BROMOCRIPTINE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C32H40BrN5O5
Molecular Weight	654.594
Optical Activity	UNSPECIFIED
Defined Stereocenters	6 / 6
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[H][C@@]12CCCN1C(=O)[C@H](CC(C)C)N3C(=O)[C@](NC(=O)[C@H]4CN(C)[C@]5([H])CC6=C(Br)NC7=C6C(=CC=C7)C5=C4)(O[C@@]23O)C(C)C

InChI

InChIKey=OZVBMTJYIDMWIL-AYFBDAFISA-N

InChI=1S/C32H40BrN5O5/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/h6,8-9,13,16-18,23-25,34,42H,7,10-12,14-15H2,1-5H3,(H,35,39)/t18-,23-,24+,25+,31-,32+/m1/s1

HIDE SMILES / InChI

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 297 Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8787038	Agonist 2662	36.0 nM [Ki]
Dopamine D3 receptor 91 Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8787038	Agonist 2662	197.0 nM [Ki]
Dopamine D1 receptor 101 Target ID: CHEMBL2056 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8787038	Agonist 2662	2.2 µM [Ki]
Adrenergic receptor alpha-2 113 Target ID: CHEMBL2093864 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20138024	Activator 1410

Conditions

Condition	Modality	Highest Phase	Product
Parkinson's disease 225 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/017962s065s068lbl.pdf	Palliative	Approved 8360	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 2.67839996E11
Acromegaly 20 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/017962s065s068lbl.pdf	Primary	Approved 8360	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 2.67839996E11
Hyperprolactinemia-associated dysfunctions 2 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/017962s065s068lbl.pdf	Primary	Approved 8360	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 2.67839996E11
Type 2 diabetes mellitus 256 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020866lbl.pdf	Primary	Approved 8360	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 1.24139523E12

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 (max) 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 Page: p.3	unhealthy, 27-80 n = 3070 Health Status: unhealthy Condition: Type 2 diabetes mellitus Age Group: 27-80 Sex: M+F Population Size: 3070 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020866s006s007lbl.pdf Page: p.3	Disc. AE: Nausea... AEs leading to discontinuation/dose reduction: Nausea Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020866s006s007lbl.pdf Page: p.3
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 Page: p.1691, 1699	unhealthy, 55+/-1 n = 314 Health Status: unhealthy Condition: Type 2 diabetes mellitus Age Group: 55+/-1 Sex: M+F Population Size: 314 Sources: https://pubmed.ncbi.nlm.nih.gov/11139820 Page: p.1691, 1699	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 Page: p.1691, 1699
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 Page: p.1505, 1507	unhealthy, 59.5 +/- 10.2 n = 2054 Health Status: unhealthy Condition: Type 2 diabetes mellitus Age Group: 59.5 +/- 10.2 Sex: M+F Population Size: 2054 Sources: https://pubmed.ncbi.nlm.nih.gov/20332352 Page: p.1505, 1507	Disc. AE: Nausea... AEs leading to discontinuation/dose reduction: Nausea Sources: https://pubmed.ncbi.nlm.nih.gov/20332352 Page: p.1505, 1507
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 Condition: Parkinson's Disease 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 Page: p.978	unhealthy n = 1 Health Status: unhealthy Condition: Parkinson's Disease Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/22216518 Page: p.978	Sources: https://pubmed.ncbi.nlm.nih.gov/22216518 Page: p.978
30 mg 1 times / day multiple, oral (total) 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 Condition: Prolactinomas\|Hypogonadism\|Galactorrhea syndromes\|Infertility 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 (max) 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 Page: p.3	unhealthy, 27-80 n = 3070 Health Status: unhealthy Condition: Type 2 diabetes mellitus Age Group: 27-80 Sex: M+F Population Size: 3070 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020866s006s007lbl.pdf Page: p.3
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 Page: p.1691, 1699	unhealthy, 55+/-1 n = 314 Health Status: unhealthy Condition: Type 2 diabetes mellitus Age Group: 55+/-1 Sex: M+F Population Size: 314 Sources: https://pubmed.ncbi.nlm.nih.gov/11139820 Page: p.1691, 1699
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 Page: p.1691, 1699	unhealthy, 55+/-1 n = 314 Health Status: unhealthy Condition: Type 2 diabetes mellitus Age Group: 55+/-1 Sex: M+F Population Size: 314 Sources: https://pubmed.ncbi.nlm.nih.gov/11139820 Page: p.1691, 1699
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 Page: p.1691, 1699	unhealthy, 55+/-1 n = 314 Health Status: unhealthy Condition: Type 2 diabetes mellitus Age Group: 55+/-1 Sex: M+F Population Size: 314 Sources: https://pubmed.ncbi.nlm.nih.gov/11139820 Page: p.1691, 1699
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 Page: p.1691, 1699	unhealthy, 55+/-1 n = 314 Health Status: unhealthy Condition: Type 2 diabetes mellitus Age Group: 55+/-1 Sex: M+F Population Size: 314 Sources: https://pubmed.ncbi.nlm.nih.gov/11139820 Page: p.1691, 1699
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 Page: p.1505, 1507	unhealthy, 59.5 +/- 10.2 n = 2054 Health Status: unhealthy Condition: Type 2 diabetes mellitus Age Group: 59.5 +/- 10.2 Sex: M+F Population Size: 2054 Sources: https://pubmed.ncbi.nlm.nih.gov/20332352 Page: p.1505, 1507

