《Unit20中枢兴奋药》PPT课件.ppt

中枢兴奋药 central stimulants,鞠传霞,主要兴奋大脑皮层的药物，如咖啡因等；,根据其主要用部位可分为两类：,主要兴奋延髓呼吸中枢的药物，又称呼吸兴奋药，如尼可刹米等；,中枢兴奋药,多种原因所致CNS抑制状态（呼吸） 消耗体能，中枢过度兴奋甚至惊厥发作 辅助疗法,第一节 大脑皮层兴奋药,咖啡因(caffeine) 茶碱(theophylline) 柯柯碱,甲基黄嘌呤类(methylxanthines),History of Coffee,Date Event 850 - Coffee beans discovered - The fable says that an Ethiopian goat or sheepherder noticed that the goats were more alter after eating the wild berries. He then sampled this new delicacy. 1100 - First coffee trees and roasting of coffee beans. 1475 - Constantinople the worlds first coffee house. 1600s - Coffee enters Europe and moves quickly to the Americas 1700s - Coffee house open throughout Europe. 1723 - First coffee plants are introduced into the Americas. 1822 - First espresso machine is created in France. 1938 - First instant coffee invented by the Nestl company. 1971 - Starbucks opens its first location in Seattle, Washingtons Pike Place Market.,History of Tea,Date Event 3000 B.C. - Tea discovered in China or introduced form India 350 B.C. - First written description of Tea drinking in China. 450 A.D. - Turkish traders bargain for Tea and the Silk road is born. 800 - Tea introduced to Japan. 1450 - Japanese Tea ceremony created and popularized 1610 - Dutch bring Tea to Europe 1773 - Boston Tea party, rebellion against Englands tea tax 1776 - England sends first Opium to China to help pay for tea. 1835 - First experimental tea plantations in Assam, India. 1908 - Tea bags invented in New York.,Exposure,Most widely consumed neuroactive compound,Coffee Soda Products Tea Chocolate,Caffeine Content,1 Cup of coffee 65-175 mg 1 Cup of tea 50 mg Can of soda (12 oz) 40-50 mg Bar of chocolate (30 g) 1-35 mg,Caffeine 1,3,7 Trimethylxanthine,Theophylline 1,3 Dimethylxanthine,药理作用,咖啡因,中枢兴奋作用强,茶碱,兴奋心肌、松弛平滑肌和利尿作用强,精神振奋、减轻疲劳、思维活跃 （对大脑皮层有选择性兴奋作用） 大剂量: 呼吸加深加快、血压升高 （兴奋延脑呼吸中枢和血管运动中枢） 过量：CNS广泛兴奋导致惊厥,药理作用,1. 中枢兴奋作用,小剂量：兴奋迷走神经心率 大剂量：直接兴奋心肌心率 直接扩张血管：外周阻力改善冠脉循环 收缩脑血管：缓解偏头痛,药理作用,2. 心血管作用,舒张支气管平滑肌和胆道平滑肌 肾小管滤过率 对钠重吸收 刺激胃酸和胃蛋白酶分泌,药理作用,3. 其他作用,抑制磷酸二酯酶, 使cAMP降解减少, 细胞内cAMP浓度升高 竞争性拮抗腺苷受体(腺苷有镇静、抗惊厥及收缩支气管平滑肌等作用),作用机制,Normal Action of Adenosine,Action of Caffeine,1.对抗中枢抑制：严重传染病或中枢抑制药中毒等引起的昏睡、呼吸循环衰竭; 2.治疗头痛：与解热镇痛药伍用 3.治疗偏头痛：与麦角制剂配伍用,临床应用,咖啡因,中枢兴奋作用强,临床应用,茶碱,哮喘 慢性阻塞性肺疾病 急性左心衰肺水肿等,外周作用强,过量可致激动不安、失眠，心悸，心律失常，惊厥,不良反应,哌醋甲酯(methylphenidate)利它林(ritalin),较温和的中枢兴奋作用 机制：增加脑内单胺类递质浓度,巴比妥类及其它中枢抑制药中毒 轻度抑郁症 小儿遗尿症(兴奋大脑皮层而易被尿意唤醒) 小儿多动症(增加NA、DA等，补充脑干网状结构上行激活系统递质),哌醋甲酯(methylphenidate)利它林(ritalin),应用,第二节 呼吸中枢兴奋药,尼可刹米（可拉名） 二甲弗林（回苏灵） 洛贝林（山梗菜碱）,直接兴奋延髓呼吸中枢 刺激颈动脉体化学感受器反射性地兴奋呼吸中枢 选择性高, 安全性大 临床上用于各种原因引起的呼吸性中枢抑制,尼可刹米(nikethamide)可拉明(coramin),直接兴奋呼吸中枢 安全范围小, 过量