啡药理作用and作用机制研究.ppt

单击此处编辑母版标题样式,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,*,吗啡,的药理作用,And,作用机制,全科班第二小组,morphine,汇报人：曹群群,Pharmacokinetics,First-pass elimination is extensive bioavailability is low.,Passes through BBB and placenta,（,胎盘）,barrier.,Excretes,：,kidney,，,secretes in milk,药理作用,中枢神经系统,平滑肌,心血管系统,免疫系统,Pharmacological Effects,一、,CNS,1,、,Analgesia,镇痛,2,、,Sedation,镇静,3,、,Cough suppression,镇咳,4,、,Respiratory depression,抑制呼吸,消除焦虑、紧张、恐惧等,欣快感,直接抑制咳嗽中枢，使咳嗽反射减轻或消失,Respiratory depression,therapy dosage:,respiratory rate,and,tid,volume,.,toxic dosage:,1,）,respiratory failure.,2,）,Sensitivity of respiratory center,to CO2.,3,）,(-)respiratory center,Analgesia,镇痛,Stronger:,510mg,Extensive:,various pain,chronic,pain,(,钝痛,),acute,pain,（锐痛）,Longer,：,4,6 hours,镇痛时,意识清醒,其他感觉不受影响,Morphine,（）,Opioid,receptors,模拟内源性阿片肽作用,增强内源性镇痛系统的功能,analgesia,镇 痛,Mechanism of action,内源性镇痛系统,脑啡肽神经元,脑啡肽,阿片受体,结合,20%,Mechanism of action,morphine,阿片,-R,脑啡肽,Others,兴奋支配瞳孔的副交感神经,瞳孔缩小。,急性中毒时：针尖样瞳孔,Miosis,(,缩瞳,),：,兴奋,延髓,CTZ,恶心、,呕吐,抑制丘脑下部释放：,促性腺释放激素,促肾上腺皮质激素释放因子,二,.Smooth muscle,(1),Constipation,(,便秘,):,（,-,）,CNS,便意迟钝,(+),gastroenteric,（胃肠道）,smooth muscle,propulsive peristaltic waves,(,推进性,蠕动,),Pharmacological Effects,(2),biliary,pressure:,constricts,biliary,smooth muscle,biliary,colic,(,胆绞痛,),(3),Urinary retention,(,尿潴留,),(4)bronchial SM(+),-induced asthma,(,诱发哮喘,),三,.,Cardiovascular system,(1),Hypotension,(,低血压,),:,a.Cause peripheral,vasodilation,.,(,外周血管舒张,),b.,Increase histamine,（,组胺）,release,.,c.,Respiratory depression,CO,2,vasodilation,2.,Intracranial pressure,（,颅内压,）,respiratory depression,CO,2,Cerebral,vasodilation,.,3.Protections,of,myocardiac,ischemia,simulate ischemic preconditioning,(,模拟缺血性预适应,),(,),lymphopoiesis,(,淋巴细胞增殖,),secretion of cellular factors,（细胞因子的分泌）,(,),immunoreaction,induced,by HIV.,四,Inhibit,immunoreaction,Clinical Uses,1,.Analgesia,镇痛：其它镇痛药无效的急性锐痛,心梗剧痛：,前提：,BP,正常,机理：镇痛、镇静、扩血管,biliary,colic(,胆绞痛,):,with atropine,一个前提三个机理,2.Cardiogenic asthma,强心甙类,加强心肌收缩力,速尿,减轻心脏负荷,氨茶碱,强心，松弛支气管平滑肌,吗啡,治疗,心源性哮喘,吗啡,扩张外周血管,外阻 心负荷,镇静,消除焦虑恐惧心负荷,呼吸中枢对,CO,2,的敏感性缓解浅快呼吸,Diarrhea from almost any cause,can be controlled.,3.Diarrhea,（止泻）,全体成员：,赵 丹,柏小三、曹群群、陈利、鞠建龙、刘迎辉、卢国庆、祁义民、任少男、宋兰兰、王干彪、张成玉、张亚琴、赵一奇、邹创创,