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Pharmacology > 2.2 Anti-Angina Drugs > Flashcards

2.2 Anti-Angina Drugs Flashcards

1
Q

prototype, used for dynamite manufacture

A

Nitroglycerin

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2
Q

Release nitric oxide in vascular smooth muscle target tissues

A

NITRATES & NITRITES

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3
Q

removal of nitrates in a stepwise fashion

A

organic nitrate reductase

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4
Q

Oral bioavailability: nitroglycerin and isosorbide dinitrate is

A

low (10-20%)

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5
Q

Nitroglycerin concentrations are not affected by the route of administration (T/F)

A

False

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6
Q

NITRATES & NITRITES

Preferred route

A

sublingual route - Avoids first pass effect

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7
Q

NITRATES & NITRITES

Preparations

A

Sublingual, Tablet forms, Topical

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8
Q

NITRATES & NITRITES

Duration of effect

A

BRIEF (15-30 minutes)

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9
Q

NITRATES & NITRITES

Total dose to be given must be limited

A

True

to avoid excessive effect

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10
Q

Organic nitrate; ORAL long acting (>6 hrs)

A

Pentaerythritol (PETN)

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11
Q

highly volatile liquids
Available in fragile glass ampules
Obsolete now for angina

A

Amyl nitrite and other nitrates

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12
Q

2 metabolites of nitrates

A

2-dinitroglycerin derivative

5-mononitrate

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13
Q

Metabolite of nitrate that has significant vasodilator efficacy & probably provides most of the therapeutic effect (oral nitroglycerin)

A

2-dinitroglycerin derivative

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14
Q

Metabolite of nitrate that an active metabolite of nitroglycerin. Available as isosorbide mononitrate (oral).

A

5-mononitrate

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15
Q

Nitroglycerin activation requires

A

enzymatic action.

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16
Q

NITRATES & NITRITES

Can be denitrated by

A

glutathione S-transferase in Smooth muscle & other cells

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17
Q

2 Dehydrogenase isoforms that are key in (+) and release of Nitric Oxide from nitroglycerin & pentaerythritol tetranitrate

A

Dehydrogenase isoform 2 (ALDH2) & Isoform 3 (ALDH3)

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18
Q

response evoked when hypotensive doses are given.

A

Autonomic reflex

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19
Q

Nitroglycerin relaxes all types of smooth muscle regardless of cause of preexisting muscle tone.

A

True

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20
Q

(T/F)
Arteries: respond in lowest concentration
Veins: slightly higher

A

False
Veins: respond in lowest concentration
Arteries: slightly higher

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21
Q

result with effective dose:

  • Marked relaxation of veins
  • Increase venous capacitance
  • Decrease ventricular preload
  • Decrease pulmonary vascular pressure and heart size.
A

Nitrates

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22
Q

Common SE of nitroglycerin & amyl nitrate (2)

A

Temporal artery pulsations & throbbing headache + meningeal artery pulsations

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23
Q

compensatory responses (+) by Baroreceptors & hormonal mechanism responding to decrease arterial pressure are indirect effects of

A

Nitrates

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24
Q

diverts blood from normal to ischemic areas of the myocardium through dilation of collateral vessels.

A

Nitroglycerin

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25
Q

Nitroglycerin also exerts a strong negative inotropic effect on the heart via nitric oxide. *T/F)

A

False

weak negative inotropc effect

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26
Q

Nitrates readily release nitric oxide in erectile tissue as well as vascular smooth muscle and activate guanylyl cyclase > inc cGMP > dephosphorylation (myosin light chains & relaxation > enhance erection (T/F)

A

True

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27
Q

NO release from nitroglycerin > (+) guanylyl cyclase (platelets e.g. smooth m.) > inc cGMP > dec in platelet aggregation (T/F)

A

True

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28
Q

No survival benefit when nitroglycerin is used in acute myocardial Infarction

A

True

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29
Q

IV nitroglycerin may be able in unstable angina.

A

True

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30
Q

Methemoglobin: has very high affinity to oxygen

A

False

Very low affinity

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31
Q

In adults: the plasma level of nitrate resulting from large doses (organic & inorganic nitrates) is too high and causes significant methemoglobinemia (T/F).

