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:

AvPAK

INN (International Name):

ENTACAPONE

Composition:

ENTACAPONE 200 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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.

Product summary:

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.                      NDC 50268-295-15 (10 tablets per card,  5 cards per carton). Dispensed in Unit Dose Package.  For Institutional Use Only. Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]  Manufactured for: AvKARE, Inc. Pulaski, TN  38478 Mfg. Rev. 04/16 AV 11/16 (P) AvPAK

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ENTACAPONE- ENTACAPONE TABLET, FILM COATED
AVPAK
----------
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-
14
15
3
5
hydroxy-L-phenylalanine (3-OMD) in the brain and periphery.
The mechanism of action of entacapone is believed to be through its
ability t