CABERGOLINE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

REMEDYREPACK INC.

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Cabergoline Tablets, USP are indicated for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas. Cabergoline Tablets, USP 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, USP are white to off-white, oval shaped, flat face, beveled edge tablet containing 0.5 mg Cabergoline USP. Each tablet is scored on one side and has the letters "IN" and the letter "G" on either side of breakline. The other side of the tablet is engraved with the number "118".  Cabergoline Tablets, USP are available as follows: Bottle of 8 tablets NDC 50742-118-08 Store at 20° to 25°C (68° to 77°F) [see USP controlled room temperature]. Dispense in original container. Rx only Manufactured for: Ingenus Pharmaceuticals, LLC Orlando, FL 32839-6408 Made in India Revised: 07/2019

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

CABERGOLINE- CABERGOLINE TABLET
REMEDYREPACK INC.
----------
CABERGOLINE TABLETS, USP
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.
Its molecular formula is C
H
N
O
, and its molecular weight is 451.62. The structural formula is
as follows:
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.
Cabergoline Tablets, USP for oral administration, contains 0.5 mg of
Cabergoline USP. Inactive
ingredients consist of microcrystalline cellulose, croscarmellose
sodium, citric acid, and magnesium
stearate.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION: The secretion of prolactin by the anterior
pituitary is mainly under hypothalmic
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.
26
37
5
2
2
1
1
2
1
2
In the 8-we