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1、AnticonvulsantEffectsofDrugsXXX（ChinaPharmaceuticalUniversity，639LongmianAvenue,Nanjing,Jiangsu,China210009）ABSTRACT:OBJECTIVE:TostudytheanticonvulsantefficacyofPhenytoinsodiumandPhenobarbitalandvalproateonconvulsion.METHODS:Theanticonvulsantactivityofthedrugswas
2、evaluatedbythemaximalelectroshock(MES)testandremeflinseizuretest.Inducedratsweretreatedbyintraperitonealinjection,thenobservetheincubationperiod(uptotailsupright45°)anddegreeofreactionofeachmouse(spasm,fallingdown,stiffordeath).RESULTS:1.InMESexperiment,thedegree
3、ofconvulsion:ThePhenobarbitalgroup(P<0.05vsnormalsalinegroup)wasthelightest,andtheNSgroupwastheseverestone.2.Inremeflinexperiment,thesimilarresultwasobservedbetweenvalproategroupandNSgroup(P<0.01).CONCLUSION:Phenobarbitalhasbetteranti-convulsioneffectthanPhenytoi
4、nsodiumonconvulsioninducedbyelectroshock,andvalproatehasasignificanteffecttoanti-convulsioninducedbyremeflin.KEYWORDSPhenytoinsodium;Phenobarbital;valproate;remeflin;anti-convulsionIntroductionPhenytoinsodium:itsmechanismofaction:Itcanblocksodiumchannels(voltage-
5、,frequency-,andtimedependentfashion)andinhibitthegenerationofactionpotentialsandItcanincreasethefunctionofinhibitorytransmitterGABA,inhibitnerveterminaltouptakeGABAandinducetheincreasingofGABAreceptor,therebyenhanceGABA-mediatedpostsynapticinhibition.Phenobarbita
6、l:itsmechanismofaction:Phenobarbitalcaninhibittheparadoxicaldischargeofepilepsyfocusselectively,enhancestimulationofsurroundingtissuesandblockdischargediffusetonormaltissuesandPhenobarbitalfacilitateGABA-mediatedinhibitionofneuronalactivity.Valproateisbroadspectr
7、umantiepilepticdrug,whichisusedtoalltypesofepilepsy;itsmechanismisthatenhancingtheenzymaticactivityofglutamatedecarboxylase.AndInhibitingGABAreuptakeandsynapseinactivationviareleasingsynapsefrontalmembraneGABAandthenenhanceGABApostsynapticinhibitionRemeflin,acent
8、ralstimulatewhichcandirectlyexciterespiratorycenter,canproduceconvulsionwithover-dose.Theprotectiveeffectsofdrugsonconvulsionproducedbyremeflincanbeusedtoscree
