a. saturated fats b. compound lipids c. eicosanoids d. all of the above

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Organic Pharmaceutical Chemistry
C 74. Which of the following functional groups is the most basic?
a. imide b. amide c. amine d. aniline

A 75. Derivatives of benzylsulfonylureas are:


a. oral hypoglycemics b. diuretics c. anti-inflammatory d. spasmolytic

D 76. A necessary precursor of visual pigment is:


a. tocopherol b. retinal c. ergosterol d. retinal

C 77. Paracetamol is a/an:


a. salicylate b. pyrazolone c. aniline derivative d. azocine derivative

B 78. All of the following are progestins except:


a. norethindrone b. testosterone c. ethynodiol diacetate d. progesterone

C 79. Aspirin is to salicylic acid as morphine is to:


a. codeine b. methadone c. heroin d. pentazocine

A 80. The functional group in pyridoxine is:


a. alcohol b. amine c. carboxylic acid d. ketone

A 81. Ascorbic acid and tetracycline are:


a. enols b. esters c. ethers d. amines

C 82. MAO is classified as a/an:


a. protein inhibitor b. complexing agent c. enzyme d. hormone

C 83. When used in pharmaceutic preparations, the purpose of hydroquinone, lecithin and alpha tocopherol is:
a. humectant c. oil soluble antioxidant
b. demelanizing agent d. emulsifying agent

D 84. Naturally occurring alkaloids, derivatives of tropane are:


a. nasal decongestants b. analgesic c. vasoconstrictor d. bronchodilator

A 85. Local anesthetics that is not a derivative of benzoic acid is:


a. lidocaine b. procaine c. dibucaine d. bupivacaine

C 86. All of the following are macrolide antibiotics, except:


a. erythromycin b. oleandomycin c. vancomycin d. spiramycin

B 87. Ativan has this generic name:


a. triazolam b. lorazepam c. flurazepam d. tranexamic acid

B 88. Plasil is:


a. acyclovir b. metoclopramide c. diclofenac sodium d. tranexamic acid

C 89. The principal hydrolytic degradation product of aspirin is:


a. methyl salicylate b. acetyl chloride c. salicylic acid d. salicylamide

D 90. Barbiturates containing a sulfur atom are usually:


a. short acting b. intermediate acting c. long acting d. ultra short acting

D 91. Although the prostaglandins are hormone-like, they may closely resemble which of the following
chemically?
a. enzymes b. porphyrins c. proteins d. lipids

A 92. The onset and duration of barbiturate action is mainly a function of its:
a. lipid solubility c. plasma binding
b. renal excretion d. method of administration

B 93. The prototype narcotic antagonist is:


a. nalorphine b. naloxone c. levallorphan d. meperidine

D 94. Lysergic acid diethylamide is:


a. derived from mushroom c. histamine analog
b. a parasympathetic drug d. ergot derivative

B 95. Orthohydroxybenzoic acid is:


a. acetic acid b. salicylic acid c. oxalic acid d. citric acid

B 96. Diamox has a generic name of:


a. allopurinol b. acetazolamide c. dimethylxanthine d. theophylline

C 97. Diphenoxylate is a structural analog of:


a. dilantin b. codeine c. meperidine d. naloxone

B 98. Cevitamic acid is:


a. folic acid b. ascorbic acid c. nicotinic acid d. glacial acetic acid

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Organic Pharmaceutical Chemistry
B 99. Chloroquine is the generic name of:
a. atabrine b. artane c. aralen d. akineton

D 100. Kantrex belongs to this type of antibiotics:


a. penicillins b. cephalosphorins c. macrolides d.. aminoglycosides

B 101. Epinephrine is also known as:


a. tocopherol b. adrenalin c. emetine d. levarterenol

C 102. 1,3-dimethylxanthine is:


a. caffeine b. theobromine c. theophylline d. aminophylline

C 103. Of the following penicillin congeners, the one with the broadest spectrum of action is:
a. pen V b. methicillin c. carbenicillin d. oxacillin

C 104. Zantac is:


a. cimetidine b. famotidine c. ranitidine d. nizatidine

B 105. Cytotec is:


a. sucralfate b. misoprostol c. omeprazole d. pirenzepine

B 106. Ma huang is a/an:


a. imidazole alkaloid b. alkaloidal amine c. purine d. steroidal alkaloid

B 107. Procaine is a/an:


a. amine b. ester c. alcohol d. ketone

D 108. The functional group found in codeine and scopolamine is a/an:


a. amine b. alcohol c. ester d. ether

C 109. Aureomycin is:


a. kanamycin b. erythromycin c. chlortetracycline d. oxytetracycline

A 110. Bonamine is:


a. meclizine b. dramamine c. scopolamine d. aspirin

C 111. Polyene antibiotics include:


I. nystatin II . amphotericin B III. Griseofulvin
a. I only b. III only c. I and II d. II and III

A 112. Among the three xanthines, it is drug of choice for obtaining a stimulating effect of the CNS.
a. caffeine b. theophylline c. theobromine d. all of the above

D 113. A polysaccharide that is used as plasma expander is:


a. starch b. insulin c. dextrose d. dextran

B 114. The combination type oral contraceptive pill contains:


a. an androgen and a progestin c. an androgen and an estrogen
b. an estrogen and progestin d. FSH and LH

B 115. Simethicone is chemically classified as a/an:


a. wax b. silicone c. sulfur d. ketone

C 116. An acidifying agent employed in effervescent salts and refrigerant drinks:


a. acetic acid b. lactic acid c. tartaric acid d. citric acid

D 117. This is an analgesic agent that is used to lessen severity of labor pains in obstetrics:
a. colchicines b. codeine c. apomorphine d. Demerol

B 118. Benzaldehyde is synthetic:


a. cinnamon oil b. bitter almond oil c. corn oil d. rose oil

B 119. The ring common among penicillins and cephalosphorins:


a. benzene ring b. B-lactam ring c. thiazole ring d. phenothiazone

C 120. Retin-A is:


a. alltoin b. adapalene c. tretinoin d. benzoyl peroxide

A 121. Barbiturates with an intermediate duration of action:


a. amorbital b. Phenobarbital c. pentobarbital d. secobarbital

B 122. Vitamin C is extremely important in wound healing. Its principal effect is on the:
a. maturation of osteoblast c. reduction of inflammation
b. collagen formation d. epithelial proliferation

E 123. CNS depressants with skeletal muscular relaxant property, except:


a. Methacarbamol, USP c. Baclofen e. Meprobamate
b. Carisoprodol, USP d. Buspirone

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Organic Pharmaceutical Chemistry
C 124. The drug of choice for the treatment of genital herpes being potent against DNA formation:
a. Symmetrel b. Herplex c. Acyclovir d. Vidarabine

A 125. The drug most effective against malarial parasites in the liver but not effective against parasites within
erythrocytes:
a. primaquine b. pyrimethamine c. quinacrine d. chloroquine

B 126. Feldene is:


a. sulindac b. piroxicam c. indomethacin d. ketoprofen

C 127. Voltaren is:


a. acemetacin b. ibuprofen c. diclofenac d. naproxen

C 128. Depo-Provera is:


a. cyproterone acetate c. medroxyprogesterone acetate
b. nandrolene decanoate d. leuproreline acetate

B 129. Which of the following actions of histamine is not blocked by H1 antagonist:


a. increase in salivary excretion c. vasodilation
b. increase in gastric secretions d. itchiness

A 130. Opium is an example of:


a. narcotic analgesic c. antipyretic analgesic
b. non-steroidal analgesic d. anti-inflammatory analgesic

D 131. Which of the following penicillin derivatives is both acid-stable and resistant to penicillinase?
a. methicillin c. ampicillin e. phenoxymethyl penicillin
b. disodium carbenicillin d. oxacillin

B 132. A diuretic that will manifest a competitive inhibition of the action of aldosterone:
a. Triamterene b. Spirinolactone c. Furosemide d. Chlorothiazide

A 133. Sulfonamides are metabolized by humans principally by:


a. acetylation c. oxidation e. methylation
c. deamination d. conjugation

A 134. Streptomycin and other aminoglycoside antibiotics are:


a. ototoxic c. hyperglycemic e. goiterogenic
b. carcinogenic d. hepatotoxic

D 135. Benzalkonium chloride is a germicidal surfactant which rendered inactive in the presence of:
a. organic acid c. cationic surfactants e. inorganic salts
b. gram-negative organisms d. soaps

B 136. Acetazolamide (Diamox) is rarely the drug of choice for diuretic therapy because it:
a. is too potent
b. causes systemic acidosis and alkaline urine
c. is habit forming
d. does not exhibit tachyphylaxis
e. induces enzymes, especially carbonic anhydrases

C 137. The antipsychotic drug loxapine succinate (Loxitane) is a _____ compound:


a. phenothiazine c. dibenzoxazepine e. butyrophenone
b. benzodiazepine d. thioxanthene

B 138. Diphenoxylate (Lomotil) is an agent useful in the treatment of diarrhea. It is structurally similar to:
a. kaolin c. diphenhydantoin e. oxalic acid
b. meperidine d. pectin

A 139. Which of the following is classified as a broad-spectrum antibiotic?


a. ampicillin c. sodium methicillin e. potassium phenethicillin
b. penicillin G d. sodium cloxacillin

B 140. An antimanic agent:


a. haloperidol b. lithium salts c. LSD d. phenol

A 141. Liquefied phenol, USP:


a. phenol containing 10% water c. carbol-fuchsin solution
b. phenol as surgical antiseptic d. treatment of tinea infection

B 142. Castellani’s paint:


a. phenol containing 10% water c. phenol as surgical antiseptic
b. carbol-fuchsin solution d. antibacterial dye

A 143. This is an effective antidote for the treatment of poisoning by copper:


a. penicillamine b. dimercaprol c. lugol’s solution d. castellani’s paint

B 144. Tetracycline is:


a. an intermediate spectrum, bactericidal c. a broad spectrum, bactericidal
b. a broad spectrum, bacteriostatic d. an intermediate spectrum, bacteriostatic

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Organic Pharmaceutical Chemistry
B 145. Which of the following is not soluble in or miscible with alcohol, USP?
a. ether b. acacia c. methanol d. Phenobarbital e. water

D 146. The drug used in all types of tuberculosis is:


a. ethambutol c. streptomycin e. p-aminosalicylic acid
b. cycloserine d. isoniazid

B 147. Levarterenol (Levophed) is:


a. L-epinephrine c. Isoproterenol e. L-ephedrine
b. L-norepinephrine d. L-dopa

A 148. The most active aminoglycoside against Mycobacterium tuberculosis is:


a. streptomycin c. neomycin e. kanamycin
b. amikacin d. tobramycin

B 149. The most effective agent in the treatment of Rickettsia, Mycoplasma and Chlamydia infection is:
a. penicillin G c. vancomycin e. bacitracin
b. tetracycline d. gentamicin

E 150. Aluminum and calcium salts inhibit the intestinal absorption of which of the following agents?
a. Isoniazid c. Phenoxymethyl penicillin e. Tetracycline
b. Chloramphenicol d. Erythromycin

C 151. Which of the following penicillins is resistant to penicillinase?


a. Polymyxin B c. Dicloxacillin e. Streptomycin
b. Penicillin G d. Carbenicillin

B 152. The quinolone derivative effective against P. Aeruginosa is:


a. norfloxacin c. ofloxacin e. lomefloxacin
b. ciprofloxacin d. enoxacin

B 153. Which of the following penicillins is resistant to penicillinase?


a. Ampicillin c. Carbenicillin e. Mezlocillin
b. Oxacillin d. Ticarticillin

C 154. Rancidity of fats may be due to:


a. reduction to alcohols c. oxidation of double bonds e. hydrogenation
b. impurities d. saponification

A 155. A thiazide diuretic can:


a a. enhance action of amphetamines d. enhance action of oral hypoglycemics
b. antagonize action of guanethidine e. antagonize action of tricyclic antidepressants
b c. antagonize action of digitalis drugs

E 156. Surfactants are characterized by:


a. the presence of water-solubilizing groups d. the presence of fat-solubilizing groups
c b. negative charges e. the presence of water-solubilizing and fat-solubilizing
c. positive charges groups in the same molecule
d
A 157. Piperazine citrate (Antepar), gentian violet, pyrivinium pamoate (Povan) and thiabendazole
(Mintezol) are all:
a. anthelmintics c. antiseptics e. anticholinergics
b. dyes d. scabicides

B 158. AZT or Azidothymidine is used in the treatment of:


a. Koch’s infection b. HIV or AIDS c. carbuncle d. ringworm

A 159. Is a folate-reductase inhibitor:


a. Trimethoprim b. Sulfonamides c. Penicillin d. Tetracycline

B 160. The structure of this class of antibiotic has a beta-lactam ring and a thiazolidine ring.
a. Tazobactam b. Penicillin c. Cephalosporins d. Monobactam

C 161. The generic name of Duracef:


a. Cephradine b. Cephazoline c. Cephadroxil d. Cephalexin

D 162. The preparation is used as pediculicide:


a. Ultralan cream b. Trimycin ointment c. Betronavate ointment d. Kwell lotion

B 163. An antibiotic that is obtained from Streptomyces noursei:


a. Amphotericin B b. Nystatin c. Griseofulvin d. Clindamycin

B 164. The plant containing the anticancer drug, vincristine and vnblastine:
a. Mayapple b. Periwinkle c. European year d. Datura alba

A 165. A very common adverse reaction of alkylating agents used in the treatment of cancer:
a. alopecia b. miosis c. mydriasis d. ataxia

