Product Information
Registration Status: ActiveCOMTAN TABLET 200mg is approved to be sold in Singapore with effective from 1999-11-29. It is marketed by NOVARTIS (SINGAPORE) PTE LTD, with the registration number of SIN11234P.
This product contains Entacapone 200mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by ORION CORPORATION (ESPOO PLANT) in SLOVENIA, andLek d.d. (Primary and Secondary Packager) in FINLAND.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Entacapone is a selective, reversible catechol-O-methyl transferase (COMT) inhibitor for the treatment of Parkinson's disease. It is a member of the class of nitrocatechols. When administered concomittantly with levodopa and a decarboxylase inhibitor (e.g., carbidopa), increased and more sustained plasma levodopa concentrations are reached as compared to the administration of levodopa and a decarboxylase inhibitor.
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".
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 than after administration of levodopa and an aromatic amino acid decarboxylase inhibitor alone. It is believed that at a given frequency of levodopa administration, these more sustained plasma levels of levodopa result in more constant dopaminergic stimulation in the brain, leading to a greater reduction in the manifestations of parkinsonian syndrome.
Pharmacokinetics
- Absorption
- Entacapone is rapidly absorbed (approximately 1 hour). The absolute bioavailability following oral administration is 35%.
- Distribution
- * 20 L
- Metabolism
- Metabolized via isomerization to the cis-isomer, followed by direct glucuronidation of the parent and cis-isomer.
- Elimination
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
Active Ingredient/Synonyms
(e)-alpha-Cyano-N,N-diethyl-3,4-dihydroxy-5-nitrocinnamamide | Entacapona | Entacapone | Entacaponum | N,N-Diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl) acrylamide | Entacapone |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.