Country: United States
Language: English
Source: NLM (National Library of Medicine)
ENTACAPONE (UNII: 4975G9NM6T) (ENTACAPONE - UNII:4975G9NM6T)
Aurobindo Pharma Limited
ENTACAPONE
ENTACAPONE 200 mg
ORAL
PRESCRIPTION DRUG
Entacapone tablets, USP are indicated as an adjunct to levodopa and carbidopa to treat end-of-dose “wearing-off” in patients with Parkinson’s disease (see CLINICAL PHARMACOLOGY, Clinical Studies ). Entacapone tablets, USP effectiveness has not been systematically evaluated in patients with Parkinson’s disease who do not experience end-of-dose “wearing-off”. Entacapone tablets are contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients. Entacapone is not a controlled substance. Animal studies to evaluate the drug abuse and potential dependence have not been conducted. Although clinical studies have not revealed any evidence of the potential for abuse, tolerance or physical dependence, systematic studies in humans designed to evaluate these effects have not been performed.
Entacapone Tablets USP, 200 mg are light brownish-orange colored, film-coated, oval shaped tablets debossed “Y 16” on one side and plain on other side. Bottles of 100 NDC 65862-654-01 Bottles of 1,000 NDC 65862-654-99 Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Distributed by: Aurobindo Pharma USA, Inc. 279 Princeton-Hightstown Road East Windsor, NJ 08520 Manufactured by: Aurobindo Pharma Limited Hyderabad-500 032, India Revised: 05/2023
Abbreviated New Drug Application
ENTACAPONE - ENTACAPONE TABLET, FILM COATED AUROBINDO PHARMA LIMITED ---------- ENTACAPONE TABLETS, USP RX ONLY PRESCRIBING INFORMATION DESCRIPTION Entacapone is available as tablets containing 200 mg entacapone USP. Entacapone is an inhibitor of catechol-_O_-methyltransferase (COMT), used in the treatment of Parkinson’s disease as an adjunct to levodopa and carbidopa therapy. It is a nitrocatechol-structured compound with a relative molecular mass of 305.29. The chemical name of entacapone is (E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N- diethyl-2-propenamide. Its molecular formula is C H N O and its structural formula is: The inactive ingredients of the entacapone tablets, USP are croscarmellose sodium, glycerin, hydrogenated vegetable oil, hypromellose, iron oxide red, iron oxide yellow, lactose monohydrate, magnesium stearate, mannitol, microcrystalline cellulose, polysorbate, sodium starch glycolate, sucrose, and titanium dioxide. CLINICAL PHARMACOLOGY MECHANISM OF ACTION Entacapone is a selective and reversible inhibitor of COMT. In mammals, COMT is distributed throughout various organs with the highest activities in the liver and kidney. COMT also occurs in the heart, lung, smooth and skeletal muscles, intestinal tract, reproductive organs, various glands, adipose tissue, skin, blood cells, and neuronal tissues, especially in glial cells. COMT catalyzes the transfer of the methyl group of S-adenosyl-L-methionine to the phenolic group of substrates that contain a catechol structure. Physiological substrates of COMT include dopa, catecholamines (dopamine, norepinephrine, and epinephrine) and their hydroxylated metabolites. The function of COMT is the elimination of biologically active catechols and some other hydroxylated metabolites. In the presence of a decarboxylase inhibitor, COMT becomes the major metabolizing enzyme for levodopa, catalyzing the metabolism to 3-methoxy-4- hydroxy-L-phenylalanine (3-OMD) in the brain and periphery. 14 15 3 5 The mechanism of action of entacapone is believed to be th Read the complete document