Unit 4-Angina/Coronary Artery Disease Flashcards
Aspirin
Drug class
NSAID - Antiplatelet agent
Aspirin
Mechanism
Irreversible inhibition of COX (thus no TxA2 synthesis), so blocks platelet aggregation
Aspirin
Uses
Reduction in adverse events (MI, CVA, death); for those w/stable angina, unstable angina, acute MI, prophylaxis
Aspirin
Side effects
Low-doses; if you’re allergic, you’ll get asthma
Ticlopidine
Drug class
Thienopyridine antiplatelet agent
Ticlopidine
Mechanism
Inhibits platelet aggregation by ADP;
reduces blood viscosity by decreasing plasma fibrinogen and increasing RBC deformability
Ticlopidine
Uses
Aspirin alternative
Ticlopidine
Side effects
Neutropenia and, rarely, TTP
Not really used anymore
Clopidogrel
Drug class
Thienopyridine antiplatelet agent
Clopidogrel
Mechanism
Selectively and irreversibly inhibits ADP binding to P2Y12 (blocks ADP-dependent activation of glycoprotein IIb/IIIa complex)
Clopidogrel
Uses
Great antithrombotic; standard of care w/ stent
Clopidogrel
Side effects
Bleeding
No surgical or dental procedures if patient taking this
Prasugrel
Drug class
Thienopyridine antiplatelet agent
Prasugrel
Mechanism
Irreversibly binds P2Y12 receptor (G protein-coupled chemoreceptor for ADP)
Prasugrel
Uses
Reduce thrombotic events in those w/percutaneous coronary intervention (e.g., stent)
Prasugrel
Side effects
Massive bleeding risk
Drug is limited to patients under 75 in age, greater than 60 Kg in weight, and no history of stroke or TIA.
Ticagrelor
Drug class
Adenosine-like antiplatelet agent
Ticagrelor
Mechanism
Reversibly blocks ADP receptors
Does not require hepatic activation
Ticagrelor
Uses
Great antithrombic
Ticagrelor
Side effects
Bleeding
Requires bid dosing
Dipyridamole
Drug class
Pyrimido-pyrimidine antiplatelet agent
Dipyridamole
Mechanism
Increases platelet intracellular cAMP (inhibits phosphodiesterase 5, activates adenylate cyclase, inhibits uptake of adenosine from vascular endothelium and RBCs)
Dipyridamole
Uses
Decrease peripheral vascular disease (as an adjunct); stress test of heart
Dipyridamole
Side effects
Vasodilation of coronary arteries can enhance exercise-induced ischemia (because it elevates extracellular adenosine levels)
Cilostazol
Drug class
Quinoline antiplatelet agent
Cilostazol
Mechanism
Inhibits cellular phosphodiesterase & so raises intracellular cAMP
–> inhibits platelet aggregation
Cilostazol
Uses
Treatment for claudication with peripheral vascular disease
Cilostazol
Side effects
Vasodilation
Contraindicated in heart failure
Captopril (Capoten), Enalapril (Vasotec), Lisinopril (Zestril), Ramipril (Altace), Quinapril (Accupril), Fosinopril (Monopril)
Drug class
ACE inhibitor
Captopril (Capoten), Enalapril (Vasotec), Lisinopril (Zestril), Ramipril (Altace), Quinapril (Accupril), Fosinopril (Monopril)
Mechanism
Blocks endothelial ACE from converting angiotensin I to angiotensin II (potent vasoconstrictor); as a side effect, also prevents breakdown of bradykinin (potent vasodilator)
Captopril (Capoten), Enalapril (Vasotec), Lisinopril (Zestril), Ramipril (Altace), Quinapril (Accupril), Fosinopril (Monopril)
Uses
Reduces incidence of future CAD events in patients at risk for or had vascular disease
Captopril (Capoten), Enalapril (Vasotec), Lisinopril (Zestril), Ramipril (Altace), Quinapril (Accupril), Fosinopril (Monopril)
Side effects
Dry cough, angioedema, hyperkalemia, hypotension
Short-acting; contraindicated in pregnancy, renal artery stenosis, hyperkalemia, and prior angioedema (no ARB allowed, either); caution in renal failure
Metoprolol (Lopressor), Bisoprolol (Zebeta), Atenolol (Tenormin)
Drug class
β1-selective blocker
Metoprolol (Lopressor), Bisoprolol (Zebeta), Atenolol (Tenormin)
Mechanism
Decrease contractility and HR (reduced myocardial O2 demand)
Metoprolol (Lopressor), Bisoprolol (Zebeta), Atenolol (Tenormin)
Uses
Prevent MIs, prevent sudden cardiac death, increase survival post-MI (if patients suddenly stop, really bad!)
