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.docVIP

——————————————————————————————————————————————— 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(PD)whoexperienceend-of-dose“wearing-off.”Stalevoisavailableindosecombinationsoflevodopa/carbidopa/entacapone50/12.5/200mg(Stalevo50),100/25/200mg(Stalevo100),and150/37.5/200mg(Stalevo150).AseriesofpharmacokineticstudiesdemonstratedbioequivalencebetweenStalevoandcorrespond-ingdosagesoflevodopa/carbidopaplusentacapone.AclinicaladvantageofStalevoisthatpatientscantakeonepillratherthantwo(ormore)separatetablets.Inaddition,Stalevo50and100tabletsaresmallerthanentacaponetablets.Theseadvantagesmaybeparticularlybeneficialforpatientstakingmanypills,thosewhohavedifficultyfollowingcomplexmedicationregimens,andthosewithswallowingdifficulty.MostPDpatientstakinglevodopa/carbidopaimmediate-release(IR)plusentacaponecanbedirectlyswitchedtothecorrespondingdoseStalevoproduct.ForfluctuatingPDpatientstakinglevodopa/carbidopaIRwithoutentacapone,switchingtothecorrespondingStalevotabletisanalogoustoaddingentacapone.Inswitchingpatientswhoarereceivinglevodopa/carbidopacontrolled-release(CR),itshouldbenotedthatthebioavailabilityoflevodopafromlevodopa/carbidopaCRisapproximately70–75%thatoflevodopa/carbidopaIRproducts,includingStalevo. NEUROLOGY2004;62(Suppl1):S64–S71 Whenlevodopaisadministeredwithadopadecar-boxylaseinhibitor(DDI),suchascarbidopaorbenserazide,thepredominantrouteoflevodopame-tabolismisviacatechol-O-methyltransferase(COMT)toform3-O-methyldopa(3-OMD).Entaca-poneisaselective,reversible,peripherallyactingCOMTinhibitorthatincreasesthelevodopahalf-lifeandconcentrationareaunderthecurve(AUC).1Thismakesmorelevodopaavailablefortransportintothebrainoveralongertime.When200mgentacaponeisadministeredwithlevodopa/carbidopaimmediatere-lease(IR),thelevodopaAUCisincreasedby35–40%andthehalf-lifeis