文档介绍：DESCRIPTION
DOSTINEX 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 empirical formula is C26H37N5O2, and its molecular weight is
. The structural formula is as follows:
Cabergoline is a white powder soluble in ethyl alcohol, chloroform, and N, N­
dimethylformamide (DMF); slightly soluble in hydrochloric acid; very slightly
soluble in n-hexane; and insoluble in water.
DOSTINEX Tablets, for oral administration, contain mg of cabergoline. Inactive
ingredients consist of leucine, USP, and lactose, NF.
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.
Reference ID: 2975239
Clinical Studies: The prolactin-lowering efficacy of DOSTINEX was demonstrated in
hyperprolactinemic women in two randomized, double-blind, comparative studies, one
with placebo and the other with bromocriptine. In the placebo-contro