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Bromocriptine mesylate

Bromocriptine mesylate structure

CAS No:
22260-51-1
Formula:
C32H40BrN5O5.CH4O3S
Chemical Name:
Bromocriptine mesylate
Synonyms:
Ergotaman-3′,6′,18-trione,2-bromo-12′-hydroxy-2′-(1-methylethyl)-5′-(2-methylpropyl)-,(5α)-,methanesulfonate (1:1);Ergocryptine,2-bromo-,monomethanesulfonate (salt);Ergotaman-3′,6′,18-trione,2-bromo-12′-hydroxy-2′-(1-methylethyl)-5′-(2-methylpropyl)-,(5′α)-,monomethanesulfonate (salt);Indolo[4,3-fg]quinoline,ergotaman-3′,6′,18-trione deriv.;8H-Oxazolo[3,2-a]pyrrolo[2,1-c]pyrazine,ergotaman-3′,6′,18-trione deriv.;Bromocriptine mesylate;Bromocriptine methanesulfonate;Parlodel;Bromocryptine mesylate;CB 154;Bromocryptine methanesulfonate;Pravidel;Bagren;(+)-Bromocriptine methanesulfonate;Cycloset;127931-10-6;25614-04-4;35925-33-8;58181-56-9;71185-16-5
Categories:
Active Pharmaceutical Ingredients > Nervous System Drugs

Description

Bromocriptine mesylate is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pKi of 8.05±0.2.

Bromocriptine methanesulfonate is a methanesulfonate salt. It has a role as an antiparkinson drug. It contains a bromocriptine.|Bromocriptine Mesylate is the mesylate salt of bromocriptine, a semisynthetic ergot alkaloid with dopaminergic, antidyskinetic, and antiprolactinemic activities. Bromocriptine selectively binds to and activates postsynaptic dopamine D2 receptors in the corpus striatum of the central nervous system (CNS). Activation of these D2 receptors activate inhibitory G-proteins, which inhibit adenylyl cyclase, preventing signal transduction mediated via cAMP and resulting in the inhibition of neurotransmission and an antidyskinetic effect. This agent also stimulates dopamine D2 receptors in the anterior pituitary gland, which results in the inhibition of prolactin secretion and lactation and may inhibit the proliferation of prolactin-dependent breast cancer cells.|A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.

Bromocriptine mesylate Basic Attributes

Molecular Weight：

750.7

Exact Mass：

749.209412

EC Number：

244-881-1

UNII：

FFP983J3OD

NSC Number：

169774

DSSTox ID：

DTXSID6020197

NCI Thesaurus Code：

C317

HScode：

29396900

Characteristics

PSA：

180.96000

XLogP3：

3.98220

Appearance：

white solid

Melting Point：

192-196 °C (decomp)

Boiling Point：

891.3ºC at 760 mmHg

Flash Point：

492.8ºC

Water Solubility：

H2O: 0.8 mg/mL

Storage Conditions：

2-8°C

Vapor Pressure：

0mmHg at 25°C

Toxicity：

Oral-Mouse LD50: 2502 mg/kg; Intravenous-rat LD50: 10.5 mg/kg

Flammability characteristics：

Thermal decomposition emits toxic nitrogen oxides, sulfur oxides and bromide fumes

Specific rotation：

D20 +95° (c = 1 in methanol-methylene chloride)

Collision Cross Section：

244.4 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Packing level：

Ⅲ

Transport codes：

UN 3077 9 / PGIII

wgk germany：

hazard class code：

20/21/22

safety instructions：

22-24/25-36

RTECS Number：

KE1595000

Marks：

Storage features：

Warehouse ventilated, dry and low temperature

Precautionary statement(s)：

P301 + P312 + P330

Hazard Statements：

H302-H410

GHS Classification：

|Warning|H302 (45.45%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P260, P261, P263, P264, P270, P271, P273, P281, P301+P312, P304+P312, P304+P340, P308+P313, P312, P330, P391, P405, and P501|Aggregated GHS information provided by 11 companies from 6 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Toxicity class：

moderately toxic

Drug Information

MeSH：

Agents used in the treatment of Parkinson's disease. The most commonly used drugs act on the dopaminergic system in the striatum and basal ganglia or are centrally acting muscarinic antagonists. (See all compounds classified as Antiparkinson Agents.)|Drugs that bind to and activate dopamine receptors. (See all compounds classified as Dopamine Agonists.)|Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites. (See all compounds classified as Hormone Antagonists.)