C 166. These are calcium channel blockers, except:


a. Verapamil b. Nifedipine c. Atenolol d. Diltiazem

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Organic Pharmaceutical Chemistry
A 167. The generic name of the brand Diabinese:
a. Chlorpropramide b. Glibenclamide c. Metformin d. Acetohexamide

A 168. A loop or high-ceiling diuretic:


a. Furosemide b. Sorbitol c. Spirinolactone d. Hydrochlorothiazide

A 169. This drug is used as an osmotic diuretic:


a. Mannitol b. Ethanol c. Isopropanol d. Glycitol

D 170. These drugs are narcotic analgesics, except:


a. morphine b. codeine c. nalbuphine d. mefenamic acid

C 171. This is used as an inhalation anesthetic:


a. droperidol b. thiopental c. halothane d. midazolam

B 172. Levodopa is used in the treatment of:


a. leukemia c. Alzheimer’s disease
b. Parkinson’s disease d. Tay Sach’s disease

A 173. The generic name of Nubain:


a. Nalbuphine b. Naloxone c. Pentazocine d. Methadone

D 174. Methenamine is also called:


a. Uridine b. Uracil c. Uric acid d. Urothropin

B 175. Neurotoxicity caused by Isoniazid can be treated with:


a. thiamine b. pyridoxine c. menaquinone d. ergocalciferol

D 176. A broad-spectrum anthelmintic that is effective against a variety of nematode infestations and is the generic
name of Antiox:
a. Piperazine b. Thiabendazole c. Pyrantel pamoate d. Mebendazole

B 177. A common agent in smoking cessation programs providing patches:


a. lobeline b. nicotine c. emetine d. coal tar

C 178. Thiabendazole (Mintezol), a benzimidazole derivative, is an anthelmintic drug used primarily to treat
infections caused by:
a. Ascaris c. Strongyloides e. Taenia saginata (flatworm)
b. Necator americanus (hookworm) d. Enterobios vermicularis

B 179. One of the reasons why aminoglycosides are frequently combined with other antibiotics in treating certain
infections is to:
a. prevent drug infections d. increase oral absorption
b. prevent drug emergence of resistant bacteria e. decrease systemic toxicities
c. increase renal excretion

D 180. Angiotensin-converting enzymes (ACE) inhibitors are associated with a high incidence of which of the
following adverse reactions?
a. hepatitis c. agranulocytosis e. hirsutism
b. hypokalemia d. proteinuria

D 181. Which of the following chemotherapeutic agents has a good penetrability into the cerebrospinal fluid?
a. streptomycin c. tobramycin e. cephalexin
b. gentamicin d. chloramphenicol

C 182. The scientist who can lay claim to the title of Father of Chemotherapy:
a. Robert Koch c. Paul Ehrlich e. Giuseppe Brotzu
b. Joseph Lister d. Alexander Fleming

A 183. Effective administration routes of nitroglycerin for angina pectoris include all of the following, except:
a. oral b. inravenous c. transdermal d. sublingual

A 184. This group is responsible for the bone marrow toxicity of chloramphenicol:
a. NO2 group c. OH group e. benzene group
b. NH2 group d. COOH group

D 185. Diazepam is used in the treatment of all of the following, except:


a. anxiety c. skeletal muscle spasm e. preoperative sedation
b. status epilepticus d. analgesia

E 186. Which is not true regarding ceftriaxone:


a. a 3rd generation cephalosporin c. administered parenterally e. resistant to acid
b. resistant to B-lactamase d. once daily dosing

B 187. All of the following substances are present in opium, except:


a. thebaine c. codeine e. papaverine
b. methadone d. morphine

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Organic Pharmaceutical Chemistry
B 188. An antipyretic aniline derivative with weak anti-inflammatory activity:
a. acetylsalicylic acid c. mefenamic acid e. sulindac
b. acetaminophen d. indomethacin

A 189. The most potent of the inhalation anesthetic agents:


a. methoxyflurane c. enflurane e. isoflurane
b. halothane d. nitrous oxide

C 190. Which of the following antineoplastics is not considered an antimetabolite?


a. methotrexate c. etoposide e. cytarabine
b. thioguanine d. fluorouracil

E 191. Which of the following statements is not true regarding the aminoglycoside antibiotics?
a. they are highly ionized in solution d. they are ototoxic and nephrotoxic
b. they are bactericidal e. they are easily absorbed after oral administration
c. they are more effective in alkaline medium

A 192. Baclofen, a derivative of GABA is used in:


a. spasticity in patients with multiple sclerosis c. management of spasticity in rheumatic disorders
b. parkinsonism d. spasticity of cerebral palsy

C 193. Long term use of tetracyclines in pregnant women should be avoided due to several reasons. Which of
these is not true?
a. they chelate calcium ions
b. they may predispose to discoloration of deciduous teeth in the infant
c. they are toxic to the fetus and may cause abortion
d. they can cause yellow atrophy of the liver in the mother
e e. they get deposited in growing bones

A 194. All of the following antibiotics produce neuromuscular blockade, except:


a. ampicillin c. streptomycin e. amikacin
b. kanamycin d. neomycin

B 195. For the treatment of systemic mycosis, which of the following antifungal agents can be administered by
intravenous route?
a. miconazole c. ketoconazole e. nystatin
b. amphotericin B d. clioquinol

C 196. Which of the following agents is not used for local candidiasis?
a. nystatin c. griseofulvin e. clotrimazole
b. gentian violet d. miconazole

B 197. All of the following are effective and clinically useful against worm infestation caused by Ascaris
Lumbricoides, except:
a. piperazine c. mebendazole e. thiabendazole
b. niridazole d. pyrantel pamoate

C 198. A good local anesthetic should have all of the following properties, except:
a. systemic toxicity should be low
b. effective at body fluid pH
c. onset of anesthesia should be gradual and short duration of action to avoid toxicity
d. must be effective regardless of the site of application
e. not irritant to the tissue and should not cause any permanent structural damage to nerves

D 199. From the list given below, identify the drug possessing “triad of features” which includes antiamebic.
antigiardiasis, and antitrichomonal:
a. iodoquinol c. emetine e. piperazine
b. chloroquine d. metronidazole

A 200. Heparin is a/an:


a. extract of animal tissue c. metal e. enzyme
b. extract of plant d. hormone

B 201. Amongst the following, the drug of choice for acute attack of Plasmodium vivax malaria is:
a. amodiaquine c. primaquine e. mefloquine
b. chloroquine d. quinine

B 202. Drugs which act on erythrocytic cycle of malarial parasite:


a. will be effective for radical cure c. will not be clinically effective
b. will be effective for suppressive prophylaxis d. will both be effective for prophylaxis and radical use

B 203. All statements regarding antipyretic analgesics are false, except:


a. produce fall in blood pressure c. develop drug dependence e. produce general CNS depression
b. raise the pain threshold d. relieve visceral pain

C 204. Drug of choice for ringworm infection is:


a. nystatin c. griseofulvin e. amphotericin B
b. ketoconazole d. neomycin

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Organic Pharmaceutical Chemistry
A 205. Acetaminophen is preferred over aspirin in following conditions, except:
a. rheumatic disease d. children with influenza
b. patients with peptic ulcer e. children with chicken pox
c. patients with bronchial asthma

A 206. Oral neomycin and streptomycin are used for sterilization of bowel and for dysentery because:
a. they are at least absorbed from oral route
b. the peak concentration in blood is achieved quickly
c. they are least toxic to GIT
d. they are destroyed by the gastric juice

D 207. Which of the following is the most appropriate statement about indomethacin?
a. it is a powerful analgesic only
b. it is a power anti-inflammatory only
c. it is only analgesic and anti-inflammatory without antipyretic effect
d. it is a powerful analgesic and anti-inflammatory agent with antipyretic and uricosuric actions
e. it is powerful antipyretic only

B 208. Which of the following is a depot penicillin preparation?


a. phenoxymethylpenicillin c. benzyl penicillin e. methicillin
b. benzathine penicillin d. cloxacillin

B 209. All of the following drugs interfere with platelet activity, except:
a. aspirin c. protamine e. anisindione
b. dimercaprol d. warfarin

C 210. 6-aminopenicillanic acid is:


a. major metabolite of penicillin
b. responsible for development of penicillin resistance
c. the common nucleus of all penicillins
d. a long-acting penicillin
e. minor metabolite of penicillin

A 211. Diphenoxylate, an effective antidiarrheal drug is:


a. related to meperidine c. a narcotic antagonist e. anticholinergic action
b. atropine-like drug d. a ganglion-blocking drug

E 212. Class I antiarrhythmic drugs result in decrease in heart rate of the accelerated heart and usually reduce the
rate of conduction of cardiac impulse. They include the following, except:
a.quinidine c. disopyramide e. amiodarone
b. procainamide d. phenytoin

B 213. Which of the following drugs does not reduce blood cholesterol level?
a. clofibrate c. destrothyroxine e. colestipol
b. epinephrine d. cholestyramine

D 214. Which of the following is the longest-acting nitrate?


a. glyceryl trinitrate c. erythritol tetranitrate e. isosorbide dinitrate
b. amyl nitrite d. pentaerythritol tetranitrate

A 215. Which of the following is considered a primary drug for the treatment of all seizure types except absence?
a. carbamazepine c. valproic acid e. phenobarbital
b. ethosuximide d. diazepam

C 216. Which of the following penicillins is acid stable and therefore orally effective:
a. benzathine penicillin c. cloxacillin e. piperacillin
b. procaine penicillin d. tricarcillin

D 217. A monoamine oxidase inhibitor used as an antidepressant drug:


a. amitryptiline c. clozapine e. fluoxetine
b. thioridazine d. tranylcypromine

D 218. Which of the following is not used for topical application on external surfaces?
a. mafenide c. sodium sulfacetamide e. resorcinol
b. silver sulfadiazine d. sulfisoxazole

B 219. All of the following benzodiazepines are commonly used in the treatment of anxiety, except:
a. chlordiazepoxide c. alprazolam e. diazepam
b. clonazepam d. lorazepam

D 220. Which of the following chemotherapeutic agents is not bactericidal?


a. carbenicillin c. cefuroxime e. vancomycin
b. gentamicin d. erythromycin

D 221. All of the following statements are true concerning the penicillins, except:
a. this class of antibacterials acts by damaging the cell walls of bacteria
b. piperacillin and ticarcillin have activity against Pseudomonas species
c. use of any penicillin is contraindicated in a patient who has had an allergic reaction to any one penicillin
d. they are obtained from the genus of Streptomyces
e. the addition of clavulanic acid to amoxicillin preparations protects the drug from penicillinase

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Organic Pharmaceutical Chemistry
B 222. In choosing a specific benzodiazepine for the treatment of insomnia, all of the following are considerations,
except:
a. age of the patient c. the half life of the drug e. the underlying sleep disorder being treated
b. mental status of the patient d. the absorption of the drug

D 223. An antibiotic most commonly used in topical preparations:


a. clotrimazole c. griseofulvin e. foscarnet
b. vidarabine d. bacitracin

D 224. The preferred agent for hypertensive emergencies:


a. propranolol c. captopril e. sodium nitroprusside
b. clonidine d. diazoxide

C 225. Superior to acyclovir in the treatment of herpes viruses in the CNS in neonates:
a. idoxuridine c. vidarabine e. zidovudine
b. ribavirin d. amantadine

D 226. Which of the following bases is most susceptible to alkylating agents?


a. adenosine c. thymidine e. uridine
b. cytosine d. guanine

A 227. Vincristine is used primarily in the treatment of which of the following?


a. Hodgkin’s disease c. liver cancer e. prostate cancer
b. lung cancer d. melanoma

B 228. For the treatment of systemic mycoses, which of the following antifungal agents can be administered by
intravenous route?
a. miconazole c. ketoconazole e. nystatin
b. amphotericin B d. clioquinol

E 229. Penicillin is the drug of choice for the following infective conditions, except:
a. gonococcal infection d. streptococcal infection
b. pneumococcal infection e. pseudomonal infection
c. treponema pallidum infection

B 230. All of the following drugs act as prodrugs and need to be converted in the body to active compound, except:
a. levodopa c. prednisone e. cyclophosphamide
b. salbutamol d. bacampicillin

C 231. Amongst the following the drug of choice for scabies is:
a. sulfur c. benzyl benzoate e. tannic acid
b. crotamiton d. amodiaquine

D 232. Sensitivity of gram negative bacilli to amoxicillin is due to its:


a. carboxyl group c. hydroxyl group e. carbonyl group
b. nitro group d. amino group

A 233. Bone marrow depression resulting in pancytopenia is the characteristic toxic effect of all the following
drugs, except:
a. oxytetracycline c. methotrexate e. dactinomycin
b. chloramphenicol d. mitomycin

C 234. The following antibiotic possess clinically useful antimalignant property, except:
a. mitomycin c. streptomycin e. plicamycin
b. bleomycin d. daunorubicin

A 235. This is the process utilized by Florey and Chain in isolating penicillin:
a. freeze-drying c. chromatography e. distillation
b. extraction d. x-ray

C 236. The metabolite of the red dye, prontosil, responsible for its antimicrobial property:
a. sulfisoxazole c. sulfanilamide e. sulfapyridine
b. sulfamethoxazole d. sulfacetamide

B 237. Which of the following antiviral agents is not useful for the treatment of herpes virus infection?
a. vidarabine c. trifluridine e. idoxuridine
b. interferon d. acyclovir

