等效与安全性：恩他卡朋双巴片与等量左旋多巴卡比多巴速释剂 恩他卡朋具有生物等效性

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1、等效与安全性：恩他卡朋双巴片与等量左旋多巴卡比多巴速释剂+恩他卡朋具有生物等效性Levodopa/carbidopa/entacapone(Stalevo)RobertA.Hauser,MD———————————————————————————————————————————————Articleabstract—Alevodopa/carbidopa/entacaponecombinationproduct(Stalevo)wasrecentlyapprovedtotreatpa-tientswithidiopathicParkinson’sdisease

2、(PD)whoexperienceend-of-dose“wearing-off.”Stalevoisavailableindosecombinationsoflevodopa/carbidopa/entacapone50/12.5/200mg(Stalevo50),100/25/200mg(Stalevo100),and150/37.5/200mg(Stalevo150).AseriesofpharmacokineticstudiesdemonstratedbioequivalencebetweenStalevoandcorrespond-ingdosag

3、esoflevodopa/carbidopaplusentacapone.AclinicaladvantageofStalevoisthatpatientscantakeonepillratherthantwo(ormore)separatetablets.Inaddition,Stalevo50and100tabletsaresmallerthanentacaponetablets.Theseadvantagesmaybeparticularlybeneficialforpatientstakingmanypills,thosewhohavedifficu

4、ltyfollowingcomplexmedicationregimens,andthosewithswallowingdifficulty.MostPDpatientstakinglevodopa/carbidopaimmediate-release(IR)plusentacaponecanbedirectlyswitchedtothecorrespondingdoseStalevoproduct.ForfluctuatingPDpatientstakinglevodopa/carbidopaIRwithoutentacapone,switchingtot

5、hecorrespondingStalevotabletisanalogoustoaddingentacapone.Inswitchingpatientswhoarereceivinglevodopa/carbidopacontrolled-release(CR),itshouldbenotedthatthebioavailabilityoflevodopafromlevodopa/carbidopaCRisapproximately70–75%thatoflevodopa/carbidopaIRproducts,includingStalevo.NEURO

6、LOGY2004;62(Suppl1):S64–S71Whenlevodopaisadministeredwithadopadecar-boxylaseinhibitor(DDI),suchascarbidopaorbenserazide,thepredominantrouteoflevodopame-tabolismisviacatechol-O-methyltransferase(COMT)toform3-O-methyldopa(3-OMD).Entaca-poneisaselective,reversible,peripherallyactingCO

7、MTinhibitorthatincreasesthelevodopahalf-lifeandconcentrationareaunderthecurve(AUC).1Thismakesmorelevodopaavailablefortransportintothebrainoveralongertime.When200mgentacaponeisadministeredwithlevodopa/carbidopaimmediatere-lease(IR),thelevodopaAUCisincreasedby35–40%andthehalf-lifeisp

8、rolongedfrom1.3to2.4hours.