Entacapone
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Entacapone
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| Systematic (IUPAC) name | |
| 2-cyano-3- (5-dihydroxyamino-3, 4-dioxo-1-cyclohexa-1,5-dienyl)- N,N-diethyl-prop-2-enamide | |
| Identifiers | |
| CAS number | |
| ATC code | N04 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C14H15N3O5 |
| Mol. mass | 305.286 g/mol |
| 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).
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