CABERGOLINE- cabergoline tablet
Mylan Pharmaceuticals Inc.
Cabergoline tablets contain cabergoline, a dopamine receptor agonist. The chemical name for cabergoline is 1-[(6-Allylergolin-8�-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea. Its molecular formula is C26 H37 N5 O2 , and its molecular weight is 451.6.
Cabergoline, USP is a white or almost white crystalline 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 anhydrous lactose, 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 D2 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 D1 , α1 - and α2 -adrenergic, and 5-HT1 - and 5-HT2 -serotonin receptors.
INDICATIONS AND USAGE
Cabergoline tablets are indicated for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas.
Pregnancy
Teratogenic Effects. Pregnancy Category B
DOSAGE AND ADMINISTRATION
The recommended dosage of cabergoline tablets for initiation of therapy is 0.25 mg twice a week. Dosage may be increased by 0.25 mg twice weekly up to a dosage of 1 mg twice a week according to the patient's serum prolactin level. Before initiating treatment, cardiovascular evaluation should be performed and echocardiography should be considered to assess for valvular disease.
Dosage increases should not occur more rapidly than every 4 weeks, so that the physician can assess the patient's response to each dosage level. If the patient does not respond adequately, and no additional benefit is observed with higher doses, the lowest dose that achieved maximal response should be used and other therapeutic approaches considered. Patients receiving long-term treatment with cabergoline should undergo periodic assessment of their cardiac status and echocardiography should be considered.
After a normal serum prolactin level has been maintained for 6 months, cabergoline may be discontinued, with periodic monitoring of the serum prolactin level to determine whether or when treatment with cabergoline should be reinstituted. The durability of efficacy beyond 24 months of therapy with cabergoline has not been established.
HOW SUPPLIED
Cabergoline Tablets, USP are available containing 0.5 mg of cabergoline, USP.
The 0.5 mg tablets are white to off-white, oval, scored tablets debossed with M on one side of the tablet and C on the left of the score and G on the right of the score on the other side. They are available as follows:
NDC 0378-2800-26
bottles of 8 tablets
NDC 0378-2800-93
bottles of 30 tablets
Store at 20� to 25�C (68� to 77�F).