B 238. All of the following chemotherapeutic agents are useful for prophylaxis against infections caused by
specific microorganisms, except:
a. amantadine against influenza A virus d. tetracycline against rickettsial infection
b. chloramphenicol against typhoid fever e. pyrimethamine against malaria in endemic areas
c. isoniazid against tubercular infection

E 239. The therapeutic uses of amphetamines does not include which of the following:
a. in hyperkinetic children c. obesity e. hypertension
b. narcolepsy d. parkinsonism

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Organic Pharmaceutical Chemistry
B 240. Nitrous oxide, a general anesthetic agent, is characterized by all of the features of which of the following
groups?
a. high potency, good analgesia, good skeletal muscle relaxation
b. low potency, good analgesia, poor skeletal muscle relaxation
c. high potency, poor analgesia, good skeletal muscle relaxation
d. high potency, good analgesia, poor skeletal muscle relaxation
e. low potency, good analgesia, good skeletal muscle relaxation

D 241. A drug receptor may be all of the following, except:


a. isolable enzyme c. protein or a nucleic acid
b. functional component of a cell membrane d. chelates

B 242. Mechanism of action of trimethoprim:


a. competitive inhibitor for the incorporation of PABA c. inhibits protein synthesis
b. folate reductase inhibitor d. destruction of bacterial cell wall

A 243. A drug molecule which possesses both intrinsic activity and affinity:
a. agonist b. antagonist c. poison d. none of the above

C 244. Chelating agent that is an effective antidote foe copper poisoning and used in the treatment of Wilson’s
disease:
a. deferoxamine mesylate b. dimercaprol c. penicillamine d. EDTA

A 245. Which is not a chelating agent?


a. 8-Methoxyquinoline c. 8-Hydroxyquinoline
b. 8-Mercaptoquinoline d. 4-AZA-Oxime

C 246. Dimercaprol is also known as:


a. BAL b. Dithioglycerol c. both a & b d. none of the above

A 247. Synthesized from dry hydrogen chloride and carbon monoxide at 300 degrees and 200 atm pressure:
a. tetrachloroethylene b. piperazine c. both d. none

B 248. Passive diffusion includes what drug?


a. Lipid soluble b. Lipid insoluble c. Amphoteric d. Hydrophilic

D 249. It is the tendency of the drug to combine with the receptor:


a. Efficacy b. Intrinsic activity c. Bonding d. Affinity

B 250. Brand name of Bisacodyl:


a. Gelusin MPX b. Dulcolax c. Haloperidol d. Fleet

B 251. Penicillin G
a. Methicillin b. Benzyl penicillin c. both d. none

A 252. Organo-Silicon polymers containing O and Si atoms with a substituent organic groups:
a. silicons b. alkynes c. esters d. ethers

D 253. A phenol primarily obtained from clove oil:


a. resorcinol b. cresol c. hexylresorcinol d. eugenol

D 254. Which of the following is used in the treatment of pernicious anemia?


a. thiamine b. niacin c. riboflavin d. cyanocobalamin

A 255. Classified as a macrolide antibiotic, except:


a. Bacitracin b. Erythromycin c. Spiramycin d. Oleandomycin

C 256. A macrolide antibiotic which was found in the soil of Iloilo:


a. Achromycin b. Albamycin c. Erythromycin d. Viomycin

D 257. The following antimalarials are synthetic drugs, except:


a. Atabrine b. Aralen c. Camoquin d. Quinine

A 258. Polyene antibiotics for fungi:


a. amphotericin B c. ketoconazole e. both b & c
b. miconazole d. both a & b

C 259. Also known as solvent shift:


a. facilitated transport c. bulk transport e. none of the above
b. ion-pair transport d. passive diffusion

D 260. Externally, ethyl alcohol is employed as:


a. refrigerant c. astringent
b. rubefacient d. all of the above

C 261. Carbonic acid gas:


a. oxygen c. carbon dioxide e. helium
b. nitrogen d. ammonia

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Organic Pharmaceutical Chemistry
A 262. For patients allergic to penicillins, this drug is used as alternative:
a. erythromycin c. aureomycin e. none of the above
b. spectinomycin d. lincomycin

A 263. These anti-diarrheals trap the toxins and flushes them out of your system:
a. adsorbents b. anti-motility agents c. astringents d. oral rehydration salts

A 264. Drug of choice for urinary tract infections:


a. co-trimoxazole b. gentamicin c. naprofen d. all of the above

C 265. Voltaren:
a. tolmetin b. sulindac c. diclofenac d. piroxicam

C 266. The chemical name of Phenethicillin:


a. Benzyl penicillin c. Phenoxyethyl penicillin
b. Phenoxymethyl penicillin d. Phenoxypropyl penicillin

C 267. The following are the uses of methylene blue, except:


a. antidote for cyanide poisoning c. antidote for barbiturate poisoning
b. antidote for nitrate poisoning d. none of the above

B 268. Mechanism of action of this anti-tubercular agent is to inhibit protein synthesis:


a. PZA b. Streptomycin c. INH d. Ethambutol

A 269. Compounds that result from a combination of electron donors with a metal ion to form a ring structure:
a. chelates b. ligands c. both d. none

A 270. Transport of drug molecules from the site of administration to the systemic circulation:
a. absorption c. metabolism e. toxicology
b. adsorption d. excretion

D 271. Methylsalicylate is also known as :


a. toothache drop b. oil of Jasmine c. oil of rose d. oil of wintergreen

B 272. Agents that facilitate the evacuation of bowels:


a. anti-motility agents c. astringents e. none of the above
b. cathartics d. antacids

C 273. Absolute alcohol is commercially prepared by:


a. direct distillation c. azeotropic distillations
b. fermentation d. none

B 274. Nubain:
a. meperidine c. methadone e. pentazocine
b. nalbuphine d. fentanyl

D 275. Kaopectate:
a. activated charcoal c. Oresol e. atropine sulfate
b. attaulgite d. kaolin + pectin

A 276. The least stable of all vitamins:


a. ascorbic acid c. thiamine e. menadione
b. folic acid d. retinoic acid

C 277. A change in structure of isoniazid causes:


a. an increase in the potency of the drug c. decrease in the potency of the drug
b. an increase in the duration of drug action d. none of the above

C 278. The most toxic vitamin:


a. folic acid c. retinoic acid e. pyridoxine
b. pantothenic acid d. thiamine

B 279. Major organ for excretion:


a. liver c. skin e. none of the above
b. kidney d. small intestines

B 280. Generic name of Benadryl AH:


a. guaiafenesin b. diphenhydramine c. apomorphine d. benzonatate
a
A 281. A bright red dye that was found to create remarkable cures of streptococcal infections:
a. prontosil b. methyl red c. both d. none

C 282. Halazone is a/an:


a. iodophor d. oxidizing agent
b. mercury containing anti-infective e. none of the above
c. chlorine containing anti-infective
E 283. Drug of choice for leprosy:
a. rifampicin c. prothionamide e. dapsone
b. ethonamide d. clofazimine

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Organic Pharmaceutical Chemistry
B 284. The metabolic function of niacin:
a. decarboxylation c. differentiation of epithelial tissues
b. redox reactions d. maturation of erythrocytes

B 285. Sunshine vitamin:


a. A b. D c. E d. K

B 286. The following are fat-soluble vitamins, except:


a. A b. B2 c. D d. E e. K

C 287. In terms of pH, aspirin is absorbed in the:


a. mouth c. stomach e. rectum
b. small intestines d. large intestines

B 288. Therapeutic gas used as a gas diluent/carrier:


a. oxygen b. helium c. nitrogen d. carbon dioxide

D 289. The following drugs are extensively metabolized in the liver, except:
a. Isoproterenol b. Propranolol c. Lidocaine d. Paracetamol

C 290. A dye used in vital nerve staining:


a. malachite green b. gentian violet c. methylene blue d. basic fuchsin

D 291. The excretion of weakly basic drug will be more rapid in acidic urine than in basic urine because:
a. all drugs are excreted more rapidly in acidic urine
b. the drug will exist primarily in the unionized form, which cannot easily be reabsorbed
c. weak bases cannot be reabsorbed from the kidney tubules
d. the drug will exist primarily in the ionized form, which cannot be easily reabsorbed

C 292. Superinfection is common with:


a. antibiotics which are given parenterally c. those which suppress the normal bacterial flora
b. those which are used for prolonged period d. those which are given as a depot preparation

A 293. A potentially fatal aplastic anemia is a toxicity associated with:


a. chloramphenicol b. nitrofurantoin c. clindamycin d. cephalothin

C 294. Which is not true for cephalosporins?


a. broad spectrum b. bactericidal c. affected by penicillinases d. acid-stable

D 295. Bactrim and Septrim are trade names for a fixed-dose combination of:
a. sulfamethizole and trimethoxazole c. sulfamethoxazole and phenazopyridine
b. sulfisoxazole and methenamine d. sulfamethoxazole and trimethoprim

C 296. Which of the following is most likely to cause tinnitus and hearing loss in high doses?
a. ibuprofen b. phenylbutazone c. acetylsalicylic acid d. indomethacin

B 297. Pharmacologic effects of the classic antihistamines include all of the following, except:
a. sedation with low doses c. an antipruritic effect
b. inhibition of gastric acid secretion d. drying of salivary and bronchial secretion

A 298. An example of a commercial product that is pro-drug:


a. Lasix b. Geocillin c. Morphine d. Valium

B 299. All of the following statements are correct, except:


a. sulfonamides increase the risk of neonatal kernicterus
b. ketoconazole penetrates into the CSF
c. metronidazole is effective against Enterobacter histolytica
d. mebendazole is the drug of choice in the treatment of whipworm infections

B 300. Large overdose of acetaminophen are likely to cause:


a. tinnitus b. hepatic necrosis c. agranulocytosis d. renal tubular acidosis

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Organic Pharmaceutical Chemistry
1. The standard by which substances are compares is the activity of phenol. The phenol coefficient is defined as
the ratio of a disinfectant to the dilution of phenol required to kill a given strain of the bacterium Salmonella
typhi, under carefully controlled conditions over a given time period. If, for example, the dilution of a test
compound is ten times as great as the dilution of phenol, then the phenol coefficient is 10. The phenol
coefficient of phenol is, of course one (Wilson and Gisvold, 132).
2. Miconazole (Monistat, Micatin), Clotrimazole (Lotromin, Mycelex) and Ketoconazole (Nizoral) are synthetic
antifungal agents belonging to the class of substituted imidazoles. Their antifungal effect is associated with
damage to the cell membrane with the loss of essential cellular constituents, such as potassium ion and
amino acids. Potassium sorbate is an antifungal preservative used in syrups, elixirs, ointments, and lotions
containing components such as sugars that support mold growth (Wilson and Gisvold, 147-149).
3. Sulfonamides are structural analogs and competitive antagonists of para-aminobenzoic acid (PABA) and thus
prevent normal bacterial utilization of PABA for the synthesis of folic acid. More specifically sulfonamides are
competitive inhibitors of dihydropteroate synthase. They are extensively used for urinary tract infections and
for burn therapy. The sulfonamides used for prevention and treatment of infection secondary to burn are silver
sulfadiazine and mafenide. Preparations available in the market are Mafenide acetate cream (Sulfamylon) and
Silver sulfadiazine cream (Silvadene) (Wilson and Gisvold, 200).
4. Methyl paraben, benzoic acid and potassium sorbate are preservatives while undecylenic acid is a synthetic
antifungal agent obtained from the destructive distillation of castor oil. Preservatives are added to various
liquid dosage forms and cosmetic preparations to prevent microbial contamination. Methyl paraben is a para-
hydroxybenzoic acid derivative primarily used to protect against molds. Benzoic acid and potassium sorbate
are antifungal preservatives (Wilson and Gisvold, 143).
5. Blocking the biosynthesis of folate coenzymes at more than one point in the biosynthetic pathway of bacteria
will result in a synergistic antimicrobial effect. An additional benefit is that the microbe will not be able to
develop resistance as quickly as with a single pathway blocker. This synergistic approach is widely used in
antimicrobial therapy with the combination of sulfamethoxazole and trimethoprim. The combination is known
as cotrimoxazole. It is the treatment of choice for chronic urinary tract infection (Wilson and Gisvold, 201).
6. Polyene antibiotics were first isolated from soil bacteria. Amphotericin B from Streptomyces nodosus, Nystatin
from Streptomyces noursei are examples. They appear to bind to sterols in the cell membrane to cause
disorganization and loss of cell constituents, especially potassium ion. Griseofulvin from the mold Penicillium
griseofulvin is an antifungal antibiotic but it is not a polyene. Econazole is a substituted imidazole used
topically. Salicylic acid is a synthetic antifungal agent with keratolytic property (Wilson and Gisvold, 150).
7. Penicillin G (benzyl penicillin), Penicillin V (phenoxymethyl penicillin) and Ampicillin (D-α-
aminobenzylpenicillin) are degraded by β-lactamase leading to their inactivation while Oxacilllin (5-methyl-3-
phenyl-4-isoxazolylpenicillin) is β-lactamase resistant (Wilson and Gisvold, 231).
8. The quinolones comprise a series of synthetic antibacterial agents patterned after nalidixic acid, a first
generation urinary tract anti-infective. Nalidixic acid is a nonfluorinated quinolone. It is effective against most
of the gram-negative bacteria that commonly cause UTIs but the gram-positive organisms are resistant. Its
clinical usefulness is limited by the rapid emergence of resistant strains. Most (>90%) of the drug is protein
bound and levels of free drug are therefore inadequate for treatment of systemic infections (Wilson and
Gisvold, 155).
9. The fluoroquinolones (fluorinated quinolones) enter the cell by passive diffusion through water-filled protein
channels (porins) in the outer membrane. Intracellularly, they uniquely inhibit the replication of bacterial DNA
by interfering with the action of DNA gyrase (topoisomerase II) during bacterial growth and reproduction.
Binding of the quinolone to both the enzyme and the DNA to form a ternary complex inhibits the rejoining step
and can cause cell death by inducing cleavage of the DNA. The first fluorinated quinolone, Norfloxacin, is
effective against both gram-negative and gram-positive organism in treating complicated and uncomplicated
urinary tract infections and prostatitis, but not in systemic infections (Wilson and Gisvold, 156).
10. Because strains of Mycobacterium tuberculosis resistant to a particular agent emerge during the treatment,
multiple drug therapy is employed to delay or prevent their emergence. The short course chemotherapy for
tuberculosis includes isoniazid, rifampina and pyrazinamide for 2 months, and isoniazid and rifampin for the
next 4 months. Ethambutol may also be added to this regimen (Wilson and Gisvold, 158).
11. Metronidazole is the drug of choice for amoebiasis caused by Entamoeba histolytica, giardiasis caused by
Giardia lamblia and trichomoniasis caused by Trichomonas vaginalis (Mycek, 347).
12. Generations of Cephalosporins
First generation Second Generation Third generation Fourth generation
“Ceph” “Cef” All that ends with –one and
except: Cefadroxil nothing that ends in –one –ime except:
Cefazolin and –ime except: Cefdinir
Loracarbef Cefditoren
Cefuroxime Moxalactam
Cephalexin Cefaclor Cefixime Cefepime
Cephalothin Cefamandole Cefoperazone
Cephapirin Cefonicid Ceftazidime
Cephradine Cefmetazole Ceftizoxime
Cefotetan Ceftriaxone
Cefoxitin
(Mycek, 298)
13. Acyclovir, a guanosine analog, has potent activity against several DNA viruses, including herpes simplex type
1 and type 2 viruses, varicella zoster virus (causative agent of chicken pox), and Epstein-Barr virus.
Zidovudine, a pyrimidine analog (3’azido-3’-deoxythymidine), is one of the most effective drugs currently
approved for treatment of HIV infection and AIDS. Metronidazole is the agent of choice for treating infections
caused by Entamoeba histolytica, Giardia lamblia and Trichomonas vaginalis. Chloroquine is the drug of
choice in the treatment of erythrocytic falciparum malaria, except in resistant strains (Mycek, 365).
14. Chloramphenicol, a broad spectrum antibiotic, is active not only against bacteria but also against other
microorganisms, such as rickettsia. It has excellent activity against anaerobes. But because of its toxicity, its
use is restricted to life threatening infections in which there are no alternatives (Mycek, 321).

