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bromocriptine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
ergot alkaloid derivatives	403	25614-03-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: bromocriptine bromocriptin bromocryptine ergolactin 2-bromoergocriptine bromocriptine mesylate bromocriptine mesilate	A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion. Molecular weight: 654.61 Formula: C32H40BrN5O5 CLOGP: 6.58 LIPINSKI: 2 HAC: 10 HDO: 3 TPSA: 118.21 ALOGS: -3.88 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

bromocriptine
bromocriptin
bromocryptine
ergolactin
2-bromoergocriptine
bromocriptine mesylate
bromocriptine mesilate

A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.

Molecular weight: 654.61
Formula: C32H40BrN5O5
CLOGP: 6.58
LIPINSKI: 2
HAC: 10
HDO: 3
TPSA: 118.21
ALOGS: -3.88
ROTB: 5

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
5	mg	O
5	mg	P
40	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	28 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	2.19 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	2 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.80 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
June 28, 1978	FDA	US PHARMS HOLDINGS I

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Exposure during pregnancy	62.60	19.84	56	3125	155491	63330350
Blood prolactin increased	60.97	19.84	17	3164	3486	63482355
Visual pathway disorder	58.76	19.84	8	3173	30	63485811
Neuroleptic malignant syndrome	57.77	19.84	22	3159	12034	63473807
Mediastinal fibrosis	43.96	19.84	6	3175	23	63485818
Pituitary tumour	38.26	19.84	9	3172	939	63484902
Pituitary tumour removal	37.84	19.84	5	3176	14	63485827
Hypersexuality	32.16	19.84	7	3174	515	63485326
Body height increased	31.18	19.84	5	3176	67	63485774
Maternal exposure during pregnancy	30.93	19.84	46	3135	220016	63265825

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Gambling disorder	85.60	26.35	19	1624	1641	34953647
Neuroleptic malignant syndrome	85.51	26.35	32	1611	17902	34937386
Serotonin syndrome	68.29	26.35	28	1615	19905	34935383
Muscle rigidity	65.97	26.35	23	1620	10495	34944793
Stress cardiomyopathy	60.82	26.35	15	1628	2044	34953244
Impulse-control disorder	46.21	26.35	11	1632	1290	34953998
Neonatal respiratory depression	39.98	26.35	8	1635	417	34954871
Hypersexuality	39.69	26.35	10	1633	1483	34953805
Borderline personality disorder	34.65	26.35	7	1636	383	34954905
Premature baby	33.53	26.35	17	1626	19616	34935672

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Neuroleptic malignant syndrome	117.06	19.43	47	4254	27512	79712575
Muscle rigidity	81.27	19.43	33	4268	19849	79720238
Blood prolactin increased	70.80	19.43	20	4281	3991	79736096
Visual pathway disorder	59.15	19.43	9	4292	77	79740010
Exposure during pregnancy	53.49	19.43	44	4257	101088	79638999
Blood creatine phosphokinase increased	50.94	19.43	36	4265	66054	79674033
Stress cardiomyopathy	47.22	19.43	19	4282	11147	79728940
Gambling disorder	44.51	19.43	12	4289	2014	79738073
Mediastinal fibrosis	44.17	19.43	6	4295	20	79740067
Serotonin syndrome	42.96	19.43	28	4273	44999	79695088

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	G02CB01	GENITO URINARY SYSTEM AND SEX HORMONES OTHER GYNECOLOGICALS OTHER GYNECOLOGICALS Prolactine inhibitors
ATC	N04BC01	NERVOUS SYSTEM ANTI-PARKINSON DRUGS DOPAMINERGIC AGENTS Dopamine agonists
CHEBI has role	CHEBI:48407	antiparkinson agent
CHEBI has role	CHEBI:49020	hormone antagonists
CHEBI has role	CHEBI:51065	Dopamine receptor agonist
CHEBI has role	CHEBI:66956	antidyskinetic agent
FDA CS	M0007652	Ergolines
FDA EPC	N0000175827	Ergot Derivative
MeSH PA	D018726	Anti-Dyskinesia Agents
MeSH PA	D000978	Antiparkinson Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Postencephalitic parkinsonism	indication	19972008	DOID:14332
Parkinson's disease	indication	49049000	DOID:14330
Acromegaly	indication	74107003	DOID:2449
Hyperprolactinemia	indication	237662005	DOID:12700
Type 2 Diabetes Mellitus Treatment Adjunct	indication
Neuroleptic malignant syndrome	off-label use	15244003	DOID:14464
Hypertensive disorder	contraindication	38341003	DOID:10763
Mild pre-eclampsia	contraindication	41114007
Severe pre-eclampsia	contraindication	46764007
Pregnancy-induced hypertension	contraindication	48194001

