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Winter Exam #1 - Antianginal Agents
n/a
10
Pharmacology
Graduate
12/09/2009

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Term
classic angina pectoris
Definition
caused by atherosclerotic obstruction in large coronary arteries; aka effort or stable; usually occurs when exercising
Term
variant angina or Prinzmetal's angina
Definition
reversible vasospastic reduction of flow in large coronary arteries
Term
unstable or crescendo angina
Definition
combines atherosclerotic plaque & vasospasm; results from sudden marked platelet aggregation with clot formation at site of a ruptured plaque; occurs at rest as well as during exertion; immediate precursor of myocardial infarction
Term
Primary causes of anginal pain
Definition
coronary O2 delivery is inadequate to meet myocardial oxygen demand
Term
nitrates - nitroglycerin (Minitran, Nitrostat), isosorbide dinitrate (Isordil)
Definition
duration of action from minutes to hours; sublingual tabs or transdermal patches or oral tabs; Uses: treatment of acute anginal attacks after onset, prevention of attacks before onset; rapidly denitrated in liver; first-pass effect is high;
Term
nitrates - nitroglycerin (Minitran, Nitrostat), isosorbide dinitrate (Isordil)
Definition
MoA: converts to NO --> increases cGMP --> smooth muscle cell relaxation (more venous than arterial) --> peripheral vascular dilation --> reduced preload & reduced afterload; rapidly reduces myocardial cell tension & O2 demand --> reduction in cardiac O2 demand; Clinical Use: treats all 3 types of angina; ADRs: orthostatic postural hypotension, headache, reflex tachycardia & contractility, Na & water retention, tolerance, rebound angina; D-D Interaction: phosphodiesterase-5 inhibitors (Viagra, Cialis, Levitra) --> fatal hypotensive interaction
Term
CCBs - dihydropyridines - nifedipine (Procardia XL), amlodipine (Norvasc)
Definition
block L-type Ca channels in arterial vascular smooth muscle; prevents all types of angina, treats acute anginal attacks after onset; reduction in afterload & reduce in cardiac oxygen demand; also can reverse vasospasm in coronary arteries; ADRs: reflexly increase heart rate & contractility
Term
CCBs - verapamil (Isoptin SR, Calan), diltiazem (Cardizem)
Definition
blocks L-type Ca channels in cardiac muscle; reduce cardiac rate & contractility --> reduce cardiac oxygen demand; used for preventative treatment of all forms of angina; ADRs: CHF, AV blockade, sinus rate depression
Term
beta-blockers - metoprolol (Lopressor, Toprol-XL), atenolol (Tenormin), nadolol (Corgard), propanolol (Inderal-LA), timolol
Definition
competitive antagonists of beta-adrenergic receptors; especially beta receptors in SA node & ventricules of heart: decreases HR, cardiac contractile force, arterial BP, direct inhibitory effect on HR & contractility --> reduces cardiac O2 demand; Uses: preventative tx of angina, effective in preventing exercise-induced angina; useful in treating "silent" ischemia; used in combo with nitrates; ADRs: sinus bradycardia, AV blockade, rebound angina or HTN, asthmatic attacks, masking of tachycardia during hypoglycemic events, sedation, fatigue, sleep alterations
Term
ranolazine (Ranexa)
Definition
fatty acid oxidation inhibitor; MoA: 1) shift source of fuel used by myocardium from FAs to glucose which demands less O2 --> increased efficiency of O2 utilization; 2) selective inhibition of increased "late" inward-directed Na current caused by myocardial ischemia --> reduce ischemia-induced Ca overload & O2 demand; Uses: tx chronic stable angina with other products; ADRs: dizziness, HA, nausea, constipation, prolong cardiac QT interval
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