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1、Antianginal drugs n nAngina pectoris is the severe chest pain that occurs when coronary blood flow is inadequate to supply the oxygen required by the heart.n nThe primary cause of angina pectoris is an imbalance between the oxygen requirement of the heart and the oxygen supplied to it.Backgrounds of
2、 angina pectorisnClassification:stable;unstable;variant nMechanism:nMethods for treatment:To improve perfusion:To reduce metabolic demandnDrugs organic nitrates;calcium antagonists-Receptor blockersOrganic nitratesnPharmacological effects and mechanism:vdilate peripheral vein preload vdilate periphe
3、ral artery afterloadvDilate coronary artery perfusion of ischemic myocardium Oxygen consumptionMechanism of action in VSMnNO(EDRF)activate GC increase c-GMP activate cGMP-dependent kinase decrease Ca induce de-phosphorylation of the myosin light chain relaxation nPharmacokinetics:very low bioavailab
4、ility per os Subligual Rapid onset(25min)nAcute adverse effects:postural hypotensiom,throbbing headachenTolerance:because of depletion of free SH groupsnClinic use:to treat and prevent all of the angina-Receptor blockersnPharmacological effects:Myocardial constrictionHeart rateClinic use:stable and
5、unstable anginaPropranolol not for variant angina because of coronary artery contraction due to its-receptor blocked and -receptor relatively activated.Propranolol+nitroglycerin Oxygen consumptionCalcium channel blockersnPharmacological effects:Cardiac contractility,heart rate Peripheral vessels dil
6、ation,afterloaddilate coronary artery,release its spasmCa2+overload apoptosis,necrosisnClinic use:variant anginavNifedipine not for unstable angina,+-Receptor blockersMyocardial oxygen consumptionOther drugs for anginanAnti-platelet drugs:aspirin,persantinnChinese medicine:salvia miltiorrhiza,panax notogensengnATP sensitive potassium channel openers