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Bromocriptine, originally marketed as Parlodel and subsequently under many brand names, [1] is an ergoline derivative and dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease, hyperprolactinaemia, neuroleptic malignant syndrome, and, as an adjunct, type 2 diabetes.
[58] [59] If the prolactinoma does not initially respond to dopamine agonist therapy, such that prolactin levels are still high or the tumor is not shrinking as expected, the dose of the dopamine agonist can be increased in a stepwise fashion to the maximum tolerated dose. [3] Another option is to consider switching between dopamine agonists.
Absorption of bromocriptine oral dose is approximately 28%; however, only 6% reaches the systemic circulation unchanged, due to a substantial first-pass effect. Bromocriptine reaches mean peak plasma levels after about 1–1.5 hours after a single oral dose. The drug has high protein binding, ranging from 90-96% bound to serum albumin.
Cabergoline is frequently used as a first-line agent in the management of prolactinomas due to its higher affinity for D 2 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 ...
A prolactinoma is a tumor of the pituitary gland that produces the hormone prolactin.It is the most common type of functioning pituitary tumor. [1] Symptoms of prolactinoma are due to abnormally high levels of prolactin in the blood (hyperprolactinemia), or due to pressure of the tumor on surrounding brain tissue and/or the optic nerves.
Dopamine agonists, cabergoline and bromocriptine bind to specific dopamine receptors to block the secretion pathway of prolactin and shrink the size of tumor (prolactinoma), which subsequently treat infertility caused by elevated level of prolactin. [46] (See also : Hyperprolactinaemia) Chemical structure of Bromocriptine
Prolactin has a wide variety of effects. It stimulates the mammary glands to produce milk (): increased serum concentrations of prolactin during pregnancy cause enlargement of the mammary glands and prepare for milk production, which normally starts when levels of progesterone fall by the end of pregnancy and a suckling stimulus is present.
Prolactin inhibitors are mainly used to treat hyperprolactinemia (high prolactin levels). [1] Agonists of the dopamine D 2 receptor such as bromocriptine and cabergoline are able to strongly suppress pituitary prolactin secretion and thereby decrease circulating prolactin levels, and so are most commonly used as prolactin inhibitors. [1]
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