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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.
Whereas D 2 receptor agonists suppress prolactin secretion, dopamine D 2 receptor antagonists like domperidone and metoclopramide have the opposite effect, strongly inducing the pituitary secretion of prolactin, and are sometimes used as prolactin releasers, for instance to correct hypoprolactinemia (low prolactin levels) in the treatment of lactation failure. [2]
Bromocriptine is a D 2 receptor agonist and D 1 receptor antagonist with a binding affinity to D 2 receptors of anterior pituitary cells, exclusively on lactotrophs. Bromocriptine stimulates Na +, K +-ATPase activity and/or cytosolic Ca 2+ elevation and therefore reduction of prolactin which leads to no production of cAMP.
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. [3] It is taken by mouth. Cabergoline is an ergot derivative and a potent dopamine D 2 receptor agonist. [4]
Dopamine receptor flow chart. Dopamine receptors are all G protein–coupled receptors, and are divided into two classes based on which G-protein they are coupled to. [1] The D 1-like class of dopamine receptors is coupled to Gα s/olf and stimulates adenylate cyclase production, whereas the D 2-like class is coupled to Gα i/o and thus inhibits adenylate cyclase production.
The opposite of an indication is a contraindication, [4] a reason to withhold a certain medical treatment because the risks of treatment clearly outweigh the benefits. In the United States, indications for prescription drugs are approved by the FDA. Indications are included in the Indications and Usage section of the Prescribing Information.
Ergotamine interacts with serotonin, adrenergic, and dopamine receptors. [17] [18] It is an agonist of serotonin receptors including the 5-HT 1 and 5-HT 2 subtypes. [17]Ergotamine is an agonist of the serotonin 5-HT 2B receptor and has been associated with cardiac valvulopathy. [19]
Two isomers of ergocryptine exist, α-ergocryptine and β-ergocryptine. [2] The beta differs from the alpha form only in the position of a single methyl group, which is a consequence of the biosynthesis in which the proteinogenic amino acid leucine is replaced by isoleucine . β-Ergocryptine was first identified in 1967 by Albert Hofmann . [ 3 ]