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1、Antianginal Drugs,抗心绞痛药,Objectives,Know the major classes of drugs used to treat angina and their mechanisms of action抗心绞痛药分类、代表药及其作用机制,What is Angina pectoris?,冠脉供氧不足引起的暂时性急剧心肌缺血所致的临床综合征，表现为胸骨后疼痛，并可放射到左臂。是冠状动脉粥样硬化性心脏病（冠心病的常见症状。,It is the principle symptom of ischemic heart diseaseThe condition is c
2、haracterized by sudden,severe substernal pain or pressure,Oxygen supply,Oxygen demand,coronary atherosclerosis 冠状动脉硬化，95%coronary artery spasm 冠状动脉痉挛coronary thrombosis 冠状动脉血栓形成,myocardial contractility心肌收缩力HR心率Sports,mood modification运动、情绪改变,Angina pectoris patterns,Factors affecting myocardial oxy
3、gen demand and oxygen supply,Chemical structures of two nitrates,Nitroglycerine硝酸甘油,Isosorbide dinitrate硝酸异山梨酯,Pharmacological mechanism,Organic nitrates NO guanylyl cyclase(鸟苷酸环化酶)GTP cGMPcGMP dependent protein kinase intracellular Ca2+vascular smooth muscle relaxation,Oxygen demand,venous relaxati
4、on 静脉舒张,artery relaxation（large dose)动脉舒张(大剂量),venous return回心血量,preload前负荷,ventricular end-diastolic volume心室舒张末期容积,ventricular wall tension心室壁张力,VET心室射血时间,afterload后负荷,Oxygen demand耗氧量,TPR总外周阻力,Oxygen supply,ventricular wall tension心室壁张力,coronary blood flow(especially the ischemic myocardium)冠脉供血(
5、特别是缺血区心肌),coronary artery relaxation冠脉舒张,Oxygen supply,ventricular wall tension心室壁张力,subendocardial vascular resistance 心内膜下血管阻力,ventricular pressure 心室内压,blood flow from the epicardial to ischemic zone of endocardial血液从心外膜流向心内膜缺血区,coronary steal 冠脉窃血,Pharmacokinetic Properties of Nitrates,Routes of
6、 Administration,GTN can be administered by sublingually,inhalation,transdermal or buccal.Its not suitable for maintenance therapy.IV nitrogylcerin can be used to treat severe recurrent unstable angina.GTN可吸入、颊部、透皮或舌下含服；作用时间短，不适合维持治疗;静注用于不稳定型的严重复发。,bid,Qd,5-ISMN is not subject to first-pass metabolis
7、m and is 100%available after oral administration.slowly onset,long duration.口服生物利用度高，起效慢，维持久,Clinical Uses,Adverse Effects of Nitrovasodilators,NGT maybe cause methemoglobinemia when admistreated it with long-term and large dose.长期大剂量应用NGT可致高铁血红蛋白血症,Tolerance and Dependence with Nitrovasodilators,Ef
8、fects of nitrates alone and with-blockers in angina pectoris,Ca2+Channel Blockers,DHPs,Non-DHPs,Relative Cardiovascular Effects of Calcium Channel Blockers,Verapamil+Diltiazem+Nifedipine+0Nicardipine+0+0,Compound,Coronary vasodilation,Suppression of cardiac contractility,Suppression of SA node,Suppr
9、ession of AV node,Clinical Uses of CCBs,Treatment strategy,Interaction of Drugs,Nitrate esters,RBs,Nifedipine,VerapamilDiltiazem,Partial Fatty Acid Oxidation(pFox)Inhibitors部分脂肪酸氧化酶抑制剂,ATP-sensitive potassium channel opener ATP敏感钾离子通道开放剂,Chinese herbal medicine,selective PDE5 inhibitoract on cGMP,伐地那非Vardenafil,他达拉非Tadalafil,AMI治疗,
