各论教材抗心绞痛药.pptVIP

抗心绞痛药Antianginal Drugs;What’s Angina pectoris Cause and the classification of angina pectoris : Atheromatous obstruction of the large coronary vessels (atherosclerotic angina, classic angina); 劳累性心绞痛：稳定型，初发型，恶化型 Transient spasm of localized portions of the large coronary vessels (angiospastic or variant angina); 自发性心绞痛：卧位型，变异型，急性冠脉功能不全，梗死后心绞痛 Both causes 混合性心绞痛 Unstable angina pectoris: initial onset type(初发型); accelerated type(恶化型); spontaneous type（自发型） associated with atherosclerosis plaque and thrombus formation may lead to myocardial infarction;Coronary vessels: blood supply for the heart;;Coronary atherosclerosis: cause of cardiac ischemia;preload;Myocardial oxygen demand is diminished by: Reducing contractility Reducing heart rate Reducing the preload Reducing the afterload Myocardial oxygen supply is increased by: Dilating conduct coronary arteries ( ? coronary blood flow) Promoting regional distribution ( ? in ischemic regions) Treatments: Non-drug treatment:经皮冠状动脉成形术(percutaneous transluminal coronary angioplasty, PTCA), 冠脉搭桥术 ( coronary artery bypass graft surgery, CABG ) Drug treatment;Antianginal Drugs;Nitrates Nitrites (硝酸酯类 和亚硝酸酯类) ;- Pharmacokinetics Low oral bioavailability (eg, 硝酸甘油nitroglycerin and 硝酸异山梨酯isosorbide dinitrate, typically 10–20%). Sublingual(舌下) is normally used. Transdermal (透皮)and buccal (经口颊)absorption from slow release preparations. Amyl(戊基) nitrite and related nitrites can be used with inhalation route. Duration of effect is very brief (unchanged nitrate t1/2=2-8 minutes, partially denitrated metabolites longer t1/2= 3 hrs). So micro-pump is very common in hospital usage.; - Pharmacological actions Dilating vessels and reducing heart loads wall tension ?; reflex tachycardia Redistribution of coronary circulation dilating conduct artery: collateral circulation (侧支循环)? reducing wall tensi