Pharmaceutical Organic Chemistry Answer Key PDF

Summary

This document contains questions and answers related to pharmaceutical organic chemistry. Topics discussed include bond length, bond polarity, hybridization of orbitals, bond strength (energy), naming organic structures, reactions of different classes of organic compounds, and their solubility. The document is an exam-style worksheet, covering various aspects of pharmaceutical chemistry.

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Pharmaceutical Organic Chemistry Answer key 1. The following statement is/are true regarding the relationship of bond length and bond polarity except: a. As the bond polarity increase, the bond length decreases b. A C-F bond has a longer bond length than C-C c. As bond polarity...

Pharmaceutical Organic Chemistry Answer key 1. The following statement is/are true regarding the relationship of bond length and bond polarity except: a. As the bond polarity increase, the bond length decreases b. A C-F bond has a longer bond length than C-C c. As bond polarity increases the bond length also increases d. A and B only e. B and C only 2. The following statement/s is/are true regarding the relationship of hybridization of orbitals and bond length: a. As the s character increases, the bond length increases b. As the s character increases, the bond length decreases c. The bond length of acetylene is longer than the bond length of ethylene d. The bond length of ethane is shorter than the bond length of ethylene e. None of the choices 3. Bond strength or bond energy is the energy necessary to break the only bond in a diatomic molecule or to dissociate the bonded atoms to their bond state. Which of the following statements is/are true regarding its relationship with orbital hybridization, bond length and bond poarity? a. When the s character of the bonding orbitals increases, the bond energy also increases b. When the polarity of the bond increases, the bond energy also increases c. Bond energy and bond length has inverse relationship. d. All of the choices e. A and B only 4. What is the name of the following structure? a. 4 methyl hexane b. Isohexane c. 3-methyl hexane d. 2-ethyl pentane e. 2-propyl butane 5. What is the name of the following structure? a. 2-methylpentene b. 4-methylpentene c. 2-methylpentane d. 4-methylpentene e. 2-methylpentyne 6. What is the name of the following structure: CH3CH2CH2-C=CH a. 1- pentyne b. N-propylacetylene c. 4-pentyne d. 1-pentatriene e. A and B 7. The following structure is the side chain of amino acid tryptophan. What is the name of the following structure? a. Purine b. Pyrimidine c. Indole d. Quinolene e. Pyridine 8. The structure of nucleic acid base cytosine, uracil and thymine is based on following N-ring. What is the name of the following structure? a. Pyridine b. Piperidine c. Pyrazine d. Piperazine e. Pyrimidine 9. Organic pharmaceuticals are often complex molecules which have a variety of acidic and basic functional groups. The behaviour of these groups in an aqueous environment will influence the activity of the drug and its absorption in the different compartments of the body. Which of the following statement is/are true regarding the pH of the medium and the acidic/basic property of the drug? a. The pKa is a property of the drug molecule, while pH is the property of the medium b. Acidic drugs will most likely be dissociated in a basic medium c. Basic drugs will most likely be dissociated in an acidic medium d. The sum of the negative logarithm of dissociation constant of the acid and its conjugate base is always equal to 14 e. All of the above 10. Which of the following statements is/are true regarding drug distribution and pKa? a. Indomethacin (pKa=4.5) will be absorb from the stomach rather than intestinal mucosa b. Ephedrine (pKa=9.6) will be absorb from the intestinal mucosa rather than the stomach c. Both indomethacin and ephedrine will be absorbed from the stomach rather than the intestinal mucosa d. Both indomethacin and ephedrine will be absorbed from the intestinal mucosa rather than the stomach e. A and B only 11. These lipid soluble compounds are also paraffin or saturated hydrocarbons. They commonly undergo halogination and combustion reaction and, in vivo, terminal carbon or side chain hydroxylation may occur. a. Alkanes b. Alkenes c. Aromatic hydrocarbon d. Alkynes e. Alkyl halides 12. These lipid soluble compounds are also known as olefins and unsaturated hydrocarbons. Their common reactions are the addition of hydrogen or halogenation, hydration (to form glycols), and oxidation (to form peroxides). a. Alkanes b. Alkenes c. Aromatic hydrocarbon d. Alkynes e. Alkyl halides 13. The structure of these compounds is based on benzene. These molecules exhibit multicenter bonding, which confers unique chemical properties. a. Alkanes b. Alkenes c. Aromatic hydrocarbon d. Alkynes e. Alkyl halides 14. Which of the following alcohols is the most water soluble? a. Methanol b. Ethanol c. Propanol d. Butanol e. Phentanol 15. Which of the following statement is /are true regarding oxidation of alcohols? a. Primary alcohols are oxidized to ketones b. Secondary alcohols are oxidized to aldehydes and then to acids c. Tertiary alcohols ordinarily are not oxidized d. A and B only e. All of the statements are correct 16. Which of the following compounds has a general formula of R-O-R with an oxygen bonded to 2 carbon atoms? a. Aldehydes b. Ether c. Phenols d. Ketones e. Esters 17. These compounds have a general formula of R-CHO and contain a carbon group (C=O). The common reactions of these compounds are oxidation and hemiacetal and acetal formation. a. Aldehydes b. Ether c. Phenols d. Ketones e. Esters 18. Which of the following statements is/are correct about the water solubility of amines? a. Branching decreases water solubility b. Secondary amines are more water soluble than primary amines c. Tertiary amines are the least water soluble compared to primary and secondary amines d. A and B only e. A and C only 19. These compounds have a general formula of RCOOR and commonly undergo hydrolysis to form carboxylic acid and alcohol. a. Ketones b. Ether c. Esters d. Amides e. Carboxylic acid 20. These compounds have a general formula of RCOOH and commonly undergo salt formation with bases, esterification and decaroxylation. a. Ketones b. Ether c. Esters d. Amides e. Carboxylic acid 21. Which of the following classes of organic compounds reacts to form salts with hydrochloric acid? a. b. c. d. e. 22. Which of the following terms best describes the following reaction: a. Acetylation b. Reductive cleavage c. Oxidative deamination d. Decarboxylation e. N-dealkylation 23. Which of the following functional group when added to a benzene nucleus, decreases the lipid solubility of the benzene I. A carboxylic acid group II. An ethyl group III. A phenolic group a. I only is correct b. III only is correct c. I, II, III are correct d. II and III are correct e. I and III are correct 24. For questions 24-26, refer to the drug molecule : The drug molecule is soluble in I. An aqueous base II. An aqueous acid III. Water a. I only is correct b. III only is correct c. I, II, III are correct d. II and III are correct e. I and III are correct 25. Decomposition the drug molecule at room temperature most likely would occur by a. Hydrolysis of the ester b. Reduction of the carboxylic acid c. Oxidation of the ester d. A and B only e. B and C only 26. Reactions that will be possible metabolic pathways for the drug molecule include I. Ring hydroxylation II. Glucuronide formation III. Enzymatic hydrolysis a. I only is correct b. III only is correct c. I, II, III are correct d. II and III are correct e. I and III are correct 27. Which of the following statements is/are true regarding drugs? a. Drug are compounds that interact with a biological system to produce a biological response b. No drug is totally safe c. Poisons a t low doses can be used a s drugs d. Drugs used in high dosed can be considered as poisons e. All of the above 28. Most drugs bind to their targets by means of intermolecular bonds. Which of the following statements is/are true regarding these forces? a. An ionic or electrostatic bond is the strongest of the intermolecular bonds and takes place between groups having opposite charges b. Hydrogen bonds are very weak interactions that involve interaction between hydrophobic regions of different molecules c. Van der Waals forces of interaction are cost by transient dipole-dipole interaction d. A and B only e. A and C only 29. A range of the following compounds in increasing strength of carbonyl oxygen as a hydrogen bond acceptor: a. IV, III, II, I b. I, II, III, IV c. II, III, I, IV d. I, III, IV, II e. III, II, I, IV 30. This is the type of enzyme inhibition where the drug react with the enzyme and forms a covalent bond. a. Reversible inhibition b. Irreversible inhibition c. Competitive inhibition d. Uncompetitive inhibition e. Non-competitive inhibition 31. These type of inhibitor binds to the enzyme substrate complex in which its effect cannot be overcome by increasing the substrate concentration a. Reversible inhibitor b. Irreversible inhibitor c. Competitive inhibitor d. Uncompetitive inhibitor e. Allosteric inhibitor 32. Which of the following drugs is incorrectly match with its target enzyme? a. Imatinib: tyrosine kinase b. Zidovudine: HIV reverse transcriptase c. Zileuton: 5 lipoxygenase d. 5-flourouracil: Bactericidal topoisomerase e. Sildenafil: phosphodiesterase enzyme 33. This type of inhibitor binds to a binding site different from the active site. They alter the shape of the enzyme such that the active site is no longer recognizable. a. Reversible inhibitor b. Irreversible inhibitor c. Competitive inhibitor d. Uncompetitive inhibitor e. Allosteric inhibitor 34. Evaluate the following statements: Antagonists can mimic the natural messengers and activate receptors. Antagonist can bind to the receptor but they do not activate it. a. Both statements are correct b. Both statements are incorrect c. Only the first statement is correct d. Only the second statement is correct. 