抗癫痫药物研究现状与新进展-应义

110ChinaPharmaceuticals201210202120Vol．21，No．20，October20，2012ST[J]．2007354295－304．[2]．C[J]．2001298499．[3]．C[J]．2006183323－325．[4]．[M]．2006311．(2012－02－24)檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨檨··SynthesisReports325027epilepsyEP。、、。。R971+．6A1006－4931(2012)20－0110－03、。500080%[1]。[2]。AEDCBZ、PHT、VPA、PB、、、。10。1[3]1．1。1～3min1～2h。。1．21。1～2s、、。。。1．3。、。1．4、、、、、、、、。2680%。AED、、、、。[4]。12γ－GABAGABA34LNPQRT。。1980[5]。。4GABA。33．1dilantinphenytoinsodium3～4d。Na+GABA。、。phenobarbitalluminal111ChinaPharmaceuticals201210202120Vol．21，No．20，October20，2012··SynthesisReports。。。primidonemysolinePEMA、。。3．2diazepamvalium。、、。clomazepamclomapin5。。3．3ethosuximide。phensuximidemilontin。trimethadionetridione2～4d。。vanillin。acetazolamidediamoxNa+K+HCO3－GABA。。。3．4sulthiameospolt。。carbamazepinetegretol。3．5sodium2－propylvaleratesodiumvalproateVPA。。。γ－GABAGABAGABA30%～50%。valpramide2。TPM19951999。/AMPAGABA。9%～17%19～23h70%～97%。[6]。Lennox－Gastaut。0．5mg/kg0．5～1．0mg/kg4．0～8．0mg/kg。、、、、、、、、、、。、40%。LTG19911999。。Lennox－Gastaut、West。55%。5～15mg/kg2[7]。、、。、、、、、。10%4。22．8%1%。LTG、、15h59h。levetiracetamS－α－－2－－1－C8H14N2O2[8]。synapticvesicle2ASV2ACA1Nβ－carbolinesGABAGABAGABA[9－13]。。/[14]。3．63pregabalin3－－5－SGABA、。、、。GABA、P/Qα2－δCa2+。6303．15%、112ChinaPharmaceuticals201210202120Vol．21，No．20，October20，2012··SynthesisReports3．12%、1．18%、0．16%[15]。21．05%、。4－。。1μmol/L。2%。CGP47292。CGP47292。P450。CYP2E1CYP3A4[16]。、、、、、。3200mg/d、、、、、、、、、。、、、、、、、、、、、、。1acosamideLCMFDA200881016/17FDA[17]。－2CRMP－2。[18－19]。。3brivaracetam、。3。Ganaxolone。ganaxolone。Perampanelα－－3－－5－－4－AMPA。AMPAAMPAperampanel。perampanel2。3carisbamatebrivaracetam2AretigabineFDAEMEA。4、、。、、“”。。[e-mail]。[1]．[M]．152005211．[2]．[J]．2003192134．[3]．[J]．2004353244．[4]JiaoZZhongMKShiXJetal．Therapeuticdragmonitoringofantiepilep-sydrugs[J]．ChinacilinPharmacy2004136386－389．[5]SchmutzMBruggerFGentschCetal．Oxcarbazepinepreclinicalanti-convulsantprofileandputtivemechanismsofaction[J]．Epilepsia199435Suppl547－50．[6]．[J]．20063322．[7]．[J]．200027299－101．[8]StefanHFeuersteinTJ．Novelanticonvulsantdrugs[J]．PharmacolTher2007113(1)165－183．[9]LynchBALambengNNockaKetal．ThesynapticvesicleproteinSV2Aisthebindingsitefortheantiepilepticdruglevetiracetam[J]．ProcNatlA-cadSciUSA2004101269861－9866．[10]KaminskiRMMatagneALeclercqKetal．SV2Aproteinisabroad－spectrumanticonvulsanttargetfunctionalcorrelationbetweenproteinbindingandseizureprotectioninmodelsofbothpartialandgeneralizedepilepsy[J]．Neuropharmacology2008544715－720．[11]LukyanetzEAShkrylVMKostyukPG．SelectiveblockadeofN－typecalciumchannelsbylevetiracetam[J]．Epilepsia20024319－18．[12]FrenchJA．Theroleofnewantiepilepticdrugs[J]．AmJManagCare200177S209－S214．[13]RadtkeRA．Pharmacokineticsoflevetiracetam[J]．Epilepsia200142Suppl424－27．[14]．[J]．200917(2)190－193195[15]BaldinettiFUthmanBBazilCetal．Safetyandtolerabilityprofileofpregabalininthelong－termtreatmentofpatientswithpartialonsetseizures[J]．Epilepsia200647Suppl13S1422－S1421．[16]McleanMJSchmutZMPozzaMetal．Theinfluenceofrufinamideonsodiumcurrentsandactionpotentialfiringinrodentneurons[abstractno．3．062][J]．Epilepsia200546Suppl8S296．[17]WwhnerTBauerSHhmerHMetal．Sixmonthsofpostmarketingexpe-riencewithadjunctivelacosamideinpatientswithpharmacoresistantfocalepilepsyatatertiaryepilepsycenterinGermany[J]．EpilepsyBehav2009163423－425．[18]BialerMJohannessenSILevyRHetal．Progressreportonnewantiepilep-ticdrugsAsummaryoftheTenithEilatconferenceEILATIX[J]．EpilepsyRes20098311－43．[19]ShaibaniAFaresSSelamJLetal．LacosamideinpainfuldiabeticneuropathyAn18－weekdouble－blindplacebocontrolledtrial[J]．JPain2009108818－828．(2012－03－05)