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Bromocriptine: Wikis

  

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Bromocriptine
Systematic (IUPAC) name
Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'alpha-(2

-methylpropyl)-

Identifiers
CAS number 25614-03-3
ATC code G02CB01 N04BC01
PubChem 31101
DrugBank APRD00622
ChemSpider 28858
Chemical data
Formula C32H40BrN5O5 
Mol. mass 654.595
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 28% of oral dose absorbed
Metabolism  ?
Half life 12-14 hours
Excretion 85% bile (faeces)
Therapeutic considerations
Pregnancy cat. B(US)
Legal status  ?
Routes oral
 Yes check.svgY(what is this?)  (verify)

Bromocriptine (Parlodel, Cycloset), an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease (PD), neuroleptic malignant syndrome, and type 2 diabetes.

Contents

Indications

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. In 2009, bromocriptine mesylate was approved by the FDA for treatment of type 2 diabetes under the trade name Cycloset (VeroScience). It is currently unknown how this drug improves glycemic control, but it has been shown to reduce HbA1c by ~0.5%.

Side effects

Bromocriptine use has been associated with causing or worsening psychotic symptoms (its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine).[1] It can also cause nausea and vomiting through stimulation of the brainstem vomiting centre, vasospasm due to its ergot derivation and fibrosis of multiple organs similar to methysergide, which stimulates fibroblasts.

Chemistry

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.

See also

External links

References

  1. ^ Boyd, Alan (1995). "Bromocriptine and psychosis: A literature review". Psychiatric Quarterly 66 (1): 87?95. doi:10.1007/BF02238717. http://www.springerlink.com/content/y42v466374524k1m/. Retrieved 2008-09-06. 







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