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Bromocriptine (originally marketed as Parlodel, subsequently under many names) is an ergoline derivative and dopamine agonist that is used in the treatment of pituitary tumors, Parkinson’s disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes.
Contents
1 Indications
2 Side effects
3 Pharmacology
4 Chemistry
5 History
6 Society and culture
7 See also
8 References
9 External links
Indications
Bromocriptine is used to treat acromegaly and conditions associated with hyperprolactinemia like amenorrhea, infertility, and hypogonadism, prolactin-secreting adenomas ; it is also used to prevent ovarian hyperstimulation syndrome.
It is also used 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.
Side effects
Most frequent side effects are nausea, orthostatic hypotension, headaches, and vomiting through stimulation of the brainstem vomiting centre. 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.
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.
Pharmacology
Bromocriptine is a potent agonist at dopamine D2 receptors
Bromocriptine agonizes the following monoamine receptors:
Dopamine D 1 family
D 1 (K i =682 nM)
D 5 (K i =496 nM)
Dopamine D 2 family
D 2 (K i =2.96 nM)
D 3 (K i =5.42 nM)
D 4 (K i =328 nM)
Serotonin 5-HT
5-HT 1A (K i =12.9 nM)
5-HT 1B (K i =355 nM)
5-HT 1D (K i =10.7 nM)
5-HT 2A (K i =107 nM)
5-HT 2B (K i =56.2 nM)
5-HT 2C (K i =741 nM)
5-HT 6 (K i =33 nM)
Adrenergic α family
α 1A (K i =4.17 nM)
α 1B (K i =1.38 nM)
α 1D (K i =1.12 nM)
α 2A (K i =11.0 nM)
α 2B (K i =34.7 nM)
α 2C (K i =28.2 nM)
Adrenergic β family
β 1 (K i =589 nM)
β 2 (K i =741 nM)
Chemistry
Like all ergopeptides, bromocriptine is a cyclol ; two peptide groups of its tri peptide moiety are crosslinked, forming the >N-C(OH)

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