Entacapone

Indications
 Oral
Adjunct to levodopa treatment in Parkinson's disease
Adult: 200 mg with each levodopa/dopa decarboxylase inhibitor dose. Max: 200 mg 10 times daily.
Contraindications
 History of neuroleptic malignant syndrome and nontraumatic rhabdomyolysis. Phaeochromocytoma. Hepatic impairment.
Warnings / Precautions
 Levodopa-induced orthostatic hypotension may be aggravated. Abrupt withdrawal. Concomitant use with a selective MAO-A and MAO-B inhibitor, or concomitant use with a selective MAO-A plus a selective MAO-B inhibitor. Biliary obstruction. Impairs ability to drive and operate machinery. Pregnancy and lactation. Children and elderly.
Adverse Reactions
 Dyskinesia, GI symptoms, reddish brown urine discoloration, fatigue, insomnia, paroniria, confusion, hallucinations, dizziness, orthostatic/postural hypotension, vertigo, headache, leg cramps, hyperkinesia, tremor and increased sweating.
Drug Interactions
 Drugs metabolised by COMT e.g. adrenaline, apomorphine, dobutamine, dopamine, isoprenaline, methyldopa, noradrenaline and remiterol. Iron preparations and levodopa. Avoid ethanol.
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Lab Interactions
 Slight decrease in Hb, erythrocyte count and haematocrit. Increases in liver enzymes.
Food Interactions
 Avoid ethanol.
Mechanism of Actions
 Entacapone is a selective, reversible, peripheral inhibitor of COMT, an enzyme involved in the metabolism of dopamine and levodopa. It is used in patients with Parkinson's disease and "end-of-dose" motor fluctuations that cannot be stabilised on levodopa combinations alone.
Absorption: Plasma concentrations peak about 1 hr after oral doses. Bioavailability: About 35%.
Distribution: 98% bound to plasma proteins.
Excretion: Mainly excreted in the faeces; about 10-20% being excreted in the urine, mainly as glucuronide conjugates.
Administration
 May be taken with or without food.
ATC Classification
 N04BX02 - entacapone ; Belongs to the class of other dopaminergic agents used in the management of Parkinson's disease.
Available As
  • Entacapone 10 mg

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