Antiangial drug classes

Question 1

What is the prototype organic nitrate

Answer 1

nitroglycerin

Question 2

MOA of nitroglycerin

Answer 2

prodrug metabolized to NO in VSM by ALDH2, relaxes VSM and dilates blood vessels reducing preload

Question 3

efficacy of nitroglycerin

Answer 3

increases exercise tolerance and reduces symptoms, but produces no survival benefit

Question 4

Cardiovascular effects of nitroglycerin

Answer 4

no inotropic or chronotropic effects at usual doses, at higher doses reflex tachycardia due to decreased MAP

Question 5

Pharmacogenetics of nitroglycerine

Answer 5

ALDH2 polymorphism (30-50% in asians) reduces clinical efficacy

Question 6

Pharmacokinetics of nitroglycerin

Answer 6

Oral or cutaneous preps for slow onset, long duration, but most common are sublingual NTG, fast acting short duration

Question 7

Adverse effects of nitroglycerin

Answer 7

headaches, orthostatic hypotension, reflex tachycardia

Question 8

Drug interactions of nitroglycerin

Answer 8

vasodilator drugs for ED (blood pressure)

alcohol (ALDH2)

Question 9

Two classes of CCBs

Answer 9

Dihydropyridines and heart rate-lowering

Question 10

Prototype dihydropyridines

Answer 10

nifedipine

Question 11

Heart-rate lowering prototypes

Answer 11

verapamil, diltiazem

Question 12

MOA of CCBs

Answer 12

block voltage gated L-type calcum channels by binding alpha-1 subunit. increase vasodilation decrease afterload

Question 13

Efficacy of CCBs

Answer 13

prophylaxis for angina attacks, no survival benefit

Question 14

Features of Nifedipine

Answer 14

greater inhibitory action on VSM than myocardium, little effect on SA and AV nodes

Question 15

Features of Verapamil and diltiazem

Answer 15

Also act on SA and AV nodal tissue decreasing heart rate and contractility , less potent vasodilators

Question 16

Difference between verapamil and diltiazem

Answer 16

diltiazem produces less cardiac depression and is better tolerated

Question 17

Adverse effects of verapamil

Answer 17

dradyarrhythmias, cardiac depression, constipation

Question 18

Adverse effects of diltiazem

Answer 18

bradyarrhythmias, cardiac depression

Question 19

Adverse effects of nifedipine

Answer 19

reflex tahycardia, flushing, peripheral edema

Question 20

Beta blocker for angina

Answer 20

propranalol

Question 21

MOA of propranalol for angina

Answer 21

decreases heart rate, contractile force and systemic blood pressure.

Question 22

Efficacy of propranalol

Answer 22

reduces severity and frequence of angina attacks, reduces mortality, not effective for vasospastic angina.

Question 23

Therapeutic approach to angina

Answer 23

beta blockers w/ nitroglycerin as needed, CCBs second line as monotherapy.

Question 24

Prototype PDE5 Inhibitor

Answer 24

sildenafil (viagra)

Question 25

MOA of sildenafil

Answer 25

inhibits PDE-5 (isoform in VSM of corpora cavernosum) prevents cGMP degredation, allows dilation and erection.

Question 26

Pharmacokinetics of sildenafil

Answer 26

1 hr before anticipated sexual activity 2-4 hr duration, decreased by high fat diet. Metabolized by CYP3A4

Question 27

Adverse effects of sildenafil

Answer 27

hedache flushing, nasal congestion, dyspepsia, abnormal vision, hearing loss, priapism

Question 28

Drug interactions with sildenafil

Answer 28

can potentiate the effects of organic nitrates and alpha blockers