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 CoffeeDate Event850 - 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 Americas1700s - 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 TeaDate Event3000 B.C. - Tea discovered in China or introduced form India350 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 popularized1610 - Dutch bring Tea to Europe1773 - Boston Tea party, rebellion against Englands tea tax1776 - 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.ExposureMost widely consumed neuroactive compoundCoffee Soda Products Tea ChocolateCaffeine Content1 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 mgCaffeine 1,3,7 TrimethylxanthineNNNNCH3CH3CH3OO137Theophylline 1,3 DimethylxanthineNNNNHCH3CH3OO137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v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Positive Response Calming effect3Signal ProteinAdenosine binds to receptor2Normal Action of AdenosineAdenosine ReceptorAdenosineCell MembraneOutside CellInside Cell1Caffeine inactivates receptor2Action of CaffeineCaffeine1 Adenosine ReceptorNo Response Resulting in Stimulation3Adenosine can not bindCaffeine1.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, 过量易惊厥 各种原因引起的中枢性呼吸抑制二甲氟林(dimefline，回苏灵) 选择性刺激颈动脉体和主动脉弓 的化学感受器, 反射性地兴奋延髓 呼吸中枢 安全范围大, 不易引起惊厥 用于治疗新生儿窒息、小儿感染 性疾病所致呼吸衰竭及CO中毒山梗菜碱(lobeline，洛贝林)