医学院药理学研究所.pptVIP

UNIT Ⅴ Drugs Affecting the Cardiovascular System 医学院药理学研究所 刘慧青 Drugs Affecting the Cardiovascular System Antiarrhythmic Drugs Drugs used in Congestive Heart Failure Antihypertensive Agents Drugs used in Angina Pectoris Antiatherosclerotic Drugs  CHAPTER 24 Drugs Affecting the ion channels of Cardiovascular System Ion Channels of Cardiovascular System Sodium channels Calcium channels Potassium channels characteristic ： Permeation, selectivity, gating CALCIUM CHANNEL  BLOCKERS  (Calcium Antagonists) Section 1 Ca2+ and Calcium Channels  Ⅰ. Ca2+ and the Regulation of   Ca2+ in the cells Ⅱ．The classification of  calcium channel ROC: receptor operated calcium channel VDC: voltage dependent calcium channel : L、T、N、P、Q、R Ⅲ. Molecular Structure of  Calcium Channel  Section 2  Calcium Channel Blockers Ⅰ. Classification  1. WHO（1987） Selective Calcium Channel Blockers: Phenylalkylamines (苯烷胺类) ： verapamil（维拉帕米） Dihydropyridines（二氢吡啶类）： nifedipine（硝苯地平） Benzothiazepines（苯硫卓类）： diltiazem（地尔硫卓）  Non Selective calcium Channel  Blockers: Flunarizines (氟桂利嗪类） Prenylamines（普尼拉明类） Others 2. IUPHAR（1992） 3. According to the applying time of drugs: First-generation: verapamil、 nifedipine、 diltiazem Second- generation : felodipine、 nimoldipine 、nicardipine et al Third-generation : pranidipine、 amlodipine et al Ⅱ.The fashion of action 药物与离子通道的相互作用及亲和性与通道所处状态和药物的理化性质相关 维拉帕米、地尔硫卓与激活态或失活态通道结合，↓通道开放的频率 硝苯地平与失活态通道结合， 延长通道恢复所需时间。 Section 3  Pharmacology and Clinical Uses Pharmacological actions 1) Action on myocardiac a. Negative inotropic effect b. Negative frequency action and