Bromocriptine  

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

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.

Furthermore, this drug is in a particular class of drugs that are sometimes used to stimulate parts of the HPTA (hypothalamus pituitary testicular axis) which is beneficial for bodybuilders when they have finished a cycle of steroids. The drug in turn aids the pituitary in stimulating the Leydig cells in the testicles.

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, at a doseage of 5mg/day orally, has also been used to suppress the immune system in organ transplant patients.^[1]

Since bromocriptine acts as a dopamine agonist, it has potential use in treating cocaine addiction, as the addictive effects of cocaine are caused by its blocking dopamine reuptake. Although bromocriptine has negligible subjective effects when administered alone, studies show it has the potential to significantly ease the cocaine withdrawal syndrome.^[2][3] It is this action that also makes it useful in neuroleptic malignant syndrome.^[4]

There appear to be some connections between insulin insensitivity and dopamine. A company called Veroscience ^[5] 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.^[6] There are also some connections between temperature and dopamine and serotonin production.^[7] 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.^[8] However, a recent Cochrane review found a lack of evidence to support this view.^[9]

Side effects

Bromocriptine use has been associated with causing or worsening psychotic symptoms (it mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine).^[10]

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

• Cabergoline

External links

• www.AcromegalyCommunity.com: Emotional and communal support for those touched by Acromegaly- page discussing drug, side effects, and prescription programs
• MedlinePlus DrugInfo medmaster-a682079
• http://www.drugs.com/pro/bromocriptine.html

References

Recent Bromocriptine Forums  View All  

Bromocriptine Usage And Dodage i was prescribed with Bromocriptine, but i'am confused beacuse i see there are two types: the capsules which are 5mg and the tablets 2.5 mg. my doctor prescribed me to take 1/2 tablet each night, but he means half of the 2.5 mg or the 5 mg one. Iam confused because maybe I think that he menat half of the capsule (5mg) which is the 2.5 tablet. Iam currently taking half of the 2.5 mg, is this right or I should take the 2.5 entirely, which is the half of the 5 mg? HELP PLEASEEE!!!! Friday, 7/3/2009 4:42:24 PM  1 Reply

Bromocriptine indications, side effects of this drug Friday, 7/8/2005 11:54:45 AM  Post a Reply