35. The following factors must be considered in designing an agonist: a. The drug must have the correct binding groups. b. Specific functional groups must be correctly positioned. c. The size and shape of the drug molecule. d. A and B only e. All of the above 36. Which of the following statements is/are true regarding structurally-specific and structurally non specific drugs? I. The biologic effect of structurally non specific drugs is more closely correlated with the physical properties of the molecules than with the chemical structure. II. Examples of structurally non specific drugs are 6-mercaptopurine, phenothiazines, pyrimethamine, and primaquine. III. The biologic effect of structurally specific drugs, although not completely independent of the physical properties, depends on certain chemical structure on drug molecule. Chemical reactivity of the drug plays an important role as reflected in bonding propensities and exactness of fit on the receptors. IV. General anesthetics, hypnotics and volatile insecticides are typical examples of structurally specific drugs. a. I only is correct b. III only is correct c. I, II, III, and IV is correct d. II and IV is correct e. I and III is correct 37. Which of the following drug-enzyme pairs is/are correctly matched? I. Penicillins – transpeptidase II. Cephalosphorins – transpeptidase III. Pyrimethamine – Dihydrofolate reductase IV. Epinephrine – Adenylyl cyclise a. I only is correct b. III only is correct c. I, III, and IV are correct d. I, II, and IV are correct e. I, II, III, and IV are correct 38. It is generally conceived that an exact fit of the drug molecule and receptor is necessary to evoke maximal biologic response that is imperative to consider the stereochemical makeup of drugs. Which of the following statements is/are true regarding the biologic activity of some stereochemical isomers? I. Only the (-) isomer of ascorbic acid has antiscorbutic activity\ II. Only the D isomers of alpha and beta glucose show high affinity for the red blood cell sugar transfer stem. III. Only the (-) isomer of alpha methyldopa has hypotensive activity IV. Only the D(threo) isomer has high anti-bacterial activity a. I only is correct b. III only is correct c. I,III, and IV are correct d. I, II, and IV are correct e. I, II, III, and IV are correct 39. What is the rate-limiting step in drug absorption of orally administered solid dosage forms? a. Dissolution rate b. Metabolism rate c. Elimination rate d. A and B only e. B and C only 40. Which of the following factors can influence the dissolution rate of drugs from solid dosage forms and hence, the therapeutic activity? I. Solubility, particle size, crystalline form and salt form of the drug II. Rate of disintegration in the gastrointestinal lumen III. Gastric pH, motility and presence of food at the absorption site a. I only is correct b. III only is correct c. I, II, and III are correct d. II and III are correct e. I and III are correct 41. Which of the following statements is/are true regarding renal excretion of drugs? I. Renal excretion involves three processes: glomerular filtration, secretion and tubular reabsorption. II. Both the free drug and the drug bond to plasma proteins are filtered by the kidneys. III. Drugs with high lipid/water partition coefficients are reabsorbed readily while those with low lipid/water partition coefficients are unable to diffuse back across the tubular membrane and are excreted in the urine unless reabsorbed by an active carrier system. IV. Altering the pH of urine can result to termination of biologic activity of weakly acidic and basic drugs. a. I only is correct b. III only is correct c. I, III, and IV are correct d. I, II, and IV are correct e. I, II, III, and IV are correct 42. Which of the following statements is/are true regarding Phase I and Phase II Metabolic reactions? I. Phase I reactions include oxidation, hydroxylation, reduction and hydrolysis-enzymatic reactions in which a new functional group in introduced into the drug molecule or an existing functional group is modified making the drug more polar and more readily excreted. II. Phase II reactions are enzymatic syntheses whereby a functional group is masked by the addition of a new group, for example, acetyl, sulphate, glucoronic acid or certain amino acids, which increases the polarity of the drug. III. Most drugs undergo phase I reactions only. IV. Drugs that are resistant to drug-metabolizing enzymes or that are hydrophilic are excreted largely unchanged. a. I only is correct b. III only is correct c. I, III, and IV are correct d. I, II, and IV are correct e. I, II, III, and IV are correct 43. Which of the following statements regarding NADPH-Dependent Oxidative Reactions in Liver Microsomes is/are correct? I. Aniline is converted to p-Aminophenol by aromatic hydroxylation II. Codeine is converted to morphine and formaldehyde by N-dealkylation. III. Imipramine is converted to Despiramine by O-dealkylation IV. Amphetamine is converted to Phenylacetone by deamination a. II only is correct b. III only is correct c. I and IV are correct d. II and III are correct e. I, II, III and IV are correct 44. Phase I metabolic transformation introduce new and polar functional groups into the molecule, which may produce one or more of the following changes, except: a. Decreased pharmacologic activity-deactivation b. Increased toxicity – intoxication c. Altered pharmacologic activity d. Increased pharmacologic activity – activation e. None of the choices 45. Which of the following Phase II pathway is correctly paired with their activated conjugating immediate? I. Glucoronic acid conjugation: uridine phosphate glucoronic acid (UDP-GA) II. Sulfate conjugation: 3’-phospho adenosine-5’-phosphosulfate (PAPS) III. Methylation: S-adenosylmethionine IV. Amide synthesis: Coenzyme A a. II only is correct b. III only is correct c. I and IV are correct d. II and III are correct e. I, II, III, and IV are correct 46. Sulfonamides can undergo which metabolic pathway? I. Acetylation at the N4 amino group II. Conjugation with glucoronic acid or sulphate at the N4 amino group III. Acetylation or conjugation with glucoronic acid at the N1 amino group\ IV. Hydroxylation and conjugation in the heterocyclic ring, R a. II only is correct b. III only is correct c. I and IV are correct d. II and III are correct e. I, II, III, and IV are correct 47. The first purely synthetic antimicrobial drug which was developed by Paul Erlich. This drug was used in the treatment of tryponosomiasis and syphilis. a. Prontosil b. Salvarsan c. Phenol d. Streptomycin e. Penicillin 48. Which of the following antibacterial agents acts by inhibiting the metabolism of microbial organism but not of the host? a. Sulfonamides b. Polymyxins c. Penicillins d. Rifamycin e. Nalidixic acid 49. Which of the following antibacterial agents inhibit s bacterial cell wall synthesis? a. Sulfonamides b. Polymyxins c. Penicillins d. Rifamycin e. Nalidixic acid 50. Which of the following antibacterial agent can interact with the plasma membrane of bacterial cells to affect membrane permeability? a. Sulfonamides b. Polymyxins c. Penicillins d. Rifamycin e. Nalidixic acid 51. Which of the following antibacterial agents can disrupt the synthesis of essential proteins and enzyme required for the cell’s survival? a. Sulfonamides b. Polymyxins c. Penicillins d. Rifamycin e. Nalidixic acid 52. This antibacterial agent can inhibit the nucleic acid transcription and replication which prevents cell division and.or protein synthesis. a. Sulfonamides b. Polymyxins c. Penicillins d. Rifamycin e. Nalidixic acid 53. For questions 53-55, refer to the general structure of sulphonamides below: Which part of the drug’s structure is essential for drug activity? a. Aromatic ring b. Sulphonamide group c. P-amino group d. A and B only e. All of the above 54. Which of the following statements is/are correct regarding the structure-activity relationship of sulphonamides? I. The p-amino group must be unsubstituted unless it is a prodrug or when the body can further metabolize it to generate the active compound. II. Extra substitution of the aromatic ring increases activity. III. The sulphonamide nitrogen must be primary or secondary. a. I and II only b. I and III only c. I only d. II only e. All of the above 55. Which part of the drug molecule can only be varied to retain the antibacterial activity? a. Aromatic ring b. p-amino group c. R2 d. A and B e. None of the choices 56. A sulphonamide used in combination with pyrimethamine in the treatment of Malaria. a. Sulfadiazine b. Sulfathiazole c. Sulfadoxine d. Sulfamethoxazole e. Sulfones 57. It is an orally active dyaminopyridine structure which has proved to be highly selective antibacterial and antimalarial agent often given in conjunction with sulfamethoxazole. It inhibits the enzyme dihydrofolate reductase leading to the inhibition of DNA synthesis and cell growth. a. Pyrimethamine b. Trimethoprim c. Pralidoxime d. Cotrimoxazole e. Fansidar 58. Successfully isolated penicillin using processes such as freeze-drying and chromatography. a. Alexander Flemming b. Florey and Chain c. Dorothy Hodgkins d. Beechams e. None of the above 59. Below is the general structure of penicillins. Which part of its structure is not essential for activity? a. The free carboxylic acid b. The strained B-lactam ring c. The acyl amino side chain d. The bicyclic system e. The sulphur atom 60. Addition of electron-withdrawing group into the acyl side chain of penicillin structure will render the drug a. resistant to acid hydrolysis b. Protected from B-lactamase enzymes c. Broaden the spectrum of activity d. A and B only e. All of the above 61. What is the effect of steric shields to the penicillin structure? a. It will make the drug stable in acidic conditions. b. It will be protected from B-lactamase enzymes c. It will have a broad spectrum of activity d. All of the above e. None of the above 62. This drug is a penicillin analogue with isoxazolyl incorporated in the acyl side chain making it useful against Staphylococcus aureus infections and acid resistant. a. Flucloxacillin b. Ampicillin c. Carbenicillin d. Piperacillin e. Tazobactam 63. Which of the following broad-spectrum penicillin analogues do not have a urea functional group at the alpha-position? a. Azlocillin b. Mezlocillin c. Ticarcillin d. Piperacillin e. None of the choices 64. Which of the following broad spectrum penicillin analogues has carboxylic acid group in the acyl side chain? a. Azlocillin b. Mezlocillin c. Ticarcillin d. Piperacillin e. None of the choices 65. Which of the following amino acids are the biosynthetic precursors of penicillin? a. Alanine b. Cysteine c. Valine d. A and B only e. B and C only 66. Which of the following statements is incorrect regarding the chemical structure of cephalosporins? a. Cephalosporins contain a bicyclic system containing a 4-membered B-lactam ring. b. The B-lactam ring of cephalosporins is fused to five-membered dihydrothiazine ring. c. Biosynthetic precursors of its skeleton is the same as that of penicillins. d. A and B e. B and C 67. Which of the following statements correctly describe/s the structure of carbapenems such as imipenem and meropenem? a. Absence of sulphur atom in the bicyclic ring system b. It has no acyl amino side chain c. The lactam ring is fused to a sic membered ring d. A and B only e. All of the above 68. Clavulanic