资源描述：
《药理学课件南开大学第十五章影响自体活性物质的药物》由会员上传分享，免费在线阅读，更多相关内容在教育资源-天天文库。
1、组胺和抗组胺药HistamineandAntihistamineAgents南开大学医学院张京玲王侃代红胜HistamineandAntihistamineAgents目的了解组胺与变态反应的关系。掌握抗组胺药H1、H2受体拮抗剂的作用与应用。HistamineandAntihistamineAgents内容组胺：来源，内源性组胺与过敏反应的关系，作用，为诊断用药。H1、H2受体的划分。HistamineandAntihistamineAgents内容抗组胺药：H1受体阻断剂：对H1受体的阻断作用。中枢作用
2、及其它。临床用途，主要不良反应。苯海拉明、异丙嗪（非那根）、氯苯那敏（扑尔敏）、布克利嗪（安其敏）。H2受体阻断剂：对H2受体的阻断作用。西米替丁（甲氰咪呱）的抑酸作用，对消化性溃疡病的评价，不良反应。HistamineandAntihistamineAgentsHistamineanditsagonistsHistamineantagonistsH1receptorantagonistsH2receptorantagonistsHistamineIntroductionHistamineisbiologi
3、callyactiveaminethatisfoundinmanytissue(suchasmastcellsorbasophils),hascomplexphysiologicandpathologiceffects,andisoftenreleasedlocally.Togetherwithendogenouspeptides,prostaglandinsandleukotrienes,andcytokines,theyaresometimescalledautacoidsorlocalhormones
4、HistaminereceptorsubtypesReceptorSubtypeDistributionPostreceptorMechanismH1Smoothmuscle,endothelium,brain↑IP3,DAGH2Gastricmucosa,cardiacmuscle,mastcells,brain↑cAMPH3Presynaptic:brain,myentericplexus,otherneuronsGprotein-coupledHistaminereceptorsubtypesRece
5、ptorSubtypeEffectsafterbeingactivatedH1bronchoconstrictionandcontractionofintestinalS.M.ExpandbloodvesselPermeability↑stimulatesensorynerveendingsH2Causegastricacid,gastricpepsinandintrinsicfactorproduction.Causeadecreaseinsystolicanddiastolicbloodpressure
6、andaincreaseinheartrate.HistaminereceptorsubtypesReceptorSubtypePartiallySelectiveAgonistsPartiallySelectiveAntagonistsH12-(m-Flurophenyl)-histamineDiphenhydramine,promethazine,astemizoleH2Dimaprit,impromidine,amthamineCimetidine,ranitidineH3R-α-Methylhist
7、amineThioperamideHistaminePharmacodynamics❶Secretorytissue❷Smoothmuscle❸Cardiovascularsystem❹The“tripleresponse”ReceptorSubtypeEffectsafterbeingactivatedH1bronchoconstrictionandcontractionofintestinalS.M.ExpandbloodvesselPermeability↑stimulatesensorynervee
8、ndingsH2Causegastricacid,gastricpepsinandintrinsicfactorproduction.Causeadecreaseinsystolicanddiastolicbloodpressureandaincreaseinheartrate.❹The“tripleresponse”Intradermalinjectionofhistaminecausesacharacteri
