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Org Chem PACOP > 201-250 > Flashcards

201-250 Flashcards

1
Q

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

A

Competitive inhibitor

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2
Q

Physostigmine inhibit which of the following enzyme?
A. Adenosine deaminase
B. Arabinosyl transferase
C. Acetylcholinesterase
D. 3’,5’-cyclic GMP phosphodiesterase
E. Aldehyde dehydrogenase

A

Acetylcholinesterase

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3
Q

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

A

3’,5’-cyclic GMP phosphodiesterase

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4
Q

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

A

Arabinosyl transferase

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5
Q

Which of the following drugs for diabetes inhibits the enzyme a-glucosidase?
A. Acarbose
B. Miglitol
C. Glimepiride
D. Metformin
E. Rosiglitazone

A

Miglitol

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6
Q

Which of the following drugs for diabetes inhibits the enzyme a-amylase?
A. Acarbose
B. Miglitol
C. Glimepiride
D. Metformin
E. Rosiglitazone

A

Acarbose

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7
Q

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

A

None

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8
Q

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

A

None

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9
Q

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

A

All of the above

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10
Q

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

A

All of the above

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11
Q

Which of the following phenolic drugs has an expectorant activity?
A. Amiodaquine
B. Guaiacol
C. Hydroxymorphinans
D. Diethylstilbestrol
E. Hexylresorcinol

A

Guaiacol

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12
Q

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

A

Methylrosaniline chloride

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13
Q

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
B. Phenolpthalein
C. Basic fuchsin
D. Methylrosaniline chloride
E. None of the choices

A

Basic fuchsin

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14
Q

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
D. Diloxanide furoate
E. Suramin

A

Trimetextrate

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15
Q

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
B. Mefenamic acid
C. Ibuprofen
D. Acetaminophen
E. Antipyrine

A

Ibuprofen

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16
Q

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
B. Mefenamic acid
C. Ibuprofen
D. Acetaminophen
E. antipyrine

A

Mefenamic acid

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17
Q

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
B. Mefenamic acid
C. Ibuprofen
D. Acetaminophen
E. antipyrine

A

Acetaminophen

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18
Q

The following are synthetic estrogens except:
A. Chlorotrianisene
B. Diethylstilbestrol
C. Benzestrol
D. B and C only
E. None of the choices

A

None of the choices

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19
Q

Which of the following estrogens is an estradiol metabolite originally obtained from the urine of
horses especially pregnant mares?
A. Equilin sodium sulfate
B. Ethinyl estradiol
C. Estriol
D. Diethylstilbestrol
E. Dienestrol

A

Equilin sodium sulfate

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20
Q

Which of the following progestins is classified as a derivative of testosterone?
A. Megestrol acetate
B. Norgestrel
C. Norethindrone
D. Ethinodiol acetate
E. Dimethisterone

A

Megestrol acetate

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21
Q

Which of the following progestins are classified as derivative of testosterone?
A. Ethisterone
B. Chlormadinone acetate
C. Medroxyprogesterone
D. A and B only
E. B and C only

A

Ethisterone

22
Q

Which of the following prodrugs was designed to improve the membrane permeability of its
active metabolite?
A. Enalapril
B. Levodopa
C. Pivampicillin
D. A and C only
E. All of the above

A

All of the above

23
Q

Which of the following prodrugs was designed to prolong the drug activity of its active
metabolite?
A. Cyclophosphamide
B. Azathioprine
C. Chloramphenicol palmitate
D. Chloramphenicol succinate
E. Hetacillin

A

Azathioprine

24
Q

Which of the following prodrugs was designed to lower water solubility of the active metabolite?
A. Cyclophosphamide
B. Azathioprine
C. Chloramphenicol palmitate
D. Chloramphenicol succinate
E. Hetacillin

A

Chloramphenicol palmitate

25
Q

Which of the following prodrugs was designed to mask the toxic side effects of its active
metabolite?
A. Cyclophosphamide
B. Azathioprine
C. Chloramphenicol palmitate
D. Chloramphenicol succinate
E. Hetacillin

A

Cyclophosphamide

26
Q

Which of the following prodrugs was designed to increase the water solubility of the active
metabolite?
A. Cyclophosphamide
B. Azathioprine
C. Chloramphenicol palmitate
D. Chloramphenicol succinate
E. Hetacillin

A

Chloramphenicol succinate

27
Q

Which of the following prodrug was designed to increase the chemical stability of the active
metabolite?
A. Cyclophosphamide
B. Azathioprine
C. Chloramphenicol palmitate
D. Chloramphenicol succinate
E. Hetacillin

A

Hetacillin

28
Q

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
B. Geometric isomer
C. Conformational isomer
D. All of the above
E. None of the choices

A

Optical isomer

29
Q

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
B. Geometric isomer
C. Conformational isomer
D. All of the above
E. None of the choices

A

Geometric isomer

30
Q

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
B. Geometric isomer
C. Conformational isomer
D. All of the above
E. None of the choices

A

Conformational isomer

31
Q

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

A

They are generally short acting due to rapid hydrolysis in the plasma

32
Q

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

A

They are generally long acting and are metabolized in the liver

33
Q

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

A

A and B only

34
Q

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

A

butyrophenone, haloperidol

35
Q

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

A

All of the above

36
Q

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

A

A and B only

37
Q

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

A

A and B only

38
Q

What is the pharmacologic category of structure I?
A. Opioid antagonist
B. Anxiolytic
C. Antidepressant
D. General anesthetic
E. Local anesthetic

A

Local anesthetic

39
Q

Structure II belongs to what pharmacologic category?
A. Opioid antagonist
B. Anxiolytic
C. Antidepressant
D. General anesthetic
E. Local anesthetic

A

Antidepressant

40
Q

Structure III belongs to what part of pharmacologic class?
A. Opioid antagonist
B. Anxiolytic
C. Antidepressant
D. General anesthetic
E. Local anesthetic

A

General anesthetic

41
Q

Structure IV belongs to what part of pharmacologic class?
A. Opioid antagonist
B. Anxiolytic
C. Antidepressant
D. General anesthetic
E. Local anesthetic

A

General anesthetic

42
Q

Give the amino acid of the autacoids with the following structure.
A. tyrosine
B. Phenylalanine
C. Tryptophan
D. Histidine
E. Serine

A

Histidine

43
Q

Give the amino acid of the autacoids with the following structure.
A. tyrosine
B. Phenylalanine
C. Tryptophan
D. Histidine
E. Serine

A

Tryptophan

44
Q

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

A

II only

45
Q

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
B. II,III
C. III, IV
D. II only
E. I only

A

III, IV

46
Q

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 only

47
Q

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 and III only

48
Q

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, and III

49
Q

Which of the following drugs is metabolized by CYP1A?
A. Acetaminophen
B. Fluoroquinolones
C. Imipramide
D. Theophyliine
E. All of the above

A

All of the above

50
Q

Which of the following drugs is metabolized by CYP4B?
A. prostaglandin
B. Carbamazepine
C. Dapsone
D. Hydrocortisone
E. All of the above

A

Prostaglandin

Org Chem PACOP (6 decks)

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