Bromocriptine: A Comprehensive Review
Abstract
Bromocriptine is a dopamine agonist that has been used for over four decades for a variety of indications. In this review, we provide a comprehensive overview of the pharmacology of bromocriptine, its clinical indications, pharmacokinetics, side effects, and drug interactions. In addition, we discuss the current evidence for the use of bromocriptine in infertility, Parkinson’s disease, prolactinomas, and type 2 diabetes.
Introduction
Bromocriptine is a dopamine receptor agonist used for over four decades for a variety of indications, including infertility, Parkinson’s disease, prolactinomas, and type 2 diabetes. The drug is a semisynthetic derivative of ergot alkaloids and is structurally related to lysergic acid diethylamide (LSD). It is a selective agonist at dopamine D2 and D3 receptors, and is thought to be more potent than other drugs in this class, such as pergolide and cabergoline. The pharmacology, pharmacokinetics, side effects, and drug interactions are discussed in this review. In addition, we discuss the evidence for the use of bromocriptine in the treatment of infertility, Parkinson’s disease, prolactinomas, and type 2 diabetes.
Pharmacology
Bromocriptine is a semisynthetic derivative of ergot alkaloids and is structurally related to lysergic acid diethylamide (LSD). It is a selective agonist at dopamine D2 and D3 receptors, and is thought to be more potent than other drugs in this class, such as pergolide and cabergoline. It has a high affinity for D2 receptors (Ki = 0.02 nM) and a low affinity for D3 receptors (Ki = 1.3 nM). The drug has a slow onset of action, with peak concentrations reached within 4-6 hours after oral administration. The pharmacodynamic effects of bromocriptine are mediated by its ability to activate presynaptic D2 receptors, resulting in increased dopaminergic transmission.
Pharmacokinetics
Bromocriptine is rapidly and completely absorbed after oral administration. Peak plasma concentrations are reached within 2-4 hours and the bioavailability of the drug is approximately 80%. The drug is extensively metabolized by the liver and has an elimination half-life of 4-6 hours.
Clinical Indications
Bromocriptine has been used for a variety of indications, including infertility, Parkinson’s disease, prolactinomas, and type 2 diabetes.
Infertility
Bromocriptine has been used to treat hyperprolactinemic infertility, a condition in which high levels of prolactin interfere with ovulation. The drug has been shown to decrease prolactin levels, increase gonadotropin levels, and improve fertility rates.
Parkinson’s Disease
Bromocriptine has been used to treat Parkinson’s disease for over four decades. The drug is thought to improve symptoms by increasing dopaminergic transmission in the brain. It is typically used in combination with other drugs, such as levodopa, to increase its efficacy.
Prolactinomas
Bromocriptine is the drug of choice for the treatment of prolactinomas, which are benign tumors of the pituitary gland. The drug is effective in decreasing prolactin levels and in shrinking the tumor.
Type 2 Diabetes
Bromocriptine has been studied for the treatment of type 2 diabetes. The drug is thought to improve glycemic control by increasing glucose uptake in skeletal muscle.
Side Effects
The most common side effects of bromocriptine are nausea, vomiting, dizziness, and headache. Other serious side effects include hypotension, syncope, confusion, and hallucinations.
Drug Interactions
Bromocriptine is metabolized by the liver and can be affected by other drugs that are metabolized by the same enzymes. It can also interact with drugs that affect dopaminergic transmission, such as antipsychotics and antidepressants.
Conclusion
Bromocriptine is a dopamine agonist that has been used for over four decades for a variety of indications. In this review, we provided a comprehensive overview of the pharmacology, pharmacokinetics, clinical indications, side effects, and drug interactions of bromocriptine. The drug is effective in decreasing prolactin levels, improving fertility rates, and treating Parkinson’s disease and type 2 diabetes. The most common side effects of bromocriptine are nausea, vomiting, dizziness, and headache.
References
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