药理学课件南开大学第十五章影响自体活性物质的药物

药理学课件南开大学第十五章影响自体活性物质的药物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。药理学课件南开大学第十五章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。药理学课件南开大学第十五章影响自体活性物质的药物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。药理学课件南开大学第十五章影响自体活性物质的药物HistamineandAntihistamineAgentsHistamineanditsagonistsHistamineantagonistsH1receptorantagonistsH2receptorantagonists药理学课件南开大学第十五章影响自体活性物质的药物HistamineIntroductionHistamineisbiologicallyactiveaminethatisfoundinmanytissue(suchasmastcellsorbasophils),hascomplexphysiologicandpathologiceffects,andisoftenreleasedlocally.

Togetherwithendogenouspeptides,prostaglandinsandleukotrienes,andcytokines,theyaresometimescalledautacoidsorlocalhormones药理学课件南开大学第十五章影响自体活性物质的药物HistaminereceptorsubtypesReceptorSubtypeDistributionPostreceptorMechanismH1Smoothmuscle,endothelium,brain↑IP3,DAGH2Gastricmucosa,cardiacmuscle,mastcells,brain↑cAMPH3Presynaptic:brain,myentericplexus,otherneuronsGprotein-coupled药理学课件南开大学第十五章影响自体活性物质的药物HistaminereceptorsubtypesReceptorSubtypeEffectsafterbeingactivatedH1bronchoconstrictionandcontractionofintestinalS.M.ExpandbloodvesselPermeability↑stimulatesensorynerveendingsH2Causegastricacid,gastricpepsinandintrinsicfactorproduction.Causeadecreaseinsystolicanddiastolicbloodpressureandaincreaseinheartrate.药理学课件南开大学第十五章影响自体活性物质的药物HistaminereceptorsubtypesReceptorSubtypePartiallySelectiveAgonistsPartiallySelectiveAntagonistsH12-(m-Flurophenyl)-histamineDiphenhydramine,promethazine,astemizoleH2Dimaprit,impromidine,amthamineCimetidine,ranitidineH3R-α-MethylhistamineThioperamide药理学课件南开大学第十五章影响自体活性物质的药物HistaminePharmacodynamics❶Secretorytissue❷Smoothmuscle❸Cardiovascularsystem❹The“tripleresponse”ReceptorSubtypeEffectsafterbeingactivatedH1bronchoconstrictionandcontractionofintestinalS.M.ExpandbloodvesselPermeability↑stimulatesensorynerveendingsH2Causegastricacid,gastricpepsinandintrinsicfactorproduction.Causeadecreaseinsystolicanddiastolicbloodpressureandaincreaseinheartrate.药理学课件南开大学第十五章影响自体活性物质的药物❹The“tripleresponse”

Intradermalinjectionofhistaminecausesacharacteristicwheal-and-flareresponse,whichinvolvesanerythema,anedematouswhealandaredirregularflaresurroundingthewheal.药理学课件南开大学第十五章影响自体活性物质的药物HistamineHistamineClinicaluseofhistamine

Tobeusedintestinggastricacidsecretionanddiagnosisofleprosy.Decreaseofgastricacidcanbeseeninmalignantanemiaandtrueachlorhydia药理学课件南开大学第十五章影响自体活性物质的药物HistamineandAntihistamineAgentsHistamineanditsagonistsHistamineantagonistsH1receptorantagonistsH2receptorantagonists药理学课件南开大学第十五章影响自体活性物质的药物PhysiologicantagonistsEpinephrineReleaseinhibitorsCromolynHistaminereceptorantagonistsH1receptorantagonistsH2receptorantagonistsHistamineAntagonists药理学课件南开大学第十五章影响自体活性物质的药物HistamineandAntihistamineAgentsHistamineanditsagonistsHistamineantagonistsH1receptorantagonistsH2receptorantagonists药理学课件南开大学第十五章影响自体活性物质的药物H1receptorantagonistsChemistryFirst-generationblockersDiphenhydramine,promethazine,astemizoleSecond-generationblockers

Cimetidine,ranitidine药理学课件南开大学第十五章影响自体活性物质的药物rapidlyabsorbedorallywidelydistributedandthefirst-generationdrugsentertheCNSreadily.MostmetabolizedintheliverMostexcretedfromthekidneyPharmacokinetics药理学课件南开大学第十五章影响自体活性物质的药物H1receptorantagonistsPharmacodynamics❶HistamineReceptorBlockade❷CNSInhibition❸AnticholinoceptoractionandLocalanesthesiaReceptorSubtypeEffectsafterbeingactivatedH1bronchoconstrictionandcontractionofintestinalS.M.ExpandbloodvesselPermeability↑stimulatesensorynerveendingsH2Causegastricacid,gastricpepsinandintrinsicfactorproduction.Causeadecreaseinsystolicanddiastolicbloodpressureandaincreaseinheartrate.药理学课件南开大学第十五章影响自体活性物质的药物药理学课件南开大学第十五章影响自体活性物质的药物H1receptorantagonists❶AllergicReaction❷NauseaandVomiting❸SedationandhypnogenesisClinicalUses药理学课件南开大学第十五章影响自体活性物质的药物Toxicity

Sedation,antimuscarinicaction,drugallergy,cardiacarrhythmias(astemizole)andpossibleteratogeniceffects.H1receptorantagonists药理学课件南开大学第十五章影响自体活性物质的药物HistamineandAntihistamineAgentsHistamineanditsagonistsHistamineantagonistsH1receptorantagonistsH2receptorantagonists药理学课件南开大学第十五章影响自体活性物质的药物H2receptorantagonistsChemistry&PharmacokineticsCimetidineRanitidineFamotidineNizatidine药理学课件南开大学第十五章影响自体活性物质的药物H2receptorantagonistsPharmacodynamicsAcidsecretionandgastricmotilityCardiovascularsystemimmunologicalregulationReceptorSubtypeEffectsafterbeingactivatedH1bronchoconstrictionandcontractionofintestinalS.M.ExpandbloodvesselPermeability↑stimulatesensory