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(clonazepam,CZP),1.50.1mgCZPWistar,CZP,51020,5,,,CZP,,,AnexperimentalandclinicalstudyonrectaladministrationofclonazepamJiangLi,CaiFangcheng.ChildrensHospital,ChongqingUniversityofMedicalSciences,Chongqing630014AbstractTostudytheefficacyofrectaladministrationofclonazepam(CNP),theauthorsad2ministratedCNPrectallytoWistarratsinadoseof1.5mgökgandtochildreninadoseof0.1mgökg.ThepharmacokineticsdemonstratedthatinbothratsandchildrenCNPwasrapidlyabsorbedfromrectumwithatherapeuticandpeakbloodlevelat5and1020minutes,respectively.At5minafterCNPadministration,EEGpatternsweresignificantlychangedwithcompletedisappearanceofepilepticdischarges.CNPalsoeffectivelypreventedsevereseizuresinducedbymegimide.Therewerenoobviouslypathologicalchangesofrectalmucosaoranysideeffectinchildren.TheresultssuggestthatCNPadministratedrectallyisasafe,quickandeffectivewaytocontrolseizures,whichcanbeusedeasilyandconvenientlyforoutpatients.KeywordsClonazepamAdministration,rectumPharmacokineticsPharmacology(clonazepamCZP)[1],,[2],,CZP1.CZP:Wistar7,250300g:6300142cm,1.5mgökgCZP()51015203045601201801.0ml,,-20Waters,CZPCZPSigma,,3P87(),2.CZP:Wistar20,220300g,2()40mgökg;CZPCZP1.5mgökg,152[3]Ono7,51202ChinJPediatr,April1997,Vol.35,No.43.CZP:Wistar5,250300g,145308F8(EEG)[4]EEG5,CZP30,CZPCZP51015EEG120();10,BEAM(JEC)EEG(BEAM)(D)(B)CZP[5]4.CZP:Wistar10,240300g,CZP6,2CZP0.1mgökg[1],2,2;CZP3,,10%,,HE1.CZP:7,4683,1725,,CZP6cm12#3cm,0.1mgökgCZP51530-20[6],CZP2.CZP:6,2,3,17810,6.540kg1020,(EEG),,2,283ö(1939ö)CZP0.050.10mgökg(0.602.50mg),EEG10,12051530EEG23,10BEAM[7];3;,:t;F,q:V21.CZP:13P87,CZP,CZP,15(156)17CZP(xqsxq,LgöL)CZPCZP0()()301001953174574161099186057121512522120421220124271802272.CZP:CZP22(%)5(%)(xqsxq,)1010010100107010211013918112CZP105010004010714017012P0.050.010.010.010.013.CZP:EEGDEEG,CZP5B,DBEAM34.CZP:,CZP,3021997435435BEAMBD(xqsxq,%)BCZPtDCZPt31161133514019()531142103914115331133333510016261921133143110321121138181153213473334191102814111331924153011210381211134111835160192712113341639F014517101116127:3P0.01;CZP,33P0.05,P0.011.CZPCZP(4):5,5LgöL;515,24147,256LgöL4CZPCZPEEGBEAM(xqsxq)CZP(LgöL,n=7)xqsxqBEAMB(%)(n=6)EEG(ö)(n=6)0020161112718311()515153135102612251811591241133152211213121533193217314361731033301213215611261139185143351121333F71312131810:,3P0.05,33P0.012.CZP:EEG38,B;1018,4,250%75%;60,73ö(224ö);120,2BEAM4,,;,3CZP,5,,[8],1015[9],80%[10],CZP,,CZP,1561475,,EEGBEAM[5,7];EEG,CZP1870LgöL[8],Huaug,,550LgöL[7],(0.1mgökg)CZP,55LgöL,267,CZPCZP,pH,[7],,13,[2]CZP24,,,0.1mgökg,CZP402ChinJPediatr,April1997,Vol.35,No.4,CZP,,,,1MorselliPL.TheTreatmentofEpilepsia:principlesandpractice,1sted.London:Philadelphia,19931752762.2vanHoogdalemEJ,deBoerAG,BreimerDD.Pharma2cokineticsofrectaladministration.PartI.ClinPharma2cokinet,1991,21:11.3,OnoJ,WalsonPD.1,1993,28:486.4HornE,WeberR.Transientepileptiformexperienceaf2fectsthedurationofpenicillin2inducedconvulsiveactivityintheawakerat.AchiveItalBiol,1993,131:47.5WandemaJW,SansomLN,Dios2ViEitezMC,etal.Phar2macokinetic2pharmacodynamicmodelingoftheelectroence2phalographiceffectsofBenzodiazepines.JPharmacolExpTher,1991,257:472.6,..,1994,10:365.7BrowneTR.Clonazepam.ArchNeurol,1976,33:326.8RylanceGW,PoultonJ,CherryRC,etal.Plasmaconcen2trationofclonazepamaftersinglerectaladministration.ArchDisChild,1986,61:186.9GravesNM,KrielRL,Rectaladministrationofantiepilep2ticdrugsinchildren.PediatrNeurol,1987,3:321.10SusumnS.Antiepilepticdrugs,3rded.NewYork:RavenPressLtd,19891735779.(:1996201226:1996205227)(:)ÏÏ,,1,,8,541:,,1,14,4,,X47,56göL76göL:38.3,14ö7kPa(105ö52.5mmHg),,,,,,,,:102göL,8.8109öL,166109öL,,,:,35.1(13.3),:100034,,Ï0.27,Ï0.670.41(1.29),X200ml,,,56göL,:,,X,1,,,,5,X,,:Ï,,;3,,,XÏ,(:1996210203:1996212230)(:)50219974354