BROMOCRIPTINE MESYLATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C32H40BrN5O5.CH4O3S
Molecular Weight	750.7
Optical Activity	UNSPECIFIED
Defined Stereocenters	6 / 6
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CS(O)(=O)=O.CC(C)C[C@@H]1N2C(=O)[C@](NC(=O)[C@H]3CN(C)[C@@H]4CC5=C(Br)NC6=CC=CC(=C56)C4=C3)(O[C@@]2(O)[C@@H]7CCCN7C1=O)C(C)C

InChI

InChIKey=NOJMTMIRQRDZMT-GSPXQYRGSA-N

InChI=1S/C32H40BrN5O5.CH4O3S/c1-16(2)12-24-29(40)37-11-7-10-25(37)32(42)38(24)30(41)31(43-32,17(3)4)35-28(39)18-13-20-19-8-6-9-22-26(19)21(27(33)34-22)14-23(20)36(5)15-18;1-5(2,3)4/h6,8-9,13,16-18,23-25,34,42H,7,10-12,14-15H2,1-5H3,(H,35,39);1H3,(H,2,3,4)/t18-,23-,24+,25+,31-,32+;/m1./s1

HIDE SMILES / InChI

Molecular Formula	CH4O3S
Molecular Weight	96.106
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C32H40BrN5O5
Molecular Weight	654.594
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	6 / 6
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/017962s065s068lbl.pdf
Curator's Comment: description was created based on several sources, including: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020866lbl.pdf | https://www.drugs.com/mtm/bromocriptine.html

Bromocriptine is an ergot derivative with potent dopamine receptor agonist activity, which activates post-synaptic dopamine receptors. Bromocriptine is indicated for the treatment of dysfunctions associated with hyperprolactinemia. Bromocriptine therapy is indicated in the treatment of acromegaly and in the treatment of the signs and symptoms of idiopathic or postencephalitic Parkinson’s disease. It is approved as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Some commonly reported adverse reactions include nausea, fatigue, dizziness, vomiting and headache. Bromocriptine may interact with dopamine antagonists, butyrophenones and certain other agents.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Dopamine D2 receptor 311 Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8787038	Agonist 2752	36.0 nM [Ki]
Dopamine D3 receptor 97 Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8787038	Agonist 2752	197.0 nM [Ki]
Dopamine D1 receptor 106 Target ID: CHEMBL2056 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8787038	Agonist 2752	2.2 µM [Ki]
Adrenergic receptor alpha-2 114 Target ID: CHEMBL2093864 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20138024	Activator 1447

