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Org Chem PACOP > 151-200 > Flashcards

151-200 Flashcards

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1
Q

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,II,III,IV are correct

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2
Q

Which of the following drugs is/are a butyrophenone derivative?
I. thioridazine
II. Fluphenazine
III. Droperidol
IV. Haloperidol

A

III and IV are correct

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3
Q

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 esterification or 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

A

Maximal analgesic effects are observed with the free phenolic group at the 3 position.

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4
Q

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

A

A and B

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5
Q

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

A

Dihydromorphine and dihydrocodeine is more potent than the parent compound morphine.

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6
Q

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

A

A and B

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7
Q

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

A

Digoxin is less toxic than digitoxin because of its additional hydroxyl group that makes it
more hydrophilic.

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8
Q

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

A

It relaxes the vascular smooth muscle (vasodilation)

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9
Q

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
B. Dypirydamole
C. Papaverine
D. Diltiazem
E. Nifedipine

A

Dypirydamole

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10
Q

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
B. Flecainide
C. Quinidine
D. Tocainide
E. Procainamide

A

Quinidine

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11
Q

An antiarrythmic drug that is an ᾳ-methyl analog structurally related to monoethylglycinexylide,
the active metabolite of xylocaine.
A. Disopyramide
B. Flecainide
C. quinidine
D. Tocainide
E. Procainamide

A

Tocainide

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12
Q

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

A

It irreversibly inhibits platelet aggregation by acetylating cyclooxygenase enzyme

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13
Q

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 therapy
D. A and B only
E. B and C only

A

A and B

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14
Q

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

A

III & Iv only

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15
Q

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,III only

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16
Q

Which of the following statements is true regarding halogenated anesthetic agents?
I. Addition of halogen atoms to ethers or hydrocarbons decreases flammability
II. Addition of halogen atoms to ethers or hydrocarbons often increases anesthetic potency.
III. Addition of halogen atoms to ethers or hydrocarbons decreases flammability
IV. Addition of halogen atoms to ethers or hydrocarbons often decreases anesthetic potency

A

I & II only

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17
Q

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

A

All of the above

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18
Q

Which of the following acids has mycobacteriostatic activity?
A. Propionic acid
B. Chaulmoogric acid
C. Mandelic acid
D. Salicylic acid
E. Amino acid

A

Chaulmoogric acid

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19
Q

Which of the following alcohols has a local anesthetic property?
A. Benzyl alcohol
B. 2-propanol
C. Ethanol
D. 2-pyridinemethanol
E. choline

A

Benzyl alcohol

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20
Q

Which of the following amino ethers has antihistamine property?
A. Dimethisoquin
B. Benzidioxanes
C. Clomiphene
D. Phenoxybenzamine
E. Methoxyphenamine

A

Benzidioxanes

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21
Q

Which of the following halogenated compounds has hypnotic properties?
A. Ethyl chloride
B. Carbon tetrachloride
C. Chloral
D. Hexachlorophene
E. Chloroform

A

Chloral

22
Q

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

A

A and C

23
Q

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

A

B and C

24
Q

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

A

Aromatic hydrocarbon

25
Q

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

A

Cetirizine

26
Q

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
B. Alkene
C. AlkyneAll
D. Alkane
E. All of the above

A

All of the above

27
Q

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

A

Glutamic acid

28
Q

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

A

Phenylalanine

29
Q

Wich of the following drugs is an ethylenediamine antihistamine?
A. Tripelennamine
B. Diphenhydramine
C. Promethazine
D. Astemizole
E. All of the above

A

Tripelennamine

30
Q

Which of the following drugs in an example of tricyclic antihistamine?
A. Tripelennamine
B. Diphenhydramine
C. Promethazine
D. Astemizole
E. All of the above

A

Promethazine

31
Q

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

A

Diphenhydramine

32
Q

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

A

Astemizole

33
Q

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

A

Rate theory

34
Q

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

A

Occupational theory

35
Q

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

A

Induced fit theory

36
Q

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

A

Activation aggregation theory

37
Q

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

A

Molecular pertubation theory

38
Q

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

A

A and B

39
Q

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

A

They can bind to regions of the receptor that are not involved in binding the natural ligand

40
Q

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

A

Inverse agonist

41
Q

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

A

Desensitization

42
Q

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

A

Sensitization

43
Q

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

A

Tolerance

44
Q

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

A

Dependence

45
Q

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

A

Affinity

46
Q

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

A

Efficacy

47
Q

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

A

Potency

48
Q

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

A

Suicide substrates

49
Q

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

A

Allosteric inhibitors

50
Q

These are enzyme inducers that are designed to mimic the transition state of an enzymecatalyze 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

A

Transition state analogue

Org Chem PACOP (6 decks)

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