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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.
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
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 .
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]
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 ...
5617 19109 Ensembl ENSG00000172179 ENSMUSG00000021342 UniProt P01236 P06879 RefSeq (mRNA) NM_000948 NM_001163558 NM_001163530 NM_011164 RefSeq (protein) NP_000939 NP_001157030 NP_001157002 NP_035294 Location (UCSC) Chr 6: 22.29 – 22.3 Mb Chr 13: 27.24 – 27.25 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Prolactin (PRL), also known as lactotropin and mammotropin, is a protein ...