|Trade names||Parlodel, Cycloset, others|
|Other names||Bromocriptine mesilate, bromocriptine mesylate, 2-Bromoergocriptine; CB-154|
|Main uses||Prolactinoma, Parkinson's disease, acromegaly, neuroleptic malignant syndrome, type 2 diabetes, to stop milk production|
|Side effects||Nausea, headache, tiredness, dizziness, constipation, sleepiness|
|Bioavailability||28% of oral dose|
|Elimination half-life||12–14 hours|
|Excretion||85% bile (feces), 2.5–5.5% urine|
|Chemical and physical data|
|Molar mass||654.606 g·mol−1|
|3D model (JSmol)|
Bromocriptine, sold under the brand name Parlodel among others, is a medication used to treat prolactinomas, Parkinson's disease, acromegaly, neuroleptic malignant syndrome, and stop milk production. It may also be used in type 2 diabetes. It is taken by mouth.
Common side effects include nausea, headache, tiredness, dizziness, constipation, and sleepiness. Other side effects may include low blood pressure, and pericardial effusions, confusion. It has been used by many pregnant women without any evidence of harm to the baby. It works by activating dopamine receptors and decreasing the release of prolactin.
Bromocriptine was patented in 1968 and approved for medical use in 1975. It is available as a generic medication. In the United Kingdom 30 pills of 2.5 mg cost the NHS about £75 as of 2021. In the United States this amount costs about 30 USD.
Bromocriptine is used to treat acromegaly and conditions associated with hyperprolactinemia like amenorrhea, infertility, hypogonadism, and prolactin-secreting adenomas. It is also used to prevent ovarian hyperstimulation syndrome and to treat Parkinson's disease.
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.
A quick-release formulation of bromocriptine, is also used to treat type 2 diabetes. When administered within 2 hours of awakening, it increases hypothalamic dopamine level and as a result decreases hepatic glucose production. It therefore acts as an adjunct to diet and exercise to improve glycemic control.
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 receptors). 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. It is a bile salt export pump inhibitor.
After long-term use of dopamine agonists, 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.
|Site||Affinity (Ki [nM])||Efficacy (Emax [%])||Action|
|Notes: All receptors are human except α2D-adrenergic, which is rat (no human counterpart), and 5-HT7, which is rat/mouse.|
Bromocriptine is a partial agonist of the dopamine D2 receptor. It also interacts with other dopamine receptors and with various serotonin and adrenergic receptors. Bromocriptine has additionally been found to inhibit the release of glutamate by reversing the GLT1 glutamate transporter.
As an antagonist of the serotonin 5-HT2B receptor, bromocriptine has not been associated with 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.
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.
Society and culture
As of July 2017, bromocriptine was marketed under many brand names worldwide, including Abergin, Barlolin, Brameston, Brocriptin, Brom, Broma-Del, Bromergocryptine, Bromergon, Bromicon, Bromocorn, Bromocriptin, Bromocriptina, Bromocriptine, Bromocriptine mesilate, Bromocriptine mesylate, Bromocriptine methanesulfonate, Bromocriptini mesilas, Bromocriptinmesilat, Bromodel, Bromokriptin, Bromolac, Bromotine, Bromtine, Brotin, Butin, Corpadel, Cripsa, Criptine, Criten, Cycloset, Degala, Demil, Deparo, Deprolac, Diacriptin, Dopagon, Erenant, Grifocriptina, Gynodel, kirim, Kriptonal, Lactodel, Medocriptine, Melen, Padoparine, Palolactin, Parlodel, Pravidel, Proctinal, Ronalin, Semi-Brom, Serocriptin, Serocryptin, Suplac, Syntocriptine, Umprel, Unew, Updopa, Upnol B, and Volbro.
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