Conditions

Condition	Modality	Highest Phase	Product
Parkinson's disease 232 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/017962s065s068lbl.pdf	Palliative	Approved 8583	PARLODEL Approved Use Hyperprolactinemia-Associated Dysfunctions Bromocriptine mesylate tablets are indicated for the treatment of dysfunctions associated with hyperprolactinemia including amenorrhea with or without galactorrhea, infertility or hypogonadism. Bromocriptine mesylate tablets treatment is indicated in patients with prolactin-secreting adenomas, which may be the basic underlying endocrinopathy contributing to the above clinical presentations. Reduction in tumor size has been demonstrated in both male and female patients with macroadenomas. In cases where adenectomy is elected, a course of bromocriptine mesylate tablets therapy may be used to reduce the tumor mass prior to surgery. Acromegaly Bromocriptine mesylate tablets therapy is indicated in the treatment of acromegaly. Bromocriptine mesylate tablets therapy, alone or as adjunctive therapy with pituitary irradiation or surgery, reduces serum growth hormone by 50% or more in approximately ½ of patients treated, although not usually to normal levels. Since the effects of external pituitary radiation may not become maximal for several years, adjunctive therapy with bromocriptine mesylate tablets offers potential benefit before the effects of irradiation are manifested. Parkinson's Disease Bromocriptine mesylate tablets are indicated in the treatment of the signs and symptoms of idiopathic or postencephalitic Parkinson's disease. As adjunctive treatment to levodopa (alone or with a peripheral decarboxylase inhibitor), bromocriptine mesylate tablets therapy may provide additional therapeutic benefits in those patients who are currently maintained on optimal dosages of levodopa, those who are beginning to deteriorate (develop tolerance) to levodopa therapy, and those who are experiencing end of dose failure on levodopa therapy. Bromocriptine mesylate tablets therapy may permit a reduction of the maintenance dose of levodopa and, thus may ameliorate the occurrence and/or severity of adverse reactions associated with long-term levodopa therapy such as abnormal involuntary movements (e.g., dyskinesias) and the marked swings in motor function (on-off phenomenon). Continued efficacy of bromocriptine mesylate tablets therapy during treatment of more than 2 years has not been established. Data are insufficient to evaluate potential benefit from treating newly diagnosed Parkinson's disease with bromocriptine mesylate tablets. Studies have shown, however, significantly more adverse reactions (notably nausea, hallucinations, confusion and hypotension) in bromocriptine mesylate treated patients than in levodopa/carbidopa treated patients. Patients unresponsive to levodopa are poor candidates for bromocriptine mesylate tablets therapy. Launch Date 1978
Acromegaly 21 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/017962s065s068lbl.pdf	Primary	Approved 8583	PARLODEL Approved Use Hyperprolactinemia-Associated Dysfunctions Bromocriptine mesylate tablets are indicated for the treatment of dysfunctions associated with hyperprolactinemia including amenorrhea with or without galactorrhea, infertility or hypogonadism. Bromocriptine mesylate tablets treatment is indicated in patients with prolactin-secreting adenomas, which may be the basic underlying endocrinopathy contributing to the above clinical presentations. Reduction in tumor size has been demonstrated in both male and female patients with macroadenomas. In cases where adenectomy is elected, a course of bromocriptine mesylate tablets therapy may be used to reduce the tumor mass prior to surgery. Acromegaly Bromocriptine mesylate tablets therapy is indicated in the treatment of acromegaly. Bromocriptine mesylate tablets therapy, alone or as adjunctive therapy with pituitary irradiation or surgery, reduces serum growth hormone by 50% or more in approximately ½ of patients treated, although not usually to normal levels. Since the effects of external pituitary radiation may not become maximal for several years, adjunctive therapy with bromocriptine mesylate tablets offers potential benefit before the effects of irradiation are manifested. Parkinson's Disease Bromocriptine mesylate tablets are indicated in the treatment of the signs and symptoms of idiopathic or postencephalitic Parkinson's disease. As adjunctive treatment to levodopa (alone or with a peripheral decarboxylase inhibitor), bromocriptine mesylate tablets therapy may provide additional therapeutic benefits in those patients who are currently maintained on optimal dosages of levodopa, those who are beginning to deteriorate (develop tolerance) to levodopa therapy, and those who are experiencing end of dose failure on levodopa therapy. Bromocriptine mesylate tablets therapy may permit a reduction of the maintenance dose of levodopa and, thus may ameliorate the occurrence and/or severity of adverse reactions associated with long-term levodopa therapy such as abnormal involuntary movements (e.g., dyskinesias) and the marked swings in motor function (on-off phenomenon). Continued efficacy of bromocriptine mesylate tablets therapy during treatment of more than 2 years has not been established. Data are insufficient to evaluate potential benefit from treating newly diagnosed Parkinson's disease with bromocriptine mesylate tablets. Studies have shown, however, significantly more adverse reactions (notably nausea, hallucinations, confusion and hypotension) in bromocriptine mesylate treated patients than in levodopa/carbidopa treated patients. Patients unresponsive to levodopa are poor candidates for bromocriptine mesylate tablets therapy. Launch Date 1978
Hyperprolactinemia-associated dysfunctions 2 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/017962s065s068lbl.pdf	Primary	Approved 8583	PARLODEL Approved Use Hyperprolactinemia-Associated Dysfunctions Bromocriptine mesylate tablets are indicated for the treatment of dysfunctions associated with hyperprolactinemia including amenorrhea with or without galactorrhea, infertility or hypogonadism. Bromocriptine mesylate tablets treatment is indicated in patients with prolactin-secreting adenomas, which may be the basic underlying endocrinopathy contributing to the above clinical presentations. Reduction in tumor size has been demonstrated in both male and female patients with macroadenomas. In cases where adenectomy is elected, a course of bromocriptine mesylate tablets therapy may be used to reduce the tumor mass prior to surgery. Acromegaly Bromocriptine mesylate tablets therapy is indicated in the treatment of acromegaly. Bromocriptine mesylate tablets therapy, alone or as adjunctive therapy with pituitary irradiation or surgery, reduces serum growth hormone by 50% or more in approximately ½ of patients treated, although not usually to normal levels. Since the effects of external pituitary radiation may not become maximal for several years, adjunctive therapy with bromocriptine mesylate tablets offers potential benefit before the effects of irradiation are manifested. Parkinson's Disease Bromocriptine mesylate tablets are indicated in the treatment of the signs and symptoms of idiopathic or postencephalitic Parkinson's disease. As adjunctive treatment to levodopa (alone or with a peripheral decarboxylase inhibitor), bromocriptine mesylate tablets therapy may provide additional therapeutic benefits in those patients who are currently maintained on optimal dosages of levodopa, those who are beginning to deteriorate (develop tolerance) to levodopa therapy, and those who are experiencing end of dose failure on levodopa therapy. Bromocriptine mesylate tablets therapy may permit a reduction of the maintenance dose of levodopa and, thus may ameliorate the occurrence and/or severity of adverse reactions associated with long-term levodopa therapy such as abnormal involuntary movements (e.g., dyskinesias) and the marked swings in motor function (on-off phenomenon). Continued efficacy of bromocriptine mesylate tablets therapy during treatment of more than 2 years has not been established. Data are insufficient to evaluate potential benefit from treating newly diagnosed Parkinson's disease with bromocriptine mesylate tablets. Studies have shown, however, significantly more adverse reactions (notably nausea, hallucinations, confusion and hypotension) in bromocriptine mesylate treated patients than in levodopa/carbidopa treated patients. Patients unresponsive to levodopa are poor candidates for bromocriptine mesylate tablets therapy. Launch Date 1978
Type 2 diabetes mellitus 262 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020866lbl.pdf	Primary	Approved 8583	CYCLOSET Approved Use Drug is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Launch Date 2009

