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MEDCHEM 564 > Exam 2 Multiple Choice, True/False, etc (Atkins) > Flashcards

Exam 2 Multiple Choice, True/False, etc (Atkins) Flashcards

1
Q

Comparing digoxin to digitoxin, which of the following is true?

A) Digoxin requires a lower maintenance dose than digitoxin, possibly due to the increased serum protein binding of digoxin
B) Digitoxin, but not digoxin, inhibits the Ca2+ and Na2+ exchange protein in the plasma membrane of cardiac muscle cells
C) Digitoxin undergoes more hepatic metabolism than digoxin
D) Digoxin and digitoxin are both members of the bufadienolide class of cardiac glycosides
A

C) Digitoxin undergoes more hepatic metabolism than digoxin

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2
Q

Which is true for digoxin?

E) It includes a bipyridine ring
F) It is effective in the prevention of atrial fibrillation
G) It is a synthetic analog of a natural product found in the fox glove plant
H) It inhibits L-ty;e Ca2+ channels

A

F) It is effective in the prevention of atrial fibrillation

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3
Q

Nitric oxide, NO (dot):

A) is released from L-type Ca2+ channels in cardiac vasculature
B) inhibits L-type Ca2+ channels in cardiac vasculature
C) is the ‘active’ free radical metabolite of all anti-anginal organic nitrates
D) is the ‘active’ free radical metabolite of only the anti-anginal erythritol tetranitrate

A

C) is the ‘active’ free radical metabolite of all anti-anginal organic nitrates

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4
Q

Diltiazem is:

A) a bipyridine used for congestive heart failure
B) metabolized to desacetyl diltiazem, which contributes to the therapeutic activity
C) an arylkylamine L-type Ca2+ channel inhibitor
D) sold as a mixture of four stereoisomers

A

B) metabolized to desacetyl diltiazem, which contributes to the therapeutic activity

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5
Q

Potassium supplements are most likely to be necessary to relieve side effects of:

A) Beta blockers
B) Milrinone
C) Digoxin
D) Verapamil

A

C) Digoxin

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6
Q

Which of the following is a class 3 anti-arrhythmic that causes ‘smurf’ syndrome?

A) Procainamide
B) Bretylium tosylate
C) Amiodarone
D) Inamirinone

A

C) Amiodarone

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7
Q

Organic nitrates, such as isosorbide dinatrate:

A) Reach with DNA to down-regulate Ca2+ channel expression
B) Inhibit PDE-5 as a result of releasing nitrate ion
C) Are used for congestive heart failure
D) React with cellular thiols to yield nitrosothiols which subsequently yield nitric oxide

A

D) React with cellular thiols to yield nitrosothiols which subsequently yield nitric oxide

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8
Q

Which of the following ACE inhibitors are prodrugs that require hydrolysis to an active form?

A) Enalapril
B) Zofinopril
C) Captopril
D) Lisinopril

A

A) Enalapril

B) Zofinopril

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9
Q

Match these drugs to the following descriptions:

  • Prazosin
  • Aldomet
  • Clonidine
  • Doxazosin

A) An alpha-2 adrenergic agonist in the CNS that is used for ADHD and moderate hypertension
B) An alpha-1 adrenergic antagonist in the peripheral vasculature that is rapidly de-acetylated to an active metabolite
C) An alpha-1 adrenergic antagonist in the peripheral vasculature that is slowly de-acetylated to an active metabolite than the prototype of this drug class
D) A prodrug that is converted to alpha-methyl norepinephrine in the CNS

A

Prazosin: B) An alpha-1 adrenergic antagonist in the peripheral vasculature that is rapidly de-acetylated to an active metabolite

Aldomet: D) A prodrug that is converted to alpha-methyl norepinephrine in the CNS

Clonidine: A) An alpha-2 adrenergic agonist in the CNS that is used for ADHD and moderate hypertension

Doxazosin: C) An alpha-1 adrenergic antagonist in the peripheral vasculature that is slowly de-acetylated to an active metabolite than the prototype of this drug class

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10
Q

Which of the following statements about esmolol are true?