Metoprolol (Lopressor), Bisoprolol (Zebeta), Atenolol (Tenormin)
Side effects
Fatigue, worsening claudication, impotence (so men don’t take)
Decreased exercise tolerance, lethargy, insomnia
Contraindicated in severe bradycardia, high degree AV block, sick sinus syndrome, unstable LV failure; relative contraindication is asthma, severe depression, peripheral vascular disease
Isosorbide dinitrate (Isordil), Isosorbide mononitrate (Imdur)
Drug class
Vasodilator
Isosorbide dinitrate (Isordil), Isosorbide mononitrate (Imdur)
Mechanism
Endothelium independent vasodilator; endothelial effects (inhibits platelet aggregation, inhibits leukocyte-endothelial interactions (anti-inflammatory))
Isosorbide dinitrate (Isordil), Isosorbide mononitrate (Imdur)
Uses
For acute episodes; long-acting formulations are for those already on other drugs and still can’t control angina
Isosorbide dinitrate (Isordil), Isosorbide mononitrate (Imdur)
Side effects
Tolerance w/chronic use (need nitrate free periods of 8-12 hours), headaches, hypotension, activation of Bezold-Jarisch reflex (causes bradycardia)
Contraindicated in hypertrophic cardiomyopathy, severe aortic stenosis, significant hypotension, use of phosphodiesterase inhibitors
Nifedipine
Drug class
Calcium channel blocker - 1st generation dihydropyridine
Nifedipine
Mechanism
Interact with L-type voltage gated plasma membrane Ca channel –> decreased calcium entry into vascular smooth muscle cell, preventing contraction; causes dilation of epicardial coronary arteries, arteriolar resistance arteries
Nifedipine
Uses
Angina (3rd choice drug); Raynaud’s
Nifedipine
Side effects
Leg edema, heart failure, AV nodal blockade, reflex tachycardia
Constipation (most common), headache, flushing
Contraindicated in overt decompensated heart failure, bradycardia, sinus node dysfunction, high-degree AV block
Amlodipine (Norvasc), Felodipine (Plendil), Isradipine (Dynacirc)
Drug class
Calcium channel blocker - 2nd generation dihydropyridine
Amlodipine (Norvasc), Felodipine (Plendil), Isradipine (Dynacirc)
Mechanism
Interact with L-type voltage gated plasma membrane Ca channel –> decreased calcium entry into vascular smooth muscle cell, preventing contraction; causes dilation of epicardial coronary arteries, arteriolar resistance arteries; less heart-specific activity
Amlodipine (Norvasc), Felodipine (Plendil), Isradipine (Dynacirc)
Uses
1st line agent for coronary vasospasm; angina (3rd choice drug); Raynaud’s
Amlodipine (Norvasc), Felodipine (Plendil), Isradipine (Dynacirc)
Side effects
Leg edema (less than 1st generation), heart failure, AV nodal blockade, reflex tachycardia
Constipation (most common), headache, flushing
Contraindicated in overt decompensated heart failure, bradycardia, sinus node dysfunction, high-degree AV block
Verapamil (Calan); Diltiazem (Cardizem)
Drug class
Calcium channel blockers - non-dihydropyridine
Verapamil (Calan); Diltiazem (Cardizem)
Mechanism
Interact with L-type voltage gated plasma membrane Ca channel –> decreased calcium entry into vascular smooth muscle cell, preventing contraction; causes decreased contractility, firing rate of aberrant pacemaker sites, and conduction velocity; prolongs repolarization in SA node and AV node (–> decreases HR); less vasodilation
Verapamil (Calan); Diltiazem (Cardizem)
Uses
Hypertension, anti-anginal (chronotropic effects –> decreased myocardial oxygen demand), SVT (class IV anti-arrhythymic)
Verapamil (Calan); Diltiazem (Cardizem)
Side effects
Leg edema, bradycardia, AV nodal blockade, hypotension, worsening heart failure
Constipation (most common), headache, flushing
Contraindicated in overt decompensated heart failure, bradycardia, sinus node dysfunction, high-degree AV block