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1、药理学课件南开大学影响自体活性物质的药物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。Histamineand
2、AntihistamineAgentsHistamineanditsagonistsHistamineantagonistsH1receptorantagonistsH2receptorantagonistsHistamineIntroductionHistamineisbiologicallyactiveaminethatisfoundinmanytissue(suchasmastcellsorbasophils),hascomplexphysiologicandpathologiceffects,andisoftenrele
3、asedlocally.Togetherwithendogenouspeptides,prostaglandinsandleukotrienes,andcytokines,theyaresometimescalledautacoidsorlocalhormonesHistaminereceptorsubtypesReceptorSubtypeDistributionPostreceptorMechanismH1Smoothmuscle,endothelium,brain↑IP3,DAGH2Gastricmucosa,cardia
4、cmuscle,mastcells,brain↑cAMPH3Presynaptic:brain,myentericplexus,otherneuronsGprotein-coupledHistaminereceptorsubtypesReceptorSubtypeEffectsafterbeingactivatedH1bronchoconstrictionandcontractionofintestinalS.M.ExpandbloodvesselPermeability↑stimulatesensorynerveendings
5、H2Causegastricacid,gastricpepsinandintrinsicfactorproduction.Causeadecreaseinsystolicanddiastolicbloodpressureandaincreaseinheartrate.HistaminereceptorsubtypesReceptorSubtypePartiallySelectiveAgonistsPartiallySelectiveAntagonistsH12-(m-Flurophenyl)-histamineDiphenhyd
6、ramine,promethazine,astemizoleH2Dimaprit,impromidine,amthamineCimetidine,ranitidineH3R-α-MethylhistamineThioperamideHistaminePharmacodynamics❶Secretorytissue❷Smoothmuscle❸Cardiovascularsystem❹The“tripleresponse”ReceptorSubtypeEffectsafterbeingactivatedH1bronchoconstr
7、ictionandcontractionofintestinalS.M.ExpandbloodvesselPermeability↑stimulatesensorynerveendingsH2Causegastricacid,gastricpepsinandintrinsicfactorproduction.Causeadecreaseinsystolicanddiastolicbloodpressureandaincreaseinheartrate.❹The“tripleresponse”Intradermalinjectio
8、nofhistaminecausesacharacteristicwheal-and-flareresponse,whichinvolvesanerythema,anedematouswhealandaredirregularflaresurroundingth