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Organic Pharmaceutical Chemistry
15. Clindamycin is recommended for the treatment of a wide variety of upper respiratory, skin and tissue
infections caused by susceptible bacteria. Its activity against streptococci, staphylococci, and pneumococci is
undisputably high. It is one of the most potent against some non-spore-forming anaerobic bacteria, the
Bacteroides species in particular. However, an increasing number of reports of clindamycin-associated
gastrointestinal toxicity, which ranges in severity from diarrhea to an occasionally serious pseudomembranous
colitis, have caused some clinical experts to call for a reappraisal of the appropriate position of this antibiotic
in therapy (Mycek, 321).
16. Chemotherapy is the study of chemical agents which are selectively more toxic to the invading organisms
than the host. Selective toxicity, the property of certain chemicals to destroy one form of life without harming
another, is the cornerstone of modern antimicrobial chemotherapy. This concept is largely credited to Paul
Ehrlich, the Father of Chemotherapy (Wilson and Gisvold, 129).
17. Local anti-infective germicides, may be classified as antiseptics and disinfectants and constitute an important
group of drugs. Antiseptics are compounds that kill (-cidal) or prevent the growth of (-static) microorganisms
when applied to living tissue. A disinfectant is an agent that prevents infection by destruction of pathogenic
microorganisms when applied to inanimate objects (Wilson and Gisvold, 129-130).
18. Iodine is one of the oldest known and remains one of the most effective and useful germicides available today.
Various nonionic and cationic surfactants have found to act as solubilizers for iodine by forming complexes
that retain the germicidal properties of iodine. These complexes also reduce the volatility of iodine and
essentially remove its irritant property. Povidone-iodine is a complex with nonionic surfactant polymer,
polyvinylpyrrolidone. This water-soluble complex releases iodine slowly. It provides a nontoxic, nonirritating,
nonvolatile, and nonstaining form of iodine. Approximately 10% of available iodine is present in the complex
(Wilson and Gisvold, 135-136).
19. Benzalkonium chloride (new Merthiolate) is a cationic surfactant possessing detergent, emulsifying and
wetting action. It is employed as an antiseptic for skin and mucosa, for irrigation and for storage of surgical
instruments. Chlorhexidine gluconate (Hiblicens) has a broad-spectrum antibacterial activity, but it is not active
against acid-fast bacteria, spores, or viruses. It has been employed for such topical antiseptic uses as
preoperative skin disinfection, wound irrigation, bladder irrigation, mouthwashes, and general sanitation. It is
not absorbed through skin or mucous membranes and does not cause systemic toxicity. Thimerosal (old
Merthiolate) is a mercury-containing compound. It is a weakly bacteriostatic antiseptic that is applied topically
as an aqueous solution or as an ointment (Wilson and Gisvold, 141).
20. The quinolones enter the cell by passive diffusion through water-filled protein channels (porins) in the outer
membrane. Intracellularly, they uniquely inhibit the replication of bacterial DNA by interfering with the action of
DNA gyrase (topoisomerase II) during bacterial growth and reproduction. Binding of the quinolone to both the
enzyme and the DNA to form a ternary complex inhibits the rejoining step and can cause cell death by
inducing cleavage of the DNA (Mycek, 323).
21. Although in several malaria species the biguanides have some antimalarial activity, they are largely prodrugs
of their active metabolites, the dihydrotriazines. For example, chloroguanide is rapidly metabolized to the
potent antimalarial dihydrotriazine, cycloguanil. The biguanides are absorbed from the gastrointestinal tract
very quickly, but not as rapidly as quinine or chloroquine. The toxic manifestations of biguanides are very mild
in humans. Some gastrointestinal disturbances may occur of the drugs are taken on an empty stomach, but
not if they are taken after meals. With excessive doses (1 g of chloroguanide), some renal disorders such as
hematuria and albuminuria may develop (Wilson and Gisvold, 222).
22.

Erythromycin Spectinomycin Roxithromycin Clindamycin


Ilotycin Trobicin 7-chloro-7-
deoxylincomycin
(Wilson and Gisvold, 298)
23. A single intramuscular injection of cycloguanil pamoate (Camolar) can provide protection against all four
human malarial species for several months. As with all antimalarials, effectiveness is dependent upon the
malaria strain not being resistant to the drug or its structural analogues. Unfortunately, resistance develops
quickly to cycloguanil pamoate, and injection sites can be painful. The problems do not seem to be
significantly improved by combination with other antimalarial drugs. Sulfate salts of cinchonidine and
cinchonine (Quinine sulfate) may be used as antimalarials. The dextrorotatory cinchonine salt is of value in
the treatment of patients who display sensitivity to the levorotatory cinchona alkaloids. Chloroquine is the drug
of choice in the treatment of erythrocytic falciparum malaria, except in resistant strains. Amodiaquine is highly
suppressive in Plasmodium vivax and Plasmodium falcifarum infections, being three to four times as active as
quinine. However, it has no curative activity, except against Plasmodium falciparum (Wilson and Gisvold, 222).
24. Mefloquine is the most promising of a group of new antimalarial drugs. Since its FDA approval in 1989,
mefloquine has become a drug of choice for malaria suppression, particularly in areas of known chloroquine-
resistant strains. It has also been very effective in curing multidrug-resistant Plasmodium falcifarum malaria,
apparently at the erythrocytic stage in the life cycle (Wilson and Gisvold, 219).
25. Trypanosomiasis refers to two chronic and eventually fatal diseases caused by species of Trypanosoma:
African sleeping sickness (Trypanosoma brucei gambiense and Trypanosoma brucei) and American sleeping
sickness (Trypanosoma gondii). Pentamidine is a dibenzamidine used for prophylaxis and treatment of African
trypanosomiasis. Its principal use is for the treatment of pneumonia caused by the opportunistic pathogenis
protozoan Pneumocystis carinii, a frequent secondary invader associated with AIDS (Mycek, 353).
26. Clarithromycin, a methylated form of erythromycin, has a spectrum of antibacterial activity similar to that of
erythromycin, but is also effective against Haemophilus influenzae. Its activity against intracellular pathogens
such as Chlamydia, Legionella and Ueraplasma is higher than that of erythromycin. (Mycek, 317)
27. Amikacin (Amikin) is a semisynthetic aminoglycoside first prepared in Japan. The synthesis formally involves
simple acylation of the 1-amino group of the deoxystreptamine ring of kanamycin A with L-amino-alpha-
hydroxybutyric acid (Wilson and Gisvold, 278).
28. In many viral infections the clinical symptoms appear late in the course of the disease at a time when most of
the virus particles have replicated. At this late, symptomatic stage of the viral infection, administration of drugs
that block viral replication have limited effectiveness. However, some antiviral agents are useful as
prophylactic agents. For example, amantadine (Symmetrel) and its congener, rimantadine have shown to be
equally effective in preventing influenza A infections (Mycek, 363).

MANOR Review Center 38


Organic Pharmaceutical Chemistry
29. Ofloxacin has better oral bioavailability than the other fluoroquinolones, but it is generally less active against
the Enterobacteriaceae and Pseudomonas aeruginosa. Levo-ofloxacin is the more potent isomer of ofloxacin
(Wilson and Gisvold, 157).
30. The sulfones are primarily of interest as antibacterial agents, although there are some reports of their use in
the treatment of malarial and rickettsial infections. They are less effective agents than are the sulfonamides.
Para-aminobenzoic acid partially antagonize the action of many of the sulfones, suggesting that the
mechanism of action is similar that of the sulfonamides. It has been observed that infections that arise in
patients being treated with sulfones are cross-resistant to sulfonamides (Wilson and Gisvold, 203).
31. Thiabendazole inhibits the helminth-specific enzyme fumarate reductase. It is not known whether metal ions
are involved, or if the inhibition of the enzyme is related to thiabendazole’s anthelmintic effect. Benzimidazole
anthelmintic drugs such as thiabendazole and mebendazole also arrest nematode cell division in metaphase
by interfering with microtubule assembly. They exhibit a high affinity for tubulin, the precursor protein for
microtubule synthesis (Wilson and Gisvold, 182).
32. Mafenide acetate (Sulfamylon) is a homologue of the sulfanilamide molecule. It is employed alone or with
antibiotics in the treatment of slow-healing infected wounds. Some patients treated for burns with large
amounts of this drug developed metabolic acidosis. To overcome this side effect, a series of new organic salts
was prepared. The acetate in an ointment base proved to be the most efficacious (Wilson and Gisvold, 201).
33. The causative agents of filariasis are Wucheria bancrofti and Brugia malayi. Worms cause blockage of lymph
flow; ultimately local inflammation and fibrosis of lymphatics occurs. After years of infestation, the arms, legs,
and scrotum fill with fluid causing elephantiasis. The drug of choice for this condition is diethylcarbamazine.
34. A variety of studies have shown that the active form of sulfonamides is the N – ionized salt form (Wilson and
Gisvold, 197).
35. Crotaminon is available in 10% concentration in a lotion and a cream intended for the topical treatment of
scabies. Its antipruritic effect is probably due to a local anesthetic action (Wilson and Gisvold, 188).
36. Mebendazole is a broad spectrum anthelmintic that is effective against a variety of nematode infestations
including whipworm, pinworm, roundworm, and hookworm. Mebendazole irreversibly blocks glucose uptake in
susceptible helminthes, thereby depleting glycogen stored in the parasite. It apparently does not affect
glucose metabolism in the host. It also inhibits cell division in nematodes (Wilson and Gisvold, 182).
37. Adifax is a sympathomimetic agent that binds to alpha receptors found centrally that causing suppression of
appetite.
38. Aromatic acids and arylalkyl acids are the major substrates undergoing glycine conjugation. The conversion of
benzoic acid to its glycine conjugate, hippuric acid, is a well-known metabolic reaction in many mammalian
systems (Wilson and Gisvold, 101).
39. Active transport may be defined as energy-dependent movement of a substance through a biological
membrane against an electrochemical gradient. The substance is transported from a region of lower to one of
higher concentration or electrochemical activity. The transport rate approaches an asymptote (i.e., saturates)
as concentration increases. The transport system usually shows requirement for specific chemical structures.
Closely related chemicals are competitive for the transport system (Remington, 1111).
40. Astringents are locally applied, protein precipitants that have such a low cell penetrability that action
essentially is limited to the cell surface and the interstitial spaces. The permeability of the cell membrane is
reduced, but the cells remain viable. The astringent action is accompanied by contraction and wrinkling of the
tissue and by blanching. Mucus and other secretions may be reduced. Astringents are used therapeutically to
arrest hemorrhoid and to check diarrhea, reduce inflammation of mucous membranes, promote healing,
toughen skin, or decrease sweating (Remington, 1205).
41. Along with the antimuscarinic agent scopolamine, certain H1 receptor blockers, such as diphenhydramine,
dimenhydrinate, cyclizine, and meclizine, are the most effective agents for the prevention of the symptoms of
motion sickness. The antihistamines prevent or diminish vomiting and nausea mediated by both the
chemoreceptor and vestibular pathways (Mycek, 424).
42. Attapulgite is a double-chain structure with rather large open spaces between the chains. These spaces are
occupied by water molecules, which provide hydrogen boding to hold the chains together. It has adsorptive
properties similar to kaolin (Remington, 370).
43. Vitamin E designates the group of compounds that exhibit qualitatively the biological activity of alpha-
tocopherol. Studies that led to its discovery as an essential factor in animal metabolism showed that it was,
among other things, necessary for reproduction in rats. It often is called the antisterility vitamin, an
inappropriate term, since it is not known to specifically function in this capacity in humans (Remington, 1801).
44. Vitamin D3 is not itself the active form of the vitamin, and in the body it is hydroxylated firstly to 25-
hydroxyvitamin D3 (calcidiol) by an enzyme in the liver, and then to 1alpha, 25- dihydroxyvitamin D3 (calcitriol)
by a kidney enzyme. Calcitriol is then transported to the bones, intestine, and other organs (Dewick, 241).
45. Although it is suggested that chloral hydrate, per se, may act as a hypnotic, it is also recognized that chloral
hydrate is very quickly converted to trichloroethanol and the latter compound is generally assumed to account
for almost all of the hypnotic effect (Wilson and Gisvold, 373).
46. A sample drug excreted via the saliva is lidocaine.
47. Etretinate (Tegison), a vitamin A derivative, is indicated for the treatment of severe recalcitrant psoriasis.
Because of its potential severe adverse effects, therapy should be limited to those diseases that do not
respond to standard therapies. Isotretinoin (Accutane) is indicated for the treatment of severe recalcitrant
cystic acne. Tretinoin (Retinoic Acid, Retin-A) is indicated for topical treatment of acne vulgaris. It appears to
exert its action by decreasing adhesion of corneocytes and by increasing the proliferation of the follicular
epithelium (Wilson and Gisvold, 833-834).
48. Structurally specific drugs are those whose activity depends on their ability to bind on a specific receptor.
49. The antibacterial potencies of primary alcohols increase with molecular weight up to C8, where the “cutoff” is
reached. Beyond this point, water solubility is less than the minimum effective concentration, and the apparent
potency decreases with molecular weight. Branching decreases antibacterial potency; hence, the isomeric
alcohols follow the order primary>secondary>tertiary (Wilson and Gisvold, 130).
50. In strongly acidic solutions (pH <3) penicillin undergoes a complex series of reactions leading to a variety of
inactive degradation products. The first step appears to involve rearrangement to the penicilennic acid. This
process is initiated by protonation of the beta-lactam nitrogen followed by nucleophilic attack of the acyl
oxygen atom on the beta-lactam carbonyl carbon. The subsequent opening of the beta-lactam ring
destabilizes the thiazoline ring, which then suffers acid-catalyzed ring opening to form the penicillenic acid
(Wilson and Gisvold, 234-235).

