Bromocriptine

Drugbox
IUPAC_name = Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'alpha-(2-methylpropyl)-


CAS_number=25614-03-3
ATC_prefix=G02
ATC_suffix=CB01
ATC_supplemental=ATC|N04|BC01
PubChem=31101
DrugBank=APRD00622
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 = ?
routes_of_administration= oral

Bromocriptine (brand names include Parlodel), an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors and Parkinson's disease.

Uses

Amenorrhea, female infertility, galactorrhea, hypogonadism, and acromegaly may 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 prolactin production 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 transplant patients. [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 cocaine addiction, 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 withdrawal syndrome. [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 insensitivity and dopamine. A company called Veroscience [ [http://www.veroscience.com/research.html VeroScience ] ] is using bromocriptine to treat diabetes and obesity, and their website postulates a connection between neurotransmitters and seasonal variation in insulin sensitivity 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 diabetes are more likely to develop Parkinson's disease, which is characterized by a dopamine deficiency in the brain.

Parkinson's disease

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 levodopa would 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 review found 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.]

ide effects

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]

tructure

Like all ergopeptides, bromocriptine is a cyclol; two peptide groups of its tripeptide moiety (shown in black at the upper left of the Figure) are crosslinked, forming the >N-C(OH)< juncture between the two rings with the amide functionality.

ee also

Cabergoline

External links

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* http://www.drugs.com/pro/bromocriptine.html

References