麻醉性镇痛药(学习资料)

《麻醉性镇痛药(学习资料)》由会员上传分享，免费在线阅读，更多相关内容在教育资源-天天文库。

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

2、2AnalgesicsDefinitionDrugsthatselectivelyinhibittheperception(sensation)ofthepainClassification1-Peripheral:-Causal:Atropine,NSAIDs-Non-causal2-Central:-NarcoticanalgesicsPeripheralanalgesicsCausal-TreatthecauseExample:Atropine(antispasmodic)AspirinNon-causal-Nottreat

3、thecauseExamples:1-Localanaesthetics(forsuperficialtumor)2-Counter-irritant(applypainthatcounteractormasktheoriginalonee.g.acupuncture)NarcoticsNSAIDsExamplesMorphineAspirinSiteofactionCortex&thalamusPeripheralAntagonistNaloxoneNoantagonistUsesSever&deeppaine.g.cancer

4、,MI&anginalpainDullpaine.g.headache,toothache&backachePotencyHighLowSideeffectAddictionNoaddiction.↑inbleedingtendency&ulcerMechanismstimulateopiatesreceptors(m,k,d)andreliefthepainInhibitsPGsynthesisbyinhibitionofCOX-2Theactionslistedforantagonistsareseenwiththeantag

5、onistalone.Allthecorrelationsinthistablearebasedonstudiesinratsandmice,whichoccasionallyshowspeciesdifferences.10SectiontwoMorphineNaturallyoccurringinthepoppy(16%)-OnlyneedstobeisolatedVerystrongpainrelieverbutalsoveryaddictive(2ndtoHeroin)Usuallyinjectedbutcanbesmok

6、ed,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-COCH3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14152.3Mechanis

7、msofActionMostneuronsreacttoopioidswithahyperpolarization,reflectinganincreaseinK+conductance.Ca2+influxintonerveterminalsduringexcitationisdecreased,leadingtoadecreasedreleaseoftransmittersanddecreasedsynapticactivity.Dependingonthecellpopulationaffected,thissynaptic

8、inhibitiontranslatesintoadepressantorexcitanteffect.Morphineandopioidsproduceanalgesia,affectmoodandrewardingbehavior,andalt