MANOR Review Center 39


Organic Pharmaceutical Chemistry
51. Glutarol disinfectant solution (glutaraldehyde) is a dialdehyde used as a dilute solution for equipment and
instruments that cannot be autoclaved. The commercial product (Cidex) is a stabilized alkaline glutaraldehyde
solution (Wilson and Gisvold, 132).
52. Substitution of an electron-withdrawing group in the alpha-position of benzylpenicillin has been shown to
markedly stabilize the penicillin to acid-catalyzed hydrolysis. Thus, the phenoxymethyl-, alpha-aminobenzyl,
and alpha-halobenzylpenicillins are significantly more stable than benzylpenicillins in acid solutions (Wilson
and Gisvold, 236).
53. It was found that increasing the steric hindrance at the alpha-carbon of the acyl group increased resistance to
staphylococcal beta-lactamase, with maximal resistance being observed with quaternary substitution. Bulkier
substituents are required to confer effective beta-lactamase resistance among five-membered ring
heterocyclic derivatives (Wilson and Gisvold, 237).
54. Vancomycin is a tricyclic glycopeptide that has become increasingly important because of its effectiveness
against multiple drug resistant organisms such as methicillin-resistant staphylococci (Mycek, 308).
55. A tumor is benign if the tumor mass may be removed by surgery and regression of remaining cells occur.
Metastasis is not evident and cells originating from the tumor do not invade other tissues or cause damage to
surrounding tissues.
56. One gram mass of tumor is equivalent to one billion cancer cells.
57. Bromhexine and acetylcysteine are mucolytics. They reduce the viscosity of the abnormally viscid pulmonary
secretion in patients with tracheobronchial and bronchopulmonary disease. Caramiphen is an antitussive
whose activity is less than that of codeine. It has been shown to have both central and bronchodilator activity.
The frequency of side effects is lower than with the narcotic antitussives (Wilson and Gisvold, 656, 789).
58. The common side effects of long term corticosteroid therapy are negative calcium balance (osteoporosis),
impaired wound healing (increased risk of infection), increased appetite, hypertension, edema, peptic ulcer,
euphoria and psychosis. These side effects are diminished when the drug is given via inhalation.
59. Surgery is usually the first treatment of endometrial or breast cancer, but in advanced cases for whom surgery
would not be possible, progestins (depo-provera) have provided palliative treatment (Wilson and Gisvold,
703).
60. Ethosuximide conforms very well to the general structural pattern for antiabsence activity. The drug is more
active and less toxic than trimethadione; consequently, it has emerged as the drug of choice for typical
absence seizures (Wilson and Gisvold, 390).
61. Butylated hydroxytoluene (BHT) is an antioxidant employed to retard oxidative degradation of oil and fats in
various cosmetics an dpharmaceuticals. It is a potent carcinogen (Remington, 1015).
62. Para-nitrobenzene azo-resorcinol, a pink dye, gives a violet precipitate with pentavalent antimony in the
presence of hydrochloric acid.
63. Guaiafenesin is composed of guaiacol, a phenol volatile oil derived from Fagus grandiflora (Fam. Fagaceae)
found in over the counter expectorants (Tyler, 128). It is used for the symptomatic relief of respiratory
conditions characterized by a dry, nonproductive cough and the presence of mucus in the respiratory tract
(Remington, 1303).
64. Mescaline (3,4,5,-trimethoxy-beta-phenylethylamine) is regarded as the first of a series of hallucinogens or
psychotomimetics (Tyler, 244).
65. Methoxyflurane is the most potent inhalation anesthetic because of its high lipid solubility. Prolonged
administration is associated with the metabolic release of fluoride, which is toxic to the kidneys. Therefore,
methoxyflurane is rarely used outside of obstetrics practice. It finds use in child-birth because it does not relax
the uterus when briefly inhaled (Mycek, 114).
66. Ergotamine has in the past been the drug of choice for treatment of moderate-to-severe migraine. Ergotamine
and dihydroergotamine have similar actions to sumatriptan, but they have less selectivity for the serotonin
receptors. Ergotamine can be given orally, sublingually, rectally or nasally, and is effective in about 50% of
patients. Dihydroergotamine, a derivative of ergotamine, is administered intravenously and has an effect
similar to that of sumatriptan, but nausea is a common adverse effect (Mycek, 428).
67. Enflurane is the anesthetic of choice for patients with asthma.
68. Ibuprofen was the first priopionic acid derivative to become available in the United States. It has bee joined by
naproxen, fenoprofen, ketoprofen, flurbiprofen and oxaprozin (Mycek, 408).
69. Iodine is one of the oldest known and remains one of the most effective and useful germicides available today.
Various nonionic and cationic surfactants have found to act as solubilizers for iodine by forming complexes
that retain the germicidal properties of iodine. These complexes also reduce the volatility of iodine and
essentially remove its irritant property. Such complexes are called iodophors. Povidone-iodine is a complex
with nonionic surfactant polymer, polyvinylpyrrolidone. This water-soluble complex releases iodine slowly. It
provides a nontoxic, nonirritating, nonvolatile, and nonstaining form of iodine. Approximately 10% of available
iodine is present in the complex (Wilson and Gisvold, 135-136).
70. Benzyl alcohol (phenylmethanol) is found unesterified in oil of Jasmine and as exters of acetic acid, cinnamic
acid, and benzoic acids in gum benzoin, storax resin, Peu balsam, tolu balsam, and in some volatile oils. It is
commonly used as a preservative in vials of injectable drugs in concentrations of 1% to 4% in water or saline
solution (Wilson and Gisvold, 144).
71. A characteristic of cancer cells is their lack of normal growth controls.
72. Polychlorinated biphenyls are carcinogenic substances obtained from paper products.
73. The prostaglandins are one group of naturally occurring 20-carbon fatty acid derivatives produced by oxidative
metabolism of 5,8,11,14-eicosatetraenoic acid, which is also called arachidonic acid. Other so-called
eicosanoids produced in the complex biological oxidation scheme called the arachidonic acid cascade are
thromboxane A2, the leukotrienes, and the highlight potent antithrombotic agent, prostacyclin (Wilson and
Gisvold, 867).
74. Among the following functional groups (imide, amide, amine, aniline), amine is the most basic.
75. In 1942, para-aminobenzenesulfonamidoisopropyl-thiadiazole (an antibacterial sulfonamide) was found to
produce hypoglycemia. These results stimulated the research for the development of synthetic hypoglycemic
agents, several of which are in use today. Sulfonylureas became widely available in 1955 for treatment of
nonkeratosis-prone mild diabetes and are still the drug of choice (Wilson and Gisvold, 577).
76. Retinoids (vitamin A and analogues) are now known to act as signaling molecules which regulate diverse
aspects of cell differentiation, embryonic development, growth, and vision. For the processes of vision, retinol
needs to be converted first by oxidation into the aldehyde all-trans-retinal, and then by enzymatic
isomerization to cis-retinal (Dewick, 212).

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Organic Pharmaceutical Chemistry
77. The introduction of aniline derivatives as analgesics is based on the discovery that aniline has antipyretic
properties. The hydroxylated anilines, better known as the aminophenols, possess strong antipyretic and
analgesic action. The acetylation of the amine group provides N-acetyl-para-aminophenol (acetaminophen;
paracetamol) (Wilson and Gisvold, 665).
78. Progestins are compounds that have biological activities similar to progesterone. Progesterone promotes the
development of a secretory endometrium that can accommodate implantation of a newly formed embryo.
Examples are the following: progesterone, norgestrel, norethindrone, megestrol acetate and ethynodiol
diacetate (Wilson and Gisvold, 701, 704).
79. Aspirin (acetyl salicylic acid) is the product of the acetylation of salicylic acid. Heroin (diacetyl morphine) is
the product of the acetylation of morphine (Wilson and Gisvold, 647).
80. Pyridoxine is chemically known as 6-methyl-3,4-pyridinedimethanol. The functional group present is alcohol
(Wilson and Gisvold, 854).
81. Ascorbic acid and tetracyclines are enols.
82. Monoamine oxidase (MAO) is a mitochondrial enzyme found in neural and other tissues, such as gut and
liver. In the neuron, MAO function as a “safety valve” to oxidatively deaminate and inactivate any excess
neurotransmitter molecules (norepinephrine, dopamine, and serotonin) that may leak out of synaptic vesicles
when the neuron is at rest (Mycek, 123).
83. When used in pharmaceutical preparations, the purpose of hydroquinone, lecithin and alpha-tocopherol is to
act as oil soluble antioxidant. An antioxidant is an agent that inhibits oxidation and thus is used to prevent the
deterioration of preparations by the oxidative process (Ansel, 88).
84. Opioids are therapeutically used for analgesia, treatment of diarrhea and relief of cough (Mycek, 137).
85. Mixtures of sulfonamides and agents of a chemical class of local anesthetics, the aminobenzoic acid
derivatives, should be avoided because of a potential pharmacologic incompatibility. A hydrolysis product of
these agents is p-aminobenzoic acid (PABA). Sulfonamides are considered competitive inhibitors of the
incorporation of PABA in the biosynthesis of dihydrofolate (Wilson and Gisvold, 593, 593).
86. The macrolide antibiotics are macrocyclic lactones with a ring size typically 12-16 atoms, and with extensive
branching through methyl substituents. Examples of these are erythromycin, azithromycin, clarithromycin,
oleandromycin and spiramycin. Vancomycin is a tricyclic glycopeptide that inhibits bacterial cell wall synthesis
(Dewick, 92-94).
87. Lorazepam (Ativan) is a benzodiazepine used as anxiolytic (Wilson and Gisvold, 366).
88. Metoclopramide (Plasil) is highly-effective at high doses against the highly emetogenic cisplatin, preventing
emesis in 30 to 40% of patients and reducing emesis in the majority (Mycek, 242).
89. Aspirin is stable in dry air, but in the presence of moisture, it slowly hydrolyzes into acetic acid and salicylic
acid (Wilson and Gisvold, 660).
90. Barbiturates containing a sulfur atom are usually ultrashort-acting. Ultrashort-acting barbiturates may be
administered intravenously in aqueous solutions for the induction of anesthesia. Thiamytal sodium (sodium 5-
allyl-5-(1-methyl-butyl)-2-thiobarbiturate) and thiopental sodium (sodium 5-ethyl-5(1-methylbutyl)-2-
thiobarbiturate) are examples (Wilson and Gisvold, 361-363).
91. Although the prostaglandins are hormone-like, they may closely resemble lipids chemically. The
prostaglandins are one group of naturally occurring 20-carbon fatty acid derivatives produced by oxidative
metabolism of 5,8,11,14-eicosatetraenoic acid, which is also called arachidonic acid (Wilson and Gisvold,
867).
92. The onset and duration of action of barbiturate action is mainly a function of its lipid solubility. Short-acting
barbiturates are more lipid soluble than long-acting barbiturates.
93. The prototype narcotic antagonist is naloxone. It is used as the agent of choice for treating narcotic
overdosage. It is almost seven times more active than nalorphine in antagonizing the effects of morphine. It
shows no withdrawal effects after long-term administration (Wilson and Gisvold, 653).
94. Lysergic acid diethylamide (LSD) does not occur in nature but is prepared by semisynthesis. It is derived from
ergot, the dried sclerotium of Claviceps purpurea (Tyler, 236).
95. Salicylic acid (ortho-hydroxybenzoic acid) is a strong acid with antiseptic and keratolytic properties (Wilson
and Gisvold, 146).
96. Acetazolamide (Diamox) was introduced in 1950 as the first orally effective, nonmercurial antidiuretic available
to the physician. It has a relatively restricted use today because of its limited efficacy and the refractoriness
that develops to its diuretic action within the first week of continuous therapy. However, it remains the most
important carbonic anhydrase inhibitor available and serves as the prototypic agent in its class (Wilson and
Gisvold, 516-517).
97. Diphenoxylate is a structural analog of meperidine. Although this drug has a strong structural relationship to
the meperidine-type analgesics it has very little, if any, such activity itself. Its most pronounced activity is its
ability to inhibit excessive gastrointestinal motility, an activity reminiscent of the constipating side effect of
morphine itself (Wilson and Gisvold, 650).
98. Ascorbic acid (cevitamic acid) is frequently administered with methenamine to improve the effectiveness of
this antibacterial agent. Because ascorbic acid increases the chelation of iron by deferroxamine, it is used in
the treatment of chronic iron deficiency (Wilson and Gisvold, 860).
99
Atabrine Artane Aralen Akineton
Quinacrine Trihexyphenidyl Chloroquine phosphate Biperiden
hydrochloride
(Wilson and Gisvold, 885, 887)
100. Kanamycin sulfate (Kantrex) is an aminoglycoside whose use is usually restricted to infections of the
intestinal tract and to systemic infections arising from gram negative bacilli (e.g. Klebsiella, Proteus,
Enterobacter, and Serratia) that have developed resistance to other antibiotics (Wilson and Gisvold, 277-
278).
101. Epinephrine (Adrenalin) was initially isolated from the medulla of adrenal glands of animals used for food. It
is used in the treatment of heart block or circulatory collapse but its use is limited because of its tendency to
induce cardiac arrhythmias. It increases systolic pressure by increasing cardiac output, and it lowers diastolic
pressure by causing an overall decrease in peripheral resistance; the net result is little change in mean blood
pressure. It is sometimes useful in the treatment of glaucoma, because it apparently reduces the formation of
aqueous humor, which results in a lowering of intraocular pressure. Local application is limited, but is of value
as a constrictor in hemorrhage or nasal congestion (Wilson and Gisvold, 422).

