10 Facts About Cabergoline

Cabergoline, sold under the brand name Dostinex among others, is a dopaminergic medication used in the treatment of high prolactin levels, prolactinomas, Parkinson's disease, and for other indications.

Cabergoline is an ergot derivative and a potent dopamine D2 receptor agonist.

Cabergoline was patented in 1980 and approved for medical use in 1993.

Cabergoline is frequently used as a first-line agent in the management of prolactinomas due to its higher affinity for D2 receptor sites, less severe side effects, and more convenient dosing schedule than the older bromocriptine, though in pregnancy bromocriptine is often still chosen since there is less data on safety in pregnancy for cabergoline.

Cabergoline requires slow dose titration to minimise side effects.

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Cabergoline has been associated with cardiac valvulopathy due to activation of 5-HT2B receptors.

Cabergoline is rapidly and extensively metabolized in the liver and excreted in bile and to a lesser extent in urine.

Cabergoline was first synthesized by scientists working for the Italian drug company Farmitalia-Carlo Erba in Milan who were experimenting with semisynthetic derivatives of the ergot alkaloids, and a patent application was filed in 1980.

Cabergoline was first marketed in The Netherlands as Dostinex in 1992.

Cabergoline was studied in one person with Cushing's disease, to lower adrenocorticotropic hormone levels and cause regression of ACTH-producing pituitary adenomas.