acid is a beta-lactamase inhibitor used in combination with amoxicillin and other B- lactamase antibiotics. Which of the following statements correctly describe clavulanic acid? a. Clavulanic acid has a strained lactam ring in its structure. b. It has no amino acyl side chain compared to other B-lactam antibiotics c. Sulfur atom is essential for its activity against lactamases d. A and B only e. All of the above 69. Clavulanic acid, Sulbactam and tazobactam are B-lactamase inhibitors that act as suicide substrates are administered with B-lactam antibiotics to prevent their degradation. Which of the following combinations are correctly matched to their brand names? a. Sulbactam + Piperacillin = Zosyn b. Tazobactam + Ticarcillin = Timentin c. Clavulanic acid + amoxicillin = Augmentin d. A and B only e. A and C only 70. This antibiotic was isolated from Streptomyces garyphalus and inhibits bacterial cell wall synthesis by mimicking the structure of D-Alanine and inhibiting the enzymes L-Alanine racemase and D-Ala-D-Ala ligase. a. Bacitracin b. Vancomycin c. D-cycloserine d. Aztreonam e. Teicoplanin 71. A polypeptide complex produced from Bacillus subtilis that binds and inhibits the carrier lipid responsible for carrying the cell wall components across the cell membrane. a. Bacitracin b. Vancomycin c. D-cycloserine d. Aztreonam e. Teicoplanin 72. A glycopeptide antibiotic isolated from Streptomyces orientalis. a. Bacitracin b. Vancomycin c. D-cycloserine d. Valinomycin e. Teicoplanin 73. A glycopeptide antibiotic isolated from Actinomyces teichomyceticus a. Bacitracin b. Vancomycin c. D-cycloserine d. Aztreonam e. Teicoplanin 74. An antibiotic composed of 16 amino acids that is described as a ‘tunnelling’ molecule that act on the plasma membrane and result in the uncontrolled movement of ions across cell membrane leading to cell death. a. Daptomycin b. Gramicidin A c. Valinomycin d. Polymyxin B e. All of the above 75. An ionophore antibiotic with a cyclic structure obtained from Streptomyces fermentation that acts on the plasma membrane structure by allowing the uncontrolled movement of ions across the cell membrane. This ionophore is specific for potassium ions over sodium ions. a. Daptomycin b. Gramicidin A c. Valinomycin d. Polymyxin B e. All of the above 76. A polypeptide antibiotic derived from Bacillus polymyxa which can cause leakage of small molecules such as nucleosides from the cell resulting to cell death. a. Daptomycin b. Gramicidin A c. Valinomycin d. Polymyxin B e. All of the above 77. A cyclic lipopeptide derived from a bacterial strain of Streptomyces roseosporus and works by disrupting multiple functions of bacterial cell membrane. a. Daptomycin b. Gramicidin A c. Valinomycin d. Polymyxin B e. All of the above 78. A bactericidal protein synthesis inhibitor that was isolated from Streptomyces griseus. This antibiotic contains a carbohydrate and basic amine groups in its structure. a. Chlortetracycline b. Streptomycin c. Chloramphenicol d. Lincomycin e. Erythromycin 79. A bacteriostatic antibiotic which inhibits protein synthesis by binding to the 30s subunit of ribosomes and preventing aminoacyl tRNA from binding. This drug was isolated from Streptomyces aureofasciens. a. Chlortetracycline b. Streptomycin c. Chloramphenicol d. Lincomycin e. Erythromycin 80. Which of the following antibiotics has a large lactone ring, a ketone group and a glycosidically linked amino sugar in its structure? a. Chlortetracycline b. Streptomycin c. Chloramphenicol d. Lincomycin e. Erythromycin 81. Clindamycin, a sulphur containing antibiotic, must not be given with which of the following drugs because of having the same binding site at the ribosomes? a. Chlortetracycline b. Chloramphenicol c. Erythromycin d. A and B only e. B and C only 82. Quinupristin and Dalfupristin are streptogramins isolated from a. Streptomyces griseus b. Streptomyces pristinaespiralis c. Acremonium chrysogenu d. Streptomyces nodosus e. Streptomyces erythreus 83. Which of the following drug is an oxazolidinone that can prevent the formation of 70s ribosome by binding to the 50s subunit? a. Quinupristin b. Linezolid c. Ofloxacin d. Metronidazole e. Proflavine 84. Nalidixic acid was the first therapeutically agent in the class of compounds that inhibits topoisomerase enzymes, resulting in inhibition of replication and transcription. Which of the following is related to nalidixic acid? a. Quinupristin b. Linezolid c. Ofloxacin d. Metronidazole e. Proflavine 85. An aminoacridine agent used topically to treat deep surface wounds. It can interact directly with bacterial DNA by intercalation. a. Quinupristin b. Linezolid c. Ofloxacin d. Metronidazole e. Proflavine 86. The antibiotic isolated from Streptomyces mediterranei which inhibits Gram positive bacteria and works by binding noncovalently to DNA-dependent RNA polymerase and inhibiting the start of RNA synthesis. The flat naphthalene ring and several of the hydroxyl groups in its structure are essential for activity, and the drug exists in as zwitterions giving it good solubility in both aqueous acid and lipids. a. Rifamycin B b. Methenamine c. Metronidazole d. Isoniazid e. Nitrofurantoin 87. A nitroimidazole structure introduced as an anti-protozoal agent and later became anti bacterial agent. Its mechanism of action involves the drug entering the bacterial cell wall where the nitro group is reduced and free radicals are formed and act on DNA. a. Rifamycin B b. Methenamine c. Metronidazole d. Isoniazid e. Nitrofurantoin 88. A drug used to treat urinary tract infections where it degrades in acid conditions to give formaldehyde as the active agent. a. Rifamycin B b. Methenamine c. Metronidazole d. Isoniazid e. Nitrofurantoin 89. An antiviral drug that has a nucleoside-like structure and contains the same nucleic acid base as deoxyguanosine, but lacks the complete sugar ring. It specifically inhibits viral DNA polymerase and used in the treatment of infections due to herpes simplex 1 and 2 as well as varicella-zoster viruses. a. Acyclovir b. Idoxuridine c. Podophyllotoxin d. Fomivirsen e. Imiquimod 90. Which of the following is the valine ester prodrug of acyclovir useful in the treatment of varicella- zoster virus infections? a. Cidofovir b. Penciclovir c. Valaciclovir d. Famciclovir e. Ganciclovir 91. Which of the following antiviral drug is an analogue of deoxythymidine used in the treatment of herpes keratitis? The triphosphate form of this drug inhibits viral DNA polymerase as well as thymidylate synthetase. a. Acyclovir b. Idoxuridine c. Podophyllotoxin d. Fomivirsen e. Imiquimod 92. A plant product used in the treatment of genital warts caused by DNA virus papilloma virus. a. Acyclovir b. Idoxuridine c. Podophyllotoxin d. Fomivirsen e. Imiquimod 93. This drug consists of 21 nucleotides and phosphothionate backbone. It is a DNA antisense molecule that blocks the translation of viral RNA and is used against retinal inflammation caused by CMV in AIDS patients. a. Acyclovir b. Idoxuridine c. Podophyllotoxin d. Fomivirsen e. Imiquimod 94. A nucleoside reverse transcriptase inhibitor which is an analogue of deoxythymidine where the 3’hydroxyl group is replaced by an azido group. a. Zidovudine b. Didanosine c. Lamivudine d. Abacavir e. Efavirenz 95. The anti-HIV drug contains inosine as the nucleic acid base and is converted through a series of enzyme reaction to 2’,3’-dideoxyadenosine triphosphate which is the active drug. a. Zidovudine b. Didanosine c. Lamivudine d. Abacavir e. Efavirenz 96. Which of the following anti-HIV drug is an analogue of deoxycytidine where the 3’ carbon has been replaced by sulphur? a. Zidovudine b. Didanosine c. Lamivudine d. Abacavir e. Efavirenz 97. The only guanosine analogue that is used against HIV infections and Hepatitis B. a. Zidovudine b. Didanosine c. Lamivudine d. Abacavir e. Efavirenz 98. A second generation non-nucleoside reverse transcriptase inhibitor that has a benzoxaxinone structure. a. Zidovudine b. Didanosine c. Lamivudine d. Abacavir e. Efavirenz 99. Which of the following statements is/are correct regarding anti-HIV drugs? a. NRTIs are prodrugs that are converted by cellular enzymes to active triphosphates which act as enzyme inhibitors and chain terminators. b. NNRTIs act as enzyme inhibitors by binding to an allosteric binding site. c. PIs are designed to act as transition state inhibitors d. A and B only e. All of the above 100. Below is the structure of chloramphenicol, a bacteriostatic agent that binds to the 50s subunit of ribosome. Which part of its structure is essential for drug activity? a. The nitro group b. The 2 alcohol groups c. The dichloroacetamide group d. A and B only e. All of the above 101. Which substituent of chloramphenicol is responsibe for its toxic effect? a. The nitro group b. The 2 alcohol groups c. The dichloroacetamide group d. The aromatic ring e. A and B only 102. Which of the following statements is correct regarding Erythromycin? I. Erythromycin binds to the 50s subunit of bacterial ribosomes II. When administered together with chloramphenicol, their bacteriostatic effect will increase. III. The ketone and 2 alcohol groups in its structure are responsible for its acid sensitivity. IV. Increasing the size of the macrocycle to a 16-membered ring can increase the acid stability of the molecule. a. I, II, III, IV b. I, III, IV c. I, II, IV d. II, III e. III, IV 103. Amantadine is one of the earliest antiviral drugs used clinically against flu. Which of the following statements is correct regarding amantadine? I. Amantadine is an adamantine related to rimantadine. II. It inhibits the penetration and uncoating of the influenza virus. III. It can inhibit replication of the influenza virus by blocking a viral ion channel called matrix (M2) protein IV. At high concentrations, it can alter pH of endosomes and prevent the acidic environment required by the hemagglutinins to fuse the viral membrane with that of the endosome. a. I, II, III, IV b. I, III, IV c. I, II, IV d. II, III e. III, IV For nos. 104-107, please refer to the structures below: 104. Which among the given structures can be intercalating agent which can slide between the base pairs of the DNA double helix and thereby can inhibit the enzymes involved in the replication and transcription processes? a. Structure I b. Structure II c. Structure III d. Structure IV e. II and III 105. Which among the given structures is an antimetabolite that can inhibit the enzymes involved in the synthesis of DNA or its nucleotide building blocks? a. Structure I b. Structure II c. Structure III d. Structure IV e. II and III 106. Which of the given structures can form strong covalent bonds with the nucleophilic groups on DNA which can eventually result to cross-linking of strands? a. Structure