C_max

Value	Dose	Co-administered	Analyte	Population
628 pg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/017962s081lbl.pdf	5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BROMOCRIPTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
2377 pg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/017962s081lbl.pdf	5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BROMOCRIPTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
4.85 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/017962s081lbl.pdf	5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BROMOCRIPTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
4% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/017962s081lbl.pdf	5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BROMOCRIPTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
4.8 mg 1 times / day multiple, oral Recommended Dose: 4.8 mg, 1 times / day Route: oral Route: multiple Dose: 4.8 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020866s006s007lbl.pdf	unhealthy, 27-80 Health Status: unhealthy Age Group: 27-80 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020866s006s007lbl.pdf	Disc. AE: Nausea... AEs leading to discontinuation/dose reduction: Nausea Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020866s006s007lbl.pdf
4.8 mg 1 times / day multiple, oral MTD Dose: 4.8 mg, 1 times / day Route: oral Route: multiple Dose: 4.8 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/11139820	unhealthy, 55+/-1 Health Status: unhealthy Age Group: 55+/-1 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11139820	Disc. AE: Nausea, Dizziness... AEs leading to discontinuation/dose reduction: Nausea (4%) Dizziness (2.8%) Asthenia (1.5%) Rhinitis (1.5%) Sources: https://pubmed.ncbi.nlm.nih.gov/11139820
4.8 mg 1 times / day multiple, oral MTD Dose: 4.8 mg, 1 times / day Route: oral Route: multiple Dose: 4.8 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20332352	unhealthy, 59.5 +/- 10.2 Health Status: unhealthy Age Group: 59.5 +/- 10.2 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/20332352	Disc. AE: Nausea... AEs leading to discontinuation/dose reduction: Nausea Sources: https://pubmed.ncbi.nlm.nih.gov/20332352
100 mg 1 times / day multiple, oral Highest studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2758194 https://www.healthline.com/health/bromocriptine-oral-tablet#about	unhealthy Health Status: unhealthy Sources: https://pubmed.ncbi.nlm.nih.gov/2758194 https://www.healthline.com/health/bromocriptine-oral-tablet#about	Sources: https://pubmed.ncbi.nlm.nih.gov/2758194 https://www.healthline.com/health/bromocriptine-oral-tablet#about
300 mg single, oral Highest studied dose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: https://pubmed.ncbi.nlm.nih.gov/22216518	unhealthy Health Status: unhealthy Sources: https://pubmed.ncbi.nlm.nih.gov/22216518	Sources: https://pubmed.ncbi.nlm.nih.gov/22216518
30 mg 1 times / day multiple, oral Recommended Dose: 30 mg, 1 times / day Route: oral Route: multiple Dose: 30 mg, 1 times / day Sources: https://www.medicines.org.uk/emc/product/1202/smpc#POSOLOGY	unhealthy Health Status: unhealthy Sources: https://www.medicines.org.uk/emc/product/1202/smpc#POSOLOGY	Sources: https://www.medicines.org.uk/emc/product/1202/smpc#POSOLOGY

