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Flashcards in Antiangial drug classes Deck (28):
1

What is the prototype organic nitrate

nitroglycerin

2

MOA of nitroglycerin

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

3

efficacy of nitroglycerin

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

4

Cardiovascular effects of nitroglycerin

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

5

Pharmacogenetics of nitroglycerine

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

6

Pharmacokinetics of nitroglycerin

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

7

Adverse effects of nitroglycerin

headaches, orthostatic hypotension, reflex tachycardia

8

Drug interactions of nitroglycerin

vasodilator drugs for ED (blood pressure)
alcohol (ALDH2)

9

Two classes of CCBs

Dihydropyridines and heart rate-lowering

10

Prototype dihydropyridines

nifedipine

11

Heart-rate lowering prototypes

verapamil, diltiazem

12

MOA of CCBs

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

13

Efficacy of CCBs

prophylaxis for angina attacks, no survival benefit

14

Features of Nifedipine

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

15

Features of Verapamil and diltiazem

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

16

Difference between verapamil and diltiazem

diltiazem produces less cardiac depression and is better tolerated

17

Adverse effects of verapamil

dradyarrhythmias, cardiac depression, constipation

18

Adverse effects of diltiazem

bradyarrhythmias, cardiac depression

19

Adverse effects of nifedipine

reflex tahycardia, flushing, peripheral edema

20

Beta blocker for angina

propranalol

21

MOA of propranalol for angina

decreases heart rate, contractile force and systemic blood pressure.

22

Efficacy of propranalol

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

23

Therapeutic approach to angina

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

24

Prototype PDE5 Inhibitor

sildenafil (viagra)

25

MOA of sildenafil

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

26

Pharmacokinetics of sildenafil

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

27

Adverse effects of sildenafil

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

28

Drug interactions with sildenafil

can potentiate the effects of organic nitrates and alpha blockers