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Bromocriptine | CAS No: 25614-03-3 | GMP-certified suppliers

A medication that addresses hyperprolactinemia-related disorders, supports management of Parkinsonian symptoms, and serves as adjunct therapy for select patients with acromegaly.

Therapeutic categories

Adrenergic AgonistsAdrenergic alpha-1 Receptor AgonistsAdrenergic alpha-1 Receptor AntagonistsAdrenergic alpha-2 Receptor AgonistsAdrenergic alpha-AgonistsAdrenergic alpha-Antagonists
Generic name
Bromocriptine
Molecule type
small molecule
CAS number
25614-03-3
DrugBank ID
DB01200
Approval status
Approved drug, Investigational drug, Withdrawn drug
ATC code
N04BC01

Primary indications

  • For the treatment of galactorrhea due to hyperprolactinemia, prolactin-dependent menstrual disorders and infertility, prolactin-secreting adenomas, prolactin-dependent male hypogonadism, as adjunct therapy to surgery or radiotherapy for acromegaly or as monotherapy is special cases, as monotherapy in early Parksinsonian Syndrome or as an adjunct with levodopa in advanced cases with motor complications
  • Bromocriptine has also been used off-label to treat restless legs syndrome and neuroleptic malignant syndrome

Product Snapshot

  • Oral small‑molecule API available in multiple tablet and capsule presentations
  • Used for prolactin‑related endocrine disorders, acromegaly adjunct therapy, and Parkinson’s disease management, with additional off‑label neurological applications
  • Marketed in the US and Canada with a mix of approved, investigational, and withdrawn statuses depending on product form and indication

Clinical Overview

Bromocriptine (CAS 25614-03-3) is a semisynthetic ergot-derived lysergamide with potent dopaminergic activity. It is indicated for the treatment of hyperprolactinemia-associated galactorrhea, prolactin‑dependent menstrual disorders, infertility, prolactin‑secreting adenomas, and prolactin‑related male hypogonadism. Additional uses include monotherapy for early Parkinsonian syndrome, adjunct therapy with levodopa in advanced disease, and adjunct or alternative therapy for acromegaly. Off‑label applications reported in clinical practice include restless legs syndrome and management of neuroleptic malignant syndrome. Approval for prevention of physiological lactation was withdrawn due to safety concerns.

Bromocriptine acts primarily as a dopamine D2 receptor agonist with activity at D3 receptors and lower‑affinity interactions across several serotonergic and adrenergic receptor subtypes. Its antiparkinsonian effect is linked to postsynaptic D2 stimulation within the nigrostriatal pathway, improving motor coordination in the context of dopaminergic deficit. In the tuberoinfundibular pathway, D2 activation suppresses prolactin secretion, forming the basis for its efficacy in hyperprolactinemic disorders. In acromegaly, bromocriptine reduces somatotropin secretion in some patients. Receptor interactions at 5‑HT1B and 5‑HT2B have been associated with reports of pulmonary fibrosis.

Mechanistically, D2 receptor activation reduces intracellular cAMP, inhibits IP3‑mediated calcium release, and decreases calcium influx, contributing to suppression of prolactin release and modulation of growth hormone output. Signal transduction effects include inhibition of MAPK and ERK kinase pathways via Raf‑dependent mechanisms.

Bromocriptine is metabolized primarily by CYP3A pathways and is both a substrate and inhibitor of CYP3A4. It also interacts with P‑glycoprotein transport systems. Reported adverse effects include nausea, orthostatic hypotension, hallucinations, impulse‑control symptoms, and rare fibrotic complications.

Relevant brands include formulations of bromocriptine mesylate commonly used worldwide for endocrine and neurologic indications. For API procurement, suppliers should ensure control of ergot‑related impurities, confirmation of stereochemical integrity, and compliance with pharmacopeial specifications and regional GMP standards.

