Antianginals Flashcards

1
Q

What are the nitrates?

A

Nitroglycerin, Isosorbide Dinitrate, Amyl Nitrite

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2
Q

What is the MOA of Nitroglycerine?

A

Rapidly actin; sublingual; high first pass effect; spray; can be given as patch or ointment for prolonged action (prophylaxis)

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3
Q

When would you use Nitroglycerine?

A

Stable, variant, and unstable angina; used sublingually for acute and topical and SR for long-term

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4
Q

What are the side effects of Nitroglycerine?

A

Excessive vasodilation (decrease BP), headache, reflex tachycardia, dizziness (orthostatic hypotension), flushing, throbbing headache (meningeal artery dilation), severe hypotension when mixed with ED drugs; can have tolerance/rebound effect

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5
Q

What is the MOA of Isosorbide Dinitrate?

A

Rapidly acting; sublingual; can be given orally or topically for prolonged action (prophylaxis)

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6
Q

When would you use Isosorbide Dinitrate?

A

Stable, variant, and unstable Angina; acute attacks (sublingual prep)

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7
Q

What are the side effects of Isosorbide Dinitrate?

A

Excessive vasodilation (decrease of BP), headache, reflex tachycardia, dizziness (orthostatic hypotension), flushing, throbbing headache (meningeal artery dilation), hypotension when mixed with ED drugs; can have tolerance/rebound effect

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8
Q

What is the MOA of Amyl Nitrite?

A

Convert to NO > Vasodilation (veins affected more than arteries); inhalation

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9
Q

When would you use Amyl Nitrite?

A

Stable, variant, and unstable Angina; acute attacks (sublingual prep)

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10
Q

What are the side effects of Amyl Nitrite?

A

Excessive vasodilation (decrease of BP), headache, reflex tachycardia, dizziness (orthostatic hypotension), flushing, throbbing headache (meningeal artery dilation), hypotension when mixed with ED drugs; can have tolerance/rebound effect

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11
Q

What are the Ca channel blockers?

A

Verapamil, Diltiazem, Nifedipine, Amlodipine, Nicardipine

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12
Q

What is the MOA of Verapamil?

A

Block L-type Ca channels, preventing Ca influx > decreased arteriolar tone (decreased afterload), cardiac depression (decreases HR and contractility) > less O2 requirement

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13
Q

When would you use verapamil?

A

Stable and variant angina to relieve chest pain; fast atrial/nodal arrhythmias to slow HR/AV conduction

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14
Q

What are the side effects of verapamil?

A

High doses/toxicity may cause CHF; constipation, flushing, dizziness; AV blockade, sinus node depression

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15
Q

What is the MOA of Diltiazem?

A

Block L-type Ca channels, preventing Ca influx > decreased arteriolar tone (decreased afterload), cardiac nodal and muscle cells; decreases HR, AV conduction , myocardial contractility better than Verapamil

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16
Q

When would you use Diltiazem?

A

Stable and variant angina; posses both cardiac and vasodilator activity

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17
Q

What are the side effects of Diltiazem?

A

Excessive dilation (decrease of BP) > reflexive tachycardia, dizziness (orthostatic hypotension), flushing, throbbing headache (meningeal artery dilation); potential severe hypotension with erectile dysfunction treatment (sildenafil, etc.)

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18
Q

What is the MOA of Nifedipine?

A

Dihydropyridine; Block L-type Ca channels, preventing Ca influx > decreased arteriolar tone (decreased afterload) in vascular smooth muscle, cardiac nodal and muscle cells; causes arteriolar dilation and less cardiac depression

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19
Q

When would you use Nifedipine?

A

Stable angina esp. vasospastic angina (Prinzmetal’s)

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20
Q

What are the side effects of Nifedipine?

A

Avoid short-acting agents; excessive vasodilation > reflex tachycardia, nausea, lightheadedness, dizziness, headache, peripheral edema

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21
Q

What is the MOA of beta blockers?

A

Inhibit beta-1, decreasing HR and contractility, which decreases cardiac O2 demand

22
Q

When would you use beta blockers?

A

Stable, unstable, and silent angina; NOT a vasodilator

23
Q

What are the side effects of beta blockers?

A

Excess cardiac depression when used with Ca channel blocker

24
Q

What is the MOA of Amlodipine?

A

Dihydropyridine; blocks L-type Ca channels > no Ca influx in vascular smooth muscle, cardiac nodal and muscle cells; causes arteriolar dilation and less cardiac depression

25
Q

When would you use Amlodipine?

A

Stable angina esp. vasospastic angina (Prinzmetal’s)

26
Q

What are the side effects of Amlodipine?