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.98	acidic
pKa2	12.93	acidic
pKa3	5.98	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 0.8MG BASE	CYCLOSET	VEROSCIENCE	N020866	May 5, 2009	RX	TABLET	ORAL	7888310	July 25, 2023	IMPROVEMENTS OF GLYCEMIC CONTROL IN INDIVIDUALS WITH TYPE 2 DIABETES WHO HAVE ONE OR MORE SPECIFIED CARDIOVASCULAR RISK FACTORS
EQ 0.8MG BASE	CYCLOSET	VEROSCIENCE	N020866	May 5, 2009	RX	TABLET	ORAL	8137992	July 25, 2023	IMPROVEMENTS OF GLYCEMIC CONTROL IN INDIVIDUALS WITH TYPE 2 DIABETES WHO HAVE ONE OR MORE SPECIFIED CARDIOVASCULAR RISK FACTORS
EQ 0.8MG BASE	CYCLOSET	VEROSCIENCE	N020866	May 5, 2009	RX	TABLET	ORAL	8137993	July 25, 2023	IMPROVEMENTS OF GLYCEMIC CONTROL IN INDIVIDUALS WITH TYPE 2 DIABETES WHO HAVE ONE OR MORE SPECIFIED CARDIOVASCULAR RISK FACTORS
EQ 0.8MG BASE	CYCLOSET	VEROSCIENCE	N020866	May 5, 2009	RX	TABLET	ORAL	8137994	July 25, 2023	IMPROVEMENTS OF GLYCEMIC CONTROL IN INDIVIDUALS WITH TYPE 2 DIABETES WHO HAVE ONE OR MORE SPECIFIED CARDIOVASCULAR RISK FACTORS
EQ 0.8MG BASE	CYCLOSET	VEROSCIENCE	N020866	May 5, 2009	RX	TABLET	ORAL	10688155	June 7, 2030	ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES BY ADMINISTERING BROMOCRIPTINE MESYLATE AND A FIRST-PHASE INSULIN SECRETAGOGUE AS RECITED IN CLAIM 1 AND WHEREIN THE EFFECTS ARE AS RECITED IN CLAIM 1
EQ 0.8MG BASE	CYCLOSET	VEROSCIENCE	N020866	May 5, 2009	RX	TABLET	ORAL	10688155	June 7, 2030	ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES BY ADMINISTERING BROMOCRIPTINE MESYLATE AND A FIRST-PHASE INSULIN SECRETAGOGUE AS RECITED IN CLAIM 1 AND WHEREIN THE EFFECTS ARE AS RECITED IN CLAIMS 1 AND 10
EQ 0.8MG BASE	CYCLOSET	VEROSCIENCE	N020866	May 5, 2009	RX	TABLET	ORAL	10688155	June 7, 2030	ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES BY ADMINISTERING BROMOCRIPTINE MESYLATE AND A FIRST-PHASE INSULIN SECRETAGOGUE AS RECITED IN CLAIM 1 AND WHEREIN THE EFFECTS ARE AS RECITED IN CLAIMS 1 AND 11
EQ 0.8MG BASE	CYCLOSET	VEROSCIENCE	N020866	May 5, 2009	RX	TABLET	ORAL	10688155	June 7, 2030	ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES BY ADMINISTERING BROMOCRIPTINE MESYLATE AND A FIRST-PHASE INSULIN SECRETAGOGUE AS RECITED IN CLAIM 1 AND WHEREIN THE EFFECTS ARE AS RECITED IN CLAIMS 1 AND 13
EQ 0.8MG BASE	CYCLOSET	VEROSCIENCE	N020866	May 5, 2009	RX	TABLET	ORAL	10688155	June 7, 2030	ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES BY ADMINISTERING BROMOCRIPTINE MESYLATE AND A FIRST-PHASE INSULIN SECRETAGOGUE AS RECITED IN CLAIM 1 AND WHEREIN THE EFFECTS ARE AS RECITED IN CLAIMS 1 AND 9
EQ 0.8MG BASE	CYCLOSET	VEROSCIENCE	N020866	May 5, 2009	RX	TABLET	ORAL	10688155	June 7, 2030	ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES BY ADMINISTERING BROMOCRIPTINE MESYLATE AND A FIRST-PHASE INSULIN SECRETAGOGUE AS RECITED IN CLAIM 22 WHEREIN THE EFFECTS ARE AS RECITED IN CLAIM 22

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	AGONIST	Ki	9.70	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN	AGONIST	Ki	7.50	IUPHAR
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN		Ki	5.86	DRUG MATRIX
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	6.13	PDSP
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN	AGONIST	Ki	6.20	IUPHAR
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	8	WOMBAT-PK
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	5.70	DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	7.90	WOMBAT-PK
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	7	WOMBAT-PK
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.30	WOMBAT-PK

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External reference:

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ID	Source
08Y	PDB_CHEM_ID
002117	NDDF
002118	NDDF
10007	MMSL
116656002	SNOMEDCT_US
142426	RXNORM
22260-51-1	SECONDARY_CAS_RN
31101	PUBCHEM_CID
3365	INN_ID
35	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Bromocriptine Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-7096	CAPSULE	5 mg	ORAL	ANDA	21 sections
Bromocriptine mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0574-0106	TABLET	2.50 mg	ORAL	ANDA	22 sections
Bromocriptine mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0781-5325	TABLET	2.50 mg	ORAL	ANDA	18 sections
Bromocriptine Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5667	TABLET	2.50 mg	ORAL	ANDA	22 sections
Bromocriptine Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	60687-286	TABLET	2.50 mg	ORAL	ANDA	18 sections
Bromocriptine Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	60687-286	TABLET	2.50 mg	ORAL	ANDA	18 sections
Bromocriptine Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	60687-286	TABLET	2.50 mg	ORAL	ANDA	18 sections
BROMOCRIPTINE MESYLATE	HUMAN PRESCRIPTION DRUG LABEL	1	63304-158	CAPSULE	5 mg	ORAL	NDA	14 sections
BROMOCRIPTINE MESYLATE	HUMAN PRESCRIPTION DRUG LABEL	1	63304-962	TABLET	2.50 mg	ORAL	NDA	14 sections
Bromocriptine mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	65841-654	CAPSULE	5 mg	ORAL	ANDA	1 sections

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