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Organic Pharmaceutical Chemistry
102. Methylxanthines
Caffeine Theophylline Theobromine Aminophylline
1,3,7-trimethylxanthine 1,3-dimethylxanthine 3,7-dimethylxanthine Ethylenediamine salt of
theophylline
(Wilson and Gisvold, 396)
103. Of the following penicillin congeners (pen V, methicillin, carbenicillin, oxacillin), the one with the broadest
spectrum of action is carbenicillin. It has activity against Pseudomonas aeruginosa (Mycek, 301).
104. H2-histamine receptor blockers
Cimetidine Famotidine Nizatidine Ranitidine
Tagamet Pepcid, H2-Bloc Zantac
(Wilson and Gisvold, 891, 896, 902, 905)
105. Misoprostol (Cytotec) is a modified prostaglandin analog which shows potent gastric antisecretory and
gastroporotective effects when administered orally. This prostaglandin derivative should be absolutely
avoided in pregnant women owing to its potential to induce abortion (Wilson and Gisvold, 874).
106. Ma huang, an alkaloidal amine, is the entire plant or the overground portion of Ephedra sinica Stapf (Family
Gnetaceae). In Chinese characters, “ma” means astringent and “huang” means yellow, probably referring to
the taste and color of the drug (Tyler, 240).
107. All local anesthetics consist of a hydrophilic amino group linked through a connecting group of variable
length to a lipophilic aromatic residue. An ester linkage is present in procaine (Mycek, 117-118).
108. The functional group found in codeine and scopolamine is an ether.
109. Chlortetracycline hydrochloride (Aureomycin hydrochloride) was isolated by Duggar in 1948 from
Streptomyces aureofaciens (Wilson and Gisvold, 288).
110. Meclizine (Bonamine) is a moderately potent antihistamine used as an antinauseant in the prevention and
treatment of motion sickness and in the treatment of nausea and vomiting associated with vertigo and
radiation sickness (Wilson and Gisvold, 618).
111. Polyene antibiotics include amphotericin B (from Streptomyces nodosus) and nystatin (from Streptomyces
noursei). They appear to bind with sterols in the cell membrane to cause disorganization and loss of cell
constituents, especially potassium ion (Wilson and Gisvold, 150-151).
112. Caffeine enjoys wide use as a CNS stimulant. Theophylline has some use as a CNS stimulant. Its CNS
stimulant properties are more often encountered as side effects, sometimes severe and potentially life-
threatening, of its use in bronchial asthma therapy. Theobromine has very little CNS activity (Wilson and
Gisvold, 396).
113. Dextran is a polyglucan that is formed from sucrose by the action of a transglucosylate enzyme system
(dextran sucrase) present in Leuconostoc mesenteroides. Dextran is used as plasma expander in cases of
shock or pending shock caused by trauma, hemorrhage, or severe burns (Tyler, 43).
114. The combination type oral contraceptive pill, containing an estrogen and progestin, is the most common type
(Mycek, 268).
115. Simethicone is a mixture of fully methylated linear siloxane polymers containing repeating units of the formula
[-(CH3)2SiO)n, stabilized with trimethylsiloxy end-blocking units of the formula [(CH3)3SiO-], and silicon dioxide
(Remington, 1242).
116. Effervescent salts are granules or coarse to very coarse powders containing a medicinal agent in a dry
mixture usually composed of sodium bicarbonate, citric acid, and tartaric acid. Tartaric acid is an acidifying
agent employed in effervescent salts and refrigerant drinks (Ansel, 177).
117. Meperidine hydrochloride (Demerol hydrochloride) exerts an analgesic effect that lies between those of
morphine and codeine, but it shows little tendency toward hypnosis. Its most important use seems to be in
lessening the severity of labor pains in obstetrics, and with barbiturates or tranquilizers, to produce amnesia
(Wilson and Gisvold, 649).
118. Benzaldehyde is synthetic bitter almond oil.
119. The ring common among penicillins and cephalosporins is the beta-lactam ring. The cephalosporins are
closely related both structurally and functionally to the penicillins (Mycek, 304).
120. Tretinoin (Retin-A) is indicated for topical treatment of acne vulgaris and was initially used systemically.
Howver, therapeutic doses frequently resulted in hypervitaminosis A. it appears to exert its action by
decreasing the adhesion of corneocytes and by increasing the proliferation of the follicular epithelium (Wilson
and Gisvold, 833).
121. Barbiturates
Short duration of action Intermediate duration of action (3 to Long duration of action
(less than 3 hours) 6 hours) (6 hours or more)
Pentobarbital Amobarbital Barbital
Secobarbital Butabarbital Metharbital
Talbutal Phenobarbital
(Wilson and Gisvold, 369).
122. Vitamin C is extremely important in wound healing. Its potential is on the formation of collagen.
123. Carisoprodol, Methacarbamol, Baclofen and Buspirone are CNS depressants with skeletal muscular relaxant
property (Wilson and Gisvold, 373-376).
124. Acyclovir has a greater specificity than vidarabine against herpes viruses. Herpes simplex virus-1, herpes
simplex virus-2, varicella zoster, and some Epstein-Barr virus-mediated infections are sensitive to acyclovir,
but cytomegalovirus is resistant. Acyclovir is the treatment of choice in herpes simplex encephalitis. The most
common use of acyclovir is in therapy of genital herpes infections (Mycek, 366).
125. Primaquine is an 8-aminoquinoline that eradicates exoerythrocytic forms of malarial parasites in the liver.
Because of its lack of activity against the erythrocytic schizonts, primaquine is often used in conjunction with
a schizonticide (Mycek, 349).
126. Feldene is piroxicam (Wilson and Gisvold, 665).
127. Voltaren is diclofenac (Wilson and Gisvold, 665).
128. Depo-provera is medroxyprogesterone acetate (Wilson and Gisvold, 704).
129. H2 receptors stimulate gastric hydrochloric acid secretion (Mycek, 421).
130. Opium is the air-dried milky exudates obtained by incising the unripe capsules of Papaver somniferum
(Family Papaveraceae). It acts chiefly on the central nervous system; its action first stimulates and then
depresses nerve response. It is an example of a narcotic analgesic (Tyler, 214,216).

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131. Oxacillin sodium is the salt of asemisynthetic penicillin that is highly resistant to inactivation by penicillinase.
It is also relatively resistant to acid hydrolysis and, therefore, may be administered orally with good effect
(Wilson and Gisvold, 242).
132. Spironolactone inhibits the reabsorption of 2-3% of the filtered load of sodium at the collecting tubule by
competitively inhibiting the actions of aldosterone (Wilson and Gisvold, 529).
133. Acetylation constitutes an important metabolic route for drugs containing primary amino groups. This group
encompasses primary aromatic amines, sulfonamides, hydrazines, hydrazides, and primary aliphatic amines.
The amide derivatives formed from acetylation of these amino functionalities are generally inactive and
nontoxic (Wilson and Gisvold, 109).
134. The undesirable side effects of aminoglycosides, particularly ototoxicity and nephrotoxicity, have led to
restrictions in their systemic use to serious infections or infections caused by bacterial strains resistant to
other agents (Wilson and Gisvold, 272).
135. Benzalkonium chloride is a cationic surfactant. Cationic surfactants are quaternary ammonium compounds
that ionize in water and exhibit surface-active properties. They are inactivated by soaps and other anionic
detergents (Wilson and Gisvold, 137).
136. Acetazolamide (Diamox) is rarely the drug of choice for diuretic therapy because it causes systemic acidosis
and alkaline urine (Mycek, 227).
137. The antipsychotic drug loxapine succinate (Loxitane) is a dibenzoxazepine compound (Wilson and Gisvold,
405).
138. Diphenoxylate is a structural analog of meperidine. Although this drug has a strong structural relationship to
the meperidine-type analgesics it has very little, if any, such activity itself. Its most pronounced activity is its
ability to inhibit excessive gastrointestinal motility, an activity reminiscent of the constipating side effect of
morphine itself (Wilson and Gisvold, 650).
139. With penicillin, another goal in the research on semisynthetic penicillins – an antibacterial spectrum broader
than that of penicillin G – has been attained. This product is active against the same gram-positive organisms
that are susceptible to other penicillins, and it is more active against some gram-negative bacteria and
enterococcal infections (Wilson and Gisvold, 243).
140. The indication for lithium salts are acute mania and as a prophylactic to prevent occurrence of he mania of
bipolar manic-depressive illness (Wilson and Gisvold, 386-387).
141. Liquefied Phenol, USP is phenol containing 10% water (Wilson and Gisvold, 132).
142. Castellani’s paint is carbol-fuchsin solution (Wilson and Gisvold, 140).
143. Penicillamine is an effective antidote for the treatment of poisoning by copper.
144. Tetracycline is a broad spectrum, bacteriostatic agent Mycek, 311).
145. Acacia is insoluble in alcohol, but almost completely soluble in twice its weight of water at room temperature
(Remington, 1030).
146. The drug used in all types of tuberculosis is isoniazid. Isoniazid is a remarkably effective agent and continues
to be one of the primary drugs for the treatment of tuberculosis (Wilson and Gisvold, 160).
147. Levarterenol (Levophed) is L-norepinephrine (Wilson and Gisvold, 423).
148. One of the greatest virtues of streptomycin is its effectiveness against the tubercle bacillus (Wilson and
Gisvold, 275).
149. The tetracyclines are truly broad-spectrum antibiotics with the broadest spectrum of any known antibacterial
agents. They are active against a wide range of gram-positive bacteria, spirochetes, mycoplasmas,
rickettsiae, and chlamydiae (Wilson and Gisvold, 284).
150. Stable chelate complexes are formed by the tetracyclines with many metals, including calcium, magnesium,
and iron. Such chelates are usually very insoluble in water, accounting for the impairment in absorption of
most tetracyclines in the presence of milk, calcium-, magnesium-, and aluminum-containing antacids, and
iron salts (Wilson and Gisvold, 283).
151. Dicloxacillin is an antistaphylococcal penicillin and is penicillinase-resistant (Mycek, 300).
152. Norfloxacin is effective against both gram-negative (including Pseudomonas aeruginosa) and gram-positive
organisms in treating complicated and uncomplicated UTIs and prostatitis, but not in systemic infections
(Mycek, 324).
153. Oxacillin is an antistaphylococcal penicillin and is penicillinase-resistant (Mycek, 300).
154. Rancidity of fats may be due to oxidation of double bonds.
155. A thiazide diuretic can enhance the action of amphetamine.
156. Surfactants are characterized by the presence of water-solubilizing and fat-colubilizing groups in the same
molecule. These are substances that absorb to surfaces or interact to reduce surface or interfacial tension.
May be used a swetting agents, detergents or emulsifying agents (Ansel, 90).
157. Piperazine citrate (Antapar), gential violet, pyrivinium pamoate (Povan) and thiabendazole (Mintezol) are
anthelmintics (Wilson and Gisvold, 180).
158. Zidovudine (Azidothymidine; AZT) is active against retroviruses, a group of RNA viruses responsible for AIDS
and certain types of leukemias (Wilson and Gisvold, 172).
159. Trimethoprim is a folate-reductase inhibitor (dihydrofolate reductase inhibitor) (Mycek, 293).
160. The penicillins contain a beta-lactam-thiazolidine structure (Dewick, 402).
161. Duracef is Cephadroxil (Remington, 1527).
162. Lindane (Kwell) is employed locally as a cream, lotion, or shampoo for the treatment of scabies and
pediculosis. Pediculicides are compounds effective in the treatment of infections caused by the three species
of sucking lice known as Pediculus humanus var. capitis (the head louse), P. humanus var. corporis (the body
louse) and Phthirius pubis (the crab louse) (Wilson and Gisvold, 188; Remington, 1565).
163. An antibiotic that is obtained from Streptomyces noursei is nystatin (Wilson and Gisvold, 150).
164. Vincristine and vinblastine are alkaloids with anticancer activity obtained from the Madagascar periwinkle
Catharanthus roseus (Dewick, 330).
165. Alkylating agents exert their cytotoxic effects by covalently binding to nnucleophilic groups on various cell
constituents. The most common adverse reactions to these agents is alopecia (Mycek, 387,389).
166. Verapamil, Nifedipine and Diltiazem are calcium-channel blockers. Atenolol is a beta-blocker (Mycek, 184,
187).
167. The generic name of Diabinese is chlorpropramide (Wilson and Gisvold, 892).
168. Furosemide is a loop or high ceiling diuretic that acts on the ascending loop of Henle (Mycek, 227).
169. Mannitol is used as an osmotic diuretic. Osmotic diuretics are a mainstay of treatment for patients with
increased intracranial pressure, or acute renal failure due to shock, drug toxicities and trauma. It is not
absorbed when given orally. The agent can only be given intravenously (Mycek, 233).

