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1、镇痛药Analgesics北京协和医学院基础医学院药理学系叶菜英AnalgesicsPrimaryeffectonCNS,eliminateoreasepainselectively,tolessenthenervousofpatients,theseagentsrelievepainwithoutproducingalossofconsciousness.Theyareusedprimarilytorelieveacuteandchronicitypainofanyorigin.AnalgesicsIthasbeenknowforcenturiesthatextract
2、softheopiumpoppycanbeusedtorelievepainandtreatdiarrhea.In1806,MorphinewasfirstisolatedfromthejuiceoftheopiumpoppybyGermanpharmacistFriedrichSertürner.Duringthe1950s,aseriesofmorphine-likepotentanalgesicsweresynthesized,suchaspethidine,methadone,etorphine,fentanyl.AnalgesicsPainisacomplexs
3、ubjectivesensation,andakindofprotectiveresponsewhenorganismsufferthenociceptivestimulus.Painisalsothebasisforthedoctorsdiagnosingdiseases.Itusuallyaccompanyanxiety,dread,horror,discomfortandsoon,tocausethepatientsdisorder,evenshock.Acutepainthathasbeenmadeadefinitediagnosis,shoulduseanalg
4、esicsimmediately.Butitisinadvisabletousenarcoticanalgesicswhenapainhasn`tbecertified,inordertoavoidmisdiagnosis.Opium(阿片类药物)【Classification】chemicalconstitutionaffinityandintrinsicactivityAgonists:Morphine,Pethidine,adanton……Antagonists:Naloxone,NaltrexonePartialagonist:Pentazocine,Nalorp
5、hine【Physiologicaldisposition】takeorally,injection→passthroughthebloodbrainbarrier→hepaticmetabolism→renalexcretionHOHOONCH3morphineOpiatealkaloids(阿片生物碱类)Morphine(1806，10%ofopiumtotalbase）Codeine（1832,methyl-morphine）Heroin（1874,acetomorphine,powerfuladdictivedrugs）PhenanthreneIsoquinoli
6、nePapaverine阿片生物碱类PoppyFreshcapsuleofopiumpoppyPCutcapsuleshowinglatexexudingfromcutPoppy镇痛药阿片生物碱类含阿片生物碱类植物：罂粟MorphineChemicalconstitutionStructuralfeatures17positionRis－CH3……agonists17positionRis－CH2CH＝CH2……antagonists7positionNCH2CH－……inreversiblecompoundMechanismsandEffectsOpioidrecept
7、orIn1973,threeAmericanlabsdiscoveredthereceptoratthesametime.Existoncellmembrane,glycoproteinHighaffinitySaturabilityStereospecificityDistributionofdefiniteareaSpecificityantagonistsTypesandeffectsμ(mu)δ(delta)κ(kappa)Analgesiaabovespinalcordlevelspinalcordlevelspin
