IUPAC_name = Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'alpha-(2-methylpropyl)-
C=32 | H=40 | Br=1 | N=5 | O=5
molecular_weight = 654.595
bioavailability= 28% of oral dose absorbed
metabolism = ?
elimination_half-life= 12-14 hours
excretion = 85% bile (faeces)
pregnancy_US = B
legal_status = ?
Bromocriptine (brand names include Parlodel), an
ergolinederivative, is a dopamine agonistthat is used in the treatment of pituitary tumorsand Parkinson's disease.
Amenorrhea, female infertility, galactorrhea, hypogonadism, and acromegalymay all be caused by pituitary problems, such as hyperprolactinaemia, and therefore, these problems may be treated by this drug.
It has also been used in some countries to prevent lactation following childbirth if the mother does not wish to breastfeed; one of dopamine's effects on the pituitary is as an antagonist of
prolactinproduction by lactotrophs. However, the FDA removed this indication in 1995, because of concerns with respect to an increased risk of heart attack, seizure and stroke.
Because of prolactin's role in stimulating proliferation of the
T-lymphocytes of the immune system, bromocriptine has also been used to suppress the immune system in organ transplantpatients. [Clodi M, Kotzmann H, Riedl M, Schmidt A, Barnas U, Muhlbacher F, Mustafa G, Horl WH, Waldhausl W, Mayer G, Luger A., 1997. [http://ndt.oxfordjournals.org/cgi/content/abstract/12/4/748 The long-acting dopamine agonist bromocriptine mesylate as additive immunosuppressive drug after kidney transplantation] . Nephrol Dial Transplant. 1997 Apr;12(4):748-52.]
Since bromocryptine acts as a dopamine agonist, it has potential use in treating
cocaineaddiction, as the addictive effects of cocaine are caused by it blocking dopamine reuptake. Although it has negligible subjective effects when administered alone, studies show it has the potential to significantly ease the cocaine withdrawalsyndrome. [Campbell A, Baldessarini RJ, Cremens C, Teicher MH, Marsh E, Kula NS, 1989. Bromocriptine antagonizes behavioral effects of cocaine in the rat. Neuropsychopharmacology 1989 Sep; 2(3):209-24.] [KL Preston, JT Sullivan, EC Strain and GE Bigelow, 1992. Effects of cocaine alone and in combination with bromocriptine in human cocaine abusers. J Pharmacol Exp Ther. 1992 Jul;262(1):279-91.]
There appear to be some connections between
insulin insensitivityand dopamine. A company called Veroscience [ [http://www.veroscience.com/research.html VeroScience ] ] is using bromocriptine to treat diabetesand obesity, and their website postulates a connection between neurotransmitters and seasonal variation in insulinsensitivity among vetebrate animals. [Bromocriptine improves glycaemic control and serum lipid profile in obese Type 2 diabetic subjects: a new approach in the treatment of diabetes. Expert Opin Investig Drugs. 1999 Oct;8(10):1683-1707.] There are also some connections between temperature and dopamine and serotonin production. [http://sulcus.berkeley.edu/mcb/165_001/papers/manuscripts/_281.html] In addition, new research indicates that patients with diabetesare more likely to develop Parkinson's disease, which is characterized by a dopamine deficiency in the brain.
Bromocriptine is an agonist of D2 dopamine receptors and has therefore been used as a treatment for Parkinson's disease. Early studies suggested that treating patients with bromocriptine before
levodopawould delay the onset of side effects such as dyskinesia. [JL Montastruc, O Rascol, JM Senard and A Rascol, 1994. BA randomised controlled study comparing bromocriptine to which levodopa was later added, with levodopa alone in previously untreated patients with Parkinson's disease: a five year follow up. Journal of Neurology, Neurosurgery, and Psychiatry, 1994, Vol 57, 1034-1038] However, a recent Cochrane reviewfound a lack of evidence to support this view. [van Hilten J, Ramaker C, Stowe R, Ives Nj., 2007. Bromocriptine/levodopa combined versus levodopa alone for early Parkinson's disease. Cochrane Database Syst Rev. 2007 Oct 17;(4):CD003634.]
Bromocriptine use has been associated with causing or worsening psychotic symptoms. [cite journal |author= |year=1995 |title=Bromocriptine and psychosis: A literature review|journal=Psychiatric Quarterly |volume=66 |issue=1 |pages=87-95 |doi=10.1007/BF02238717 |url=http://www.springerlink.com/content/y42v466374524k1m/ |accessdate=2008-09-06]
Like all ergopeptides, bromocriptine is a
cyclol; two peptide groups of its tri peptidemoiety (shown in black at the upper left of the Figure) are crosslinked, forming the >N-C(OH)< juncture between the two rings with the amidefunctionality.
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BROMOCRIPTINE — Autre nom du mésylate de 2 bromo 見 ergocryptine, la bromocriptine est un alcaloïde semi synthétique de la série des 9 10 ergopeptides, c’est à dire des peptides de l’ergot de seigle, inscrite au tableau A. L’introduction d’un atome de brome en… … Encyclopédie Universelle
Bromocriptine — ██████████90 … Wikipédia en Français
bromocriptine — noun Etymology: by shortening & alteration from bromoergocryptine, from brom + ergocryptine, an ergot derivative, from ergo + Greek kryptos hidden more at crypt Date: 1975 a polypeptide ergot derivative C32H40BrN5O5 that mimics the activity of… … New Collegiate Dictionary
bromocriptine — /broh meuh krip teen/, n. Pharm. an ergot derivative, C32H40BrN5O5, that inhibits prolactin and growth hormone secretions and stimulates dopamine production in the brain, used to prevent postpartum lactation and in the treatments of acromegaly… … Universalium
bromocriptine — noun An ergoline derivative and dopamine agonist used in the treatment of pituitary tumours and Parkinsons disease … Wiktionary
bromocriptine — A semisynthetic ergot derivative that slows dopamine turnover, inhibits prolactin secretion and release of prolactin by thyrotropin releasing hormone, and retards tumor growth and hence is used in the … Medical dictionary
bromocriptine — bro·mo·crip·tine … English syllables
bromocriptine — n. a dopamine receptor agonist, derived from ergot, that is used in the treatment of parkinsonism. It is also used to treat disorders associated with excessive secretion of prolactin (such as prolactinoma), since it inhibits the secretion of this … The new mediacal dictionary
bromocriptine — ˌbrōmōˈkripˌtēn noun ( s) Etymology: by shortening & alteration from bromoergocryptine, from International Scientific Vocabulary brom + ergocryptine, an ergot derivative, from ergo (II) + Greek kryptos hidden + International Scientific Vocabulary … Useful english dictionary
bromocriptine mesylate — bro·mo·crip·tine mes·y·late (bro″mo kripґtēn) [USP] an ergot alkaloid that acts as a dopamine agonist; used to suppress prolactin secretion in the treatment of pituitary prolactinomas and of hyperprolactinemia associated amenorrhea,… … Medical dictionary