Identification & chemistry

Generic name Bromocriptine
Molecule type Small molecule
CAS 25614-03-3
UNII 3A64E3G5ZO
DrugBank ID DB01200

Pharmacology

SummaryBromocriptine is a dopamine D2‑selective agonist that modulates G‑protein signaling to reduce intracellular cAMP and calcium flux, leading to inhibition of prolactin release and support of dopaminergic activity in motor pathways. Its pharmacodynamic profile is dominated by D2 and D3 receptor engagement, with additional interactions across serotonergic and adrenergic receptors that contribute to both therapeutic and off‑target effects. These actions underpin its use in conditions involving prolactin excess and dopaminergic pathway dysfunction.
Mechanism of actionThe dopamine D<sub>2</sub> receptor is a 7-transmembrane G-protein coupled receptor associated with G<sub>i</sub> proteins. In lactotrophs, stimulation of dopamine D<sub>2</sub> receptor causes inhibition of adenylyl cyclase, which decreases intracellular cAMP concentrations and blocks IP3-dependent release of Ca<sup>2+</sup> from intracellular stores. Decreases in intracellular calcium levels may also be brought about via inhibition of calcium influx through voltage-gated calcium channels, rather than via inhibition of adenylyl cyclase. Additionally, receptor activation blocks phosphorylation of p42/p44 MAPK and decreases MAPK/ERK kinase phosphorylation. Inhibition of MAPK appears to be mediated by c-Raf and B-Raf-dependent inhibition of MAPK/ERK kinase. Dopamine-stimulated growth hormone release from the pituitary gland is mediated by a decrease in intracellular calcium influx through voltage-gated calcium channels rather than via adenylyl cyclase inhibition. Stimulation of dopamine D<sub>2</sub> receptors in the nigrostriatal pathway leads to improvements in coordinated muscle activity in those with movement disorders.
PharmacodynamicsBromocriptine stimulates centrally-located dopaminergic receptors resulting in a number of pharmacologic effects. Five dopamine receptor types from two dopaminergic subfamilies have been identified. The dopaminergic D1 receptor subfamily consists of D<sub>1</sub> and D<sub>5</sub> subreceptors, which are associated with dyskinesias. The dopaminergic D2 receptor subfamily consists of D<sub>2</sub>, D<sub>3</sub> and D<sub>4</sub> subreceptors, which are associated with improvement of symptoms of movement disorders. Thus, agonist activity specific for D2 subfamily receptors, primarily D<sub>2</sub> and D<sub>3</sub> receptor subtypes, are the primary targets of dopaminergic antiparkinsonian agents. It is thought that postsynaptic D<sub>2</sub> stimulation is primarily responsible for the antiparkinsonian effect of dopamine agonists, while presynaptic D<sub>2</sub> stimulation confers neuroprotective effects. This semisynthetic ergot derivative exhibits potent agonist activity on dopamine D<sub>2</sub>-receptors. It also exhibits agonist activity (in order of decreasing binding affinity) on 5-hydroxytryptamine (5-HT)<sub>1D</sub>, dopamine D<sub>3</sub>, 5-HT<sub>1A</sub>, 5-HT<sub>2A</sub>, 5-HT<sub>1B</sub>, and 5-HT<sub>2C</sub> receptors, antagonist activity on &alpha;<sub>2A</sub>-adrenergic, &alpha;<sub>2C</sub>, &alpha;<sub>2B</sub>, and dopamine D<sub>1</sub> receptors, partial agonist activity at receptor 5-HT<sub>2B</sub>, and inactivates dopamine D<sub>4</sub> and 5-HT<sub>7</sub> receptors. Parkinsonian Syndrome manifests when approximately 80% of dopaminergic activity in the nigrostriatal pathway of the brain is lost. As this striatum is involved in modulating the intensity of coordinated muscle activity (e.g. movement, balance, walking), loss of activity may result in dystonia (acute muscle contraction), Parkinsonism (including symptoms of bradykinesia, tremor, rigidity, and flattened affect), akathesia (inner restlessness), tardive dyskinesia (involuntary muscle movements usually associated with long-term loss of dopaminergic activity), and neuroleptic malignant syndrome, which manifests when complete blockage of nigrostriatal dopamine occurs. High dopaminergic activity in the mesolimbic pathway of the brain causes hallucinations and delusions; these side effects of dopamine agonists are manifestations seen in patients with schizophrenia who have overractivity in this area of the brain. The hallucinogenic side effects of dopamine agonists may also be due to 5-HT<sub>2A</sub> agonism. The tuberoinfundibular pathway of the brain originates in the hypothalamus and terminates in the pituitary gland. In this pathway, dopamine inhibits lactotrophs in anterior pituitary from secreting prolactin. Increased dopaminergic activity in the tuberoinfundibular pathway inhibits prolactin secretion making bromocriptine an effective agent for treating disorders associated with hypersecretion of prolactin. Pulmonary fibrosis may be associated bromocriptine’s agonist activity at 5-HT<sub>1B</sub> and 5-HT<sub>2B</sub> receptors.
Targets
TargetOrganismActions
Dopamine D2 receptorHumansagonist
Dopamine D3 receptorHumansagonist
5-hydroxytryptamine receptor 1DHumansagonist

