Antianginals Flashcards
What are the nitrates?
Nitroglycerin, Isosorbide Dinitrate, Amyl Nitrite
What is the MOA of Nitroglycerine?
Rapidly actin; sublingual; high first pass effect; spray; can be given as patch or ointment for prolonged action (prophylaxis)
When would you use Nitroglycerine?
Stable, variant, and unstable angina; used sublingually for acute and topical and SR for long-term
What are the side effects of Nitroglycerine?
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
What is the MOA of Isosorbide Dinitrate?
Rapidly acting; sublingual; can be given orally or topically for prolonged action (prophylaxis)
When would you use Isosorbide Dinitrate?
Stable, variant, and unstable Angina; acute attacks (sublingual prep)
What are the side effects of Isosorbide Dinitrate?
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
What is the MOA of Amyl Nitrite?
Convert to NO > Vasodilation (veins affected more than arteries); inhalation
When would you use Amyl Nitrite?
Stable, variant, and unstable Angina; acute attacks (sublingual prep)
What are the side effects of Amyl Nitrite?
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
What are the Ca channel blockers?
Verapamil, Diltiazem, Nifedipine, Amlodipine, Nicardipine
What is the MOA of Verapamil?
Block L-type Ca channels, preventing Ca influx > decreased arteriolar tone (decreased afterload), cardiac depression (decreases HR and contractility) > less O2 requirement
When would you use verapamil?
Stable and variant angina to relieve chest pain; fast atrial/nodal arrhythmias to slow HR/AV conduction
What are the side effects of verapamil?
High doses/toxicity may cause CHF; constipation, flushing, dizziness; AV blockade, sinus node depression
What is the MOA of Diltiazem?
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
When would you use Diltiazem?
Stable and variant angina; posses both cardiac and vasodilator activity
What are the side effects of Diltiazem?
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.)
What is the MOA of Nifedipine?
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
When would you use Nifedipine?
Stable angina esp. vasospastic angina (Prinzmetal’s)
What are the side effects of Nifedipine?
Avoid short-acting agents; excessive vasodilation > reflex tachycardia, nausea, lightheadedness, dizziness, headache, peripheral edema
What is the MOA of beta blockers?
Inhibit beta-1, decreasing HR and contractility, which decreases cardiac O2 demand
When would you use beta blockers?
Stable, unstable, and silent angina; NOT a vasodilator
What are the side effects of beta blockers?
Excess cardiac depression when used with Ca channel blocker
What is the MOA of Amlodipine?
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
When would you use Amlodipine?
Stable angina esp. vasospastic angina (Prinzmetal’s)
What are the side effects of Amlodipine?
Avoid short-acting agents; excessive vasodilation > reflex tachycardia, nausea, lightheadedness, dizziness, headache, peripheral edema
What is the MOA of Nicardipine?
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
When would you use Nicardipine?
Stable angina esp. vasospastic angina (Prinzmetal’s)
What are the side effects of Nicardipine?
Avoid short-acting agents; excessive vasodilation > reflex tachycardia, nausea, lightheadedness, dizziness, headache, peripheral edema
What are the beta blockers?
Carvedilol, Labetalol, Nebivolol, Atenolol, Metoprolol
What is the MOA of Carvedilol?
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
When would you use Carvedilol?
Stable, silent, and unstable angina (prophylaxis); NOT VARIANT
What are the side effects of Carvedilol?
When combined with Ca channel blocker > additive cardiac depressant; avoid with intrinsic sympathetomimetic activity (pindolol)
What is the MOA of Labetalol?
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
When would you use Labetalol?
Stable, silent, and unstable angina (prophylaxis); NOT VARIANT
What are the side effects of Labetalol?
When combined with Ca channel blocker > additive cardiac depressant; avoid with intrinsic sympathetomimetic activity (pindolol)
What is the MOA of Nebivolol?
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
What are the side effects of Nebivolol?
When combined with Ca channel blocker > additive cardiac depressant; avoid with intrinsic sympathetomimetic activity (pindolol)
When would you use Nebivolol?
Stable, silent, and unstable angina (prophylaxis); NOT VARIANT
What is the MOA of Atenolol?
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
When would you use Atenolol?
Stable, silent, and unstable angina (prophylaxis); NOT VARIANT
What are the side effects of Atenolol?
When combined with Ca channel blocker > additive cardiac depressant; avoid with intrinsic sympathetomimetic activity (pindolol)
What is the MOA of Metoprolol?
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
When would you use Metoprolol?
Stable, silent, and unstable angina (prophylaxis); NOT VARIANT
What are the side effects of Metoprolol?
When combined with Ca channel blocker > additive cardiac depressant; avoid with intrinsic sympathetomimetic activity (pindolol)
What are the metabolism modifiers and rate inhibitors?
Ranolazine, Trimetazidine, Ivabradine
What is the MOA of Ranolazine?
Inhibits late phase of Na current; modifies fatty acid oxidation; causes reduction in Na/Ca intracellular overload > improved diastolic function
When would you use Ranolazine?
Chronic angina alone or in combo with other therapies; when failed other therapies
What are the side effects of Ranolazine?
Prolongs QT interval; avoid with other drugs that prolong QT interval
What is the MOA of Trimetazidine?
Metabolic modulator; pFOX inhibitor; partially inhibits fatty acid oxidation > reduced oxygen requirement per unit ATP production
When would you use Trimetazidine?
Stable angina
What is the MOA of Ivabradine?
Inhibits funny Na channel in SA node; Reduces heart rate > decreased cardiac work
