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34 Cards in this Set
- Front
- Back
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pathogenetic mechanisms of angina pectoris?
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atherosclerosis
spasm |
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major determinants of myocardial O2 demand and supply?
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demand: wall stress (pressure, radius, thickness), contractility, heart rate;
supply: coronary blood flow |
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take home messages from table of nitrate and nitrite drugs?
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long versus short acting division
can be administered by variety of routes |
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organic nitrates?
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nitroglycerin
isosorbide dinitrate (ISDN) isosorbide-5-mononitrate (ISMN) |
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organic nitrates actions?
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vascular smooth muscle relaxation (veins > arteries) - also relax other smooth muscle;
modest antiplatelet effect |
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organic nitrates mechanism?
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release of NO which stimulates cGMP production leading to relaxation
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organic nitrates effect on O2 demand?
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decreased systemic BP leading to decreased preload;
sympathetic reflex increase in HR and contractility |
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organic nitrates effect on O2 supply?
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some coronary artery dilation;
increased flow to ischemic areas via collateral vessels; decreased LVEDP may increase subendocardial perfusion; relieves coronary spasm |
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clinical uses of organic nitrates?
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relief of acute attack of angina;
prophylaxis of attacks; vasospastic angina |
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preparations of organic nitrates?
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sublingual
oral topical |
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use of sublingual preparations and duration of action?
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relieving acute attacks;
prevent attack if taken pre-exercise; rapid onset (1-3 min) with 20-30 min duration |
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which organic nitrates undergo significant first pass metabolism?
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nitroglycerin
ISDN |
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which organic nitrate has nearly 100% bioavailability?
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ISMN
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use of oral preparation of organic nitrates and duration of action?
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long term prevention;
peak effect about 60-90 min |
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topical preparations of organic nitrates onset and duration of actions?
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onset of effect about 30-60 min;
peak effect 1-2 hours |
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what is problematic with topical preparations of organic nitrates and how has it been addressed?
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development of tolerance due to continuous exposure;
interrupt therapy for 8-12 hours and efficacy returns |
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adverse effects of organic nitrates?
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headaches
orthostatic hypotension contraindicated with sildenafil, tadalafil, vardenafil |
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sildenafil?
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aka viagra;
inhibits phosphodiesterase 5 to increase cGMP and cause vasodilation |
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contraindications for organic nitrates?
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sildenafil
tadalafil vardenafil |
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β blocker effects on O2 demand and delivery?
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decreased HR, BP, contractility decrease demand;
increased LVEDV increase demand; increased perfusion time; unopposed α constriction |
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clinical use and effects in chronic stable angina of β blockers?
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effective in prevention of attacks in patients with exertional angina
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adverse effects of β blockers?
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β blocker withdrawal
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Ca channel blocker mechanism?
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interact with L-type Ca channels to decrease cellular uptake of Ca
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clinical uses of Ca channel blockers?
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hypertension
angina certain cardiac arrhythmias |
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which class of CCBs have higher vascular selectivity and what are the predominant effects?
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dihydropyridines: mainly arterial vasodilation
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miscellaneous CCBs?
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verapamil
diltiazem |
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cardiac effects of CCBs?
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decrease sinus node pacemaker rate;
decrease AV conduction; decreased contractility |
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which CCBs have greatest cardiac effects?
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verapamil
diltiazem |
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all CCBs have this cardiac effect?
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decreased contracility (although blunted by SNS activation with dihydropyridines)
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clinical uses of CCBs?
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effective in vasospastic and chronic effort-associated angina
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adverse effects of CCBs?
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excessive vasodilation (dizziness, hypotension, heaadache, flushing);
constipation, peripheral edema; aggrevation of ischemia with dihydropyridines; concerns with safety of immediate release nifedipine |
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ranolazine?
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newer drug approved for chronic angina
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ranolazine pharmacokinetics?
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oral
extensive metabolism P-glycoprotein substrate |
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ranolazine adverse effects?
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dizziness
headache constipation nausea increased QT interval |
