Entacapone

• Antiparkinson Agents
• Antidyskinetics
• Central Nervous System Agents
• ATC:N04BX02

• Comtan
• Entacapona [Inn-Spanish]
• Entacapone [Usan:Inn]
• Entacaponum [Inn-Latin]

No information avaliable

C₁₄H₁₅N₃O₅

http://www.rxlist.com/cgi/generic3/entac.htm

Entacapone FDA

No hay información disponible

305.286 g/mol

No information avaliable

No hay información disponible

Solid

0.53

Tableta

Para que una combinación con levodopa / carbidopa para tratar a pacientes con enfermedad de Parkinson idiopática que presentan los signos y síntomas de fin de dosis "wearing-off".

La entacapona se utiliza en el tratamiento de la enfermedad de Parkinson como coadyuvante al tratamiento con levodopa / carbidopa. La entacapona es un inhibidor selectivo y reversible de la catecol-O-metiltransferasa (COMT). En los mamíferos, la COMT se distribuye a través los diversos órganos con mayor actividad en el hígado y el riñón. COMT también ocurre en el corazón, pulmón, músculo liso y esquelético, tracto intestinal, la reproducción órganos, las glándulas diferentes, el tejido adiposo, piel, células de la sangre y los tejidos neuronales, especialmente en las células gliales. COMT cataliza la transferencia del grupo metilo de la S-adenosil-L-metionina en el grupo fenólico de sustratos que contienen una estructura catecol. Sustratos fisiológicos de COMT son dopa, las catecolaminas (dopamina, norepinefrina y epinefrina) y sus metabolitos hidroxilados. La función de la COMT es la eliminación de los catecoles biológicamente activos y algunos otros metabolitos hidroxilados. En presencia de un inhibidor de la descarboxilasa, la COMT se convierte en la principal enzima para metabolizar la levodopa, , Que cataliza el metabolismo de 3-metoxi-4-hidroxi-L-fenilalanina (3-OMD) en el cerebro y la periferia.

La entacapona se absorbe rápidamente (aproximadamente 1 hora). La biodisponibilidad absoluta tras la administración oral es del 35%.

Efectos secundarios incluyen aumentar la aparición de hipotensión ortostática, rabdomiolisis severa, discinesia, alucinaciones, hipercinesia, hipocinesia, mareos, fatigu, efectos gastrointestinales, como náuseas e diarrea dolor abdominal estreñimiento

Patients should be instructed to take C.M.A. only as prescribed.

Patients should be informed that hallucinations can occur.

Patients should be advised that they may develop postural (orthostatic) hypotension with or without symptoms such as dizziness, nausea, syncope, and sweating. Hypotension may occur more frequently during initial therapy. Accordingly, patients should be cautioned against rising rapidly after sitting or lying down, especially if they have been doing so for prolonged periods, and especially at the initiation of treatment with COMTAN.

Patients should be advised that they should neither drive a car nor operate other complex machinery until they have gained sufficient experience on C.M.A. to gauge whether or not it affects their mental and/or motor performance adversely. Because of the possible additive sedative effects, caution should be used when patients are taking other CNS depressants in combination with COMTAN.

Patients should be informed that nausea may occur, especially at the initiation of treatment with COMTAN.

Patients should be advised of the possibility of an increase in dyskinesia.

Patients should be advised that treatment with entacapone may cause a change in the color of their urine (a brownish orange discoloration) that is not clinically relevant. In controlled trials, 10% of patients treated with C.M.A. reported urine discoloration compared to 0% of placebo patients.

Although C.M.A. has not been shown to be teratogenic in animals, it is always given in conjunction with levodopa/carbidopa, which is known to cause visceral and skeletal malformations in the rabbit. Accordingly, patients should be advised to notify their physicians if they become pregnant or intend to become pregnant during therapy.

Entacapone is excreted into maternal milk in rats. Because of the possibility that entacapone may be excreted into human maternal milk, patients should be advised to notify their physicians if they intend to breastfeed or are breastfeeding an infant.

Humanos y otros mamíferos