吗啡的药理作用and作用机制.ppt
吗,啡,?,?,为,什,么,?,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 CO2 vasodilation,2. Intracranial pressure(颅内压) respiratory depression CO2 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CO2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,