A

False

too low to cause significant methemoglobinemia

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32
Q

Methemoglobinemia: if excessive > treated with (1) which is now being replaced by (2)

A

IV methylene blue

hydroxocobalamin (form of vit.B12

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33
Q

Nitrates

Contraindication

A

elevated intracranial pressure

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34
Q

Continuous exposure to nitrates > isolated smooth muscle may develop complete tolerance (tachyphylaxis) (T/F)

A

True

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35
Q

Nitrates

Tolerance may be due to (3)

A

(a) systemic compensation
(b) significant sympathetic discharge occurs
(c) Diminished bioactivation of organic nitrates and to a lesser degree loss of soluble guanylate cyclase responsiveness

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36
Q

Nitrates

What supplementation may partially reverse tolerance, reduce availability of sulfhydryl donors

A

Cysteine

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37
Q

Other organic nitrates: less susceptible than nitroglycerin to tolerance (T/F)

A

True

38
Q

Nitrate

Tolerance Prevented by: treatment with antioxidants that protect ALDH3 (T/F)

A

False

ALDH2

39
Q

Nitrates

Carcinogenic derivative:

A

Nitrosamines

40
Q

Nitrate Effects in Angina of Effect: (True except)
A. Decreased venous return to the heart & resulting reduction of intracardiac volume are important beneficial hemodynamic effects.
B. Decrease arterial pressure
C. Decreased intraventricular pressure, dec left ventricular pressure assoc with dec wall tension (Laplace relation)
D. Inc myocardial oxygen requirement
E. Increase caliber of large epicardial coronary arteries

A

Dec myocardial oxygen requirement

41
Q

Major mechanism of relief of effort angina:

A

reduction of oxygen demand

42
Q

Nitrate Effects in Variant Angina

By relaxing the epicardial cardiac veins’ smooth muscle > relieving cardiac vein spasm.

A

False

By relaxing the epicardial coronary arteries’ smooth muscle > relieving coronary artery spasm

43
Q 
Nitrate Effects in Unstable angina (True except)
A. Dilate epicardial coronary erteries
B. Reduce myocardial oxygen demand
C. Decrease platelet aggregation
D. All
E. None
A

None

44
Q

Clinical Use of Nitrates:

most frequently used

A

NTG, SL

45
Q 
Clinical Use of Nitrates:
rapid onset (1-3 min), for immediate treatment
A

NTG, SL

46
Q

Clinical Use of Nitrates:

not suitable for maintenance therapy

A

NTG, SL

47
Q

Clinical Use of Nitrates:
(restricted to) Severe, recurrent rest angina
Hemodynamic effects quickly reversed by discontinuation

A

NTG, IV

48
Q

Clinical Use of Nitrates:

Prolonged blood conc. > develop tolerance

A

NTG- Buccal, oral, transdermal

49
Q

Nitro-Vasodilator with vasodilating effect in normal coronary arteries and with angina that reduces relative risk of fatal and nonfatal coronary events in patients receiving the drug

A

Nicorandil

50
Q

A nicotinamide nitrate ester that reduces both preload & afterload

A

Nicorandil

51
Q

prodrug that is converted to a nitric oxide-releasing metabolite and is efficient comparable to that of organic nitrates and is not subject to tolerance

A

Molsidomine

52
Q

necessary for the contraction of smooth and cardiac muscle

A

transmembrane calcium influx

53
Q

first clinically useful member of Calcium channel - blockung drugs

A

Verapamil

54
Q

a vasodilator alkaloid found in the opium poppy

A

papaverine

55
Q

prototype of the dihydropyridine family of calcium channel blockers

A

Nifedipine

56
Q

The voltage-gated T-type calcium channel is the dominant type in cardiac and smooth muscle (T/F)

A

False

L-type calcium channel is dominant

57
Q

Calcium channel - blocking drugs consists of α1 (the larger, pore-forming subunit), α2, β, γ, and δ subunits (T/F)

A

True

58
Q

Which Calcium channel - blocking drugs have been demonstrated to bind to one site on the α1 subunit (2)?

A

Nifedipine and other dihydropyridines

59
Q

verapamil and diltiazem appear to bind to identical receptors (T/F)

A

False

bind to closely related but not identical receptors in another region of the same subunit

60
Q

Binding of a drug to the verapamil or diltiazem receptors allosterically affects dihydropyridine binding (T/F)

A

True

61
Q

receptor regions of verapamil and diltiazem are stereospecific (T/F)

A

False
receptor regions are stereoselective, since marked differences in both stereoisomer-binding affinity and pharmacologic potency are observed for enantiomers of verapamil, diltiazem, and optically active nifedipine congeners.