I b. Structure II c. Structure III d. Structure IV e. II and III 107. Which of the given structures can be classified as an alkylating agent? a. Structure I b. Structure II c. Structure III d. Structure IV e. II and III 108. A semi-synthetic analogue of camptothecin given intravenously and is a prodrug used in combination with fluorouracil and folinic acid for the treatment of advanced colorectal cancer. a. Oblimersen b. Calicheamicin c. Carboplatin d. Irinotecan e. Cyclophosphamide 109. An antisense drug designed to inhibit the mRNA molecules that code for proteins which suppress apoptosis. a. Oblimersen b. Calicheamicin c. Carboplatin d. Irinotecan e. Cyclophosphamide 110. A natural product that reacts with nucleophiles to produce diradical species. Its reaction with DNA ultimately leads to cutting of the DNA chains. a. Oblimersen b. Calicheamicin c. Carboplatin d. Irinotecan e. Cyclophosphamide 111. It is the most commonly used alkylating agent in cancer chemotherapy, the metabolism of which produces arcolein which is toxic to the bladder and kidneys. a. Oblimersen b. Calicheamicin c. Carboplatin d. Irinotecan e. Cyclophosphamide 112. An alkylating agent that can cause intrastrand cross-linking preferref over cisplatin for the intravenous treatment of advanced ovarian tumors because of its less severe side effects. a. Oblimersen b. Calicheamicin c. Carboplatin d. Irinotecan e. Cyclophosphamide 113. Which of the following drugs is not an alkylating agent used in cancer chemotherapy? a. Carmustine b. Busulfan c. Procarbazine d. Mitomycin C e. None of the choices 114. A thiopurine prodrug which is converted to its corresponding monophosphate that inhibits purine synthesis. a. Methotrexate b. 5-fluorouracil c. 6-mercaptopurine d. Pentostatin e. Cytarabine 115. An antimetabolite that is very similar in structure to the natural folates differing only in additional amino and methyl groups. It inhibits the enzyme dihydrofolate reductase which is responsible in maintaining levels of the enzyme cofactor tetrahydrofolate. a. Methotrexate b. 5-fluorouracil c. 6-mercaptopurine d. Pentostatin e. Cytarabine 116. This drug acts as a prodrug for a suicide inhibitor. It is converted in the body to the fluorinated analogue of 2’deoxyuridylic acid monophosphate which then combines with the enzyme thymidylate synthase and the cofactor. a. Methotrexate b. 5-fluorouracil c. 6-mercaptopurine d. Pentostatin e. Cytarabine 117. An anti-leukemia drug isolated from Streptomyces antibioticus and is a powerful inhibitor of Adenosine deaminase. a. Methotrexate b. 5-fluorouracil c. 6-mercaptopurine d. Pentostatin e. Cytarabine 118. A prodrug analogue of 2’deoxycytidine which inhibits DNA polymerases. a. Methotrexate b. 5-fluorouracil c. 6-mercaptopurine d. Pentostatin e. Cytarabine 119. Which of the following pairs is correctly matched? I. Glucocorticoids: Megestrol acetate II. Progestins: prednisone III. Estrogens: Diethylstilbestrol IV. Androgens: Fluoxymesterone a. I, II, III, IV b. I, II c. III, IV d. I, III e. II, IV 120. A decapeptide analogue of the luteinizing hormone – releasing hormone designed to be more resistant to peptidase degradation. a. Goserelin b. Raloxifene c. Cyproterone acetate d. Anastrazole e. 4-hydroxyandrostenedione 121. A reversible competitive inhibitor of the enzyme aromatase , the design of which is based on structure of amino gluthetimide. a. Goserelin b. Raloxifene c. Cyproterone acetate d. Anastrazole e. 4-hydroxyandrostenedione 122. This mode of therapy involves an antibody which has catalytic activity designed to activate a prodrug. a. Antibody-directed enzyme prodrug therapy (ADEPT) b. Antibody-directed abzyme prodrug therapy (ADAPT) c. Gene -directed enzyme prodrug therapy (GDEPT) d. Photodynamic therapy e. All of the above 123. This mode of therapy involves the delivery of a gene that codes for an enzyme capable of activating an anticancer prodrug into a cancer cell. a. Antibody-directed enzyme prodrug therapy (ADEPT) b. Antibody-directed abzyme prodrug therapy (ADAPT) c. Gene -directed enzyme prodrug therapy (GDEPT) d. Photodynamic therapy e. All of the above 124. This involves irradiation of tumors containing porphyrin photosensitizers resulting to the production of reactive oxygen species which are fatal to the cell. a. Antibody-directed enzyme prodrug therapy (ADEPT) b. Antibody-directed abzyme prodrug therapy (ADAPT) c. Gene -directed enzyme prodrug therapy (GDEPT) d. Photodynamic therapy e. All of the above 125. This therapy involves an antibody-enzyme conjugate that is targeted to specific cancer cells. Once the antibody has become attached to the outer surface of cancer cells, a prodrug is administered which is activated by the enzyme at the tumor site. a. Antibody-directed enzyme prodrug therapy (ADEPT) b. Antibody-directed abzyme prodrug therapy (ADAPT) c. Gene -directed enzyme prodrug therapy (GDEPT) d. Photodynamic therapy e. All of the above 126. Which of the following statements is true regarding acetylcholine? I. It is very useful in treating such conditions that requires it because it can be readily synthesized in the laboratory. II. It is easily hydrolyzed in the stomach by acid catalysis and cannot be given orally. III. It is administered intravenously as it is stable in blood because of the absence of enzymes such as esterases. IV. There is no selectivity of action upon administration of acetylcholine. a. I, II, III, IV b. I, II c. III, IV d. I, III e. II, IV For nos. 127-129, refer to the structure of acetylcholine below; 127. Which part of the acetylcholine structure can be altered without decreasing its activity on cholinergic receptors? a. The quaternary nitrogen b. The ester functional group c. The ethylene bridge between the ester and nitrogen d. All of the above e. None of the choices 128. Which part of the acetylcholine structure is essential for activity? a. The quaternary nitrogen b. The ester functional group c. The ethylene bridge between the ester and nitrogen d. All of the above e. None of the choices 129. Which of the following statements is incorrect regarding the structure-activity relationship of acetylcholine? a. Replacing the nitrogen atom with a neutral carbon atom increases the activity b. The overall size of the molecule cannot be altered greatly. c. There must be two methyl groups on the nitrogen. d. A and B e. B and C 130. Which of the following statements is true regarding acetylcholine analogues? a. Addition of steric shield in the ethylene bridge renders resistance to chemical and enzymatic hydrolysis b. Changing the ester to a carbamate increases resistance to hydrolysis c. Changing the ester to a carbamate makes it selective to muscarinic receptor d. A and B e. B and C For nos. 131-132, refer to the structures below: 131. Which of the given structures is more stable to acid hydrolysis than acetylcholine? a. I b. II c. III d. I & II e. All of the above 132. Which of the given structures is more selective to muscarinic receptor than nicotinic receptor? a. I b. II c. III d. I & II e. All of the above 133. Given below is the general structure of muscarinic antagonists which was mostly based on the structure of atropine. Which of the following statements is true regarding the structural features of muscarinic antagonists? a. The alkyl group on nitrogen can be larger than methyl b. The nitrogen can be tertiary or quaternary c. Very large acyl groups (R1 and R2) are allowed d. A and B only e. All of the above 134. Physostigmine is a carbamate inhibitor of the enzyme acetylcholinesterase which was first isolated from Physostigma venenosum. Which of its functional group/s is/are essential for its activity? a. Carbamate group b. Benzene ring c. Pyrrolidine ring d. A and C only e. All of the above For nos. 135-141, refer to the general structure below: 135. Which part of the catecholamine is not important in the binding site interactions? a. The 2 phenolic groups b. Secondary alcohol c. Ionized amine d. The aromatic ring e. A and B only 136. Which part of the catecholamine structure is involved in Van der Waals interactions? a. The 2 phenolic groups b. Secondary alcohol c. Ionized amine d. The aromatic ring e. A and B only 137. Which part of the catecholamine structure is involved in ionic binding to the receptor site? a. The 2 phenolic groups b. Secondary alcohol c. Ionized amine d. The aromatic ring e. A and B only 138. Which part of the catecholamine structure is involved in H-bonding to the receptor binding site? a. The 2 phenolic groups b. Secondary alcohol c. Ionized amine d. The aromatic ring e. A and B only 139. Which of the following modifications to the catecholamine structure can increase alpha-2 receptor activity? a. Increasing the size of N-alkyl substituent b. Addition of an alpha methyl group c. Removal of the phenolic groups d. A and B only e. B and C only 140. Which of the following modifications to the catecholamine structure can increase the selectivity for beta receptors? a. Increasing the size of N-alkyl substituent b. Addition of an alpha methyl group c. Removal of the phenolic groups d. A and B only e. B and C only 141. Which of the following modifications to the catecholamine structure can result to a significant drop in activity for the beta receptor? a. Increasing the size of N-alkyl substituent b. Addition of an alpha methyl group c. Removal of the phenolic groups d. A and B only e. B and C only For nos. 142-144, refer to the general structure of aryloxypropranolamine below: 142. Which of the following statements is true about the SAR of aryloxypropranolamines? a. A secondary amine is essential for activity. b. The alcohol group on the side chain is essential for activity. c. Substitution in the methylene bridge increases the activity. d. A and B only e. B and C only 143. Which of the following is incorrect about the SAR of aryloxypropranolamines? a. Variation of the aromatic ring is possible. b. Heteroaromatic rings can be introduced to the system. c. Substitution on the side chain methylene group increases metabolic stability. d. Adding an N-arylethyl group is detrimental. e. A, B, and C only 144. What is the clinical indication of aryloxypropranolamines? a. Asthma b. Hypertension c. For cardiogenic shock d. Obesity e. All of the above 145. Which of the following statements is/are true regarding the structural features required for the hypnotic activity of barbiturates? (refer to the structure of barbituric acid) I. Replacement of sulphur for the carbonyl oxygen at carbon 2 results in quick onset and short duration of action. II. Within the same series of barbituric acid derivatives, the branched chain isomer has greater activity and shorter duration. The greater the branching, the more potent the drug. III. Within the same series of barbituric