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 1579 substrate 1709		substrate 1193

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1437	CYP3A 189 CYP2C8 688 CYP2C19 985 CYP4A11 102 OATP1A2 61 OATP2B1 103 P-gp 1527	P-gp 257

Drug as perpetrator

Target	Modality	Activity
CYP3A4 1909	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/017962s081lbl.pdf	yes [IC50 1.69 uM]
P-gp 1626	inhibitor 3240 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 1626	inducer 1542 Sources: https://pubmed.ncbi.nlm.nih.gov/9111066/	yes

Drug as victim

Target	Modality	Activity
CYP2C19 985	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/017962s081lbl.pdf Page: 3.0	inconclusive
CYP2C8 688	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/31147443/	likely
CYP2D6 1193	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/31147443/	likely
CYP4A11 102	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/31147443/	likely
CYP3A 189	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/017962s081lbl.pdf Page: 3.0	yes
CYP3A4 1709	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/020866Orig1s000ClinPharmR.pdf Page: 26.0	yes
OATP1A2 61	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/32343897/	yes
OATP2B1 103	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/32343897/	yes
P-gp 1527	substrate 3326 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
ZINC	ZINC000053683151	http://zinc15.docking.org/substances/ZINC000053683151
eMolecules	1933648	https://www.emolecules.com/cgi-bin/more?vid=1933648
eMolecules	36518002	https://www.emolecules.com/cgi-bin/more?vid=36518002

