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Bromocriptine, sold under the brand name Parlodel among others, is an ergoline derivative and dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease, hyperprolactinaemia, neuroleptic malignant syndrome, and, as an adjunct, type 2 diabetes.
It was patented in 1968 and approved for medical use in 1975.
Since the late 1980s it has been used, off-label, to reduce the symptoms of cocaine withdrawal but the evidence for this use is poor. Bromocriptine has been successfully used in cases of galactorrhea precipitated by dopamine antagonists like risperidone.
A quick-release formulation of bromocriptine, Cycloset, is also used to treat type 2 diabetes.. For label updates see FDA index page for NDA 020866 When administered within 2 hours of awakening, it increases hypothalamic dopamine level. That results to a significant weight loss as well as decreases in blood glucose levels, hepatic glucose production, and insulin resistance. It therefore acts as an adjunct to diet and exercise to improve glycemic control and cardiovascular risk.
Bromocriptine use has been anecdotally associated with causing or worsening psychosis symptoms (its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine receptors). It should be understood, however, that the greater affinity bromocriptine and many similar antiparkinson's drugs have for the D2S receptor form (considered to be mostly present at inhibitory D2 autoreceptor locatations) relative to the D2L form, sufficiently low partial agonist activity (ie where a molecule binding to a receptor induces limited effects while preventing a stronger ligand like dopamine from binding), and, possibly, the functional selectivity of a particular drug may generate antidopaminergic effects that are more similar than oppositional in nature to antipsychotics.
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 estimated to range between 0.005% and 0.04%. Additional safety precautions and stricter prescribing rules were suggested based on the data. "EMA rät vom Abstillmittel Bromocriptin ab", article in Ärzteblatt It is a bile salt export pump inhibitor.
After long-term use of , a withdrawal syndrome may occur during dose reduction or discontinuation with the following possible side effects: anxiety, panic attacks, dysphoria, depression, agitation, irritability, suicidal ideation, fatigue, orthostatic hypotension, nausea, vomiting, diaphoresis, generalized pain, and drug cravings. For some individuals, these withdrawal symptoms are short-lived and they make a full recovery, for others a protracted withdrawal syndrome may occur with withdrawal symptoms persisting for months or years.
Despite acting as a serotonin 5-HT2A receptor agonist, bromocriptine is described as non-.
As a silent antagonist of the serotonin 5-HT2B receptor, bromocriptine has been said not to pose a risk of cardiac valvulopathy. This is in contrast to other ergolines acting instead as 5-HT2B receptor agonists such as cabergoline and pergolide but is similar to lisuride which likewise acts as a 5-HT2B receptor antagonist. However, in other research, bromocriptine has subsequently been found to be a partial agonist of the serotonin 5-HT2B receptor and has been associated with cardiac valvulopathy and related complications. In any case, bromocriptine seems to have lower risk than certain other drugs.
Bromocriptine is a semisynthetic derivative of a natural ergot alkaloid, ergocryptine (a derivative of lysergic acid), which is synthesized by bromination of ergocryptine using N-bromosuccinimide.
A quick-release formulation of bromocriptine was approved by the FDA in 2009.
As of July 2017 it was also sold as a combination drug with metformin as Diacriptin-M, and as a veterinary drug under the brand Pseudogravin.
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