ADME / PK

AbsorptionApproximately 28% of the oral dose is absorbed; however due to a substantial first pass effect, only 6% of the oral dose reaches the systemic circulation unchanged. Bromocriptine and its metabolites appear in the blood as early as 10 minutes following oral administration and peak plasma concentration are reached within 1-1.5 hours. Serum prolactin may be decreased within 2 hours or oral administration with a maximal effect achieved after 8 hours. Growth hormone concentrations in patients with acromegaly is reduced within 1-2 hours with a single oral dose of 2.5 mg and decreased growth hormone concentrations persist for at least 4-5 hours.
Half-life2-8 hours
Protein binding90-96% bound to serum albumin
MetabolismCompletely metabolized by the liver, primarily by hydrolysis of the amide bond to produce lysergic acid and a peptide fragment, both inactive and non-toxic. Bromocriptine is metabolized by cytochrome P450 3A4 and excreted primarily in the feces via biliary secretion.
Route of eliminationParent drug and metabolites are almost completely excreted via the liver, and only 6% eliminated via the kidney.

Formulation & handling

  • Oral small‑molecule lysergamide with low aqueous solubility, requiring solubility‑enhancing or dispersion approaches for consistent dissolution.
  • Solid‑state API is lipophilic (LogP ~3.9), supporting use of lipidic or controlled‑release matrices to manage absorption variability.
  • Typically administered with food to reduce gastric irritation, so formulations may consider GI tolerability and robustness to fed‑state conditions.

Regulatory status

LifecycleMost legacy U.S. patents for the API expired between 2012 and 2015, with an additional secondary patent expiring in 2023, while remaining protections extend to 2032, indicating mixed maturity. With commercialization limited to the U.S. and Canada, the market shows partial generic exposure but retains some patent-based exclusivity through the early 2030s.
MarketsCanada, US
Supply Chain
Supply chain summaryBromocriptine is supplied by a large number of manufacturers and repackagers, indicating a well‑established generic supply base alongside the original developer. Branded and generic products are available in major regulated markets, including the United States and Canada. While several older U.S. patents have expired, allowing broad generic competition, later patents extending into 2032 suggest that certain protected formulations or uses may still limit full generic entry in specific segments.

Safety

ToxicitySymptoms of overdosage include nausea, vomiting, and severe hypotension. The most common adverse effects include nausea, headache, vertigo, constipation, light-headedness, abdominal cramps, nasal congestion, diarrhea, and hypotension.
High Level Warnings:
  • Overexposure may elicit pronounced gastrointestinal distress (nausea, vomiting) and marked decreases in blood pressure, requiring controls to limit acute hypotensive events during handling
  • Routine handling should account for CNS‑active effects such as headache, vertigo, and light‑headedness, which indicate the compound’s potential to affect vestibular and autonomic pathways
  • Material management should consider its propensity to cause abdominal cramping, constipation or diarrhea, reflecting broad smooth‑muscle and dopaminergic activity relevant to occupational exposure assessment

Bromocriptine is a type of Dopamine agonists


Dopamine agonists are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that act on the dopamine receptors in the brain. These compounds mimic the effects of dopamine, a neurotransmitter involved in various physiological processes such as movement, cognition, and emotions.

Dopamine agonists are commonly used in the treatment of neurological disorders, particularly Parkinson's disease and restless legs syndrome. They work by binding to dopamine receptors and stimulating them, thereby increasing dopamine activity in the brain. This helps to alleviate the symptoms associated with these conditions, such as tremors, rigidity, and muscle stiffness.

One of the key advantages of dopamine agonists is their ability to provide long-lasting relief compared to other medications. They are available in different formulations, including oral tablets, transdermal patches, and injectable solutions, allowing patients to choose the most suitable administration method.

However, like any medication, dopamine agonists may have side effects. These can include nausea, dizziness, hallucinations, and compulsive behaviors. It is important for healthcare professionals to closely monitor patients using dopamine agonists to minimize the occurrence and severity of these side effects.