  1. Esmolol is a beta-1 selective adrenergic antagonist
  2. Esmolol is a prodrug used to prevent cardiac arrythmias
  3. Hydrolysis of esmolol yields a beta-1 selective adrenergi cantagonist
  4. Esmolol is an aryloxypropanolamine
A
  1. Esmolol is a beta-1 selective adrenergic antagonist

4. Esmolol is an aryloxypropanolamine

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11
Q

Indicate whether each statement refers to either ACE inhibitors, ARBs, or both:

  1. Analog of peptide angiotensin II
  2. Cause a dry cough as a common side effect
  3. Chelate Zn2+ ions in the active site of its target, in their active form
  4. Bind to angiotentin II receptors, of subclass (AT-II)I
A
  1. Analog of peptide angiotensin II
    BOTH
  2. Cause a dry cough as a common side effect
    ACE
  3. Chelate Zn2+ ions in the active site of its target, in their active form
    ACE
  4. Bind to angiotentin II receptors, of subclass (AT-II)I
    ARB
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12
Q

Indicate whether each statement refers to either (A) dopamine, (B) dobutamine, both or neither:

  1. One stereoisomer is a vasoconstrictor, one stereoisomer is a vasodilator and both have positive inotropic effects
  2. Has little dopaminergic agonist activity
  3. Enzymatically converted to norepinephrine
  4. Mainly metabolized by CYP3A4
  5. Mainly metabolized by glucuronosyl transferases to glucuronides
  6. Has one chiral center
A
  1. One stereoisomer is a vasoconstrictor, one stereoisomer is a vasodilator and both have positive inotropic effects
    B
  2. Has little dopaminergic agonist activity
    B
  3. Enzymatically converted to norepinephrine
    A
  4. Mainly metabolized by CYP3A4
    None
  5. Mainly metabolized by glucuronosyl transferases to glucuronides
    B
  6. Has one chiral center
    B
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13
Q

Comparing metoprolol and nadolol, which would you expect to have the longer duration, which is beta-1 selective?

A

Metoprolol: beta-1 selective because para substituted

Nadolol: longer duration because less N-dealkylation. The N-tert-butyl is sterically hindered than the N-isopropyl of metoprolol

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14
Q

Which of the following ACE inhibitors are prodrugs?

Captopril
Perindopril
Lisinopril
Fosinopril

A

Perindopril

Fosinopril

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15
Q

Which of the following statements about ACE inhibitors are true?

A) They have the common side effect of tachycardia
B) They inhibit the angiotensin II subtype 1 receptor
C) They mimic the structure of the peptides Angiotensin I and bradykinin
D) They contain Zn-chelating groups in order to bind bradykinin

A

C) They mimic the structure of the peptides Angiotensin I and bradykinin

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16
Q

What is the therapeutic target of the dihydropyridines?

A

L-type Ca2+ channels

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17
Q

What are the therapeutic uses of dihydropyridines?

A

Antihypertensive, angina

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18
Q

Identify between guanadrel and guanabenz which is centrally active and which is peripherally active as anti-hypertensive agents. Which has the lower pKa?

A

Guanadrel: peripheral

Guanabenz: central (lower pKa)

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19
Q

What are the therapeutic uses of ACE inhibitors?

A

Hypertension

Congestive heart failure

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20
Q

What is the advantage of aliskiren/losartan over perindopril in terms of side effects?

A

No cough, because they don’t increase bradykinin

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21
Q

True or false? Both verapamil and ivapradine are alkyl amines that inhibit Ca2+ channels.

A

False

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22
Q

True or false? Ivabradine is metabolized mainly by N-glucuronidation in contrast to verapamil which is metabolized mainly by CYPs.

A

False

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23
Q

True or false? Only ivabadine (not verapamil) inhibits Na+ channels in the sino-atrial node.

A

True

24
Q

True or false? Both verapamil and ivabradine are metabolized extensively by CYP-dependent N-dealkylate and O-dealkylation.

A

True

25
Q

True or false? Ivabradine is achiral, in contrast to verapamil for which the (S) enantiomer is more potent thant the (R) enantiomer.

A

False

26
Q

True or false? Ivabradine selectively inhibits N-type Ca2+ channels.

A

False

27
Q

Which drug(s) is an alpha-1 adrenergic antagonist and false neurotransmitter in the peripheral vasculature?

  • Clonidine
  • Apraclonidine
  • Guanethidine
  • Tolazoline
A

Guanethidine

28
Q

Which drug(s) is therapeutically used to reduce glaucoma: does not enter the CNS?

  • Clonidine
  • Apraclonidine
  • Guanethidine
  • Tolazoline
A

Apraclonidine

29
Q

Which drug(s) is a non-selective alpha-1 alpha-2 adrenergic agonist imidazoline?

