Ország: Egyesült Államok
Nyelv: angol
Forrás: NLM (National Library of Medicine)
CABERGOLINE (UNII: LL60K9J05T) (CABERGOLINE - UNII:LL60K9J05T)
Apotex Corp.
CABERGOLINE
CABERGOLINE 0.5 mg
PRESCRIPTION DRUG
Abbreviated New Drug Application
CABERGOLINE- CABERGOLINE TABLET APOTEX CORP. ---------- CABERGOLINE TABLETS 0.5 MG 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: The drug substance used in cabergoline tablet is the amorphous form of cabergoline. Cabergoline is a cream to 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, contain 0.5 mg of cabergoline. Inactive ingredients consist of lactose anhydrous, 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 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 1.0 mg twice weekly respectively. 26 37 5 2 2 Olvassa el a teljes dokumentumot