acid derivatives, the unsaturated allyl, alkenyl and cycloalkenyl analogues have greater potency than the saturated analogues with the same number of carbon atoms. IV. Methylation of one of the imide hydrogens (the transition from 5,5-disubstituted barbituric acid to 1,5,5-trisubstituted barbituric acid) increases onset and decreases duration of action. a. II only is correct b. III only is correct c. I and IV is correct d. II and III are correct e. I, II, III, and IV are correct 146. Which of the following statements describe the ideal antiepileptic drug? I. It should completely suppress seizures in doses that also cause sedation. II. It should be well tolerated, highly effective against various types of seizures and devoid of undesirable side effects on vital organs and functions III. Its onset of action should be rapid after parenteral injection for control of status epilepticus. IV. It should have a long duration of effect after oral administration for prevention of recurrent seizures. a. I only is correct b. III only is correct c. II, III, and IV are correct d. I, II, and IV are correct e. I, II, III, and IV are correct 147. Which of the following correctly describes the barbiturate 5-ethyl-5-phenylbarbituric acid? a. It is also known as Phenobarbital b. The sedative-hypnotic effect of this drug limits its use in older children and adults c. It exhibits anticonvulsant effects in doses that do not cause sedation. d. A and B only e. A and C only 148. Which of the following statements correctly describe 2-ethyl-2-methylsuccinide? a. It is widely accepted treatment of petit mal condition. b. It can cause ataxia and gingival hyperplasia. c. It is also known as Dilantin. d. A and B only e. B and C only 149. Which of the following statements correctly describe 5,5-diphenyl-2,4-imidazolidinedione? a. It is widely accepted treatment of petit mal condition. b. It can cause ataxia and gingival hyperplasia. c. It is also known as Dilantin. d. A and B only e. B and C only 150. Which of the following statements correctly describe the structure-activity relationship of tricyclic psychotropic drugs? I. Optimal psychotropic activity is observed in ring systems that have a six-membered or seven-membered central ring. II. Dihenylalamine and Diphenylmethane derivatives that lack a central ring are devoid of psychotropic activity. III. Derivatives that contain a five-membered central ring lack psychotropic activity. IV. Rigidly planar tricyclic diphenylmethane derivatives such as anthracene are inactive. a. I only is correct b. III only is correct c. II, III, and IV are correct d. I, II, and IV are correct e. I, II, III, and IV are correct. 151. Which of the following are pharmacologic responses elicited by phenothiazine? I. Antipsychotic effect II. Antiparkinsonian effect III. Anti-adrenergic, anticholinergic, antihistaminic and antiserotonin effects IV. Antiemetic effect A. I only is correct D. I,II,IV are correct B. III only is correct E. I,II,III,IV are correct C. II, III,IV are correct 152. Which of the following drugs is/are a butyrophenone derivative? I. thioridazine II. Fluphenazine III. Droperidol IV. Haloperidol A. I only is correct D. III and IV are correct B. IV only is correct E. I,II,III & IV are correct C. I and II are correct For numbers. 153-157, refer to the structure of morphine. Which of the following statement is/are true regarding modifications at the phenolic function at position 3? A. masking the hydroxyl group at position 3 by either esterificationor etherification increases all morphine type effects and almost always increases convulsant action. B. Methylmorphine, also known as codeine, is more potent than morphine. C. Maximal analgesic effects are observed with the free phenolic group at the 3 position. D. A and B only E. B and C only 154. Which of the following statements is/are true regarding modifications of the alcoholic function at position 3? A. Masking the hydroxyl group at position 6 increases all morphine type effects. B. 6-ethylmorphine and 3,6-diacetylmorphine are more potent than morphine itself. C. The oxygen function at position 6 is essential for analgesic activity D. A and B only E. B and C only 155. Which of the following statements is/are true regarding the 7-8 double bond? A. Reduction of the 7-8 double bonds in morphine results in a decrease in activity. B. Dihydromorphine and dihydrocodeine is more potent than the parent compound morphine. C. Unsaturation is essential for activity D. A and B only E. B and C only 156. Which of the following statements is correct regarding the tertiary nitrogen? A. Conversion of the tertiary nitrogen to a quaternary nitrogen results in a decrease of analgesic activity B. Increasing the chain length to propyl on the nitrogen results in a compound that has antagonistic properties to morphine effects. C. Increasing the chain length to propyl on the nitrogen results in a compound that has increased morphine type effects. D. A and B E. B and C 157. Which of the following statements correctly describe the cardiac glycosides digoxin and digitoxin? A. Digoxin is more toxic than digitoxin because of its additional hydroxyl group that makes it more lipophilic. B. Digoxin is less toxic than digitoxin because of its additional hydroxyl grouo that makes it more hydrophilic. C. Digoxin has longer duration of action than digitoxin. D. A and B E. B and C 158. What is the probable mechanism of action of cardiac agent with the following structure? O₂NO CH ₂ CH ONO ₂ O ₂ NO CH ₂ A. It is an inotropic agent B. It relaxes the vascular smooth muscle (vasodilation) C. It inhibits the calcium ion reflux into myocardial cells D. It blocks the beta adrenergic receptor E. None of the above 159. A drug used in the treatment in myocardial insufficiency that is structurally similar to adenosine, a natural vasodilatory substance released by the myocardium during hypoxic episodes. A. Cyclandelate D. Diltiazem B. Dypirydamole E. Nifedipine C. Papaverine 160. An antiarrythmic drug composed of a quinoline ring and a bicyclic quinuclidine ring system connected by a hydroxymethylene bridge that is a member of a family of alkaloids found in cinchona bark. A. Disopyridamole D. Tocainide B. Flecainide E. Procainamide C. Quinidine 161. An antiarrythmic drug that is an ᾳ-methyl analog structurally related to monoethylglycinexylide, the active metabolite of xylocaine. A. Disopyramide D. Tocainide B. Flecainide E. Procainamide C. quinidine 162. What is the use the mechanism of action of this antiplatelet drug with the following structure: A. It blocks the platelet phosphodiesterase enzyme, therefore leading to higher cyclic adenosine monophosphate levels. B. It reversibly inhibits the cyclooxygenase enzyme C. It irreversibly inhibits platelet aggregation by acetylating cyclooxygenase enzyme D. A and C only E. None of the choices 163. Which of the following statement is true regarding agonist at the H1 and H2 receptor antagonist of histamine? A. H1 antagonist are hydrophobic molecules thus they are more likely to produce cns side effects B. H2 antagonist are hydrophobic molecules thus they are less likely to produce cns side effects C. Both H1 and H2 antagonist are indicated for ulcer theraphy D. A and B only E. B and C only 164. Which of the following statements correctly describes the ideal anesthetic agent? I. it should provide adequate muscular contraction II. It should produce rapid and uncomplicated induction and emergence III. It should have no effect on myocardium or respiration at anesthetic doses. IV. It should be non-flammable A. I, II, III, IV D. I,II only B. II,III,IV only E. III & Iv only C. II & III only 165. Which f the following statement is true regarding anesthetics? I. Along with toxicity, increasing the chain length of ethers increases the anesthetic activity. II. Along with toxicity, increasing the chain length of ethers decreases the anesthetic activity. III. Introduction of unsaturation into an aliphatic ether increases potency and shortens induction and emergence IV. Introduction of unsaturation into an aliphatic ether decreases potency and shortens induction and emergence A. I,IV only D. II,IV only B. I,III only E. none of the above C. II,III only 166. Which of the following statements is true regarding halogenated anesthetic agents? I. Addition of halogen atoms to ethers or hydrocarbons decreases flamability II. Addition of halogen atoms to ethers or hydrocarbons often increases anesthetic potency. III. Addition of halogen atoms to ethers or hydrocarbons decreases flamability IV. Addition of halogen atoms to ethers or hydrocarbons often decreases anesthetic potency. A. I & II only D. none of the above B. I & IV only C. II & III only 167. Which of the following metabolic transformation of barbiturates can lead to loss of depressant activity? A. Oxidation of substituents B. Desulfuration of 2-thiobarbiturates C. Hydrolytic cleavage of the barbituric ring D. All of the above E. None of the above 168. Which of the following acids has mycobacteriostatic activity? A. Propionic acid B. Chaulmoogric acid C. Mandelic acid D. Salicylic acid E. Amino acid 169. Which of the following alcohols has a local anesthetic property? A. Benzyl alcohol B. 2-propanol C. Ethanol D. 2-pyridinemethanol E. choline 170. Which of the following amino ethers has antihistamine property? A. Dimethisoquin B. Benzidioxanes C. Clomiphene D. Phenoxybenzamine E. Methoxyphenamine 171. Which of the following halogenated compounds has hypnotic properties? A. Ethyl chloride B. Carbon tetrachloride C. Chloral D. Hexachlorophene E. Chloroform For nos 172-175, refer to the structure of cetirizine and clemastine as shown below: Cetirizine Clemastine 172. Which of the following statements is correct regarding the structural features of cetirizine and clemastine? A. Cetirizine and clemastine can cross the blood brain barrier because of the hydrophobic aromatic rings and aliphatic hydrocarbon chains B. Cetirizine will more likely cause drowsiness than clemastine C. clemastine will more likely cause drowsiness than cetirizine D. A and B only E. A and C only 173. Which of the following functional groups can decrease the absorption of cetirizine and clemastine through the blood brain barrier? A. Aromatic hydrocarbon B. Tertiary amines C. Ether D. A and B E. B and C 174. Which of the following functional groups can increase the absorption of cetirizine and clemastine through the blood brain barrier? A. Aromatic hydrocarbon B. Tertiary amines C. Ether D. A and B E. B and C 175. If a truck driver asks you to recommend an antihistamine drug for his seasonal allergies, which of the two drugs will you recommend? A. Clemastine B. Cetirizine C. Either clemastine and cetirizine D. None of the choices 176. A 35 year old woman comes to the