62
Q

Blockade of calcium channels by verapamil and diltiazem resembles that of sodium channel blockade by local anesthetics (T/F)

A

True

63
Q

verapamil and diltiazem act from the inner side of the membrane (T/F)

A

True

64
Q

verapamil and diltiazem bind more effectively to open channels and activated channels (T/F)

A

False

OPEN channels and INACTIVATED channels

65
Q

In verapamil and diltiazem: binding of the drug reduces the frequency of opening in response to depolarization > decrease in transmembrane calcium current > smooth muscle results in long-lasting relaxation (T/F)

A

True

66
Q

In verapamil and diltiazem: decrease in transmembrane calcium current > smooth muscle results in long-lasting relaxation > reduction in contractility throughout the heart (T/F)

A

True

67
Q

In verapamil and diltiazem: decrease in transmembrane calcium current > smooth muscle results in long-lasting relaxation > decreases in AV node pacemaker rate and SA node conduction velocity (T/F)

A

False

decreases in sinus node pacemaker rate and atrioventricular node conduction velocity

68
Q

Smooth muscle responses to calcium influx through

A

ligand-gated calcium channels

69
Q

elevating the concentration of calcium will completely reverse blocks

A

False

Partially reverse

70
Q

Block can also be partially reversed by the use of drugs that decrease the transmembrane flux of calcium

A

False
Block can also be partially reversed by the use of drugs that increase the transmembrane flux of calcium, such as sympathomimetics

71
Q

Potassium channels in vascular smooth muscle are inhibited by verapamil, thus limiting the vasodilation produced by this drug

A

True

72
Q

a selective T-type calcium channel blocker that was introduced for antiarrhythmic use but has been withdrawn

A

Mibefradil

73
Q

This drug block Sodium channels as well as calcium channels byt is an obsolete antiarrhythmic drug

A

Bepridil

74
Q

In Calcium channel - blocking drugs, arterioles appear to be more sensitive than veins (T/F)

A

True

75
Q

In Calcium channel - blocking drugs, Vascular smooth muscle appears to be the most sensitive, (T/F)

A

True

76
Q

In Calcium channel - blocking drugs, orthostatic hypotension is a common adverse effect (T/F)

A

False

not common

77
Q

Men may be more sensitive than women to the hypotensive action of diltiazem (T/F)

A

False

Women may be more sensitive than men

78
Q

In Calcium channel - blocking drugs, reduction of coronary artery spasm has been demonstrated in patients with what type of angina

A

variant angina

79
Q

have a greater ratio of vascular smooth muscle effects relative to cardiac effects than do diltiazem and verapamil

A

Dihydropyridines

80
Q

Which dihydropyridine is claimed to be particularly selective for cerebral blood vessels

A

nimodipine

81
Q

Impulse generation in the sinoatrial node and conduction in the atrioventricular node—so-called

A

slow-response, or Calcium-dependent, action potential

82
Q

Sodium channel block is more with verapamil, and still less marked with diltiazem (T/F)

A

False

Sodium channel block is modest with verapamil, and still less marked with diltiazem

83
Q

dihydropyridines appear to block smooth muscle calcium channels at concentrations above those required for significant cardiac effects;(T/F)

A

False

at concentrations below those required

84
Q

verapamil or diltiazem is less depressant on the heart than dihydropyridines (T/F)

A

False

dihydropyridines is less depressant on the heart than verapamil or diltiazem

85
Q

Skeletal muscle is not depressed by the calcium channel blockers because it uses

A. Intracellular pools of calcium
B. Extracellular pools of calcium

A

Intracellular pools of calcium

86
Q

approved for use in patients who have had a hemorrhagic stroke, but it has recently been withdrawn

A

Nimodipine

87
Q

used by intravenous and intracerebral arterial infusion to prevent cerebral vasospasm associated with stroke

A

Nicardipine

88
Q

used by the intra-arterial route in stroke

A

Verapamil

89
Q

Calcium channel blockers minimally interfere with stimulus-secretion coupling in glands and nerve endings (T/F)

A

True

90
Q

has been shown to inhibit insulin release in humans, but the dosages required are greater than those used in management of angina and other cardiovascular conditions

A

Verapamil

Pharmacology (1 decks)

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