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1、AnticonvulsantEffectsofDrugsXXX（ChinaPharmaceuticalUniversity，639LongmianAvenueNanjingJiangsuChina210009）ABSTRACT:OBJECTIVE:TostudytheanticonvulsantefficacyofPhenytoinsodiumPhenobarbitalvalproateonconvulsion.METHODS:Thea

2、nticonvulsantactivityofthedrugswasevaluatedbythemaximalelectroshock(MES)testremeflinseizuretest.Inducedratsweretreatedbyintraperitonealinjectionthenobservetheincubationperiod(uptotailsupright45)degreeofreactionofeachmous

3、e(spasmfallingdownstiffdeath).RESULTS:1.InMESexperimentthedegreeofconvulsion:ThePhenobarbitalgroup(P0.05vsnmalsalinegroup)wasthelightesttheNSgroupwastheseverestone.2.Inremeflinexperimentthesimilarresultwasobservedbetween

4、valproategroupNSgroup(P0.01).CONCLUSION:PhenobarbitalhasbetteranticonvulsioneffectthanPhenytoinsodiumonconvulsioninducedbyelectroshockvalproatehasasignificanteffecttoanticonvulsioninducedbyremeflin.KEYWDSPhenytoinsodiumP

5、henobarbitalvalproateremeflinanticonvulsionIntroductionPhenytoinsodium:itsmechanismofaction:Itcanblocksodiumchannels(voltagefrequencytimedependentfashion)inhibitthegenerationofactionpotentialsItcanincreasethefunctionofin

6、hibitytransmitterGABAinhibitnerveterminaltouptakeGABAinducetheincreasingofGABArecepttherebyenhanceGABAmediatedpostsynapticinhibition.Phenobarbital:itsmechanismofaction:Phenobarbitalcaninhibittheparadoxicaldisgeofepilepsy

7、focusivelyenhancestimulationofsurroundingtissuesblockdisgediffusetonmaltissuesPhenobarbitalfacilitateGABAmediatedinhibitionofneuronalactivity.Valproateisbroadspectrumantiepilepticdrugwhichisusedtoalltypesofepilepsyitsmec

8、hanismisthatenhancingtheenzymaticactivityofglutamatedecarboxylase.InhibitingGABAreuptakesynapseinactivationviareleasingsynapsefrontalmembraneGABAthenenhanceGABApostsynapticinhibitionRemeflinacentralstimulatewhichcandirec

9、tlyexciterespiratycentercanproduceconvulsionwithoverdose.Theprotectiveeffectsofdrugsonconvulsionproducedbyremeflincanbeusedtoscreenantiepilepticanticonvulsion.Stimulatingmouseheadwithastrongelectriccurrentcancausegeneral

10、tetanicconvulsion.Ifadrugcanpreventtheoccurrenceofgeneraltitanicconvulsionwecouldinitiallysuspectthatithasantagonisticeffectongrmal.Remeflinacentralstimulantwhichcandirectlyexciterespiratycentercanprotectiveeffectsofdrug

11、sonconvulsionproducedbyremeflincanbeusedtoscreenantiepilepticsanticonvulsants.[1]Outcomemeasuresonbehavisinremeflininducedconvulsionmodel:degree0:nophenomenondegree1:tailsuprightdegree2:tumbledegree3:stiffdegree4:death.3

12、Results3.1ResultsofMESexperimentPhenobarbitalwasobvioustohavetheprotectiveeffectsonMESconvulsion(P0.05vsNmalsaline)itisbetterthanphenytoinsodiumwhichhasaweakanticonvulsanteffiancythattheconvulsionratewasbetweennmalsaline

13、groupPhenobarbitalgroup.Table1resultofprotectiveeffectsonMESconvulsionofphenytoinsodiumphenobarbital.DrugsDosage（mgkg）ConvulsionSumConvulsionRate(%)Nmalsaline——6875Phenobarbital751812.5Phenytoinsodium754850P0.05vsNmalsal

14、ine3.2ResultofremeflinexperimentTherewashighlysignificantdifference(P0.01)betweenthesodiumvalproategroupnmalsalinegroupindeathratesignificantdifference(P0.05)betweenthetwogroupsinconvulsionincubationreactionintensity.Thi

15、smeansthatsodiumvalproatehastheanticonvulsantefficacytoplayaprotectiveeffectsontheconvulsantinducedbyremeflin.Afterinjectionofremeflinmicemayexperiencedincubationperiodstiffflexionphasestraightinghindlimbphaseclonicphase

16、restationperiod.Themiceinnmalsalinegroupbehaviasfollows:walkedhaltinglyjumpedupliftedfelimbsstoodontwofeetearstowardsthebacktailsupwardslikeletterC.Themiceinsodiumvalproategroupbehavias:Walkedslowlythetailwasalmoststraig

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