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170. Morphine, codeine and nalbuphine are narcotic analgesics (Mycek, 133).
171. Halothane is the prototype to which newer inhalation anesthetics are compared. While halothane is a potent
anesthetic, it is a relatively weak analgesic (Mycek, 113).
172. Levodopa is used in the treatment of parkinson’s disease (Mycek, 84).
173. The generic name of Nubain is nalbuphine hydrochloride (Wilson and Gisvold, 902).
174. Methenamine is also called Urotropin. In order to act, methenamine must decompose at an acidic pH of 5.5
of less in the urine, thus producing formaldehyde, which is toxic to most bacteria (Wilson and Gisvold, 900;
Mycek, 327).
175. Peripheral neuropathy caused by isoniazid can be treated with pyridoxine because isoniazid competes with
pyridoxal phosphate for the enzyme apotryptophanase (Mycek, 333).
176. Mebendazole (Antiox) is a broad spectrum anthelmintic that is effective against a variety of nematode
infestations including whipworm, pinworm, roundworm, and hookworm (Wilson and Gisvold, 182).
177. Nicotine is an addictive substance. Physical dependence on nicotine develops rapidly and is severe.
Withdrawal is characterized by irritability, anxiety, restlessness, difficulty in concentrating, headaches and
insomia. The transdermal patch and chewing gum coantaining nicoting have been shown to reduce nicotine-
withdrawal symptoms and to help smokers stop smoking (Mycek, 101).
178. Thiabendazole (Mintezol), a benzimidazole derivative, is an anthelmintic drug used primarily to treat
infections caused by Strongyloides (Wilson and Gisvold, 182).
179. The aminoglycoside antibiotics, because of their potent bactericidal action against gram-negative bacilli, are
preferred for the treatment of many serious infections. However, a pattern of bacterial resistance has
developed to each of the aminoglycosides as their clinical use has become more widespread. To prevent this,
aminoglycosides are frequently combined with other antiobiotics (Wilson and Gisvold, 273).
180. Common adverse effects of ACE inhibitors are dry cough, rashes, fever, altered taste, hypotension,
hyperkalemia and proteinuria (Mycek, 186).
181. Chloramphenicol is completely absorbed via the oral route because of its high lipophilic nature and is widely
distributed throughout the body. It readily enters the normal CSF (Mycek, 320).
182. Selective toxicity, the property of certain chemicals to destroy one form of life without harming the other, is
the cornerstone of modern antimicrobial chemotherapy. This concept is largely credited to Paul Erhlich. He is
therefore the scientist who can lay claim to the title of Father of Chemotherapy (Wilson and Gisvold, 129).
183. Significant first-pass metabolism of nitroglycerin occurs in the liver. Therefore, it is common to give the drug
either sublingually, intravenously or via a transdermal patch (Mycek, 176).
184. The nitro group is responsible for the bone marrow toxicity of chloramphenicol (Wilson and Gisvold, 305).
185. Diazepam is used in the treatment of anxiety, seizures (status epilepticus), and muscle disorders (skeletal
muscle spasm). It may also be given to facilitate amnesia while causing sedation during surgery (Mycek,
90,91,116).
186. Ceftriaxone, a third generation cephalosporin, has the longest half-life of any cephalosporin (6-8 hours)
allowing once a day dosing. It is administered parenterally. It is beta-lactamase resistant but has no acid
resistance (Mycek, 305; Wilson and Gisvold, 261).
187. More than 30 different alkaloids have been obtained from opium and its extracts, some of which are
alteration products of the alkaloids occurring naturally in the drug. The most important of these are morphine,
codeine, noscapine (formerly, narcotine), papaverine, and thebaine (Tyler, 215-216).
188. Acetaminophen, an aniline derivative, is an antipyretic with weak anti-inflammatory activity (Wilson and
Gisvold, 665).
189. Methoxyflurane is the most potent inhalation anesthetic because of its high solubility in lipid (Mycek, 114).
190. Antimetabolites used in cancer therapy are methotrexate, 6-mercaptopurine, 6-thioguanine, 5-fluorouracil,
cytarabine and fludarabine (Mycek, 373).
191. The highly polar, polycationic structure of aminoglycosides prevents adequate absorption after oral
administration. Therefore, all aminoglycosides (except neomycin) must be given parenterally to achieve
adequate serum levels (Mycek, 316).
192. Baclofen, a substituted GABA analogue, is useful in spasticity involving diseases of the spinal cord (multiple
sclerosis). It depresses monosynaptic and polysynaptic transmission (Wilson and Gisvold, 375).
193. Tetracycline forms nonabsorbable chelates with calcium ions. It may deposit in the bones and primary
dentition during calcification in growing children causing discoloration and hypoplasia of the teeth and a
temporary stunting of growth. Hepatotoxicity has occurred in pregnant women who received high doses of
tetracyclines, especially if they are experiencing pyelonephritis (Mycek, 313).
194. Neuromuscular paralysis often results after direct intraperitoneal or intrapleural application of large doses of
aminoglycosides. The mechanism responsible is a decrease in both the release of acetylcholine from
prejunctional nerve endings and the sensitivity of the postsynaptic site (Mycek, 317).
195. Amphotericin B is administered by intravenous infusion. The intrathecal route is sometimes chosen for the
treatment of meningitis caused by fungi that are sensitive to amphotericin B (Mycek, 338).
196. Griseofulvin is principally fungistatic. It is effective only for the dermophytes – Trichophyton, Microsporum,
and Epidermophyton (Mycek, 343).
197. Piperazine, pyrantel pamoate, mebendazole and thiabendazole are effective and clinically useful against
worm infestation caused by Ascaris lumbricoides. Niridazole is an antischistosomal whose principal
therapeutic application is in the treatment of infections caused by Schistosoma haematobium (urinary
schistosomiasis) (Wilson and Gisvold, 180-182).
198. An ideal local anesthetic should have a rapid onset of action and a short duration of action. The action must
last long enough to allow time for the contemplated surgery, yet not so long as to entail an extended period of
recovery (Wilson and Gisvold, 585).
199. Mebendazole possesses “triad of features” which includes antiamebic, antigiardiasis, and antitrichomonal
(Wilson and Gisvold, 182).
200. Heparin is an extract of animal tissue. It is extracted for commercial use form porcine intestines or bovine
lung (Mycek, 198).
201. The drug of choice for acute attack of Plasmodium vivaz is chloroquine. It is highly specific for the asexual
form of Plasmodium vivax and Plasmodium falciparum (Mycek, 351).
202. Drugs which act on erythrocytic cycle of malarial parasite will be effective for suppressive prophylaxis.
203. Antipyretic analgesics raise the pain threshold.
204. Griseofulvin is tecommended for the systemic treatment of refractory ringworm infections of the body, nails,
hair, and feet (tinea corporus, tinea inguium, tinea capitis and tinea pedis) caused by various species of
dermatoophytic fungi, including Trichophyton, Microsporum, and Epidermophyton (Wilson and Gisvold, 154).

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205. Acetaminophen has analgesic and antipyretic activities. Aspirin is used as an antipyretic, analgesic, and
antirheumatic. Its use in rheumatism has been reviewed, and it is said to be the drug of choice (Wilson and
Gisvold, 661, 668).
206. The highly polar, polycationic structure of aminoglycosides prevents adequate absorption after oral
administration. For this reason, oral neomycin and streptomycin are used for sterilization of bowel and for
dysentery (Mycek, 316).
207. Indomethacin is a potent anti-inflammatory agent. It is also beneficial in the control of pain associated with
uveitis and postoperative ophthalmic procedures, and as an antipyretic for Hodgkin’s disease, when the fever
is refractory to other agents (Mycek, 409).
208. Benzathine penicillin is a depot penicillin preparation. It is very insoluble in water, requiring about 3000 mL to
dissolve 1 g. This property gives the compound great stability and prolonged duration of effect (Wilson and
Gisvold, 241).
209. Dimercaprol (BAL, British Anti-Lewisite) is effective topically and systemically as an antidote for poisoning
caused by arsenic, antimony, mercury, gold, and lead. It forms a chelate with the metal which is relatively
nontoxic, metabolically conjugated as glucuronides, and rapidly excreted. It does not affect platelet activity
(Wilson and Gisvold, 180).
210. 6-aminopenicillanic acid is the common nucleus of all penicillins. The members of this family differ from one
another in the R substituent attached to 6-aminopenicillanic acid residue (Mycek, 297).
211. Diphenoxylate is a structural analog of meperidine. Although this drug has a strong structural relationship to
the meperidine-type analgesics it has very little, if any, such activity itself. Its most pronounced activity is its
ability to inhibit excessive gastrointestinal motility, an activity reminiscent of the constipating side effect of
morphine itself (Wilson and Gisvold, 650).
212. Anti-arrhythmic drugs
Class I Class II Class III Class IV
(Sodium-channel blockers) (Beta-adrenoreceptor Potassium-channel (Calcium-channel blockers)
blockers) blockers
Disopyramide (IA) Esmolol Amiodarone Diltiazem
Procainamide (IA) Metoprolol Bretylium Verapamil
Quinidine (IA) Pindolol Sotalol
Lidocaine (IB) Propranolol OTHERS:
Mexiletine (IB) Adenosine
Tocainide (IB) Digoxin
Flecainide (IC)
Propafenone (IC)
(Mycek, 163)
213. Clofibrate (fibric acid derivative), cholestyramine and colestipol (bile acid binding resins), and dextrothyroxine
(thyroid hormone preparation) are used to reduce blood cholesterol levels (Wilson and Gisvold, 568-570).
214. Pentaerythritol tetranitrate relaxes smooth muscle of smaller vessels in the coronary vascular tree. It is used
prophylactically to reduce the severity and frequency of anginal attacks, and is usually administered in
sustained-release preparations to increase its duration of action (Wilson and Gisvold, 539).
215. Carbamazepine is a primary drug for the treatment of all seizure types except absence (Mycek, 145).
216. Like oxacillin, cloxacillin is relatively resistant to acid hydrolysis and, therefore, may be administered orally
with good effect (Wilson and Gisvold, 242).
217. Tranylcypromine (monoamine oxidase inhibitor), amitryptiline (tricyclic antidepressant) and fluoxetine
(selective serotonin reuptake inhibitor) are antidepressant drugs. Thioridazine (phenothiazine) and clozapine
(dibenzodiazepine) are neuroleptic drugs (Mycek, 119, 127).
218. Sulfacetamide sodium is especially suited, as a solution, for repeated topical applications in the local
management of ophthalmic infections susceptible to sulfonamide therapy (Wilson and Gisvold, 200).
219. Benzodiazepines are useful in treating the anxiety. Clonazepam is a benzodiazepine that is mainly used in
the treatment of epilepsy. It is useful in absence and myoclonic seizures (Wilson and Gisvold, 391; Mycek,
90-91).
220. Macrolides (the family of erythromycin) are generally considered to be bateriostatic. They may be cidal at
higher doses (Mycek, 317).
221. Commercial production of biosynthetic penicillins today depends chiefly on various strains of Penicillium
notatum and Penicillium chrysogenum (Wilson and Gisvold, 231).
222. In choosing a specific benzodiazepine for the treatment of insomia, the age of the patient, the underlying
sleep disorder being treated, the half-life of the drug and the absorption of the drug should be considered.
223. Bacitracin has found its widest use in topical preparations for local infections. It is not absorbed from the
gastrointestinal tract; accordingly, oral administration is without effect, except for the treatment of amebic
infections within the alimentary canal (Wilson and Gisvold, 302).
224. Hypertensive emergency is a rare, but life-theatening situation in which the diastolic blood pressure is either
over 150 mmHg (with systolic blood pressure greater than 210 mmHg) in an otherwise healthy person. The
preferred agent for hypertensive emergencies is sodium nitroprusside (Mycek, 191).
225. Superior to acyclovir in the treatment of herpes viruses in the CNS in neonates is vidarabine. It penetrates
into the brain and thus is effective in the treatment of herpes simplex encephalitis (Mycek, 368).
226. Alkylating agents exert their cytotoxic effects by covalently binding to nucleophilic groups on various cell
constituents. Alkylation of DNA is probably the crucial cytotoxic reaction that is lethal to the tumor cell.
Guanine is the most susceptible base to alkylating agents (Mycek 388).
227. Vincristine is effective against acute leukemia. It is used in the combination chemotherapy for Hodgkin’s
disease (Wilson and Gisvold, 347).
228. Amphotericin B is the drug of choice in the treatment of systemic mycoses. It is administered by intravenous
infusion (Mycek 337-338).
229. In general, gram-positive microorganisms have cell walls that are easily traversed by penicillins and therefore
9in the absence of resistance) are susceptible these drugs. Penicillin is the drug of choice for gonococcal
infection, pneumococcal infection, treponema pallidum infection, and streptococcal infection (Mycek, 299).

