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Bromocriptine

Hormone Management
CyclosetParlodel

Overview

Bromocriptine is a synthetic compound classified as an ergot alkaloid derivative. It is not an endogenous hormone but is used in medical settings to mimic or influence certain hormonal pathways. Bromocriptine is primarily produced in pharmaceutical laboratories and is available under brand names such as Cycloset and Parlodel. It belongs to the chemical class of dopamine receptor agonists, specifically targeting dopamine D2 receptors. Researchers have found that bromocriptine plays a significant role in the regulation of prolactin secretion. It is widely studied for its effects on conditions such as hyperprolactinemia, Parkinson's disease, and type 2 diabetes. Bromocriptine's ability to lower prolactin levels makes it useful in treating disorders associated with high prolactin, such as prolactinomas. Additionally, its role in modulating dopamine pathways has been explored in the context of neurodegenerative diseases and metabolic disorders. The mechanism of action of bromocriptine involves its agonistic activity at dopamine D2 receptors, which leads to the inhibition of prolactin secretion from the anterior pituitary gland. This action is mediated through the suppression of adenylate cyclase activity, reducing cyclic AMP levels and subsequently decreasing prolactin release. In the context of Parkinson's disease, bromocriptine's dopaminergic activity helps alleviate motor symptoms by compensating for dopamine deficiency. Bromocriptine exhibits a variable pharmacokinetic profile, with an oral bioavailability of approximately 6% due to extensive first-pass metabolism in the liver. Its half-life ranges from 3 to 6 hours, depending on the formulation and individual patient metabolism. The compound is metabolized primarily by the liver, and its metabolites are excreted via the biliary system. Clinically, bromocriptine is used to manage conditions like hyperprolactinemia, Parkinson's disease, and type 2 diabetes. It is approved by regulatory agencies such as the FDA for these indications. However, its use requires careful monitoring due to potential side effects and interactions with other medications. Researchers have observed that bromocriptine's regulatory standing varies by country, reflecting differences in medical guidelines and approval processes.

Mechanism of Action

Bromocriptine acts primarily on dopamine D2 receptors, leading to the inhibition of prolactin secretion from the anterior pituitary gland. This action results in decreased cyclic AMP levels, reducing prolactin release and influencing dopaminergic pathways in the brain.

Molecular Data

FormulaC32H40BrN5O5
Molecular Weight654.6 g/mol
CAS Number25614-03-3
PubChem CID31101

Half-Life & Pharmacokinetics

OralPoor bioavailability due to first-pass metabolism

Bromocriptine has a half-life of approximately 3-6 hours when taken orally, with significant first-pass hepatic metabolism.

Storage

Temperature

Store at room temperature (15-30°C)

Light

Protect from light

Form

Stable in tablet form for extended periods

Notes

Ensure packaging is tightly closed to prevent moisture exposure.

Solubility

Bromocriptine is poorly soluble in water but more soluble in organic solvents like ethanol.

Legal Status

🇩🇪DE

In Germany, bromocriptine is classified as a prescription-only medication (verschreibungspflichtig).

🇺🇸US

In the USA, bromocriptine is FDA-approved for certain conditions and requires a prescription.

🇦🇺AU

In Australia, bromocriptine is classified as a Schedule 4 (S4) prescription-only medicine.

🇬🇧UK

In the UK, bromocriptine is a prescription-only medicine (POM) under MHRA regulations.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

5 Research Publications

Late phase completed clinical trials investigating bromocriptine mesylate quick release as treatment of type 2 diabetes mellitus.

Review

Expert opinion on pharmacotherapy · 2021

Researchers found that bromocriptine mesylate quick release is a unique oral medication for adults with type 2 diabetes that has a low risk of causing low blood sugar and does not lead to weight gain. Although its effectiveness as a standalone treatment is limited, it offers significant cardiovascular benefits and is recommended as part of a combination therapy, especially for those who prefer to avoid injections.

  • Bromocriptine mesylate QR has a favorable safety profile with low hypoglycemia risk.
  • It does not cause weight gain, making it suitable for obese patients.
  • The drug is recommended for use in combination therapy, particularly for patients with cardiovascular concerns.
PubMed

Bromocriptine: old drug, new formulation and new indication.

Review

Diabetes, obesity & metabolism · 2010

Researchers found that a new quick-release formulation of bromocriptine, when taken in the morning, can help improve blood sugar control in people with type 2 diabetes. This medication works by resetting the body's internal clock and improving insulin sensitivity, and it has been shown to lower blood sugar levels effectively with minimal side effects.

  • QR-bromocriptine lowers glycated hemoglobin by 0.6-1.2%.
  • It is well tolerated, with nausea being the most common side effect.
  • The drug has been approved in the USA for treating type 2 diabetes.
PubMed

A randomized, double-blind, placebo-controlled trial to assess safety and tolerability during treatment of type 2 diabetes with usual diabetes therapy and either Cycloset or placebo.

Human

BMC endocrine disorders · 2007

Researchers observed that Cycloset, a medication for type 2 diabetes, may help lower blood sugar levels and improve lipid profiles when taken alongside standard diabetes treatments. The study included over 3,000 participants and aimed to assess the safety and effectiveness of Cycloset compared to a placebo over one year.

  • Cycloset reduced HbA1c levels by 0.55-1.2 compared to placebo.
  • It lowered plasma triglycerides and free fatty acids by approximately 25% and 20%, respectively.
  • The study evaluated safety concerning serious adverse events and cardiovascular risks.
PubMed

New long-acting bromocriptine (Parlodel MR and Parlodel LAR) in the treatment of pituitary tumours with hyperprolactinemia.

Human

Endokrynologia Polska · 1992

Researchers observed that new long-acting forms of bromocriptine, Parlodel MR and Parlodel LAR, effectively reduced high prolactin levels in patients with pituitary tumors. Most patients experienced significant improvements in symptoms, such as the disappearance of unwanted milk production and restored menstrual cycles. Additionally, Parlodel LAR had fewer side effects compared to the standard treatment.

  • Serum prolactin levels returned to normal in 36 out of 40 patients.
  • Significant tumor shrinkage was noted in 30 out of 35 patients with tumors.
  • Parlodel LAR was associated with the least number of side effects.
PubMed

Male hyperprolactinemia:effects on fertility.

Human

Fertility and sterility · 1979

Researchers observed that 4% of infertile men had high levels of prolactin, which can lead to issues like infertility and impotence. They identified various causes, including pituitary tumors and medication use, and found that treatment with bromocriptine was effective in improving fertility outcomes for these men.

  • 4% of infertile men had hyperprolactinemia.
  • Common symptoms included infertility, impotence, and low testosterone levels.
  • Bromocriptine treatment showed positive results for fertility.
PubMed

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This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.