Entacapone

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Entacapone
Systematic (IUPAC) name
(2E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide
Identifiers
CAS number 130929-57-6
ATC code N04BX02
PubChem 5281081
DrugBank APRD00416
Chemical data
Formula C14H15N3O5 
Mol. mass 305.286 g/mol
Synonyms
  • (E)-a-cyano-N,N-diethyl-3,4-dihydroxy-5-nitrocinnamamide
  • (E)-2-cyano-N,N-diethyl-3-(3,4-dihydroxy-5-(nitrophenyl)acrylamide
Pharmacokinetic data
Bioavailability 35%
Protein binding 98% (binds to serum albumin)
Metabolism Hepatic
Half life 0.4-0.7 hour
Excretion 90% feces, 10% urine
Therapeutic considerations
Pregnancy cat.

C(US)
Legal status

Prescription only, unscheduled (USA)
Routes Oral

Entacapone (INN) (pronounced /ˌɛntəkəˈpoʊn/, /ɛnˈtækəpoʊn/) is a catechol-O-methyl transferase inhibitor for the treatment of Parkinson's disease. When administered in conjunction with dopaminergic agents such as L-DOPA, entacapone increases the bioavailability of these compounds by facilitating their passage across the blood-brain barrier.

It is a member of the class of nitrocatechols.

The most frequent undesirable effects caused by entacapone relate to the increased effects of L-DOPA, such as involuntary movements (dyskinesias).These occur most frequently at the beginning of entacapone treatment. Others common side effects are gastrointestinal problems, including diarrhoea, nausea and abdominal pains. The substance may cause urine to turn reddish-brown. This is a harmless side effect and is not a cause for concern. In studies with entacapone, some people have reported experiencing a dry mouth.

Entacapone is developed by Orion Pharma and marketed by Novartis under the trade names Comtan and Stalevo in the United States.

Stalevo is a medication that contains carbidopa, levodopa (active ingredients in Sinemet), and entacapone (active ingredient in Comtan).

External links

  • [1] (fda website)
  • Comtan (manufacturer's website)
  • Stalevo (manufacturer's website)
v • d • e
Antiparkinson drugs: dopaminergic agents (N04B)
Dopa and derivatives
Adamantane derivatives
Dopamine agonists
MAOIs (B)
COMT inhibitors
Entacapone • Tolcapone
Other

Wikipedia content modification information:

  • This page was last modified on 1 October 2008, at 09:15.

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