药理antianginaldrugs重点分析.ppt

ANTIANGINAL DRUGS What’s the Angina Pectoris ? 分型 classifications ①劳累性心绞痛：可分为稳定型、初发型及恶化型心绞痛； ②自发性心绞痛 包括：卧位型、变异型、中间综合征和梗死后心绞痛； ③混合性心绞痛 The pathophysiology underlying angina pectoris major determinants of myocardial oxygen consumption: myocardial basic metabolism heart rate contractility wall tension ejection time blood pressure (peripheral resistance) The mechanism of antianginal drugs O2 increase supply and/or lower demand Myocardial O2 supply: Coronary blood flow, regional flow distribution Myocarial O2 –demand: amount of energy required to support the work of the heart Cardiac work influenced by: heart rate, heart contractility, myocardial wall tension Section 2 Organic nitrates 1.Drugs: Nitroglycerin (硝酸甘油) , isosorbide dinitrate(硝酸异山梨酯) isosorbide mononitrate(单硝酸异山梨酯) 硝酸甘油 nitroglycerin 发展简史 化学结构 体内过程 2.Pharmacological mechanism Organic nitrates NO  guanylyl cyclase cGMP cGMP dependent protein kinase intracellular Ca2+ vascular smooth muscle relaxation 硝酸甘油 nitroglycerin 3. Pharmacological action (1) decrease myocardiac oxygen consumption dilate venous decrease blood returning to heart decrease ventricular end-diastolic volume and pressure (large dose) dilate arterial decrease peripheral resistance decrease afterload (2) increase blood supply to ischemia area 3. Pharmacological action (3) redistribution of coronary blood flow (4) Inhibition of platelet aggregation, increase the release of PGI2 and CGRP 4.Clinical uses (1) all types of angina (2) acute myocardia infarction (3) CHF isosorbide dinitrate used in prophylaxis attack and CHF after myocardia infarction 5. adverse effects and tolerance tachycardia, flushing, throbbing headache, orthostatic hypotension, methemoglobinemia 硝酸甘油 nitroglycerin 不良反应 section 3. β-adrenoceptor blocking drugs 1.The mechanism of antiangina decrease myocardial oxygen consumption block β-adrenoceptor