CABERGOLINE tablet

Country: Сједињене Америчке Државе

Језик: Енглески

Извор: NLM (National Library of Medicine)

Активни састојак:

CABERGOLINE (UNII: LL60K9J05T) (CABERGOLINE - UNII:LL60K9J05T)

Доступно од:

Apotex Corp.

INN (Међународно име):

CABERGOLINE

Састав:

CABERGOLINE 0.5 mg

Тип рецептора:

PRESCRIPTION DRUG

Статус ауторизације:

Abbreviated New Drug Application

Карактеристике производа

CABERGOLINE- CABERGOLINE TABLET
APOTEX CORP.
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CABERGOLINE TABLETS 0.5 MG
DESCRIPTION
Cabergoline tablets contain cabergoline, a dopamine receptor agonist.
The chemical name for
cabergoline is
1-[(6-allylergolin-8ß-yl)-carbonyl]-1-[3-(dimethylamino)
propyl]-3-ethylurea. Its
molecular formula is C
H N O , and its molecular weight is 451.62. The structural formula is
as
follows:
The drug substance used in cabergoline tablet is the amorphous form of
cabergoline. Cabergoline is a
cream to white powder soluble in ethyl alcohol, chloroform, and N,
N-dimethylformamide (DMF);
slightly soluble in 0.1N hydrochloric acid; very slightly soluble in
n-hexane; and insoluble in water.
Each tablet, for oral administration, contain 0.5 mg of cabergoline.
Inactive ingredients consist of
lactose anhydrous, leucine, and magnesium stearate.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
The secretion of prolactin by the anterior pituitary is mainly under
hypothalamic inhibitory control,
likely exerted through release of dopamine by tuberoinfundibular
neurons. Cabergoline is a long-acting
dopamine receptor agonist with a high affinity for D receptors.
Results of _in vitro_ studies demonstrate
that cabergoline exerts a direct inhibitory effect on the secretion of
prolactin by rat pituitary
lactotrophs. Cabergoline decreased serum prolactin levels in
reserpinized rats. Receptor-binding
studies indicate that cabergoline has low affinity for dopamine D , α
- and α -adrenergic, and 5-HT -
and 5-HT -serotonin receptors.
CLINICAL STUDIES
The prolactin-lowering efficacy of cabergoline was demonstrated in
hyperprolactinemic women in two
randomized, double-blind, comparative studies, one with placebo and
the other with bromocriptine. In
the placebo-controlled study (placebo n=20; cabergoline n=168),
cabergoline produced a dose-related
decrease in serum prolactin levels with prolactin normalized after 4
weeks of treatment in 29%, 76%,
74% and 95% of the patients receiving 0.125, 0.5, 0.75, and 1.0 mg
twice weekly respectively.
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