pharmacy and asks you to recommend an antifungal cream rather than a spray or powder. You recommended terbinafine, an effective topical antifungal agent that is sold over the counter. What are the structural features/functional groups present in terbinafine that makes it an agent that can be used topically? A. Aromatic hydrocarbon D. Alkane B. Alkene E. All of the above C. AlkyneAll 177. Which among the following amino acids is likely to be present in the active site of the target enzyme of terbinafine and form an ionic interaction with the tertiary amine group? A. Valine B. Isoleucine C. Alanine D. Glutamic acid E. Serine 178.. Which among the following amino acids is likely to be present in the active site of the target enzyme of terbinafine and form an hydrophobic interaction with the aromatic hydrocarbons? A. Phenylalanine B. Serine C. Threonine D. Glutamic acid E. Arginine 179. Wich of the following drugs is an ethylenediamine antihistamine? A. Tripelennamine B. Diphenhydramine C. Promethazine D. Astemizole E. All of the above 180. Which of the following drugs in an example of tricyclic antihistamine? A. Tripelennamine B. Diphenhydramine C. Promethazine D. Astemizole E. All of the above 181. Which of the following drugs is an example of an ethanolamine ether antihistamine? A. Tripelennamine B. Diphenhydramine C. Promethazine D. Astemizole E. All of the above 182. Which of the following drugs has a little or no sedative qualities? A. Tripelennamine B. Diphenhydramine C. Promethazine D. Astemizole E. All of the above 183. According to this drug receptor theory, the number of drug receptor interactions per unit time determines the intensity of the biological response A. Rate theory B. Occupational theory C. Activation aggregation theory D. Induced fit theory E. Molecular pertubation theory 184. This drug receptor theory suggest that the biological response is directly related to the number of receptors bound by an agonist. A. Rate theory B. Occupational theory C. Activation aggregation theory D. Induced fit theory E. Molecular pertubation theory 185. This drug receptor theory suggest that the drug approaches the receptor, a conformational change occurs in the receptor to allow effective binding. A. Rate theory B. Occupational theory C. Activation aggregation theory D. Induced fit theory E. Molecular pertubation theory 186. According to this theory, receptors are always in dynamic equilibrium between active and inactive states. Agonist function by shifting the equilibrium toward the activated state, whereas antagonist prevent the activated state. A. Rate theory B. Occupational theory C. Activation aggregation theory D. Induced fit theory E. Molecular pertubation theory 187. This drug receptor theory suggest that two types of conformational changes exist and the rate of their existence determines the observed biological response. A. Rate theory B. Occupational theory C. Activation aggregation theory D. Induced fit theory E. Molecular pertubation theory 188. Which of the following statements correctly describes an agonist? A. these are compounds that mimics the natural ligand for receptor B. They may have similar structure to the ligand C. They can bind to regions of the receptor that are not involved in binding the natural ligand D. A and B E. B and C 189. Which of the following statements correctly describes an antagonist? A. these are compounds that mimics the natural ligand for receptor B. They may have similar structure to the ligand C. They can bind to regions of the receptor that are not involved in binding the natural ligand D. A and B E. B and C 190. These are exogenous chemical messengers that act as antagonist, but also eliminate any resting acivity associated with a receptor. A. Partial agonist B. Inverse agonist C. Hormones D. Neurotransmitters E. None of the choices 191. This condition may occur when an agonist is bound to its receptor for a long period of time. A. Sensitization B. Desensitization C. Tolerance D. Dependence E. None of the above 192. This condition may occur when an antagonist is bound to a receptor for a long period of time. The cell synthesize more receptor to counter the antagonist effect. A. Sensitization B. Desensitization C. Tolerance D. Dependence E. None of the above 193. This is a situation where increases doses of a drug over time to achieve same effect. A. Sensitization B. Desensitization C. Tolerance D. Dependence E. None of the above 194. This is related to the body’s ability to adapt to the presence of a drug. On stopping the drug, withdrawal symptoms occur as a result of abnormal levels of target receptor. A. Sensitization B. Desensitization C. Tolerance D. Dependence E. None of the above 195. This is a measure of how strongly a drug binds to a receptor. A. Potency B. Affinity C. Efficacy D. All of the above E. None of the choices 196. This is determined by measuring the maximum possible effects resulting from receptor-ligand binding A. Potency B. Affinity C. Efficacy D. All of the above E. None of the choices 197. This relates how effective a drug is in producing a cellular effect. It can be determined by measuring the concentration of drug required to produce 50% of the maximum possible effect. A. Potency B. Affinity C. Efficacy D. All of the above E. None of the choices 198. These are molecules that act as substrates for a target enzyme, but which are converted into a highly reactive species as a result of the enzyme catalyzed reaction mechanism. The species formed then reacts with amino acid residues present in the active site to form covalents bonds, and act as irreversible inhibitors. A. Transition state analogue B. Suicide substrates C. Allosteric inhibitors D. Competitive inhibitor E. All of the above 199. This type of inhibition binds to a different site other than the active site and can alter the shape of the enzyme such that the active site is no longer recognizable. A. Transition state analogue B. Suicide substrates C. Allosteric inhibitors D. Competitive inhibitor E. All of the above 200. These are enzyme inducers that are designed to mimic the transition state of an enzyme- catalyze reaction mechanism. They bind more strongly than either the substrate or product. A. Transition state analogue B. Suicide substrates C. Allosteric inhibitors D. Competitive inhibitor E. All of the above 201. The type of inhibitors that bind to the active site and compete with either substrate or cofactor. A. Transition state analogue B. Suicide substrates C. Allosteric inhibitors D. Competitive inhibitor E. All of the above 202. Physostigmine inhibit which of the following enzyme? A. Adenosine deaminase B. Arabinosyl transferase C. Acetylcholinesterase D. 3’,5’-cyclic GMP phosphodiesterase E. Aldehyde dehydrogenase 203. sildenafil, a drug for erectile dysfunction, inhibit which of the following enzyme? A. Adenosine deaminase B. Arabinosyl transferase C. Acetylcholinesterase D. 3’,5’-cyclic GMP phosphodiesterase E. Aldehyde dehydrogenase 204. ethambutol, a drug for tuberculosis, inhibit which of the following enzyme? A. Adenosine deaminase B. Arabinosyl transferase C. Acetylcholinesterase D. 3’,5’-cyclic GMP phosphodiesterase E. Aldehyde dehydrogenase 205.Which of the following drugs for diabetes inhibits the enzyme a-glucosidase? A. Acarbose B. Miglitol C. Glimepiride D. Metformin E. Rosiglitazone 206. Which of the following drugs for diabetes inhibits the enzyme a-amylase? A. Acarbose B. Miglitol C. Glimepiride D. Metformin E. Rosiglitazone 207. Which of the following drug (inhibitor)-enzyme inhibited pairs is incorrectly matched? A. terbinafine: squalene monooxygenase B. Itraconazole: sterol14a –methylase C. Caspofungin: 1,3-B-glucan synthase D. All of the above E. None of the choices 208. Which of the following drug (inhibitor)-enzyme inhibited pairs is incorrectly matched? A. Alendronate: farnesyl-diphosphate farnesyl transferase B. Mycophenolate: IMP dehydrogenase C. Cilastin: renal dehydropeptidase D. All of the above E. None of the choices 209. Which of the following drug (inhibitor)-enzyme inhibited pairs is correctly matched? A. captopril: peptidyl-dipeptidase A B. Etodolac: prostaglandin endoperoxide synthase C. Entacapone: catechol-O-methyl transferase D. All of the above E. B and C only 210. Which of the following drugs (inhibitor) enzyme inhibited pairs is correctly matched? A. atorvastatin: HMG-CoA reductase B. Oseltamivir: viral neuraminidase C. Ciprofloxacin: DNA gyrase D. All of the above E. None of the choices 211. Which of the following phenolic drugs has an expectorant activity? A. Amiodaquine B. Guaiacol C. Hydroxymorphinans D. Diethylstilbestrol E. Hexylresorcinol 212. Which of the following dyes is available as vaginal suppository for the treatment of yeast infection and has also been used orally as a anthelmintic for strongyloidiasis and oxyurias? A. Methylene blue B. Phenolpthalein C. Basic fuchsin D. Methylrosaniline chloride E. None of the choices 213. Which of the following dyes is a mixture of the chlorides of rosaniline and p-rosaniline? It is an ingredient of castellanis paint which is used topically in the treatment of fungal infection, such as ringworm and athletes foot? A. Methylene blue D. Methylrosaniline chloride B. Phenolpthalein E. None of the choices C. Basic fuchsin 214. It is a non classical folate antagonist that is structurally similar to methotrexate. It inhibits the enzyme dihydrofolate reductase and has been approved for the treatment of pneumocystis carinii in patients with aids. A. Nitoxadine B. Metronidazole C. Trimetexrate E. Suramin D. Diloxanide furoate 215. Which of the following anti-inflammatory analgesic is an arylacetic derivative that is comparable to aspirin in the treatment of rheumatoid arthritis, with a lower incidence of side effects? It has also been approved for used in primary dysmenorrhea. A. Sodium salicylate D. Acetaminophen B. Mefenamic acid E. Antipyrine C. Ibuprofen 216. Which of the following anti-inflammatory agents is an arylanthranilic acid derivative that has lower incidence of gastrointestinal bleeding than aspirin, and has been approved for use in the management of primary dysmenorrhea? A. Sodium salicylate D. Acetaminophen B. Mefenamic acid E. antipyrine C. Ibuprofen 217. Which of the following drugs is a derivative of aniline and has an analgesic and antipyretic properties? The FDA requires a warning label that read as follows: Warning: Do not give to children under 3 years of age or use for more than 10 days unless directed by a physician. A. Sodium salicylate D. Acetaminophen B. Mefenamic acid E. antipyrine C. Ibuprofen 218. The following are synthetic estrogens except: A. Chlorotrianisene D. B and C only B. Diethylstilbestrol E. None of the choices C. Benzestrol 219. Which of the following estrogens