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Entacapone

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Entacapone

Entacapone review





Entacapone is a drug classified as a COMT inhibitor (catechol-O-methyl transferase inhibitor). Entacapone belongs to a class of drugs known as nitrocatechols.

Entacapone, which is marketed as Comtan is used as a supplement to levodopa/carbidopa in treating patients diagnosed with idiopathic Parkinson’s disease. These are patients experiencing end-of-dose “wearing off” signs and symptoms.

Entacapone/Comtan is an oral drug that is made available at 200mg per tablet. Each tablet is co-administered with each dose of levodopa/carbidopa up to a maximum of 1600 mg, or 8 times over a day’s length. Administration of entacapone should always be made with levodopa/carbidopa. Comtan has no anti-Parkinsonian effect of its own.

Entacapone/Comtan has been reported to be combined with both immediate and sustained-release levodopa/carbidopa formulations. It has also been reported that entacapone/comtan may be taken with or without food.

Entacapone contains inactive ingredients such as microcrystalline cellulose, croscarmellose sodium, mannitol, hydroxypropyl methylcellulose, hydrogenated vegetable oil, polysorbate 80, sucrose, glycerol 85%, red oxide, titanium dioxide, yellow iron oxide and magnesium stearate.

The most frequently reported and one of the more serious side effects of entacapone administration is somehow related to the increase in L-DOPA effects, such dyskinesias, or involuntary muscle movement. This has been reported to occur more frequently during the onset of entacapone treatment. Another serious side effect reported with entacapone use is hallucinations.

Less alarming side effects include gastrointestinal ailments, such as diarrhea, abdominal pains and feelings of being bloated. Nausea and dizziness have also been reported to occur in some patients, along with a dry mouth. Entacapone is taken orally and broken down by both liver and kidneys, which in turn may cause urine to become red to reddish-brown in color.

Entacapone is contraindicated to patients with hypersensitivity to the drug or its contents. Patients should only take entacapone if prescribed by a physician. Entacapone is to be taken with levodopa/carbidopa doses as it does not have its own anti-Parkinson’s effects.

Caution should be exercised with patients who are taking drugs that may interfere with bilary excretion, intestinal beta-glucoronidase and glucoronidation such as antibiotics like chlorampenicol, riifampicin, and ampicillin, and other drugs such as probenecid and cholestyramine.

Entacapone is not to be taken with a non-selective MAO inhibitor. The MAO inhibitor it may be taken with is selegiline. Drugs metabolized by COMT, such as dopamine, epinephrine, norepinephrine and the like, should be given caution when taking with entacapone as it may cause an increase in the patient’s heart rate, and may also cause excessive blood pressure and erratic heartbeats (arrhythmia).

Patients taking entacapone must be warned that the use of the drug may cause hallucinations, and orthostatic hypotension with or without its known symptoms of nausea, headaches and dizziness. Entacapone users are advised not to drive, perform machinery or other tasks which require focus and attention without sufficient experience in the use of the drug as it may affect a patient’s mental and motor functions.

Prior to the use of entacapone, women must report if they are pregnant or planning to become pregnant. Although entacapone has not been reported to cause any malformation in the fetus, the use of entacapone during pregnancy must always be given extra caution.

Clinical tests on animals show that entacapone is excreted in maternal milk. As there may be a slight possibility that human maternal milk may also excrete entacapone, nursing mothers should inform their physicians if they nursing or plan to breastfeed their infants.

Entacapone has the following structural formula:

Chemical structure of entacapone


• Molecular formula of entacapone is C14H15N3O5
• Chemical IUPAC Name is 2-cyano-3-(5-dihydroxyamino-3,4-dioxo-1-cyclohexa-1, 5-dienyl)-N,N-diethyl-prop-2-enamide
• Molecular weight is 305.286 g/mol
Entacapone available : 200mg tablets

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