Entacapone (entacapone)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Entacapone is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT); concomitant administration of entacapone with levodopa and a decarboxylase inhibitor (e.g., carbidopa) results in increased and more sustained plasma levodopa concentrations compared with administration of levodopa and a decarboxylase inhibitor.
Entacapone is a selective and reversible inhibitor of COMT that is structurally and pharmacologically related to tolcapone. The drugs are nitrocatechols and are chemically and pharmacologically unrelated to other currently available antiparkinsonian agents (e.g., levodopa, carbidopa, dopamine-receptor agonists, selective MAO-B inhibitors). However, unlike tolcapone, entacapone has not been associated with hepatotoxicity (e.g., drug-induced hepatitis, fatal liver failure).
In humans, entacapone inhibits the COMT enzyme in peripheral tissues. The effects of the drug on central COMT activity in humans have not been studied. For information on COMT, see Pharmacology in Tolcapone 28:36.12.
Concomitant administration of entacapone with levodopa and a decarboxylase inhibitor (e.g., carbidopa) results in increased and more sustained plasma levodopa concentrations compared with administration of levodopa and a decarboxylase inhibitor. Sustained levodopa concentrations presumably result in more consistent dopaminergic stimulation, resulting in greater reduction in the manifestations of parkinson disease. Entacapone lacks antiparkinsonian activity when administered alone.
Entacapone is almost completely metabolized prior to excretion with only 0.2% of a dose excreted unchanged in urine. The main metabolic pathway is isomerization followed by glucuronidation to an inactive conjugate. Biliary excretion apparently is the principal route of elimination of the drug and its metabolites.
USES: This medication is used with other medications (levodopa/carbidopa) to treat Parkinson's disease. Entacapone belongs to a class of drugs known as COMT inhibitors. Many people taking levodopa for Parkinson's have problems with the effects of the levodopa wearing off between scheduled doses, causing symptoms to return or worsen.
Entacapone blocks a certain natural substance (COMT enzyme) that breaks down the levodopa in the body. This effect allows the levodopa to last longer in the system so that it doesn't wear off before the next dose.
Generic name: entacapone
Pronunciation: (en-TACK-up-own)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Entacapone
Indications
The following indications are listed for Entacapone:
- Idiopathic Parkinsonism
Also known as: Paralysis Agitans, Primary Parkinson's Disease.
Dosing
The recommended dosage of entacapone is 200 mg administered with each levodopa-carbidopa dose up to a maximum of 8 times daily (1.6 g daily). Clinical experience with dosages exceeding 1.6 g daily is limited.
To optimize patient response, reductions in the daily levodopa dosage or frequency of administration may be necessary. In clinical studies, most patients (58%) who were receiving 800 mg or more of levodopa daily or who had moderate or severe dyskinesias before initiating entacapone therapy required a reduction in levodopa dosage; the average reduction in daily levodopa dosage was about 25%.
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Known hypersensitivity to entacapone or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in 1% or more of patients receiving entacapone and more frequently than placebo include dyskinesia, nausea, hyperkinesia, diarrhea, urine discoloration, hypokinesia, dizziness, abdominal pain, constipation, fatigue, vomiting, back pain, dry mouth, dyspnea, increased sweating, anxiety, somnolence, dyspepsia, flatulence, purpura, asthenia, taste perversion, agitation, gastritis, GI disorder, and bacterial infection.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and effectiveness of entacapone have not been established in pediatric patients.
In animal reproduction studies in which entacapone was administered to pregnant rats and rabbits during the period of organogenesis, no evidence of teratogenicity was observed; however, there was an increased frequency of abortions, resorptions, decreased fetal weights, and fetal variations. When the drug was administered to female rats prior to mating and during early gestation, an increased incidence of fetal eye anomalies was observed; exposure to the drug during later stages of gestation and throughout lactation produced no evidence of developmental impairment in the offspring.
Entacapone has not been studied in pregnant women; therefore, the drug should be used during pregnancy only if the potential benefits justify the potential risks to the fetus.
Entacapone is distributed into milk in rats; caution is advised if the drug is used in nursing women.
No substantial differences in safety or pharmacokinetics of entacapone have been observed relative to younger adults.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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