  • Clonidine
  • Apraclonidine
  • Guanethidine
  • Tolazoline
A

Tolazoline

30
Q

For which drug(s) does steric hindrance result in a high proportion of “eclipsed” or “perpindicular” rings?

  • Clonidine
  • Apraclonidine
  • Guanethidine
  • Tolazoline
A

Clonidine

Apraclonidine

31
Q

Which drugs has a high pKa, leading to a large fraction of charged drug (> 99.9%)?

  • Clonidine
  • Apraclonidine
  • Guanethidine
  • Tolazoline
A

Guanethidine

32
Q

The pKa of the quanidine functional group is intermediate between clonidine and guanethidine

  • Clonidine
  • Apraclonidine
  • Guanethidine
  • Tolazoline
A

Apraclonidine

33
Q

Hydralazine is an older antihypertensive agent still in use. Which of the following is true:
A) Hydralazines release nitric oxide and causes vasodilation
B) Slow acetylators exhibit more toxicity than fast acetylators
C) Fast acetylators exhibit more toxicity than slow acetylators
D) Hydralazine has the benefit of no reflex tachycardia or reflex increase in renin secretion

A

B) Slow acetylators exhibit more toxicity than fast acetylators

34
Q

ACE inhibitors are the result of “rational drug design”. They include:
A) Sulfhydryl groups, carboxylates or phosphinate groups in the parent drug or in an activated form that binds to the active site Zn2+ ion
B) Hydrophobic groups that bind to the active site Zn2+ ion of ACE
C) Esterified carboxy groups that are hydrolyzed by the active site Zn2+ ion
D) Imidazole groups that mimic proline in the ACE substrates

A

A) Sulfhydryl groups, carboxylates or phosphinate groups in the parent drug or in an activated form that binds to the active site Zn2+ ion

35
Q

Aliskiren (Tekturn) is distinct from ACE inhibitors because:
A) it does not produce a persistent dry cough as a side effect
B) It inhibits a different form of ACE than captopril, enalapril and fosinipril
C) Its acyl proline group is sterically hindered
D) It targets the enzyme renin

A

D) It targets the enzyme renin

36
Q

Losartan was the ‘first in class’ ARB. Which of the following are true?
A) It is a prodrug requiring activation by CYP2C9
B) Inhibits AT-II subtype 2 receptors in renal, cardiac and vascular tissue
C) Is basic and easily protonated, which fascilitates formulation as Cl salts
D) None of the above

A

B) Inhibits AT-II subtype 2 receptors in renal, cardiac and vascular tissue

37
Q

Isosorbide mononitrate is useful in the treatment of angina. Which of the descriptions below is true?
A) It is an active metabolite that activates guanylate cyclase in coronary vasculature
B) Is converted to active drug, isosorbide dinitrate
C) Is an “active metabolite” of isosorbide dinitrate that reacts with thiols to generate nitric oxide
D) Inhibits the “funny” Na+ channel in coronacy vasculature

A

C) Is an “active metabolite” of isosorbide dinitrate that reacts with thiols to generate nitric oxide

38
Q

Which statements are true of amiodarone:

  • More water soluble due to incorporation of iodine atoms on aromatic ring
  • Extremely long half-life (~few months)
  • Shorter half-life due to increased water solubility
  • Causes thyroid toxicity
  • Some patients treated with the develop a skin discoloration known as “smurf syndrome”
A
  • Extremely long half-life (~few months)
  • Causes thyroid toxicity
  • Some patients treated with the develop a skin discoloration known as “smurf syndrome”
39
Q

Which of the following is true of dronedarone:

  • More water soluble due to incorporation of iodine atoms on aromatic ring
  • Extremely long half-life (~few months)
  • Shorter half-life due to increased water solubility
  • Causes thyroid toxicity
  • Some patients treated with the develop a skin discoloration known as “smurf syndrome”https://www.brainscape.com/decks/6883456/cards/quick_new_card
A
  • Shorter half-life due to increased water solubility
40
Q

Which statement(s) are true of ivabradine?

1) Extensively metabolized mainly by CYP-dependent O-demetylation and N-dealkylation to inactive metabolites
2) An L–type Ca channel blocker used for arrhythmias and congestive angina
3) Inhibits the “funny” Na+ channel and reduces oxygen demand in cardiac tissue

A

1) Extensively metabolized mainly by CYP-dependent O-demetylation and N-dealkylation to inactive metabolites
3) Inhibits the “funny” Na+ channel and reduces oxygen demand in cardiac tissue

41
Q

Which of the following statement(s) are true of verapamil?