is an estradiol metabolite originally obtained from the urine of horses especially pregnant mares? A. Equilin sodium sulfate D. Diethylstilbestrol B. Ethinyl estradiol E. Dienestrol C. Estriol 220. Which of the following progestins is classified as a derivative of testosterone? A. Megestrol acetate C. Norethindrone B. Norgestrel D. Ethinodiol acetate E. Dimethisterone 221. Which of the following progestins are classified as derivative of testosterone? A. Ethisterone D. A and B only B. Chlormadinone acetate E. B and C only C. Medroxyprogesterone 222. Which of the following prodrugs was designed to improve the membrane permeability of its active metabolite? A. Enalapril D. A and C only B. Levodopa E. All of the above C. Pivampicillin 223. Which of the following prodrugs was designed to prolong the drug activity of its active metabolite? A. Cyclophosphamide D. Chloramphenicol succinate B. Azathioprine E. Hetacillin C. Chloramphenicol palmitate 224. Which of the following prodrugs was designed to lower water solubility of the active metabolite? A. Cyclophosphamide D. Chloramphenicol succinate B. Azathioprine E. Hetacillin C. Chloramphenicol palmitate 225. Which of the following prodrugs was designed to mask the toxic side effects of its active metabolite? A. Cyclophosphamide D. Chloramphenicol succinate B. Azathioprine E. Hetacillin C. Chloramphenicol palmitate 226. Which of the following prodrugs was designed to increase the water solubility of the active metabolite? A. Cyclophosphamide D. Chloramphenicol succinate B. Azathioprine E. Hetacillin C. Chloramphenicol palmitate 227. Which of the following prodrug was designed to increase the chemical stability of the active metabolite? A. Cyclophosphamide B. Azathioprine C. Chloramphenicol palmitate E. Hetacillin D. Chloramphenicol succinate 228. These are isomer that contain at least one assymetric, or chiral, carbon atom. Each asymmetric carbon atom can exist in one of two non-superimposable isomeric forms. A. Optical isomer D. All of the above B. Geometric isomer E. None of the choices C. Conformational isomer 229. This type of isomer occurs as a result of restricted rotation about a chemical bond, owing to double bond or rigid ring system in the molecule. A. Optical isomer D. All of the above B. Geometric isomer E. None of the choices C. Conformational isomer 230. Also known as rotamers, these are non-superimposable orientation of a molecule which result from the rotation of atoms about single bonds. A. Optical isomer D. All of the above B. Geometric isomer E. None of the choices C. Conformational isomer 231. Which of the following statements is true regarding ester-type local anesthetics? A. They are generally long acting and are metabolized in the liver B. They are generally short acting due to rapid hydrolysis in the plasma C. Agents include procaine, benzocaine, lidocaine and dibucaine D. A and B only E. A and C only 232. Which of the following statements is true regarding amide-type local anesthetics? A. They are generally long acting and are metabolized in the liver B. They are generally short acting due to rapid hydrolysis in the plasma C. Agents include procaine, benzocaine, lidocaine and dibucaine D. A and B only E. A and C only 233. Which of the following statements is true regarding the antipsychotic agents in the phenothiazine class? A. Phenothiazine must have a nitrogen containing side chain substituent on the ring nitrogen for antipsychotic activity. B. Phenothiazine in which the rings and side chain nitrogen are separated by a two carbn chain have only antihistaminic activity. C. Piperidine derivative confer the greatest potency and the highest pharmacologic selectivity. D. A and B only E. B and C only 234. Which of the following pairs is correctly matched? A. butyrophenone, haloperidol B. Phenothiazine, chlorprothixene C. Thioxanthenes, thioridazine D. A and B only E. All of the above 235. Which of the following pairs of newer class of antipsychotic is correctly matched? A. dihydroinolones, molindone B. Dibenzoxazepines, loxapine C. Dibenzodiazepines, clozapine D. A and C only E. All of the above 236. Which of the following statements is true regarding tricyclic antidepressants? A. Imipramine and clompramine are derivatives of dibenzazepine B. Amitriptyline and nortriptyline are derivatives of dibenzocycloheptadiene C. TCA appear to produce their antidepressant effects by blocking the intraneuronal oxidative deamination of brain biogenic amines. D. A and B only E. All of the above 237. Which of the following statements correctly describe the structure and mechanism of action of mao inhibitors? A. Tranylcypromine is an extremely potent phenylcyclopropanolamine derivative B. Phenelzine isocarboxacid are weakly potent hydralazine derivative C. MAO inhibitors appear to act principally by reducing cns neuronal re-uptake of biogenic amines D. A and B only E. All of the above For nos. 238-240, select the most appropriate pharmacologic category for the following structures: 238. What is the pharmacologic category of structure I? A. Opioid antagonist D. General anesthetic B. Anxiolytic E. Local anesthetic C. Antidepressant 239. Structure II belongs to what pharmacologic category? A. Opioid antagonist D. General anesthetic B. Anxiolytic E. Local anesthetic C. Antidepressant 240. Structure III belongs to what part of pharmacologic class? A. Opioid antagonist D. General anesthetic B. Anxiolytic E. Local anesthetic C. Antidepressant 241. Structure IV belongs to what part of pharmacologic class? A. Opioid antagonist D. General anesthetic B. Anxiolytic E. Local anesthetic C. Antidepressant 242. Give the amino acid of the autacoids with the following structure. A. tyrosine D. Histidine B. Phenylalanine E. Serine C. Tryptophan 243. Give the amino acid of the autacoids with the following structure. A. tyrosine D. Histidine B. Phenylalanine E. Serine C. Tryptophan 244. Certain metabolites retain the pharmacologic activity of their of their parent compounds to a greater or lesser degree. Which of the following drugs produce such metabolites? I. oxidation of the mercaptopurine II. Demethylation of morphine III. Dealkylation of iproniazid IV. Isomerization of retinoic acid A. I, IV D. II only B. II,III E. I only C. III, IV 245. Which of the following biotransformation produces a metabolite with an activity different from that of their parent compound? I. oxidation of the mercaptopurine II. Demethylation of morphine III. Dealkylation of iproniazid IV. Isomerization of retinoic acid A. I, IV D. II only B. II,III E. I only C. III, IV 246. Which of the following biotransformation produces a inactive metabolite I. oxidation of the mercaptopurine II. Demethylation of morphine III. Dealkylation of iproniazid IV. Isomerization of retinoic acid A. I, IV D. II only B. II,III E. I only C. III, IV 247. Which of the following statements is true regarding oxidation reaction? I. It is a most common phase 1 of biotransformation II. Oxidation reactions can occur in the liver III. The vast majority of oxidation is catalyze by a group or mixed function oxidases known as CYP450. IV. The increased polarity of the oxidized product (metabolites) enhances their water solubility and increases their tubular reabsorption to some extent, thus favoring their excretion in the urine A. I,II,III,IV D. I and III Only B. I,II only E. II And IV only C. III, IV only 248. Which of the following statements is true regarding reduction reaction? I. It has same goal as oxidation reaction to create polar functional groups that can be easily excreted. II. Bacteria resident in the GI tract are also responsible for reductions of azo and nitro groups III. Chloramphenicol, sulfasalazine and acetohexamide can undergo reduction reaction IV. Cytochrome P450 enzymes is not involved in the reduction reaction A. I, II, III, IV D. II and III only B. I, II, III E. IV only C.I, II only 249. Which of the following drugs is metabolized by CYP1A? A. Acetaminophen D. Theophyliine B. Fluoroquinolones E. All of the above C. Imipramide 250. Which of the following drugs is metabolized by CYP4B? A. prostaglandin B. Carbamazepine C. Dapsone D. Hydrocortisone E. All of the above 251. Which of the following statements is correct regarding Phase ll reactions? l.These are reactions in which the functional groups of the original drug(or metabolite)are masked by conjugation reaction ll.These reactions require both a high-energy molecules and an enzyme lll.High-energy molecules consist of a coenzyme bound to the endogenous substrate,the parent drug,or the drug’s phase l metabolite. lV.Most conjugates are highly polar and unable to cross cell membranes,making them almost almost always pharmacology inactive and of little or no toxicity. A)l,ll,lll,lV C)land ll only E)lV only B) l,ll,lll only D)ll and lll only 252. Which of the following statements correctly describes Glucuronidation reaction? l.It is the most common conjugation pathway because of readiy available supply of glucuronic acid as well as a large variety of functional groups,which can enzymatically react with this sugar derivative. ll.The high energy form of glucuronic acid is Uridine monophosphate glucuronic acid and the enzyme involve in these reaction is glucuronyl transferase. lll.Druds that posses hydroxyl or carboxyl functional groups readily undergo glucurinidation to form esters and ethers,respectively. lV.The addition of the glucuronide moiety greatly increases the hydrophilicity of the molecule which makes it highly reabsorbed by the renal tubes. A)l,ll,lll,lV C)l,ll only E)lV only B)l,ll,lll only D)ll,lll only 253. Which of the following conjugation reactions requires 2’-phosphoadenosine-5’- phosphosulfate molecule? A) Glutathione conjugation D) Sulfate conjugation B) Acetylation E) Amino acid conjugation C) Methylation 254.Which of the following conjugation reactions require the formation of the high-energy molecule AcetylCoA A) Glutathione conjugation D) Sulfate conjugation B) Acetylation E) Amino acid conjugation C) Methylation 255. Which of the following conditions can greatly affect the metabolism of a certain drug? A) Congestive heart failure D) Increase drug dosage B) Deficiency of certain dietary minerals E) All of the above C) Deficiency of vitamins 256. Which of the following drug administration route bypasses first-pass effect A) Oral administration B) Intravenous administration C) Sublingual administration D) A and B E) B and C 257.Which of the following metabolites would be the least likely urinary excretion product of acetaminophen? A) Ether glucuronide B) Sulfate conjugate C) N-acetyl-p-benziminoqiunoneimine D) Unchange drug E) N-acetyl-p-benziminoquinoneimine with glutathione 258. Which of te following statements correctly describes the first and second generation