Entacapone

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Comtan, Comtess; Belgium: Comtan; Bulgaria: Comtan; Cyprus: Comtan; Czech Republic: Comtan, Comtess; Denmark: Comtan, Comtess; Estonia: Comtan, Comtess; Finland: Comtess; France: Comtan; Germany: Comtan, Comtess; Greece: Comtan, Comtess; Hungary: Comtan, Comtess; Ireland: Comtan, Comtess; Italy: Comtan; Latvia: Comtan, Comtess; Lithuania: Comtan, Comtess; Netherlands: Comtan, Comtess; Portugal: Comtan, Comtess; Romania: Comtan, Comtess; Slovakia: Comtan, Comtess; Spain: Comtan; Sweden: Comtan, Comtess; UK: Comtess.

North America

Canada: Comtan; USA: Comtan.

Latin America

Argentina: Comtan; Brazil: Comtan; Mexico: Comtan.

Asia

Japan: Comtan.

Drug combinations

Entacapone, Carbidopa, and Levodopa

Chemistry

Entacapone: C~14~H~15~N~3~O~5~. Mw: 305.29. E-α-Cyano-N,N-diethyl-3,4-dihydroxy-5-nitrocinnamamide. CAS-130929-57-6 (1997).

Pharmacologic Category

Antiparkinsonian Agents; Catechol-O-Methyltransferase Inhibitors. (ATC-Code: N04BX02).

Mechanism of action

A selective and reversible inhibitor of catechol-O-methyltransferase (COMT). When entacapone is taken with levodopa, the pharmacokinetics are altered, resulting in more sustained levodopa serum levels compared to levodopa taken alone.

Therapeutic use

Used as an adjunct to levodopa-carbidopa in the symptomatic treatment of idiopathic parkinsonian syndrome in patients who experience manifestations of end-of-dose «wearing-off».

Pregnancy and lactiation implications

Not recommended for use during pregnancy. Use with caution during lactation.

Unlabeled use

Contraindications

Hypersensitivity to entacapone or any component of the formulation.

Warnings and precautions

Patients ordinarily should not be treated concomitantly with entacapone and a nonselective MAOI (entacapone can be used concomitantly with a selective MAO-B inhibitor (e.g. selegiline)). Concomitant use of entacapone and drugs known to be metabolized by COMT may result in increased heart rate, arrhythmias, and excessive changes in blood pressure. May cause orthostatic hypotension and syncope when administered with levodopa/carbidopa (use with caution in patients at risk of hypotension (such as those receiving antihypertensive drugs) or where transient hypotensive episodes would be poorly tolerated (cardiovascular disease or cerebrovascular disease)). Diarrhea might occur (use with caution in lower GI disease or increased risk of dehydration (severe diarrhea rarely occurs)). May cause hallucinations. Entacapone may potentiate the adverse dopaminergic effects of levodopa and may cause or exacerbate dyskinesias. Severe rhabdomyolysis reported rarely. Retroperitoneal fibrosis, pulmonary infiltrates, pleural effusion, and thickening of the pleura reported in a few patients treated with ergot-derivative dopamine receptor agonists (entacapone may induce similar pulmonary changes). Use with caution in biliary obstruction, and in hepatic impairment or severe renal impairment. Entacapone, in conjunction with other drug therapy which alters brain biogenic amine concentrations (e.g. MAOIs, SSRIs), has been associated with a syndrome resembling neuroleptic malignant syndrome (hyperpyrexia and confusion) on abrupt withdrawal or dosage reduction (avoid abrupt withdrawal of therapy).

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