Name: | entacapone |
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PubChem Compound ID: | 4659568 |
Molecular formula: | C14H15N3O5 |
Molecular weight: | 305.286 g/mol |
Name: | entacapone |
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Name (isomeric): | DB00494 |
Drug Type: | small molecule |
Synonyms: |
Entacapone [Usan:Inn]; Entacaponum [INN-Latin]; Entacapona [INN-Spanish]
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Brand: | Comtan, Comtess |
Category: | Antidyskinetics, Antiparkinson Agents, Enzyme Inhibitors, Central Nervous System Agents |
CAS number: | 130929-57-6 |
Indication: | Used as an adjunct to levodopa / carbidopa in the symptomatic treatment of patients with idiopathic Parkinson's Disease who experience the signs and symptoms of end-of-dose "wearing-off". |
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Pharmacology: |
Entacapone is structurally and pharmacologically related to tolcapone, but unlike tolcapone, is not associated with hepatotoxicity. Entacapone is used in the treatment of Parkinson’s disease as an adjunct to levodopa/carbidopa therapy. Entacapone is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT). In mammals, COMT ...
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Mechanism of Action: |
The mechanism of action of entacapone is believed to be through its ability to inhibit COMT in peripheral tissues, altering the plasma pharmacokinetics of levodopa. When entacapone is given in conjunction with levodopa and an aromatic amino acid decarboxylase inhibitor, such as carbidopa, plasma levels of levodopa are greater and more sustained tha...
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Absorption: | Entacapone is rapidly absorbed (approximately 1 hour). The absolute bioavailability following oral administration is 35%. |
Protein binding: | 98% (bind to serum albumin) |
Biotransformation: | Metabolized via isomerization to the cis-isomer, followed by direct glucuronidation of the parent and cis-isomer. |
Route of elimination: | Entacapone is almost completely metabolized prior to excretion, with only a very small amount (0.2% of dose) found unchanged in urine. As only about 10% of the entacapone dose is excreted in urine as parent compound and conjugated glucuronide, biliary excretion appears to be the major route of excretion of this drug. |
Half Life: | 0.4-0.7 hour |
Clearance: | 850 mL/min |
Toxicity: | Side effect include increase the occurrence of orthostatic hypotension, severe rhabdomyolysis, dyskinesia, hallucinations, hyperkinesia, hypokinesia, dizziness, fatigu,e gastrointestinal effects including abdominal pain constipation diarrhea nausea |
Affected organisms: | Humans and other mammals |
Food interaction: |
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Drug interaction: |
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