Sulfonylureas? (See structure below) l.First and second generation Sulfonylureas have a bulk aliphatic substituent on the nonsufonyl have relatively simple aromatic ll.First generation Sulfonylureas have relatively simple aromatic substituents such as methyl,amino,acetyl,chloro lll Second generation Sulfonylureas have a larger aromatic substituent lV.First generation Sulfonylureas are more potent than second generation. A)l,ll,lll,lV B)l,ll,lll only C)l and ll only D)ll and lll only E)lV only 259. Which of the following is not the first generation sulfonylurea A) Glyburide B) Glipizide C) Glimperide D) All of the choices E) None of the choices 260. Which of the following is the first generation sulfonylurea A) Glyburide B) glipizide C) Glimperide D) All of the choices E) None of the choices 261. This drug has been highly effective against Schistoma mansoni.It is activated via esterification to a biological ester that spontaneously dissociates to an electrophlie,which alkylates the helminth DNA,leading to irreversible inhibition of nucleic acid metabolism. A) Praziquantel B) Oxaminiquine C) Ivermectin D) Pyrantel E) Mebendazole 262.This drug acts as a depolarizing neuromuscular blocking agent that acts as a depolarizing neuromuscular blocking agent that activates nicotinic receptors and inhibits cholinesters,ultimately leading to worm paralysis.It is used as apamoate salt,which is quite insoluble and,as a result,is not readiy absorbed improving the usefulness of the drug for the treatment of intestinal helminthes. A) Praziquantel B) Oxaminiquine C) Ivermectin D) Pyrantel E) Mebendazole 263. A drug that belongs to a class of 16-membered macrocyclic lactones extracted from Streptomyces avermitilis used in the treatment of various nematode infections.It acts either as a GABA agonist or as an inducer of chloride ion influx,leading to hyperpolarization and muscle paralysis. A)Praziquantel B)Oxaminiquine C)Ivermectin D)Pyrantel E)Mebendazole 264. It is an isoquinoline derivative with most of the biological activity found in the levo enantiomer.The compound has no activity against nematodes,but is highly effective against cestodes abd trematodes.Its mechanism of action appers to involve calcium ion redistribution either directly or indirectly and inhibition of phosphoinositide metabolism A) Praziquantel B) Oxaminiquine C) Ivermectin D) Pyrantel E) Mebendazole 265. Buspirone,a long chain arylpiperazine derivative,is an anxiolytic agent that is a partial agonist to A)5HT1A receptor B)5HT4 receptor C)5HT3 receptor D)5HT2A E)5HT1D 266. Sumatriptan and other indeleaklylamine derivatives used in the treatment of migraine is an agonist at which of the following receptors. A) 5HT1A receptor B) 5HT4 receptor C) 5HT3 receptor D) 5HT2A E) 5HT1D For nos. 267-268, refer to the following reaction pathway A)l,ll,lll,lV B)l,ll only C)lll,lV only D)l,lll E)ll,lV 268.Which of the givem reactions can be classified as Phase ll metabolism? A)l,ll,lll,lV B)l,ll only C)lll,lV only D)l,lll E)ll,lV 269.Which of the following drugs would most likely undergo nitroreduction? A)Chloramphenicol B)Procaine C)Lidocaine D)Sulfasalazine E)All of the above 270.Which of the following drugs would most likely undergo azoreduction A)Chloramphenicol B)Procaine C)Lidocaine D)Sulfasalazine E)All of the above 271.Which of the following drugs would most likely undergo ester hydrolysis A)Chloramphenicol B)Procaine C)Lidocaine D)Sulfasalazine E)All of the above 272.Which of the following drugs would likely undergo amide hydrolysis A)Chloramphenicol B)Procaine C)Lidocaine D)Sulfasalazine E)All of the above 273.This conjugation pathway is extremely important in preveting toxicity from a variety of electrophilic agents.It produces a mercaptopuric acid derivative upon reaction with an electrophile A)Glutathione conjugation B)Acetylation C)Methylation D)Sulfate conjugation E)Amino acid conjugation 274.S-adenosylmethionine is required for the conjugation reaction A)Glutathione conjugation B)Acetylation C)Methylation D)Sulfate conjugation E)Amino acid conjugation 275. Meperidine can undergo which of the following metabolic pathway? I. Hydroxylation at thr aromatic ring II. Ester hydrolysis III. N-oxidation IV. N-dealkylation A. I,II,III,IV B. I,II,III C. I,II D. I,III E. II,IV 276. Which of the following selective estrogen receptor modulators (SERMs) and antiestrogens has a triphenylethylene structure used to treat early and advanced breast carcinoma in post menopausal women? A. raloxifene B. Fulvestrant C. Tamoxifen D. Clomiphene E. None of the above 277. Which of the following SERMs and antiestrogen is a benzothiophene derivative that has been approved for the prevention and treatment of osteoporosis in menopausal women? It has antagonist properties on the endometrium and breast tissue and agonist properties on bone and cardiovascular system? A. raloxifene B. Fulvestrant C. Tamoxifen D. Clomiphene E. None of the above 278. Which of the following SERMs and antiestrogen is an antagonist structurally on the estradiol structure which is used in the treatment of women who have had disease progression after prior antiestrogen property? A. raloxifene B. Fulvestrant C. Tamoxifen D. Clomiphene E. None of the above 279. Which of the following drugs is not a nonsteroidal aromatase inhibitor? A. Letrozole B. Aminoglutethimide C. Exemestane D. A and B only E. B and C only 280. Which of the following drugs is a nonsteroidal aromatase inhibitor? A. Letrozole B. Aminoglutethimide C. Exemestane D. A and B only E. B and C only 281. An aromatase inhibitor used mainly in the treatment of cushing’s syndrome A. Letrozole B. Aminoglutethimide C. Exemestane D. A and B only E. B and C only 282. What is the probable mechanism of action of diuretic drug with the following structure? A. It increases intraluminal osmotic pressure, causing water to pass from the body into the tubules. B. It can induce dieresis by inhibiting the formation of carbonic acid within the proximal and tubular cells to limit the number of hydrogen ions available to promote sodium reabsortion C. It inhibits the Na+/Cl- symportar located in the distal convulated tubule D. It inhibits Na+/K=/Cl- transport system in the thick ascending limb loop of henle E. It inhibits sodium and water reabsorption by competitive inhibition of aldosterone 283. What is the probable mechanism of action of a diuretic drug with the following structure? A. It increases intraluminal osmotic pressure, causing water to pass from the body into the tubules. B. It can induce dieresis by inhibiting the formation of carbonic acid within the proximal and tubular cells to limit the number of hydrogen ions available to promote sodium reabsortion C. It inhibits the Na+/Cl- symportar located in the distal convulated tubule D. It inhibits Na+/K=/Cl- transport system in the thick ascending limb loop of henle E. It inhibits sodium and water reabsorption by competitive inhibition of aldosterone 284. What is the probable mechanism of action of a diuretic drug with the following structure? A. It increases intraluminal osmotic pressure, causing water to pass from the body into the tubules. B. It can induce dieresis by inhibiting the formation of carbonic acid within the proximal and tubular cells to limit the number of hydrogen ions available to promote sodium reabsortion C. It inhibits the Na+/Cl- symportar located in the distal convulated tubule D. It inhibits Na+/K=/Cl- transport system in the thick ascending limb loop of henle E. It inhibits sodium and water reabsorption by competitive inhibition of aldosterone 285. What is the probable mechanism of action of a diuretic drug with the following structure? A. It increases intraluminal osmotic pressure, causing water to pass from the body into the tubules. B. It can induce dieresis by inhibiting the formation of carbonic acid within the proximal and tubular cells to limit the number of hydrogen ions available to promote sodium reabsortion C. It inhibits the Na+/Cl- symportar located in the distal convulated tubule D. It inhibits Na+/K=/Cl- transport system in the thick ascending limb loop of henle E. It inhibits sodium and water reabsorption by competitive inhibition of aldosterone 286. Which of the following analgesic agent is 2 to 3 times more potent than morphine as analgesic and also known as heroin? A. Tramadol hydrochloride B. Normorphine C. Diphenoxylate D. Nalbuphine E. Diacetylmorphine Hydrochloride 287. Which of the following drugs represent a fragment of codeine’s structure, consisting of the phenyl and cyclohexane rings? This drug possesses opioid activity but has other analgesic activity that is not reversed by naloxone. A. Tramadol hydrochloride B. Normorphine C. Diphenoxylate D. Nalbuphine E. Diacetylmorphine Hydrochloride 288. This drug prepared by N-demethylation of morphine and has about one-fourth as active as morphine in producing analgesia but has a much lower physical dependence capacity A. Tramadol hydrochloride B. Normorphine C. Diphenoxylate D. Nalbuphine E. Diacetylmorphine Hydrochloride 289. Also known as N-cyclobutylmethylnoroxymorphone hydrochloride, this drug is analgesia of the agonist- antagonist type with little or no abuse liability. A. Tramadol hydrochloride B. Normorphine C. Diphenoxylate D. Nalbuphine E. Diacetylmorphine Hydrochloride 290. This drug has a strong structural relationship to the meperidine type analgesics and has the ability to inhibit excessive gastrointestinal motility. A. Tramadol hydrochloride B. Normorphine C. Diphenoxylate D. Nalbuphine E. Diacetylmorphine Hydrochloride 291. Which of the following modifications can affect the onset , degree and duration of insulin activity? A. Rearrangement of amino acid residues at the N- and C- terminus at the B chain of insulin B. Changing the insulin crystal type (ex. From crystalline to amorphous) C. Addition of modifying protein such as protamine D. Changing the site of injection E. All of the above 292. This is the only insulin analogue with a C14 fatty acid attached to an amino residue in the B chain of insulin A. Lispro B. Aspart C. Glulisine D. Glargine E. Detemir 293. A highly purified protein containing 165 amino acids manufactured from a strain of E. coli bearing a genetically engineered plasmid containing an interferon alfa 2a gene from leucocytes. This drug is used in patients 18 years or older for treatment of hairy cell leukemia and chronic myelogenous leukemia. A. Roferon-A B. Interon C. Aldesleukin D. Rituximab E. Gemtuzumab Ozogamicin 294. A highly purified protein produced by E.coli containing a plasmid with alfa 2b gene. This product is indicated for hairy cell leukemia and also useful in treating malignant melanoma. A. Roferon-A B. Interon C. Aldesleukin D. Rit

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