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1、1,Chapter 28,抗心绞痛药,Drugs Used in the Treatment of Angina Pectoris,2,Instructional Objectives,列举抗心绞痛药物分类及代表药。简述硝酸甘油抗心绞痛作用及机理。分析硝酸酯类与R 阻断药合用治 疗心绞痛是否合理。,3,1 Introduction (概述),The primary symptom of ischemic heart disease is angina pectoris, which caused by transient (短暂)episodes (发作) of myocardial isch
2、emia. These episodes of ischemia are due to an imbalance in the myocardial oxygen supply-demand relationship.,4,This imbalance may be caused by an increase in myocardial oxygen demand or by a decrease in myocardial oxygen supply, or sometimes by both .,5,【 Classification of Angina Pectoris 】,Stable
3、angina pectoris ( 稳定型心绞痛 ) 冠脉粥样硬化，激动或劳累时发作Unstable angina pectoris (不稳定型心绞痛) 冠脉粥样硬化，血栓，可发展为心梗 或猝死，也可恢复为稳定型心绞痛。Variant angina pectoris (变异型心绞痛) 冠脉痉挛所致，夜间或休息时发作。,6,【发病机理】,An imbalance in the myocardial oxygen supply-requirement,7,Determinants of myocardial oxygen consumption 决定心肌耗氧量因素,Ventricular wall
4、 tension (室壁张力)HR (心率)Ventricular contractility (心室收缩力)Ejection time (射血时间),8,Normal,oxygen supply,oxygen requirement,Angina,供氧,耗氧,冠脉硬化痉挛栓塞,射血时间心室容积收缩力 HR ,9,Angina is caused by narrowing of the coronary arteries,10,Principles of treatment (治疗原则) ：,耗氧,室壁张力,心率,心肌收缩力,心脏负荷,冠脉血流量,侧枝循环,心舒张时间,供氧,To recove
5、r (恢复)the balance between oxygen supply and oxygen consumption.,11,Basic actions of antianginal drugs 抗心绞痛药物的基本作用,Reduce oxygen consumption . 耗氧 2. Increase oxygen supply. 供氧3. Improve myocardial metabolism. 改善心肌代谢4. Inhibit the formation of thrombus. 抑制血栓形成,12,【 Classification of antianginal drugs
6、】 抗心绞痛药物分类,1. Organic nitrates (硝酸酯类)2. R blockers3. Calcium channel blockers (钙拮抗剂)4. Others,13,2 Organic nitrates,Nitroglycerin (硝酸甘油),【Pharmacokinetics】 1. Usually given sublingually (舌下含服). first-pass elimination 2. 可透皮吸收,14,【Pharmacological actions】,dilation of veins 扩V,preload 前负荷,dilation of
7、arteries扩A,afterload 后负荷,Note:,HR、心肌收缩力耗氧,why, oxygen consumption（ 耗氧）,耗氧,15,2. Dilates coronary artery and increase the blood flow in ischemic areas. 扩张冠脉，缺血区血流,Nitroglycerin舒张侧支血管血流重新分布 从非 缺血 区经侧枝流向缺血区缺血区血供,16,图27-2 硝酸甘油对冠脉血流分布的影响,17,3. the blood flow in subendocardial area. 心内膜下区域血供,扩VLVEDP,扩心外膜大
8、血管,扩侧枝血管,4. Protects the ischemic myocardium. 保护缺血的心肌,NO,PGI2, CGRP (降钙素基因相关肽) ,nitroglycerin,18,【Mechanism of vasodilation】 (扩血管机理),硝酸酯类与受体结合 生成NO （）鸟苷酸环化酶 cGMP （) cGMP依赖性蛋白激酶 肌球蛋 白轻链去磷酸化 扩血管,19,【Clinical uses】,All types of angina pectoris 各型心绞痛 :舌下 2. Acute myocardial infarction (AMI) 急性心肌梗死 3. Co
9、ngestive heart failure （CHF） 充血性心衰,20,【Adverse reactions】,1. Vasodilation 扩血管 ： 面颊发红、搏动性头痛、眼压、 体位性低血压、颅内压2. Tolerance 耐受性 ： 间歇给药：间隔8小时以上 补充含巯基药：卡托普利等,硝酸异山梨醇酯 单硝酸异山梨醇酯,21, 3 R Blockers,Propranolol,【Antianginal effects】(抗心绞痛作用), myocardial oxygen consumption 减少心肌耗氧量,(-) -R,HR,Contractility (收缩力) ,BP,2
10、2,Note：,射血时间,心容积,耗氧,2. blood supply in ischemic areas 缺血区供血,(1) HR 舒张期 心内膜血流(2) 增加缺血区侧支循环(3) 促氧合血红蛋白中氧的解离组织氧供,心肌收缩力,23,【Clinical uses】,Can -R blockers be used for variant angina (变异型心绞痛)?,question,1. Stable angina pectoris (稳定型心绞痛) Especially for the patients with hypertension and arrhythmia.2. Card
11、iac infarction (心肌梗死) ：慎用,收缩冠脉,24,4 Calcium Channel Blockers 钙通道阻断药,Nifedipine (硝苯地平, 心痛定)Verapamil (维拉帕米，异搏定) Diltiazem (地尔硫卓),【Mechanism】,阻钙内流,25,1. oxygen consumption 氧耗 收缩力、血管扩张、BP、心负荷2. relieve coronary arterial spasm 解除冠脉痉挛 3. Protect ischemic myocardium 保护缺血心肌：防止Ca2+超负荷4. Inhibit platelet aggregation 抑制血小板聚集,【Antianginal effects】(抗心绞痛作用),26,【Clinical uses】,Variant angina 变异性心绞痛 first choice2. Stable or unstable angina 稳定型或不稳定型 3. Acute cardiac infarction (AMI) 急性心肌梗死,27,心肌收缩力,Propranolol,冠状动脉,心室容积,HR,Nitroglycerin,扩张,收缩,射血时间,BP,