MeSH Entry Terms：

2 Bromo alpha ergocryptine

Bromocriptine mesylate Use and Manufacturing

Uses

Dopamine receptor agonist; derivative of the ergotoxin group of ergot alkaloids. Prolactin inhibitor; antiparkinsonian.

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:750.7
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:9
Rotatable Bond Count:5
Exact Mass:749.20940
Monoisotopic Mass:749.20940
Topological Polar Surface Area:181
Heavy Atom Count:48
Complexity:1320
Defined Atom Stereocenter Count:6
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

It is an agonist of dopamine receptors in the hypothalamus and pituitary gland, which can reduce the secretion of prolactin, restore normal menstrual cycles, treat reproductive dysfunction related to hyperprolactinemia, and prevent and reduce milk secretion. For patients with acromegaly, it can reduce their growth hormone levels and have a favorable effect on their clinical symptoms and glucose tolerance. Based on its dopaminergic activity, it can promote the release of endogenous dopamine from activated presynaptic nigrostriatal neurons and selectively stimulate postsynaptic receptors at the same time.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Bromocriptine Mesylate Tablets
Ingredients	Bromocriptine mesylate.
Indication	Bromocriptine is metabolized by the cytochrome P450 (CYP3A) enzyme system. Combination with macrolide antibiotics (such as erythromycin, clarithromycin, troleandomycin, spiramycin, josamycin), azole antifungal drugs (such as ketoconazole, itraconazole) or cytochrome P450 enzyme inhibitors (such as cimetidine) may increase the risk of adverse reactions due to increased blood concentrations of bromocriptine. It has been reported that combined use with octreotide can increase the blood concentration of bromocriptine, thereby increasing the risk of adverse reactions. Therefore, combined use with octreotide should be avoided. Combination with methylergonovine or other ergot alkaloids may increase the risk of adverse reactions, so combined use should be avoided. Alcohol can reduce the tolerance of bromocriptine.
Specifications	2.5 mg

Bromocriptine Mesylate Tablets
Ingredients	The active ingredient of this product and its chemical name: Bromocriptine mesylate.
Indication	When using this product, please use the following drugs with caution: 1. Erythromycin (the serum concentration of bromocriptine mesylate tablets may increase); 2. Dopamine antagonists such as phenylpropion and phenothiazines (may reduce the effect of bromocriptine mesylate tablets). 3. Antipsychotic drugs (hyperprolactinemia antagonists). 4. Smooth muscle antispasmodics "Isometheptene" (increase the toxicity of bromocriptine mesylate tablets). 5. Macrolide antibiotics (may increase the plasma concentration of bromocriptine mesylate tablets, thereby possibly increasing its toxicity). 6. Somatostatin octapeptide (increase the concentration of bromocriptine mesylate tablets). 7. Phenylpropanol (increase the toxicity of bromocriptine mesylate tablets). Avoid simultaneous use with other ergot alkaloid derivatives.
Specifications	2.5 mg

Bromocriptine Mesylate Tablets
Ingredients	Bromocriptine mesylate
Indication	When using this product, please use the following drugs with caution: 1. Erythromycin (the serum concentration of bromocriptine mesylate tablets may increase); 2. Dopamine antagonists such as phenylpropion and phenothiazines (may reduce the effect of bromocriptine mesylate tablets); 3. Antipsychotics (antagonists of hyperprolactinemia); 4. Smooth muscle spasmolytics isometheptene (increases the toxicity of bromocriptine mesylate tablets); 5. Macrolide antibiotics (may increase the plasma concentration of bromocriptine mesylate tablets, thereby possibly increasing its toxicity); 6. Somatostatin octapeptide (increases the concentration of bromocriptine mesylate tablets); 7. Phenylpropanolamine (increases the toxicity of bromocriptine mesylate tablets); 8. Avoid simultaneous use with other ergot alkaloid derivatives.
Specifications	2.5 mg

Registered Holders

CURIA Italy SRL

United States
Active
TAPI NL B.V.

France
Active
Taipei (Beijing) Pharmaceutical Technology Co., Ltd.

China
Active

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