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药物的抗惊厥作用.doc

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AnticonvulsantEffectsofDrugs XXX （ChinaPharmaceuticalUniversity，639LongmianAvenue,Nanjing,Jiangsu,China210009） ABSTRACT:OBJECTIVE:TostudytheanticonvulsantefficacyofPhenytoinsodiumandPhenobarbitalandvalproateonconvulsion.METHODS:Theanticonvulsantactivityofthedrugswasevaluatedbythemaximalelectroshock(MES)testandremeflinseizuretest.Inducedratsweretreatedbyintraperitonealinjection,thenobservetheincubationperiod(uptotailsupright45°)anddegreeofreactionofeachmouse(spasm,fallingdown,stiffordeath).RESULTS:1.InMESexperiment,thedegreeofconvulsion:ThePhenobarbitalgroup(P<0.05vsnormalsalinegroup)wasthelightest,andtheNSgroupwastheseverestone.2.Inremeflinexperiment,thesimilarresultwasobservedbetweenvalproategroupandNSgroup(P<0.01).CONCLUSION:Phenobarbitalhasbetteranti-convulsioneffectthanPhenytoinsodiumonconvulsioninducedbyelectroshock,andvalproatehasasignificanteffecttoanti-convulsioninducedbyremeflin. KEYWORDSPhenytoinsodium;Phenobarbital;valproate;remeflin;anti-convulsion Introduction Phenytoinsodium:itsmechanismofaction:Itcanblocksodiumchannels(voltage-,frequency-,andtimedependentfashion)andinhibitthegenerationofactionpotentialsandItcanincreasethefunctionofinhibitorytransmitterGABA,inhibitnerveterminaltouptakeGABAandinducetheincreasingofGABAreceptor,therebyenhanceGABA-mediatedpostsynapticinhibition. Phenobarbital:itsmechanismofaction:Phenobarbitalcaninhibittheparadoxicaldischargeofepilepsyfocusselectively,enhancestimulationofsurroundingtissuesandblockdischargediffusetonormaltissuesandPhenobarbitalfacilitateGABA-mediatedinhibitionofneuronalactivity. Valproateisbroadspectrumantiepilepticdrug,whichisusedtoalltypesofepilepsy;itsmechanismisthatenhancingtheenzymaticactivityofglutamatedecarboxylase.AndInhibitingGABAreuptakeandsynapseinactivationviareleasingsynapsefrontalmembraneGABAandthenenhanceGABApostsynapticinhibition Remeflin,acentralstimulatewhichcandirectlyexciterespiratorycenter,canproduceconvulsionwithover-dose.Theprotectiveeffectsofdrugsonconvulsionproducedbyremeflincan