1) Extensively metabolized mainly by CYP-dependent O-demetylation and N-dealkylation to inactive metabolites
2) An L–type Ca channel blocker used for arrhythmias and congestive angina
3) Inhibits the “funny” Na+ channel and reduces oxygen demand in cardiac tissue

A

1) Extensively metabolized mainly by CYP-dependent O-demetylation and N-dealkylation to inactive metabolites
2) An L–type Ca channel blocker used for arrhythmias and congestive angina

42
Q

An exciting new class of drugs used for CHF is included in the combination drug Sacubitril. t leads to increased levels of atrial natriuretic peptide, which is released by cardiac atria and helps to control several hemodynamic responses. The target of these drugs is:

A

Niprilysin

43
Q

Which of the following statements are true of minoxidil?

1) It is a prodrug
2) The major side effect of rogaine is hypertensive crisis
3) Is metabolized identically in humans and experimental animal models

A

1) Is is a prodrug

44
Q

For each pair which has the longer half-life?

  • Dronedarone and amiodarone
  • Doxazosin and prazosin
  • Mexiletine and lidocaine
A

1) Amiodarone
2) Doxazosin
3) Mexiletine

45
Q

Which drugs have inactive metabolites as a result of CYP-dependent O-demethylation?

  • dronedarone
  • amiodarone
  • doxazosin
  • prazosin
  • mexiletine
  • lidocaine
A
  • doxazosin

- prazosin

46
Q

Which statement(s) are true of ACE inhibitors?

1) Incorporation of tetrazole was a strategy to aid in formulation and to mimic the C-terminus of angiotensins
2) Causes a dry cough as a common side effect
3) Rationally designed to mimic angiotensin II
4) Chelates Zn2+ ion in the active site of its target, in the active form
5) Binds to angiotensin II receptors, subclass (AT-II)I
6) Analogs of the peptide renin

A

2) Causes a dry cough as a common side effect

4) Chelates Zn2+ ion in the active site of its target, in the active form

47
Q

Which statement(s) are true of ARB’s?

1) Incorporation of tetrazole was a strategy to aid in formulation and to mimic the C-terminus of angiotensins
2) Causes a dry cough as a common side effect
3) Rationally designed to mimic angiotensin II
4) Chelates Zn2+ ion in the active site of its target, in the active form
5) Binds to angiotensin II receptors, subclass (AT-II)I
6) Analogs of the peptide renin

A

1) Incorporation of tetrazole was a strategy to aid in formulation and to mimic the C-terminus of angiotensins
3) Rationally designed to mimic angiotensin II
5) Binds to angiotensin II receptors, subclass (AT-II)I

48
Q

The enzyme activated as a result of nitroglycerin therapy is:

A

Guanylate cyclase

49
Q

The organic nitrates can be considered as “prodrugs” because (include a chemical name/compound):

A

They are degraded to an active fragment, nitric oxide

50
Q

Which organic nitrate has the longest duration of action?

A

Mannitol hexanitrate

51
Q

Chiral centers are not normally considered with organic nitrates because:

A

The active component has no chiral centers (NO)

52
Q

True or false: the guanidine of clonidine has a higher pKa than the guanidine of apraclonidine

A

False

53
Q

True or false: clonidine has a smaller fraction of ionized, positively charged drug than apraclonidine

A

True

54
Q

True or false: The Cl atoms of apraclonidine make the para amino group positively charged

A

False

55
Q

True or false: Apraclonidine inhibits imidazoline receptors and has decongestant properties

A

False

56
Q

Which of the following statement(s) is true of dopamine:

1) The commercially available preparation is racemic
2) Has renal effects including increased Na+ excretion
3) Significant metabolism by enzymes in neural tissue
4) Pure B-2 antagonist

A

2) Has renal effects including increased Na+ excretion

3) Significant metabolism by enzymes in neural tissue

57
Q

Which of the following statement(s) is true of dobutamine:

1) The commercially available preparation is racemic
2) Has renal effects including increased Na+ excretion
3) Significant metabolism by enzymes in neural tissue
4) Pure B-2 antagonist

A

1) The commercially available preparation is racemic

MEDCHEM 564 (3 decks)

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