In conclusion, dopamine agonists are a vital subcategory of pharmaceutical APIs used to manage Parkinson's disease and restless legs syndrome. They mimic the effects of dopamine in the brain and offer long-lasting relief from symptoms. Although they can have side effects, proper monitoring and dosage adjustments can help optimize their therapeutic benefits.


Bromocriptine (Dopamine agonists), classified under Central Nervous System Agents


Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.

CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.

The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.

Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.



Bromocriptine API manufacturers & distributors

Compare qualified Bromocriptine API suppliers worldwide. We currently have 5 companies offering Bromocriptine API, with manufacturing taking place in 4 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.

SupplierTypeCountryProduct originCertificationsPortfolio
Producer
India India CoA35 products
Producer
United States Italy CEP, CoA, GMP, MSDS, USDMF106 products
Producer
Italy Unknown CEP, CoA, FDA, GMP, USDMF48 products
Producer
Slovenia Unknown CoA, JDMF, USDMF32 products
Distributor
United States World BSE/TSE, CEP, CoA, GMP, MSDS, USDMF441 products

When sending a request, specify which Bromocriptine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).

Use the list above to find high-quality Bromocriptine API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.

Frequently asked questions about Bromocriptine API


Sourcing

What matters most when sourcing GMP-grade Bromocriptine?
When sourcing GMP‑grade Bromocriptine, the key considerations are verification of GMP compliance and confirmation that the material meets regulatory expectations for the United States and Canada. It is also important to assess the supplier’s ability to provide consistent quality within a broad generic supply base. Awareness of existing patents extending to 2032 helps ensure that the intended formulation or use does not conflict with protected segments.
Which documents are typically required when sourcing Bromocriptine API?
Request the core API documentation set: CoA (5 companies), USDMF (4 companies), GMP (3 companies), CEP (3 companies), MSDS (2 companies). Confirm versions and validity dates match the destination market to avoid delays in qualification.
Which manufacturers are known to produce Bromocriptine API?
Known or reported manufacturers for Bromocriptine: LGM Pharma. Evaluate their GMP history, scale, and regional coverage before requesting dossiers or allocating demand.
How can I request quotes for Bromocriptine API from GMP suppliers?
Submit quote requests through the supplier listings with your specs and required documents (specifications, target volume, delivery timeline, and destination). Providing consistent details upfront speeds comparable offers and clarifies technical feasibility.
Is a GMP audit report available for Bromocriptine manufacturers?
Audit reports may be requested for Bromocriptine: 1 GMP audit report available. Confirm the scope and recency of any audit before relying on it for qualification decisions.
How many suppliers offer Bromocriptine API on Pharmaoffer?
Reported supplier count for Bromocriptine: 5 verified suppliers. Filter listings by certifications, regions, and delivery options to match your qualification plan.
Which countries are known to manufacture Bromocriptine API?
Production countries reported for Bromocriptine: Italy (1 producer), India (1 producer). Knowing the manufacturing geography helps anticipate logistics lead times and import compliance needs.
Which certifications do suppliers of Bromocriptine usually hold?
Common certifications for Bromocriptine suppliers: CoA (5 companies), USDMF (4 companies), GMP (3 companies), CEP (3 companies), MSDS (2 companies). Always verify issuing authorities and expiry dates when reviewing audit packages.

