SANDOZ ENTACAPONE TABLET

Страна: Канада

мова: англійська

Джерело: Health Canada

Активний інгредієнт:

ENTACAPONE

Доступна з:

SANDOZ CANADA INCORPORATED

Код атс:

N04BX02

ІПН (Міжнародна Ім'я):

ENTACAPONE

Дозування:

200MG

Фармацевтична форма:

TABLET

Склад:

ENTACAPONE 200MG

Адміністрація маршрут:

ORAL

Одиниць в упаковці:

100

Тип рецепту:

Prescription

Терапевтична области:

CATECHOL-O-METHYLTRANSFERASE (COMT) INHIBITORS

Огляд продуктів:

Active ingredient group (AIG) number: 0143623001; AHFS:

Статус Авторизація:

APPROVED

Дата Авторизація:

2012-03-30

Характеристики продукта

_Sandoz Entacapone Page 1 of 49 _
PRODUCT MONOGRAPH
PR
SANDOZ ENTACAPONE
(entacapone)
tablets, 200 mg
Adjunct to levodopa and DDC inhibitor / COMT-Inhibitor
Sandoz Canada Inc.
Date of Revision:
145 Jules-Leger St.
January 21, 2014
Boucherville, QC
J4B 7K8
Control Number: 171219
_Sandoz Entacapone Page 2 of 49 _
PR
SANDOZ ENTACAPONE
(ENTACAPONE)
tablets, 200 mg
THERAPEUTIC CLASSIFICATION
Adjunct to levodopa and DDC inhibitor / COMT-Inhibitor
ACTION AND CLINICAL PHARMACOLOGY
Entacapone is a reversible, selective and mainly peripherally acting
inhibitor of catechol-O-
methyltransferase (COMT). Entacapone has no antiparkinsonian effect of
its own and is
designed for concomitant administration with levodopa preparations.
COMT catalyzes the transfer of the methyl group of
S-adenosyl-L-methionine to the phenolic
group of substrates that contain a cathecol structure. Physiological
substrates of COMT include
dopa, catecholamines (dopamine, norepinephrine, epinephrine) and their
hydroxylated
metabolites. In the presence of a dopa decarboxylase (DDC) inhibitor,
COMT becomes the
major enzyme which is responsible for the metabolism of levodopa to
3-methoxy-4-hydroxy-l-
phenylalanine (3-OMD).
The mechanism of action of entacapone is believed to be related to its
ability to inhibit COMT
and thereby alter the plasma pharmacokinetics of levodopa. When
administered with levodopa
and a DDC inhibitor (carbidopa or benserazide), entacapone
decreases the degradation of
levodopa in the peripheral tissues further by inhibiting the
metabolism of levodopa to 3-OMD
through the COMT pathway. This leads to more sustained plasma
concentrations of levodopa. It
is believed that at a given frequency of levodopa administration,
these more sustained plasma
levels of levodopa result in more constant dopaminergic stimulation in
the brain leading to
greater effects on the signs and symptoms of Parkinson’s disease.
The higher levodopa levels
also lead to increased levodopa adverse effects, sometimes requiring a
decrease in the dose of
levodopa.
In a