麻醉性镇痛药教学ppt课件

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1、ReviewNeurolepticdrugs12Chapter20NarcoticAnelgesicsObjectivesUnderstandthepharmacologicaleffects,mechanismofactions,clinicaluses,aswellasadversedrugreactionsofmorphine.Identifythetherapeuticeffectsandadversedrugreactionsofcodeineandpethidine.SectiononeIntroduction451.2AnalgesicsDefinitionDru

2、gsthatselectivelyinhibittheperception(sensation)ofthepainClassification1-Peripheral:-Causal:Atropine,NSAIDs-Non-causal2-Central:-NarcoticanalgesicsPeripheralanalgesicsCausal-TreatthecauseExample:Atropine(antispasmodic)AspirinNon-causal-NottreatthecauseExamples:1-Localanaesthetics(forsuperfic

3、ialtumor)2-Counter-irritant(applypainthatcounteractormasktheoriginalonee.g.acupuncture)NarcoticsNSAIDsExamplesMorphineAspirinSiteofactionCortex&thalamusPeripheralAntagonistNaloxoneNoantagonistUsesSever&deeppaine.g.cancer,MI&anginalpainDullpaine.g.headache,toothache&backachePotencyHighLowSide

4、effectAddictionNoaddiction.↑inbleedingtendency&ulcerMechanismstimulateopiatesreceptors(m,k,d)andreliefthepainInhibitsPGsynthesisbyinhibitionofCOX-2Theactionslistedforantagonistsareseenwiththeantagonistalone.Allthecorrelationsinthistablearebasedonstudiesinratsandmice,whichoccasionallyshowspec

5、iesdifferences.10SectiontwoMorphineNaturallyoccurringinthepoppy(16%)-OnlyneedstobeisolatedVerystrongpainrelieverbutalsoveryaddictive(2ndtoHeroin)Usuallyinjectedbutcanbesmoked,sniffedorswallowedCommonlyusedinhospitals2.1Introduction121)3位-OH的H被-CH3取代，中枢抑制作用↓。如：可待因（codeine)2)3位和6位-OH的H同时被-COCH

6、3取代，中枢抑制作用↑。如：海洛因(heroin)3)17位的-CH3被-CH2CH=CH2取代，则变为吗啡受体的部分激动药，如：丙烯吗啡(nalorphine)。若同时将6位的-OH变为=O，则变为吗啡受体的完全拮抗药，如：纳洛酮(naloxone)2.2构效关系14152.3MechanismsofActionMostneuronsreacttoopioidswithahyperpolarization,reflectinganincreaseinK+conductance.Ca2+influxintonerveterminalsduringexcitationisdecr

7、eased,leadingtoadecreasedreleaseoftransmittersanddecreasedsynapticactivity.Dependingonthecellpopulationaffected,thissynapticinhibitiontranslatesintoadepressantorexcitanteffect.Morphineandopioidsproduceanalgesia,affectmoodandrewardingbehavior,andalt