May interfere w/ metabolism of other drugs metabolised by COMT (e.g. rimiterole). May aggravate levodopa-induced orthostatic hypotension. Risk of dopaminergic effects w/ dopamine agonists (e.g. bromocriptine), selegiline, amantadine. May form chelates w/ Fe in the GI tract. Additive sedative effects w/ other CNS depressants. Potentially Fatal: Concomitant use w/ non-selective MAOIs (e.g. phenelzine) may result in inhibition of principal pathways in the metabolism of catecholamines.
May potentiate the sedative effect of alcohol.
Description: Entacapone decreases the metabolic loss of levodopa to 3-O-methyldopa (3-OMD) through inhibition of COMT enzyme leading to an increased levodopa concentration, thus, extending the duration and effect in the brain. Pharmacokinetics: Absorption: Rapidly absorbed from the GI tract. Bioavailability: 29-46%. Time to peak plasma concentration: Approx 1 hr. Distribution: Plasma protein binding: Approx 98% (primarily to albumin). Metabolism: Undergoes extensive first-pass metabolism; isomerisation to the cis-isomer, followed by direct glucuronidation of the parent and cis-isomer. Excretion: Mainly via faeces (10%); urine (approx 10-20%, as glucuronide conjugates). Elimination half-life: Approx 1.6-3.4 hr.
N04BX02 - entacapone ; Belongs to the class of other dopaminergic agents used in the management of Parkinson's disease.
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