Correlation Engine 2.0
Clear Search sequence regions
Bookmark Forward

QuickView for Entacapone (compound)

Name: entacapone
PubChem Compound ID: 4659568
Molecular formula: C14H15N3O5
Molecular weight: 305.286 g/mol
Name: entacapone
Name (isomeric): DB00494
Drug Type: small molecule
Entacapone [Usan:Inn]; Entacaponum [INN-Latin]; Entacapona [INN-Spanish]
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".
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 ...
show more »
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...
show more »
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:
Take without regard to meals.
Drug interaction:
NorepinephrineEntacapone increases the effect and toxicity of the sympathomimetic, norepinephrine.
TranylcypromineAdditive inhibition of endogenous catecholamine metabolism may increase the therapeutic/adverse effects of both agents. Concomitant therapy should be avoided.
TriprolidineThe CNS depressants, Triprolidine and Entacapone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
PhenelzinePossible hypertensive crisis with this combination
IsoproterenolEntacapone increases the effect and toxicity of the sympathomimetic, isoproterenol.
show more »