组胺和抗组胺药

组胺(zǔàn)和抗组胺(zǔàn)药

HistamineandAntihistamineAgents南开大学(nánkāidàxué)医学院张京玲王侃代红胜第一页，共三十一页。编辑课件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(zuòyòng)与应用。第二页，共三十一页。编辑课件HistamineandAntihistamineAgents内容组胺：来源(láiyuán)，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。第三页，共三十一页。编辑课件HistamineandAntihistamineAgents内容

抗组胺药：H1受体阻断剂：对H1受体的阻断(zǔduàn)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。第四页，共三十一页。编辑课件HistamineandAntihistamineAgentsHistamineanditsagonistsHistamineantagonistsH1receptorantagonistsH2receptorantagonists第五页，共三十一页。编辑课件HistamineIntroductionHistamineisbiologicallyactiveaminethatisfoundinmanytissue(suchasmastcellsorbasophils),hascomplexphysiologicandpathologiceffects,andisoftenreleasedlocally.

Togetherwithendogenouspeptides,prostaglandinsandleukotrienes,andcytokines,theyaresometimescalledautacoidsorlocalhormones第六页，共三十一页。编辑课件HistaminereceptorsubtypesReceptorSubtypeDistributionPostreceptorMechanismH1Smoothmuscle,endothelium,brain↑IP3,DAGH2Gastricmucosa,cardiacmuscle,mastcells,brain↑cAMPH3Presynaptic:brain,myentericplexus,otherneuronsGprotein-coupled第七页，共三十一页。编辑课件HistaminereceptorsubtypesReceptorSubtypeEffectsafterbeingactivatedH1bronchoconstrictionandcontractionofintestinalS.M.ExpandbloodvesselPermeability↑stimulatesensorynerveendingsH2Causegastricacid,gastricpepsinandintrinsicfactorproduction.Causeadecreaseinsystolicanddiastolicbloodpressureandaincreaseinheartrate.第八页，共三十一页。编辑课件HistaminereceptorsubtypesReceptorSubtypePartiallySelectiveAgonistsPartiallySelectiveAntagonistsH12-(m-Flurophenyl)-histamineDiphenhydramine,promethazine,astemizoleH2Dimaprit,impromidine,amthamineCimetidine,ranitidineH3R-α-MethylhistamineThioperamide第九页，共三十一页。编辑课件HistaminePharmacodynamics❶Secretorytissue❷Smoothmuscle❸Cardiovascularsystem❹The“tripleresponse”ReceptorSubtypeEffectsafterbeingactivatedH1bronchoconstrictionandcontractionofintestinalS.M.ExpandbloodvesselPermeability↑stimulatesensorynerveendingsH2Causegastricacid,gastricpepsinandintrinsicfactorproduction.Causeadecreaseinsystolicanddiastolicbloodpressureandaincreaseinheartrate.第十页，共三十一页。编辑课件❹The“tripleresponse”

Intradermalinjectionofhistaminecausesacharacteristicwheal-and-flareresponse,whichinvolvesanerythema,anedematouswhealandaredirregularflaresurroundingthewheal.第十一页，共三十一页。编辑课件HistamineHistamineClinicaluseofhistamine

Tobeusedintestinggastricacidsecretionanddiagnosisofleprosy.Decreaseofgastricacidcanbeseeninmalignantanemiaandtrueachlorhydia第十二页，共三十一页。编辑课件HistamineandAntihistamineAgentsHistamineanditsagonistsHistamineantagonistsH1receptorantagonistsH2receptorantagonists第十三页，共三十一页。编辑课件PhysiologicantagonistsEpinephrineReleaseinhibitorsCromolynHistaminereceptorantagonistsH1receptorantagonistsH2receptorantagonistsHistamineAntagonists第十四页，共三十一页。编辑课件HistamineandAntihistamineAgentsHistamineanditsagonistsHistamineantagonistsH1receptorantagonistsH2receptorantagonists第十五页，共三十一页。编辑课件H1receptorantagonistsChemistryFirst-generationblockersDiphenhydramine,promethazineSecond-generationblockers

Astemizole,acrivastine第十六页，共三十一页。编辑课件rapidlyabsorbedorallywidelydistributedandthefirst-generationdrugsentertheCNSreadily.MostmetabolizedintheliverMostexcretedfromthekidneyPharmacokinetics第十七页，共三十一页。编辑课件H1receptorantagonistsPharmacodynamics❶HistamineReceptorBlockade❷CNSInhibition❸AnticholinoceptoractionandLocalanesthesiaReceptorSubtypeEffectsafterbeingactivatedH1bronchoconstrictionandcontractionofintestinalS.M.ExpandbloodvesselPermeability↑stimulatesensorynerveendingsH2Causegastricacid,gastricpepsinandintrinsicfactorproduction.Causeadecreaseinsystolicanddiastolicbloodpressureandaincreaseinheartrate.第十八页，共三十一页。编辑课件第十九页，共三十一页。编辑课件H1receptorantagonists❶AllergicReaction❷NauseaandVomiting❸SedationandhypnogenesisClinicalUses第二十页，共三十一页。编辑课件Toxicity

Sedation,antimuscarinicaction,drugallergy,cardiacarrhythmias(astemizole)andpossibleteratogeniceffects.H1receptorantagonists第二十一页，共三十一页。编辑课件HistamineandAntihistamineAgentsHistamineanditsagonistsHistamineantagonistsH1receptorantagonistsH2receptorantagonists第二十二页，共三十一页。编辑课件H2receptorantagonistsChemistry&PharmacokineticsCimetidineRanitidineFamotidineNizatidine第二十三页，共三十一页。编辑课件H2receptorantagonistsPharmacodynamicsAcidsecretionandgastricmotilityCardiovascularsystemimmunologicalregulationReceptorSubtypeEffectsafterbeingactivatedH1bronchoconstrictionandcontractionofintestinalS.M.ExpandbloodvesselPermeability↑stimulatesensorynerveendingsH2Causegastricacid,gastricpepsinandintrinsicfactorproduction.Causeadecreaseinsystolicanddiastolicbloodpressureandaincreaseinheartrate.第二十四页，共三十一页。编辑课件第二十五页，共三十一页。编辑