CABERGOLINE tablet

البلد: الولايات المتحدة

اللغة: الإنجليزية

المصدر: NLM (National Library of Medicine)

العنصر النشط:

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

متاح من:

A-S Medication Solutions

طريقة التعاطي:

ORAL

نوع الوصفة الطبية :

PRESCRIPTION DRUG

الخصائص العلاجية:

Cabergoline tablets are indicated for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas. Cabergoline tablets are contraindicated in patients with: - Uncontrolled hypertension or known hypersensitivity to ergot derivatives. - History of cardiac valvular disorders, as suggested by anatomical evidence of valvulopathy of any valve, determined by pre-treatment evaluation including echocardiographic demonstration of valve leaflet thickening, valve restriction, or mixed valve restriction-stenosis (see WARNINGS ). - History of pulmonary, pericardial, or retroperitoneal fibrotic disorders (see WARNINGS ).

ملخص المنتج:

Product: 50090-3157 NDC: 50090-3157-0 8 TABLET in a BOTTLE / 1 in a CARTON

الوضع إذن:

Abbreviated New Drug Application

خصائص المنتج

CABERGOLINE- CABERGOLINE TABLET
A-S MEDICATION SOLUTIONS
----------
CABERGOLINE TABLETS USP
RX ONLY
DESCRIPTION
Cabergoline tablets USP contain cabergoline, USP, a dopamine receptor
agonist. The
chemical name for cabergoline, USP is
1-[(6-allylergolin-8β-yl)-carbonyl]-1-[3-
(dimethylamino)propyl]-3-ethylurea and has the following structural
formula:
C
H
N O M.W. 451.6
Cabergoline, USP is a 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 cabergoline tablet USP, for oral administration, contains 0.5 mg
of cabergoline,
USP and has the following inactive ingredients: anhydrous lactose and
leucine.
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
26
37
5
2
2
1
1
2
1
2
= 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 mg twice weekly
respectively.
In the 8-week, double-blind period of the comparative trial with
bromocriptine
(c