AEs

AE	Significance	Dose	Population
Nausea	Disc. AE	4.8 mg 1 times / day multiple, oral Recommended Dose: 4.8 mg, 1 times / day Route: oral Route: multiple Dose: 4.8 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020866s006s007lbl.pdf	unhealthy, 27-80 Health Status: unhealthy Age Group: 27-80 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020866s006s007lbl.pdf
Asthenia	1.5% Disc. AE	4.8 mg 1 times / day multiple, oral MTD Dose: 4.8 mg, 1 times / day Route: oral Route: multiple Dose: 4.8 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/11139820	unhealthy, 55+/-1 Health Status: unhealthy Age Group: 55+/-1 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11139820
Rhinitis	1.5% Disc. AE	4.8 mg 1 times / day multiple, oral MTD Dose: 4.8 mg, 1 times / day Route: oral Route: multiple Dose: 4.8 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/11139820	unhealthy, 55+/-1 Health Status: unhealthy Age Group: 55+/-1 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11139820
Dizziness	2.8% Disc. AE	4.8 mg 1 times / day multiple, oral MTD Dose: 4.8 mg, 1 times / day Route: oral Route: multiple Dose: 4.8 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/11139820	unhealthy, 55+/-1 Health Status: unhealthy Age Group: 55+/-1 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11139820
Nausea	4% Disc. AE	4.8 mg 1 times / day multiple, oral MTD Dose: 4.8 mg, 1 times / day Route: oral Route: multiple Dose: 4.8 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/11139820	unhealthy, 55+/-1 Health Status: unhealthy Age Group: 55+/-1 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11139820
Nausea	Disc. AE	4.8 mg 1 times / day multiple, oral MTD Dose: 4.8 mg, 1 times / day Route: oral Route: multiple Dose: 4.8 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20332352	unhealthy, 59.5 +/- 10.2 Health Status: unhealthy Age Group: 59.5 +/- 10.2 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/20332352

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 substrate 1946		substrate 1388

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1741	CYP3A 220 CYP2C8 810 CYP2C19 1119 CYP4A11 137 OATP1A2 67 OATP2B1 122 P-gp 2052	P-gp 301

Drug as perpetrator

Target	Modality	Activity
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/017962s081lbl.pdf	yes [IC50 1.69 uM]
P-gp 1932	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/11856485/; https://pubmed.ncbi.nlm.nih.gov/9514944/; https://pubmed.ncbi.nlm.nih.gov/18598736/	yes [Ki 6.52 uM]
P-gp 1932	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/9111066/	yes

Drug as victim

Target	Modality	Activity
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/017962s081lbl.pdf Page: 3.0	inconclusive
CYP2C8 810	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/31147443/	likely
CYP2D6 1388	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/31147443/	likely
CYP4A11 137	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/31147443/	likely
CYP3A 220	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/017962s081lbl.pdf Page: 3.0	yes
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/020866Orig1s000ClinPharmR.pdf Page: 26.0	yes
OATP1A2 67	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/32343897/	yes
OATP2B1 122	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/32343897/	yes
P-gp 2052	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/16263252/	yes

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:3181	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:3181
ChemicalBook	CB6136426	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB6136426
eMolecules	1933648	https://www.emolecules.com/cgi-bin/more?vid=1933648
eMolecules	36518002	https://www.emolecules.com/cgi-bin/more?vid=36518002
ZINC	ZINC000053683151	http://zinc15.docking.org/substances/ZINC000053683151

