美罗培南国外说明书.pdf

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1、NDA50-706/S-022Page3®MERREMI.V.(meropenemforinjection)FORINTRAVENOUSUSEONLYToreducethedevelopmentofdrug-resistantbacteriaandmaintaintheeffectivenessof®MERREMI.V.(meropenemforinjection)andotherantibacterialdrugs,MERREMI.V.shouldbeusedonlytotreatorpreventinfectionsthatareprovenorstrongl

2、ysuspectedtobecausedbybacteria.DESCRIPTION®MERREMI.V.(meropenemforinjection)isasterile,pyrogen-free,synthetic,broad-spectrum,carbapenemantibioticforintravenousadministration.Itis(4R,5S,6S)-3-[[(3S,5S)-5-(Dimethylcarbamoyl)-3-pyrrolidinyl]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-

3、azabicyclo[3.2.0]hept-2-ene-2-carboxylicacidtrihydrate.ItsempiricalformulaisC17H25N3O5S•3H2Owithamolecularweightof437.52.Itsstructuralformulais:MERREMI.V.isawhitetopaleyellowcrystallinepowder.Thesolutionvariesfromcolorlesstoyellowdependingontheconcentration.ThepHoffreshlyconstitutedso

4、lutionsisbetween7.3and8.3.Meropenemissolublein5%monobasicpotassiumphosphatesolution,sparinglysolubleinwater,veryslightlysolubleinhydratedethanol,andpracticallyinsolubleinacetoneorether.Whenconstitutedasinstructed(seeDOSAGEANDADMINISTRATION;PREPARATIONOFSOLUTION),each1gMERREMI.V.vialwi

5、lldeliver1gofmeropenemand90.2mgofsodiumassodiumcarbonate(3.92mEq).Each500mgMERREMI.V.vialwilldeliver500mgmeropenemand45.1mgofsodiumassodiumcarbonate(1.96mEq).CLINICALPHARMACOLOGYAttheendofa30-minuteintravenousinfusionofasingledoseofMERREMI.V.innormalvolunteers,meanpeakplasmaconcentrat

6、ionsareapproximately23µg/mL(range14-26)forthe500mgdoseand49µg/mL(range39-58)forthe1gdose.A5-minuteintravenousbolusinjectionofMERREMI.V.innormalvolunteersresultsinmeanpeakplasmaconcentrationsofapproximately45µg/mL(range18-65)forthe500mgdoseand112µg/mL(range83-140)forthe1gdose.Following

7、intravenousdosesof500mg,meanplasmaconcentrationsofmeropenemusuallydeclinetoapproximately1µg/mLat6hoursafteradministration.Insubjectswithnormalrenalfunction,theeliminationhalf-lifeofMERREMI.V.isapproximately1hour.Approximately70%oftheintravenouslyadministereddoseisrecoveredasunchangedm

8、erope