title: [Entacapone: is it useful as complimentary treatment with levodopa?].
abstract: Entacapone (Comtan) is a potent, selective inhibitor of peripheral catechol-O-methyltransferase (COMT) with therapeutic potential as an adjuvant to levodopa therapy in patients with Parkinson's disease. Entacapone decreases peripheral conversion of levodopa to 3-O-methyldopa increasing central extracellular levodopa and consequently striatal dopamine concentrations. At doses of 200 mg 2 to 10 times daily coadministered with levodopa/carbidopa or levodopa/benserazide entacapone may increase the duration of clinical response both after the first single dose and after repeated dosing in patients with end-of-dose fluctuations. At this dosage, it has a time to peak-plasma concentration of 1.2 hours and an elimination half life of 3.4 hours. In two multicentric, long-term (approximately 6 month), randomized and placebo-controlled studies, the duration of 'on' time was increased and the duration of 'off time' was decreased in patients who received adjunctive entacapone therapy. Moreover, patients randomized to entacapone reduced their levodopa requirements. In these and other phase III studies, entacapone was generally well tolerated, with few reported adverse events, mainly dyskinesias and gastrointestinal disorders. The dyskinesias were generally well controlled by decreasing the mean daily levodopa dose. Entacapone appears as a clinically significant and beneficial adjunct to levodopa therapy in Parkinson's disease patients with end-of-dose fluctuations.
authors.affiliation: Hospital La Fe, Valencia.
authors.forename: J A
authors.initials: JA
authors.lastname: Burguera
authors.forename: F
authors.initials: F
authors.lastname: Grandas
authors.forename: J F
authors.initials: JF
authors.lastname: Horga de la Parte
authors.forename: R
authors.initials: R
authors.lastname: Luquin
authors.forename: F
authors.initials: F
authors.lastname: Martí
authors.forename: J
authors.initials: J
authors.lastname: Matías-Guiu
authors.forename: J A
authors.initials: JA
authors.lastname: Obeso
authors.forename: J
authors.initials: J
authors.lastname: Kulisevsky
mesh_terms: D000978:Antiparkinson Agents / Q000627:therapeutic use*; D002396:Catechols / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D004359:Drug Therapy, Combination; D006801:Humans; D007980:Levodopa / Q000627:therapeutic use*; D009570:Nitriles; D010300:Parkinson Disease / Q000188:drug therapy*; D013030:Spain
chemical_list: D000978:Antiparkinson Agents; D002396:Catechols; D009570:Nitriles; D007980:Levodopa; C071192:entacapone
vernacular_title: Entacapona: es útil como tratamiento complementario a la levodopa?