PubMed

Title	Date	PubMed
Differential signalling of both wild-type and Thr(343)Arg dopamine D(2short) receptor by partial agonists in a G-protein-dependent manner.	2001-09-15	11551517
Neuroendocrine effects of d-fenfluramine and bromocriptine following repeated smoked cocaine in humans.	2001-09-01	11470342
Dopamine D(2) receptor activation causes mitogenesis via p44/42 mitogen-activated protein kinase in opossum kidney cells.	2001-09	11518777
Prolactin actions in the sheep testis: a test of the priming hypothesis.	2001-09	11514361
Bromocriptine in rheumatic and autoimmune diseases.	2001-08	11503136
Effects of dopamine d2 receptor agonists in a pituitary transplantation-induced hyperprolactinaemia/anovulation model in rats.	2001-08	11473532
Luteolytic effect of prolactin is dependent on the degree of differentiation of luteal cells in the rat.	2001-08	11466211
Upregulation of lymphocyte apoptosis as a strategy for preventing and treating autoimmune disorders: a role for whole-food vegan diets, fish oil and dopamine agonists.	2001-08	11461185
[Cerebral meningeal hemorrhage and acute cerebral angiopathy associated with the taking of phenylpropanolamine: a new case].	2001-07-31	11475816
Rehabilitative management of post-stroke visuospatial inattention.	2001-07-10	11400902
Androgen suppression and clinical improvement with dopamine agonists in hyperandrogenic-hyperprolactinemic women.	2001-07	11499189
Hepatic Encephalopathy.	2001-07	11467622
Centrally mediated effects of bromocriptine on cardiac sympathovagal balance.	2001-07	11463772
Functional characterization of basolateral and luminal dopamine receptors in rabbit CCD.	2001-07	11399652
Biphasic effects of 7-OH-DPAT on the acquisition of responding for conditioned reward in rats.	2001-06-23	11420086
Sleep attacks and antiparkinsonian drugs: a pilot prospective pharmacoepidemiologic study.	2001-06-08	11391132
Double-blind, crossover, placebo-controlled trial of bromocriptine in patients with sleep bruxism.	2001-06-08	11391125
Microvessel density in pituitary adenomas and carcinomas.	2001-06	11469692
Effect of serotonin depletion by p-chlorophenylalanine on serum prolactin levels in estrogen-treated ovariectomized rats: insights concerning the serotoninergic, dopaminergic and opioid systems.	2001-06	11456281
[Pharmacological effects of cabergoline against parkinsonism].	2001-06	11436517
Pituitary prolactin-secreting macroadenoma combined with bilateral breast cancer in a 45-year-old male.	2001-06	11434671
Neuroleptic malignant syndrome during a change from haloperidol to risperidone.	2001-06	11408988
Estrogen, prolactin, and autoimmunity: actions and interactions.	2001-06	11407318
Cerebrospinal fluid fistula as the presenting manifestation of pituitary adenoma: case report with a 4-year follow-up.	2001-06	11400039
Laboratory and clinical experience in 55 patients with macroprolactinemia identified by a simple polyethylene glycol precipitation method.	2001-06	11397880
Study of the change of prolactin and progesterone during dopaminergic agonist treatments in pseudopregnant bitches.	2001-05-31	11348786
[Reversible blindness caused by an invasive prolactinoma].	2001-05-25	11413749
Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism.	2001-05-18	11412837
Fertile estrus induced in bitches by bromocryptine, a dopamine agonist: a clinical trial.	2001-05-01	11393217
[A-56-year-old woman with parkinsonism, whose mother had Parkinson's disease].	2001-05	11428377
Central bromocriptine-induced tachycardia is reversed to bradycardia in conscious, deoxycorticosterone acetate-salt hypertensive rats.	2001-05	11393583
Clinical, endocrinological and radiography features in a child with McCune-Albright syndrome and pituitary adenoma.	2001-05	11393578
Long-term mortality results of the randomized controlled study comparing bromocriptine to which levodopa was later added with levodopa alone in previously untreated patients with Parkinson's disease.	2001-05	11391747
Pituitary tumours in adolescence: clinical behaviour and neuroimaging features of seven cases.	2001-05	11386796
Increased responsiveness to the hyperglycemic, hyperglucagonemic and hyperinsulinemic effects of circulating norepinephrine in ob/ob mice.	2001-05	11360153
Neostriatal muscarinic receptor subtypes involved in the generation of tremulous jaw movements in rodents implications for cholinergic involvement in parkinsonism.	2001-04-27	11392629
Polysomnographic measures in Parkinson's disease: a comparison between patients with and without REM sleep disturbances.	2001-04-17	11383385
Dopamine D2 receptor gene expression in human adenohypophysial adenomas.	2001-04	11444429
Cyclophosphamide plus somatostatin, bromocriptin, retinoids, melatonin and ACTH in the treatment of low-grade non-Hodgkin's lymphomas at advanced stage: results of a phase II trial.	2001-04	11385964
[Increased T1 signal of the residual normal anterior pituitary gland following medical treatment of pituitary prolactinoma].	2001-04	11353909
The role of hypertension in bromocriptine-related puerperal intracranial hemorrhage.	2001-04	11338413
Alpha-dihydroergocryptine and predictive factors in migraine prophylaxis.	2001-04	11332869
Efficacy and tolerability of dopamine agonists in a parkinsonian population.	2001-02	11487183
Neuroleptic malignant syndrome without neuroleptics.	2001-02	11358199
Clinical management of neuroleptic malignant syndrome.	2001	11525080
Clinical features and medical treatment of male prolactinomas.	2001	11482696
Are dopamine receptor agonists neuroprotective in Parkinson's disease?	2001	11419913
Pregnancy in hyperprolactinemic infertile women treated with vaginal bromocriptine: report of two cases and review of the literature.	2001	11408739
Dopamine agonists.	2001	11346030
Efficacy of monochemotherapy with docetaxel (taxotere) in relation to prolactin secretion in heavily pretreated metastatic breast cancer.	2001	11335876