Technical

What is Bromocriptine (CAS 25614-03-3) used for?
Bromocriptine is used to treat hyperprolactinemia‑related conditions such as galactorrhea, prolactin‑dependent menstrual disorders, infertility, prolactin‑secreting adenomas, and prolactin‑related male hypogonadism. It is also indicated for early Parkinson’s disease as monotherapy, as an adjunct to levodopa in advanced disease, and as adjunct or alternative therapy in acromegaly. Additional clinical uses include management of restless legs syndrome and neuroleptic malignant syndrome.
Which therapeutic class does Bromocriptine fall into?
Bromocriptine belongs to the following therapeutic categories: Adrenergic Agonists, Adrenergic alpha-1 Receptor Agonists, Adrenergic alpha-1 Receptor Antagonists, Adrenergic alpha-2 Receptor Agonists, Adrenergic alpha-Agonists. This positioning helps teams compare alternative APIs, anticipate pharmacology expectations, and align early research priorities.
What conditions is Bromocriptine mainly prescribed for?
The primary indications for Bromocriptine: For the treatment of galactorrhea due to hyperprolactinemia, prolactin-dependent menstrual disorders and infertility, prolactin-secreting adenomas, prolactin-dependent male hypogonadism, as adjunct therapy to surgery or radiotherapy for acromegaly or as monotherapy is special cases, as monotherapy in early Parksinsonian Syndrome or as an adjunct with levodopa in advanced cases with motor complications, Bromocriptine has also been used off-label to treat restless legs syndrome and neuroleptic malignant syndrome. These use cases frame the target patient populations and help prioritize formulation and safety evaluations.
How does Bromocriptine work?
The dopamine D2 receptor is a 7-transmembrane G-protein coupled receptor associated with Gi proteins. In lactotrophs, stimulation of dopamine D2 receptor causes inhibition of adenylyl cyclase, which decreases intracellular cAMP concentrations and blocks IP3-dependent release of Ca2+ from intracellular stores. Decreases in intracellular calcium levels may also be brought about via inhibition of calcium influx through voltage-gated calcium channels, rather than via inhibition of adenylyl cyclase. Additionally, receptor activation blocks phosphorylation of p42/p44 MAPK and decreases MAPK/ERK kinase phosphorylation. Inhibition of MAPK appears to be mediated by c-Raf and B-Raf-dependent inhibition of MAPK/ERK kinase. Dopamine-stimulated growth hormone release from the pituitary gland is mediated by a decrease in intracellular calcium influx through voltage-gated calcium channels rather than via adenylyl cyclase inhibition. Stimulation of dopamine D2 receptors in the nigrostriatal pathway leads to improvements in coordinated muscle activity in those with movement disorders.
What should someone know about the safety or toxicity profile of Bromocriptine?
Bromocriptine can cause gastrointestinal effects such as nausea, vomiting, abdominal cramping, constipation, or diarrhea, which may appear with routine or excessive exposure. It may also produce orthostatic hypotension, light‑headedness, vertigo, and other CNS‑active symptoms, requiring measures to prevent acute blood pressure drops during handling. Hallucinations, impulse‑control symptoms, and rare fibrotic complications have been reported, consistent with its dopaminergic and serotonergic receptor activity. Pulmonary fibrosis has been associated with interactions at 5‑HT1B and 5‑HT2B receptors.
What are important formulation and handling considerations for Bromocriptine as an API?
Bromocriptine’s low aqueous solubility and lipophilic solid‑state properties favor use of solubility‑enhancing techniques or lipidic/controlled‑release matrices to achieve consistent dissolution and absorption. Formulations should remain robust under fed‑state conditions, as the drug is commonly taken with food to limit gastric irritation. Handling should minimize moisture exposure and support uniform dispersion to avoid variability in release.
Is Bromocriptine a small molecule?
Bromocriptine is classified as a small molecule. That classification shapes process design, impurity profiling, and analytical control strategies.
Are there special stability concerns for oral Bromocriptine?
Oral Bromocriptine has low aqueous solubility, so formulations must address dissolution to ensure consistent exposure. Its lipophilicity can influence solid‑state stability and may favor lipidic or controlled‑release matrices. Because it is typically taken with food to reduce gastric irritation, the formulation should remain stable and perform consistently under fed‑state gastrointestinal conditions.

Regulatory

Where is Bromocriptine approved or in use globally?
Bromocriptine is reported as approved in the following major regions: Canada, US. Understanding geographic coverage informs regulatory filings, supply planning, and risk assessments before escalating procurement.
What’s the regulatory and patent landscape for Bromocriptine right now?
Bromocriptine is regulated for use in both Canada and the United States, where it is subject to the standard national requirements for active pharmaceutical ingredients. Patent considerations follow the respective legal frameworks in these jurisdictions, with protection and exclusivity governed by each country’s established pharmaceutical patent systems.

Pharmaoffer

How does Pharmaoffer’s Smart Sourcing Service help with Bromocriptine procurement?
Pharmaoffer's Smart Sourcing Service coordinates compliant suppliers, documentation, and competitive quotes for Bromocriptine. It centralizes outreach, follow-ups, and document validation to shorten procurement timelines.
Is Bromocriptine included in the PRO Data Insights coverage?
PRO Data Insights coverage for Bromocriptine: 176 verified transactions across 58 suppliers and 45 buyers worldwide. Use the dataset to benchmark suppliers and monitor regulatory activity where available.
Where can I access the API market report for Bromocriptine?
Market report availability for Bromocriptine: Report Available. The report highlights demand trends, pricing drivers, and supplier landscape insights for procurement planning.