A

Avoid short-acting agents; excessive vasodilation > reflex tachycardia, nausea, lightheadedness, dizziness, headache, peripheral edema

27
Q

What is the MOA of Nicardipine?

A

Dihydropyridine; Block L-type Ca channels > no Ca influx in vascular smooth muscle, cardiac nodal and muscle cells; causes arteriolar dilation and less cardiac depression

28
Q

When would you use Nicardipine?

A

Stable angina esp. vasospastic angina (Prinzmetal’s)

29
Q

What are the side effects of Nicardipine?

A

Avoid short-acting agents; excessive vasodilation > reflex tachycardia, nausea, lightheadedness, dizziness, headache, peripheral edema

30
Q

What are the beta blockers?

A

Carvedilol, Labetalol, Nebivolol, Atenolol, Metoprolol

31
Q

What is the MOA of Carvedilol?

A

Inhibition of B1 effect in heart; vasodilation; causes cardiac depression: reduced heart rate > prolonged diastole and coronary perfusion time; block tachycardia reflexed by nitrates and Ca antagonists; reduce heart contractility

32
Q

When would you use Carvedilol?

A

Stable, silent, and unstable angina (prophylaxis); NOT VARIANT

33
Q

What are the side effects of Carvedilol?

A

When combined with Ca channel blocker > additive cardiac depressant; avoid with intrinsic sympathetomimetic activity (pindolol)

34
Q

What is the MOA of Labetalol?

A

Inhibition of B1 effect in heart; vasodilation; causes cardiac depression: reduced heart rate > prolonged diastole and coronary perfusion time; block tachycardia reflexed by nitrates and Ca antagonists; reduce heart contractility

35
Q

When would you use Labetalol?

A

Stable, silent, and unstable angina (prophylaxis); NOT VARIANT

36
Q

What are the side effects of Labetalol?

A

When combined with Ca channel blocker > additive cardiac depressant; avoid with intrinsic sympathetomimetic activity (pindolol)

37
Q

What is the MOA of Nebivolol?

A

Inhibition of B1 effect in heart; vasodilation; causes cardiac depression: reduced heart rate > prolonged diastole and coronary perfusion time; block tachycardia reflexed by nitrates and Ca antagonists; reduce heart contractility

38
Q

What are the side effects of Nebivolol?

A

When combined with Ca channel blocker > additive cardiac depressant; avoid with intrinsic sympathetomimetic activity (pindolol)

39
Q

When would you use Nebivolol?

A

Stable, silent, and unstable angina (prophylaxis); NOT VARIANT

40
Q

What is the MOA of Atenolol?

A

Inhibition of B1 effect in heart; causes cardiac depression: reduced heart rate > prolonged diastole and coronary perfusion time; block tachycardia reflexed by nitrates and Ca antagonists; reduce heart contractility

41
Q

When would you use Atenolol?

A

Stable, silent, and unstable angina (prophylaxis); NOT VARIANT

42
Q

What are the side effects of Atenolol?

A

When combined with Ca channel blocker > additive cardiac depressant; avoid with intrinsic sympathetomimetic activity (pindolol)

43
Q

What is the MOA of Metoprolol?

A

Inhibition of B1 effect in heart; causes cardiac depression: reduced heart rate > prolonged diastole and coronary perfusion time; block tachycardia reflexed by nitrates and Ca antagonists; reduce heart contractility

44
Q

When would you use Metoprolol?

A

Stable, silent, and unstable angina (prophylaxis); NOT VARIANT

45
Q

What are the side effects of Metoprolol?

A

When combined with Ca channel blocker > additive cardiac depressant; avoid with intrinsic sympathetomimetic activity (pindolol)

46
Q

What are the metabolism modifiers and rate inhibitors?

A

Ranolazine, Trimetazidine, Ivabradine

47
Q

What is the MOA of Ranolazine?

A

Inhibits late phase of Na current; modifies fatty acid oxidation; causes reduction in Na/Ca intracellular overload > improved diastolic function

48
Q

When would you use Ranolazine?

A

Chronic angina alone or in combo with other therapies; when failed other therapies

49
Q

What are the side effects of Ranolazine?

A

Prolongs QT interval; avoid with other drugs that prolong QT interval

50
Q

What is the MOA of Trimetazidine?

A

Metabolic modulator; pFOX inhibitor; partially inhibits fatty acid oxidation > reduced oxygen requirement per unit ATP production

51
Q

When would you use Trimetazidine?

A

Stable angina

52
Q

What is the MOA of Ivabradine?

A

Inhibits funny Na channel in SA node; Reduces heart rate > decreased cardiac work