Patents

Sample Use Guides

In Vivo Use Guide

Type 2 diabetes mellitus: Initial dose is one tablet (0.8 mg) daily increased weekly by one tablet until maximal tolerated daily dose of 1.6 to 4.8 mg is achieved. Hyperprolactinemic Indications: The initial dosage in adults is ½ to one 2½ mg scored tablet daily. An additional 2½ mg tablet may be added to the treatment regimen as tolerated every 2-7 days until an optimal therapeutic response is achieved. The therapeutic dosage ranged from 2.5-15 mg daily in adults studied clinically. Parkinson’s Disease: The initial dose is ½ of a 2½ mg twice daily with meals. Assessments are advised at 2-week intervals during dosage titration to ensure that the lowest dosage producing an optimal therapeutic response is not exceeded. If necessary, the dosage may be increased every 14-28 days by 2½ mg/day with meals.

Route of Administration: Oral

In Vitro Use Guide

Bromocriptine has been shown to augment glutamate uptake at a concentration of 10 uM in HeLaS3 cells that stably express EAAT1, the human homolog of GLAST. Therefore, it was evaluated whether bromocriptine affects D-[3 H]aspartate uptake in HEK293/EcR cells expressing EAAT2. However, bromocriptine failed to alter D-[3 H]aspartate uptake at concentrations as high as 30 uM, suggesting that bromocriptine has little or no effect on the excitatory amino acid uptake via EAAT2.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 17:49:09 GMT 2025` Edited by `admin` on `Mon Mar 31 17:49:09 GMT 2025`
Record UNII	FFP983J3OD
Record Status	`Validated (UNII)`
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Name

Type

Language

BROMOCRIPTINE MESILATE

Preferred Name

English

BROMOCRIPTINE MESYLATE

Official Name

English

BROMOCRIPTINE MESILATE [JAN]

Common Name

English

BROMOCRIPTINE METHANESULFONATE [MI]

Common Name

English

BROMOCRIPTINE METHANESULFONATE

Common Name

English

PARLODEL

Brand Name

English

BROMOCRIPTINE MESYLATE [VANDF]

Common Name

English

Bromocriptine mesilate [WHO-DD]

Common Name

English

BROMOCRIPTINE MESILATE [EP MONOGRAPH]

Common Name

English

BROMOCRIPTINE MESYLATE [USP MONOGRAPH]

Common Name

English

BROMOCRIPTINE MESYLATE [USAN]

Common Name

English

2-BROMOERGOCRYPTINE MONOMETHANESULPHONATE (SALT)

Common Name

English

ERGOTAMAN-3',6',18-TRIONE, 2-BROMO-12'-HYDROXY-2'-(1-METHYLETHYL)-5'-(2-METHYLPROPYL)-, MONOMETHANESULFONATE (SALT), (5'.ALPHA.)-

Common Name

English

CB-154 MESILATE

Common Name

English

CYCLOSET

Brand Name

English

2-BROMOERGOCRYPTINE MESYLATE

Common Name

English

2-Bromoergocryptine monomethanesulfonate (salt)

Common Name

English

CB-154

Code

English

BROMOCRIPTINE MESYLATE [USP-RS]

Common Name

English

CB-154 MESYLATE

Code

English

NSC-755915

Code

English

ERGOTAMAN-3',6',18-TRIONE, 2-BROMO-12'-HYDROXY-2'-(1-METHYLETHYL)-5'-(2-METHYLPROPYL)-, MONOMETHANESULPHONATE (SALT), (5'.ALPHA.)-

Common Name

English

BROMOCRIPTINE MESYLATE [ORANGE BOOK]

Common Name

English

BROMOCRIPTINE MESILATE [MART.]

Common Name

English

Classification Tree Code System Code

CFR

21 CFR 216.24