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Pharm > Antianginals > Flashcards

Antianginals Flashcards

1
Q

Treatment for the immediate relief of angina, prophylaxis of angina and increase in exercise tolerance includes:

A

organic nitrates
calcium channel blockers
beta blockers
(via reducing myocardial O2 demand)

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2
Q

What is the prototype for organic nitrate?

A

Nitroglycerin

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3
Q

Nitroglycerin is a ___drug

A

Pro

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4
Q

Nitroglycerin releases __ when ….

A

NO; when metabolized by ALDH-2

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5
Q

At therapeutic doses, NTG mainly causes dilation of the ____

A

veins
(some arterial dilation can happen)

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6
Q

NTG effect on the heart is direct/indirect?

A

indirect; NTG decreases venous return which reduces cardiac preload which reduces oxygen demand

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7
Q

NTG also has a modest effect on coronary ….

A

blood flow

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8
Q

What is the MOA of NTG on coronary blood flow?

A

modest dilation of large epicardial arteries to promote flow of blood to regions os ischemia in the endocardium

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9
Q

What are the effects of NTG on small resistance vessels?

A

effects are minimal; small resistance vessels may already be maximally dilated due to autoregulation

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10
Q

NTG also has a direct vasodilation effect on ..

A

VASOSPASTIC coronary arteries

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11
Q

NTG is effective in prophylaxis and termination of

A

acute anginal attacks (abloshes ST segment depression)
improves exercise tolerance

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12
Q

does NTG have a survival benefit or prevention of MI?

A

NO

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13
Q

what are the CV effects of NTG at usual doses?

A
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14
Q

what are the CV effects of NTG as higher doses

A
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15
Q

arterioles in face/neck and meningeal arteries are sensitive/insensitive to vasodilation from NTG?

A

sensitive

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16
Q

ALDH-2 polymorphism, which has a high prevalence in patients of Asian origin, have LOW-ACTIVITY of ______. Why is this important?

A

ALDH2*2 allele and therefore have possible diminished clinical efficacy due to decreased metabolism of the prodrug

17
Q

the route of administration of organic nitrates determines …

A

time to onset and DOA

18
Q

What are the 3 forms of NTG?

A

sublingual
oral
transdermal

19
Q

forms of sublingual NTG include ____ and _____

A

tablets and sprays

20
Q

tablets and sprays (forms of sublingual NTG) bypass _____ and therefore attain therapeutic levels within in ______. This provides ____ relief but has a short ____.

A

bypasses first pass metabolism
attains therapeutic levels in 1-2 minutes
RAPID relief
DOA (< 1 hr)

21
Q

Active NTG tablets cause a ______ sensation when placed under the tongue

A

tingling

22
Q

tablets are unstable to ….

A

heat/light, moisture

23
Q

Patients should contact EMS if ______ does not terminate angina within _ minutes

A

1st dose
5 minutes

24
Q

oral or transdermal forms are available for acute relief and prophylaxis; onset is _____ (compared to sublingual) and DOA is _____ (compared to sublingual)

A

slower onset (30-60 min)
DOA is longer (4-24 hr)

25
Q

tolerance to organic nitrates occurs

A

with too frequent or sustained use and can happen within 24 hours

26
Q

“Monday morning headaches”

A
27
Q

MOA of tolerance to organic nitrates

A

NTG-mediated inactivation of ALDH-2 (i.e. mechanism based enzyme inhibition)

28
Q

tolerance to organic nitrates are most common with what kinds of formulations?

A

oral, transdermal

29
Q

how is tolerance to organic nitrates minimized?

A

minimized using eccentric dosing that provides nitrate-free intervals of 10-12 hr

30
Q

adverse effects of nitrates:

A

headache, facial flushing
orthostatic hypotension
reflex tachycardia

31
Q

one adverse effect of nitrates includes orthostatic hypotension. This is because …

A

nitrates effect on veins

32
Q

another adverse effect of nitrates is reflex tachycardia. This is because ….

A

nitrates increases O2 demand… This can negate the drugs beneficial effect. Use in combo with beta blockers or calcium channel blockers to suppress this.

33
Q

drug interactions of nitrates include:

A

-vasodilators (severe refractory hypotension and possible MI if taken within 24 hr of a PDE 5 inhibitor or alpha blocker)
-alcohol (complex interaction due to inhibition of ALDH-2, acutely worsens NTG-induced orthostatic hypotension)

34
Q

the two subclasses of ca channel blockers are

A

dihydropyridines
and
HR lowering

35
Q

an example of dihydropyridine ca channel blocker is

A

nifedipine

36
Q

an example of a HR lowering ca channel blocker is

A

verapamil

Pharm (6 decks)

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