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230.
Prodrug Active Drug
Levodopa Dopamine (Mycek, 85)
Prednisone Prednisolone (Mycek, 393)
Bacampicillin Ampicillin (Wilson and Gisvold, 244)
Cyclophosphamide Phosphoramide mustard (Mycek, 388)
Salbutamol
231. Benzyl benzoate is an effective scabicide when topically applied. Immediate relief from itching probably
results from a local anesthetic effect (Wilson and Gisvold, 187).
232. The introduction of an alpha-amino group, such in ampicillin (or amoxicillin) creates an additional asymmetric
center. It is noteworthy that the extension of antibacterial spectrum brought about by the substituent applies
only to the D-isomer, which is two to eight times more active than either the L-isomer against various species
of gram-negative bacilli (Wilson and Gisvold, 237).
233. Bone marrow depression resulting in pancytopenia is not a characteristic toxic effect of oxytetracycline.
Some adverse effects of the tetracyclines are: gastrointestinal disturbances, vertigo, liver failure, phototoxicity
and deposition of drug in bones and teeth especially in children (Mycek, 314).
234. Antibiotics used in cancer therapy owe their cytotoxic action to their interaction with DNA, leading to
disruption of DNA function. They are cell-cycle specific. Some antibiotics that have antimalignant property
are: bleomycin, dactinomycin, daunorubicin, doxorubicin, idarubicin, plicamycin and mitomycin (Mycek, 373,
384).
235. Florey and Chain utilized freeze-drying in isolating penicillin.
236. Sulfanilamide is the metabolite of the red dye, prontosil, responsible for its antimicrobial property (Wilson and
Gisvold, 191).
237. Interferon is a family of naturally occurring inducible glycoproteins that interfere with the ability of viruses to
infect cells. It has been approved for treatment of hepatitis B and C, as well as against cancers such as hairy
cell leukemia and Kaposi’s sarcoma (Mycek, 371).
238. Chloramphenicol is not used for prophylaxis but for treatment of typhoid fever.
239. The major cause of the behavioral effects of amphetamine is probably due to release of dopamine rather
than release of norepinephrine. The CNS stimulant effects of amphetamine and its derivatives have led to
their use in the therapy of depression, hyperactivity in children, narcolepsy, and appetite control.
Hypertension is an adverse effect of amphetamine (Mycek, 103-104).
240. Whereas nitrous oxide is a potential analgesic, it is a weak general anesthetic. Thus, it is frequently combined
with other more potent agents. This anesthetic does not depress respiration nor does it produce muscle
relaxation (Mycek, 114-115).
241. A drug receptor may be an isolable enzyme, a functional component of a cell membrane, a protein or a
nucleic acid.
242. The active form of folate is the tetraydro-derivative that is formed through reduction by dihydrofolate
reductase. This enzymatic reaction is inhibited by trimethoprim, leading to a decrease in the folate coenzyme
for purine, pyrimidine and amino acid synthesis (Mycek, 293).
243. A drug molecule which possesses both intrinsic activity and affinity.
244. Penicillamine is used as a chelating agent in the treatment of poisoning by heavy metals. It is an effective
antidote for copper poisoning and used in the treatment of Wilson’s disease (Mycek, 414).
245. 8-Mercaptoquinoline, 8-hydroxyquinoline and 4-AZA-oxime are chelating agents.
246. Dimecaprol is also known as BAL (British anti-Lewisite), dithioglycerol and 2,3-dimercapto-1-propanol
(Wilson and Gisvold, 180).
247. Tetrachloroethylene is synthesized from dry hydrogen chloride and carbon monoxide at 300 degrees and
200 atm pressure. The effectiveness of tetrachloroethylene as an anthelmintic is due to its local irritant
properties. Its specific use in medicine is in the treatment of hookworm infestation (Wilson and Gisvold, 180)
248. Lipid soluble drugs readily move across most biological membranes through passive diffusion. The
movement does not involve a carrier (Mycek, 4).
249. Affinity is the tendency of the drug to combine with the receptor.
250. Bisacodyl is the generic name of Dulcolax.
251. Penicillin G is benzylpenicillin (Wilson and Gisvold, 239).
252. Organo-silicon polymers containing O and Si atoms with a substituent organic group are silicons.
253. Eugenol is a phenol primarily obtained from clove oil. It has local anesthetic, as well as antiseptic activity and
is used to relieve toothaches (Wilson and Gisvold, 133-134).
254. Cyanocobalamin is the treatment of pernicious anemia.
255. Erythromycin, Spiramycin and Oleandromycin are marolide antibiotics.
256. Erythromycin is a macrolide antibiotic which was found in the soil of Iloilo.
257. Quinine is obtained from the bark of Cinchona species. It is an antimalarial agent. Quinine’s antimalarial
action is believed to be the intercalation of quinoline moiety into the DNA of the Plasmodium parasite, thereby
reducing the effectiveness of DNA to act as a template (Tyler, 208).
258. Polyene antibiotics include amphotericin B (from Streptomyces nodosus) and nystatin (from Streptomyces
noursei). They appear to bind with sterols in the cell membrane to cause disorganization and loss of cell
constituents, especially potassium ion (Wilson and Gisvold, 150-151).
259. Bulk transport is also known as solvent shift.
260. The primary medicinal uses of alcohol are external: as an antiseptic, preservative, mild counterirritant or
solvent. Rubbing alcohol is employed as an astringent, rubefacient, refrigerant and mild local anesthetic
(Wilson and Gisvold, 130).
261. Carbonic acid gas is carbon dioxide.
262. Erythromycin is effective against the same organisms as penicillin G, therefore, it is used in patients allergic
to the penicillins (Mycek, 317).
263. Adsorbents are chemically inert powders that have the ability to adsorb gases, toxins, and bacteria. The fine
state of subdivision of these inert powders confers high adsorptive capacity upon them (Remington, 1238).
264. Cotrimoxazole is the drug of choice for urinary tract infections. The synergistic antimicrobial activity of
cotrimoxazole results from its inhibition of two sequential steps in the synthesis of tetrahydrofolic acid.
Sulfamethoxazole inhibits the incorporation of PABA into folic acid, and trimethoprim prevents reduction of
dihydrofolate to tetrahydrofolate (Mycek, 294).
265. Voltaren is diclofenac sodium ((Wilson and Gisvold, 665).
266. The chemical name of phenethicillin is phenoxyethyl penicillin.

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267. The redox properties of methylene blue provide the basis for its use as an antidote in cyanide poisoning. In
high concentrations, it promotes the conversion of hemoglobin to methemoglobin, which because of its high
affinity for cyanide ion diverts it from inactivating cytochrome C. In low concentrations, methylene blue has
the opposite effects and has been used to treat drug-induced methemoglobinemia (as in nitrate poisoning)
(Wilson and Gisvold, 140).
268. Streptomycin is an aminoglycoside used to treat tuberculosis. Its mechanism of action is the inhibition of
protein synthesis (Mycek, 315).
269. Chelates consist of a partial ring of atoms that close up by holding a given atom, usually a metal, in a
molecular claw (Remington, 166).
270. Absorption is the transfer of a drug from its site of administration to the blood stream (Mycek, 4).
271. Methyl salicylate is produced synthetically or is obtained by maceration and subsequent distillation with
steam from the leaves of Gaultheria procumbens Linne (Family Ericaceae) or form the bark of Betula lenta
Linne (Familiy Betulaceae). The oil is also known as gaultheria oil, wintergreen oil, betula oil or sweet birch oil
(Tyler, 135).
272. Cathartics are agents that facilitate the evacuation of bowels.
273. Dehydrated ethanol (absolute alcohol) contains not less than 99% by weight of ethanol. It is prepared
commercially by azeotropic distillation of an ethanol and benzene mixture (Wilson and Gisvold, 131).
274. Nubain is nalbuphine hydrochloride (Wilson and Gisvold, 648).
275. Kaopectate is kaolin plus pectin. It is used medicinally as an adsorbent. It is perhaps of value in the
treatment of diarrhea caused by agents capable of being adsorbed; eg. the diarrhea of food poisoning
(Remington, 1238).
276. Ascorbic acid is the least stable of all vitamins. It is stable in the dry state but is easily oxidized n aqueous
solution in the presence of air (Remington, 1805).
277. A change in structure of isoniazid caused decrease in the potency of the drug.
278. Retinoic acid is the most toxic vitamin. Tretinoin (retinoic acid) is believed to exert its antineoplastic effect by
promoting cellular differentiation toward normal cells (Wilson and Gisvold, 834).
279. The kidney is the major organ of excretion.
280. The generic name of Benadryl AH is diphenhydramine (Wilson and Gisvold, 608).
281. In 1932, Gerhard Domagk began a study of a bright red dye, later to be named Prontosil, and found that it
caused remarkable cures of streptococcal infections of mice (Wilson and Gisvold, 191).
282. Halazone is a chlorine-containing anti-infective. Its sodium salt is used to disinfect drinking water (Wilson and
Gisvold, 136).
283. Dapsone is used in the treatment of both lepromatous and tuberculoid types of leprosy (Wilson and Gisvold,
204).
284. In the body niacin is converted to niacinamide, which is an essential constituent of coenzyme I and II that
occur in a wide variety of enzyme systems involved in the anaerobic oxidation of carbohydrates. The
coenzyme serves as a hydrogen acceptor in the oxidation of the substrate (Remington, 1808).
285. Vitamin D is known popularly as the sunshine vitamin because it is formed by the action of the sun’s
ultraviolet rays on precursor sterols in the skin (Remington, 1800).
286. Vitamins A, D, E and K are the fat-soluble vitamins.
287. Since aspirin is acidic, the relatively low pH of the stomach favors the absorption of aspirin because at low
pH, aspirin is in its unionized (more absorbable) form.
288. Helium, because of its low density compared to nitrogen, is used to prepare a gaseous mixture composed of
20% oxygen and helium. This mixture is used to alleviate respiration difficulty (Remington, 382).
289.
290. Methylene blue is a dye used in vital nerve staining.
291. The excretion of weakly basic drug will be more rapid in acidic urine than in basic urine because the drug will
exist primarily in the ionized form, which cannot be easily reabsorbed.
292. Superinfection is common with those which suppress the normal bacterial flora.
293. Hemolytic anemia occurs in patients with low levels of glucose-6-phosphate dehydrogenase. Other types of
anemia occurring as side effect of chloramphenicol include reversible anemia, which is apparently dose-
related and occurs concomitantly with therapy, and aplastic anemia, which is idiosyncratic and usually fatal
(Mycek, 321).
294.
295. Bactrim and Septrim are tradenames for a fixed-dose combination of sulfamethoxazole and trimethoprim.
296. In high doses, acetylsalicylic acid is most likely to cause tinnitus and hearing.
297. Pharmacologic effects of the classic antihistamines include sedation with low doses, an antipruritic effect and
drying of salivary and bronchial secretion.
298.
299. Ketroconazole does not enter the CNS (Mycek, 340).
300. Large overdose of acetaminophen is likely to cause hepatic necrosis.

REFERENCES:

Ansel, Howard C., et. al. Pharmaceutical Dosage Forms and Drug Delivery Systems, 7th ed. Philadelphia:
Lippincott Williams and Wilkins, 1999.
Delgado, Jaime N. and Remers, William A, ed. Wilson and Gisvold’s Textbook of Organic Medicinal and
Pharmaceutical Chemistry, 9th ed. Philadelphia: JB Lippincott Company, 1991.
Dewick, Paul M. Medicinal Natural Products: A Biosynthetic Approach. New York: John Wiley and Sons, 1997.
Gennaro, Alfonso R. Remington: The Science and Practice of Pharmacy, 20th ed. Philadelphia: Lippincott Williams
and Wilkins, 2000.
Mycek, Mary J., et. al. Pharmacology, 2nd ed. Philadelphia: Lippincott-Raven Publishers, Inc., 1997.
Tyler, Varro E., et al. Pharmacognosy, 9th ed. Philadelphia: Lea and Febiger, 1988.

MANOR Review Center 47

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