|Systematic (IUPAC) name|
|Trade names||Parlodel, Brotin|
|AHFS/Drugs.com||Monograph,International Drug Names|
|Bioavailability||28% of oral dose absorbed|
|Biological half-life||12-14 hours|
|Excretion||85% bile (faeces), 2.5-5.5% urine|
|ATC code||G02CB01 (WHO) N04BC01 (WHO)|
|Molar mass||654.595 g/mol|
Bromocriptine (INN; trade names Parlodel, Cycloset, Brotin (Pakistan)), an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes.
Amenorrhea, female infertility, galactorrhea, hypogonadism, and acromegaly may all be caused by pituitary problems, such as hyperprolactinaemia, and therefore, these problems may be treated with this drug. Bromocriptine has completely treated gestational macromastia eliminating the need for reduction surgery, in a recent case. It has also been used in treating nonpuerperal mastitis. Since the late 1980s it has been used, off-label, to reduce the symptoms of cocaine withdrawal. 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 percentage points.
Bromocriptine agonizes the following monoamine receptors:
- Dopamine D1 family
- Dopamine D2 family
- Serotonin 5-HT
- Adrenergic α family
- Adrenergic β family
Most frequent side effects are nausea, orthostatic hypotension, headaches, and vomiting through stimulation of the brainstem vomiting centre. Vasospasms with serious consequences such as myocardial infarction and stroke that have been reported in connection with the puerperium, appear to be extremely rare events. Peripheral vasospasm (of the fingers or toes) can cause Raynaud's Phenomenon. Bromocriptine use has been anecdotally associated with causing or worsening psychotic symptoms (its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine). Pulmonary fibrosis has been reported when bromocriptine was used in high doses for the treatment of Parkinson's disease.
Use to suppress milk production after childbirth was reviewed in 2014 and it was concluded that in this context a causal association with serious cardiovascular, neurological or psychiatric events could not be excluded with an overall incidence rate estimated to range between 0.005% and 0.04%. Additional safety precautions and stricter prescribing rules were suggested based on the data.
Bromocriptine is a semisynthetic derivative of a natural ergot alkaloid, ergocriptin (a derivative of lysergic acid), which is synthesized by bromination of ergocriptin using N-bromosuccinimide.
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- FS Tenant, AA Sagherian. Double-blind comparison of amantadine hydrochloride and bromocriptine mesylate for ambulatory withdrawal from cocaine dependence. Archives of General Medicine. 147: 109-112,1987.
- Pijl H, Ohashi S, Matsuda M, et al. (August 2000). "Bromocriptine: a novel approach to the treatment of type 2 diabetes". Diabetes Care 23 (8): 1154–61. doi:10.2337/diacare.23.8.1154. PMID 10937514.
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- EMA Statement "CMDh endorses restricted use of bromocriptine for stopping breast milk production"
- http://m.aerzteblatt.de/news/59857.htm "EMA rät vom Abstillmittel Bromocriptin ab", article in Ärzteblatt
- E. Fluckiger, A. Hofmann, U.S. Patent 3,752,814 (1973)
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