ENTACAPONE tablet, film coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

ENTACAPONE (UNII: 4975G9NM6T) (ENTACAPONE - UNII:4975G9NM6T)

Available from:

Aphena Pharma Solutions - Tennessee, LLC

INN (International Name):

ENTACAPONE

Composition:

ENTACAPONE 200 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Entacapone Tablets 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' 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.

Product summary:

Entacapone Tablets are supplied as 200 mg film-coated tablets for oral administration. The oval-shaped tablets are brownish-orange, unscored and embossed "W 781" on one side. Tablets are provided in HDPE containers as follows:             Bottle of 100 tablets   NDC 64679-781-02             Bottle of 500 tablets   NDC 64679-781-03 Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). [See USP Controlled Room Temperature.] Manufactured by: Orion Corporation ORION PHARMA Orionintie 1, FIN-02200 Espoo, Finland. Distributed by: Wockhardt USA LLC. 20 Waterview Blvd. Parsippany, NJ 07054 USA. Rev. July 17, 2014

Authorization status:

New Drug Application

Summary of Product characteristics

ENTACAPONE- ENTACAPONE TABLET, FILM COATED
APHENA PHARMA SOLUTIONS - TENNESSEE, LLC
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ENTACAPONE TABLETS
RX ONLY
PRESCRIBING INFORMATION
DESCRIPTION
Entacapone is available as tablets containing 200 mg entacapone.
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
empirical formula is C
H N O and
its structural formula is:
The inactive ingredients of the Entacapone Tablets are
microcrystalline cellulose, mannitol,
croscarmellose sodium, hydrogenated vegetable oil, hydroxypropyl
methylcellulose, polysorbate 80,
glycerol 85%, sucrose, magnesium stearate, yellow iron oxide, red iron
oxide, 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.
The mechanism of action of entacapone is believed to be through its
ability to inhibit COM