CABERGOLINE- cabergoline tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

NuCare Pharmaceuticals,Inc.

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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).

Product summary:

Cabergoline Tablets are a white to off-white, oval shape, flat face, beveled edge tablet containing 0.5 mg cabergoline. Each tablet is debossed P bisect line P on one side and “673" on the other side. NDC 68071-4596-8 BOTTLES OF 8 Store at controlled room temperature 20° to 25° C (68° to 77° F) [see USP]. Dispense in original container. Manufactured by: PAR PHARMACEUTICAL Chestnut Ridge, NY 10977 R11/16

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

CABERGOLINE- CABERGOLINE TABLET
NUCARE PHARMACEUTICALS,INC.
----------
CABERGOLINE TABLETS
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:
Cabergoline 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 tablet, for oral administration, contains 0.5 mg of cabergoline.
Inactive ingredients consist of citric
acid, croscarmellose sodium, magnesium stearate and microcrystalline
cellulose.
CLINICAL PHARMACOLOGY
PHARMACOKINETICS
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 mg
twice weekly, respectively.
IN THE 8-WEEK, DOUBLE-BLIND PERIOD OF THE C