Entacapone

Also known as: Entacapona, Entacaponum,

Drug #1712

Entacapone is a peripheral inhibitor of catechol-O-methyl transferase (COMT), an enzyme involved in the metabolism of dopamine and levodopa. It prevents the peripheral breakdown of levodopa, allowing more levodopa to reach the brain. Entacapone is used as an adjunct in combination preparation of levodopa and dopa decarboxylase inhibitors, in patients with Parkinson`s disease who experience end-of-dose deterioration and cannot be stabilised on these combinations.

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Primary Characteristics

Entacapone is also known as Entacapona, Entacaponum, .

It is of Synthetic origin and belongs to COMT Inhibitor.

Molecular Weight: 305.29 · pK_a: 4.5 · Solubility in Water: Insoluble · Non-proprietary name: Entacapone.

Pharmacokinetics

Absorption: Entacapone has an oral bioavailability is 37.5% (±8.5%), pre-systemic (first-pass) metabolism accounts for 92.5% (±2.5%).

Distribution: Entacapone has a volume of distribution is 20L. plasma protein binding is 98%.

Elimination: it is metabolised via liver, plasma half-life is 0.28(0.22-0.34)hr, renal excretion is 10-20%.

Indications

Entacapone is primarily indicated in conditions like Parkinson's disease.

Contraindications

Entacapone is contraindicated in conditions like Phaeochromocytoma, Neuroleptic malignant syndrome, Hepatic impairment, Pregnancy, Breast feeding.

Dosage

Entacapone's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
200 – 200 mg	—	—	PO	200 mg tablet of entacapone should be administered concomitantly with each levodopa/carbidopa dose to a maximum of 10 times daily (200 mg x 10 = 2000 mg per day).
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Entacapone in overdosage may give rise to further complications which include Hallucinations , Hallucinations , Severe illergic reactions, Difficulty in breathing, Tightness in the chest, Severe Pecsistant a watery diarrhoea, Change in the appearance of the mole.

The signs and symptoms that are produced after acute overdosage of Entacapone are CNS disterbance, Severe Psychiatric Problem, Cardiovascular disturbances.

Entacapone is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Colored (reddish-brown) urine, Constipation , Diarrhea, Dizziness, Dry mouth, Dyskinesia , Nausea, Nausea and vomiting, Rarely hepatitis, Vomiting .

Warnings / Precautions

Concurrent levodopa dose may need to be reduced by 10-30%. DRIVING: Drowsiness (include sudden onset of sleep) may affect performance of skilled task; patients who are affected should not drive or undertake potentially dangerous activities.

Interference in Pathology

Entacapone may interfere in the diagnosis of Decreased serum iron concentrations.

Available Brands

Click on a strength to view available brands.

Multi-Ingredient Combinations

Tabs

200 mg

Storage Conditions

Entacapone should be stored .

Drug Classification

1.9.1 — Drugs used in parkinsonism

Manufacturers

Manufacturers of Entacapone in Pakistan:

Obs