艾普拉唑的作用机制与临床评价

©1994-2009ChinaAcademicJournalElectronicPublishingHouse.Allrightsreserved.(,100050)R975+12B1672-2124(2009)10-0724-02::,:,CYP2C19,:,,;;ActionMechanismandClinicalEvaluationofIlaprazoleLIUTeng3,CHANGYan2lu,HANRong#(Dept.ofPharmacy,TiantanHospitalAffiliatedtoCapitalMedicalUniversity,Beijing100050,China)ABSTRACTOBJECTIVE:ToanalyzetheactionmechanismofIlaprazoleandevaluateitsclinicalefficacy.METHODS:Thepertinentliteraturebothathomeandabroadaswellastherelatedfindingsinpharmacologyandthepharmacokineticswerereviewed.RESULTS:IlaprazolehadmorepotentantiacidactionthanomeprazoleanditsmetabolismwasindependentofCYP2C19;meanwhile,Ilaprazolewasmoreeffectivethanotherprotonpumpinhibitorsforgastroesophagealrefluxdiseaseorpepticulcer.CONCLUSION:Ilaprazoleissuperiortopreviousgenerationsofprotonpumpinhibitorsinpharmacology,pharmacokineticsandclinicalefficacy,thusservingasanewchoiceforclinicalantiacidtreatment.KEYWORDSProtonpumpinhibitor;Ilaprazole;Actionmechanism3:E-mail:[e-mail]#::E-mail:[e-mail]20,19761H2,1987(PPI),,PPI(Ilaprazole,),(1),27,,,,,CYP2C19,NNHNSONMeOCH21Fig1ChemicalstructuralformulaofIlaprazole1,H+-K+-ATP,H+-K+,,,(1),,ED50ED50ED50,KwonD[1],H+-K+-ATP,H+-K+-ATP,pH714,IC5061010-6molL-1,IC50110-4molL-1,,,,ED50316mgkg-1,ED50815mgkg-1;,ED50116mgkg-1,ED50318mgkg-1(Hp),,,Hp12156125gmL-1,,30%50%,34,Hp,[2],,,(1000mgkg-1,);(100mgkg-1),;300mgkg-1;1000mgkg-1,,,1Tab1Ilaprazolevs.omeprazoleininhibitoryefficacyonpepticulcerED50316mgkg-1714mgkg-1ED501412mgkg-13213mgkg-1ED50515mgkg-1ED50215mgkg-1ED50116mgkg-1316mgkg-1724Evaluationandanalysisofdrug2useinhospitalsofChina2009Vol.9No.10©1994-2009ChinaAcademicJournalElectronicPublishingHouse.Allrightsreserved.()CYP2C19441130,5mg10mg20mg30mg40mg5,,,425pH5mg20mg10mg20mg,,24,;,10mg20mg,,476,23%77%,CYP2C19,12,5mg20mg,10mg20mg,,,412TAPTAP,(GERD)pH,10mg40mg,20mg40mgGERD,KilBJ[3],,ED50PericlouAP[4]GERDpH,5mg20mgAUCtpH,10mg20mg20mg16243(5mg10mg20mg)HoKY[5],212306,5mg20mg10mg20mg5,ALTPAST,PPI,,CYP3A4,CYP2C19pH(),,;;,,PPI,,HpPPI,PPI,PPI,[1]KwonD,ChaeJB,ParkCW,etal.EffectsofIY-81149,anewlydevelopedprotonpumpinhibitor,ongastricacidsecretioninvitroandinvivo[J].Arzneimittelforschung,2001,51(3):204.[2]KimEJ,LeeRK,LeeSM,etal.GeneralpharmacologyofIY-81149,anewprotonpumpinhibitor[J].Arzneimittelforschung,2001,51(1):51.[3]KilBJ,KimIW,ShinCY,etal.ComparisonofIY81149withomeprazoleinratrefluxoesophagitis[J].AutonPharmacol,2000,20(5-6):291.[4]PericlouAP,GoldwaterR,LeeSM,etal.AcomparativepharmacodynamicstudyofIY-81149versusomeprazoleinpatientswithgastroesophagealrefluxdisease[J].ClinPharmacolTher,2000,68(3):304.[5]HoKY,KuanA,ZaÌoF,etal.Randomized,parallel,double-blindcomparisonoftheulcer-healingeffectsofilaprazoleandomeprazoleinthetreatmentofgastricandduodenalulcers[J].JGastroenterol,2009,44(7):697.(:2009-07-20:2009-08-18)2009910725