CABERGOLINE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Ingenus Pharmaceuticals, LLC

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 32811-7193 Made in India Revised: 05/2023

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

CABERGOLINE- CABERGOLINE TABLET
INGENUS PHARMACEUTICALS, LLC
----------
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
26
37
5
2
2
1
1
2
1
2
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