PubMed

Title	Date	PubMed
Clinical features and medical treatment of male prolactinomas.	2001	11482696
Pregnancy in hyperprolactinemic infertile women treated with vaginal bromocriptine: report of two cases and review of the literature.	2001	11408739
Efficacy of monochemotherapy with docetaxel (taxotere) in relation to prolactin secretion in heavily pretreated metastatic breast cancer.	2001	11335876
Treatment of systemic lupus erythematosus with bromocriptine.	2001	11315352
Long-term persistence of symptomatic effect of selegiline in Parkinson's disease. A two-months placebo-controlled withdrawal study.	2001	11314774
Dopamine D2 receptor gene expression in human adenohypophysial adenomas.	2001 Apr	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 Apr	11385964
[Increased T1 signal of the residual normal anterior pituitary gland following medical treatment of pituitary prolactinoma].	2001 Apr	11353909
Alpha-dihydroergocryptine and predictive factors in migraine prophylaxis.	2001 Apr	11332869
Mechanisms of inverse agonism of antipsychotic drugs at the D(2) dopamine receptor: use of a mutant D(2) dopamine receptor that adopts the activated conformation.	2001 Apr	11299312
Polysomnographic measures in Parkinson's disease: a comparison between patients with and without REM sleep disturbances.	2001 Apr 17	11383385
Neostriatal muscarinic receptor subtypes involved in the generation of tremulous jaw movements in rodents implications for cholinergic involvement in parkinsonism.	2001 Apr 27	11392629
Bromocriptine in rheumatic and autoimmune diseases.	2001 Aug	11503136
Effects of dopamine d2 receptor agonists in a pituitary transplantation-induced hyperprolactinaemia/anovulation model in rats.	2001 Aug	11473532
Luteolytic effect of prolactin is dependent on the degree of differentiation of luteal cells in the rat.	2001 Aug	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 Aug	11461185
Efficacy and tolerability of dopamine agonists in a parkinsonian population.	2001 Feb	11487183
Neuroleptic malignant syndrome without neuroleptics.	2001 Feb	11358199
Dose-dependent augmentation effect of bromocriptine in a case with refractory depression.	2001 Feb	11294489
Androgen suppression and clinical improvement with dopamine agonists in hyperandrogenic-hyperprolactinemic women.	2001 Jul	11499189
Hepatic Encephalopathy.	2001 Jul	11467622
Centrally mediated effects of bromocriptine on cardiac sympathovagal balance.	2001 Jul	11463772
Functional characterization of basolateral and luminal dopamine receptors in rabbit CCD.	2001 Jul	11399652
Rehabilitative management of post-stroke visuospatial inattention.	2001 Jul 10	11400902
Microvessel density in pituitary adenomas and carcinomas.	2001 Jun	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 Jun	11456281
[Pharmacological effects of cabergoline against parkinsonism].	2001 Jun	11436517
Pituitary prolactin-secreting macroadenoma combined with bilateral breast cancer in a 45-year-old male.	2001 Jun	11434671
Neuroleptic malignant syndrome during a change from haloperidol to risperidone.	2001 Jun	11408988
Estrogen, prolactin, and autoimmunity: actions and interactions.	2001 Jun	11407318
Cerebrospinal fluid fistula as the presenting manifestation of pituitary adenoma: case report with a 4-year follow-up.	2001 Jun	11400039
Laboratory and clinical experience in 55 patients with macroprolactinemia identified by a simple polyethylene glycol precipitation method.	2001 Jun	11397880
The effect of prolactin and bromocriptine on human peripheral immune status.	2001 Mar	11314742
[A-56-year-old woman with parkinsonism, whose mother had Parkinson's disease].	2001 May	11428377
Central bromocriptine-induced tachycardia is reversed to bradycardia in conscious, deoxycorticosterone acetate-salt hypertensive rats.	2001 May	11393583
Clinical, endocrinological and radiography features in a child with McCune-Albright syndrome and pituitary adenoma.	2001 May	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 May	11391747
Pituitary tumours in adolescence: clinical behaviour and neuroimaging features of seven cases.	2001 May	11386796
Increased responsiveness to the hyperglycemic, hyperglucagonemic and hyperinsulinemic effects of circulating norepinephrine in ob/ob mice.	2001 May	11360153
Cannabinoid CB(1) receptor agonists produce cerebellar dysfunction in mice.	2001 May	11303052
Fertile estrus induced in bitches by bromocryptine, a dopamine agonist: a clinical trial.	2001 May 1	11393217
Study of the change of prolactin and progesterone during dopaminergic agonist treatments in pseudopregnant bitches.	2001 May 31	11348786
[Cerebral meningeal hemorrhage and acute cerebral angiopathy associated with the taking of phenylpropanolamine: a new case].	2001 May-Jun	11475816
Sleep attacks and antiparkinsonian drugs: a pilot prospective pharmacoepidemiologic study.	2001 May-Jun	11391132
Double-blind, crossover, placebo-controlled trial of bromocriptine in patients with sleep bruxism.	2001 May-Jun	11391125
Dopamine D(2) receptor activation causes mitogenesis via p44/42 mitogen-activated protein kinase in opossum kidney cells.	2001 Sep	11518777
Prolactin actions in the sheep testis: a test of the priming hypothesis.	2001 Sep	11514361
Neuroendocrine effects of d-fenfluramine and bromocriptine following repeated smoked cocaine in humans.	2001 Sep 1	11470342
Differential signalling of both wild-type and Thr(343)Arg dopamine D(2short) receptor by partial agonists in a G-protein-dependent manner.	2001 Sep 15	11551517
Clinical management of neuroleptic malignant syndrome.	2001 Winter	11525080

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 `Thu Jul 06 22:31:38 UTC 2023` Edited by `admin` on `Thu Jul 06 22:31:38 UTC 2023`
Record UNII	3A64E3G5ZO
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BROMOCRIPTINE

Official Name

English

SANDOZ 15-754

Code

English

2-Bromo-α-ergocryptine

Common Name

English

BROMOCRIPTINE [USAN]

Common Name

English

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

Common Name

English

ERGOCRYPTINE, 2-BROMO-

Common Name

English

Bromocriptine [WHO-DD]

Common Name

English

BROMOCRIPTINE [MI]

Common Name

English

BROMOCRIPTINE [VANDF]

Common Name

English

bromocriptine [INN]

Common Name

English

(+)-BROMOCRIPTINE

Systematic Name

English

BROMERGOCRYPTINE

Common Name

English

Classification Tree Code System Code

LIVERTOX

NBK548601