Sunday, April 1, 2012

The description of Cabergoline




Cabergoline was invented by scientists working for the Italian pharmaceutical company Farmitalia-Carlo Erba SpA in Milan in 1981/82 , who were experimenting with semisynthetic derivatives of ergot alkaloids. Farmitalia-Carlo Erba was acquired by Pharmacia in 1992, which in turn was acquired by Pfizer in 2002. The drug was FDA approved December 23, 1996. He went generic in late 2005 following U.S. patent expiration.Farmitalia filed a patent application for cabergoline in 1982, and U.S. Patent 4,526,892 issued July 1985.Cabergoline (brand names Dostinex and Cabaser), a ergot derivative, is a potent dopamine receptor agonist on D2 receptors. In vitro studies in rats indicate cabergoline has a direct inhibitory effect on the pituitary lactotroph (prolactin) cells.

Cabergoline is often used as a frontline officer in the management of prolactinomas due to greater affinity for D2 receptors, side effects less severe, and the regimen more convenient than the old one is long bromocriptine.Cabergoline duration of action of dopamine D2-receptor agonist and in vitro studies in rats show a direct inhibitory effect on prolactin secretion in pituitary cells in lactotroph. Cabergoline decreased serum prolactin levels in rats treated with reserpine.
Receptor binding studies indicate a low affinity for: dopamine D1-receptor alpha1-adrenergic receptors, α2-adrenergic-receptors.In rodents a dose-dependent increase in malignant tumors was found. The correlation is thought to be species specific. No clinical data exists on a human carcinogen.
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