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

Stem definition	Drug id	CAS RN
ergot alkaloid derivatives	460	81409-90-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: cabergoline dostinex galastop cabaser cabaseril	An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE. Molecular weight: 451.62 Formula: C26H37N5O2 CLOGP: 4.17 LIPINSKI: 0 HAC: 7 HDO: 2 TPSA: 71.68 ALOGS: -3.85 ROTB: 8 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

cabergoline
dostinex
galastop
cabaser
cabaseril

An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE.

Molecular weight: 451.62
Formula: C26H37N5O2
CLOGP: 4.17
LIPINSKI: 0
HAC: 7
HDO: 2
TPSA: 71.68
ALOGS: -3.85
ROTB: 8

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.50	mg	O
3	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	65 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	3 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.01 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Aug. 1, 1999	PMDA	PFIZER JAPAN INC.
Dec. 23, 1996	FDA

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
Blood growth hormone increased	180.98	17.41	34	8240	436	63480312
Insulin-like growth factor increased	163.91	17.41	35	8239	884	63479864
Aortic valve incompetence	114.42	17.41	39	8235	5949	63474799
Insulin-like growth factor decreased	105.26	17.41	21	8253	375	63480373
Pulmonary pain	104.63	17.41	32	8242	3458	63477290
Ovarian hyperstimulation syndrome	88.02	17.41	29	8245	3985	63476763
Pituitary tumour	81.89	17.41	20	8254	928	63479820
Blood prolactin increased	75.57	17.41	25	8249	3478	63477270
Amyloid arthropathy	69.77	17.41	16	8258	564	63480184
Needle issue	67.51	17.41	31	8243	10345	63470403

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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
Cerebrospinal fluid leakage	260.44	21.88	48	5053	488	34951342
Gambling disorder	180.12	21.88	43	5058	1617	34950213
Insulin-like growth factor increased	139.01	21.88	33	5068	1210	34950620
Aortic valve incompetence	103.11	21.88	37	5064	5867	34945963
Pneumocephalus	81.38	21.88	15	5086	152	34951678
Radiation inflammation	80.58	21.88	20	5081	885	34950945
Mitral valve incompetence	78.69	21.88	40	5061	14903	34936927
Visual pathway disorder	75.14	21.88	11	5090	19	34951811
Pulmonary pain	74.58	21.88	20	5081	1204	34950626
Pituitary haemorrhage	72.47	21.88	14	5087	186	34951644

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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
Cerebrospinal fluid leakage	236.54	15.56	54	11701	1645	79730988
Insulin-like growth factor increased	230.93	15.56	54	11701	1832	79730801
Blood growth hormone increased	178.95	15.56	37	11718	699	79731934
Pulmonary pain	175.89	15.56	52	11703	4421	79728212
Aortic valve incompetence	163.07	15.56	59	11696	9471	79723162
Gambling disorder	156.26	15.56	40	11715	1986	79730647
Pneumocephalus	117.11	15.56	23	11732	331	79732302
Needle issue	114.85	15.56	50	11705	13018	79719615
Pituitary haemorrhage	113.89	15.56	22	11733	289	79732344
Mitral valve incompetence	109.10	15.56	62	11693	28503	79704130

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	G02CB03	GENITO URINARY SYSTEM AND SEX HORMONES OTHER GYNECOLOGICALS OTHER GYNECOLOGICALS Prolactine inhibitors
ATC	N04BC06	NERVOUS SYSTEM ANTI-PARKINSON DRUGS DOPAMINERGIC AGENTS Dopamine agonists
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:48407	antiparkinson agent
CHEBI has role	CHEBI:51065	Dopamine receptor agonist
FDA CS	M0007652	Ergolines
FDA EPC	N0000175827	Ergot Derivative
MeSH PA	D018726	Anti-Dyskinesia Agents
MeSH PA	D000978	Antiparkinson Agents
MeSH PA	D002491	Central Nervous System 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
Hyperprolactinemia	indication	237662005	DOID:12700
Prevention of ovarian hyperstimulation syndrome	indication
Heart valve disorder	contraindication	368009	DOID:4079
Severe pre-eclampsia	contraindication	46764007
Retroperitoneal fibrosis	contraindication	49120005
Fibrosis of lung	contraindication	51615001	DOID:3770
Fibrosis of pericardium	contraindication	194965002
Disease of liver	contraindication	235856003	DOID:409
Breastfeeding (mother)	contraindication	413712001
Hypertensive urgency	contraindication	443482000

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🐶 Veterinary Drug Use

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🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.83	acidic
pKa2	13.48	acidic
pKa3	7.88	Basic
pKa4	5.97	Basic

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Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

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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	9.20	IUPHAR	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN	ANTAGONIST	Ki	7.90	IUPHAR
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN	AGONIST	Ki	7.70	IUPHAR
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	AGONIST	Ki	8.20	IUPHAR
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	8.85	CHEMBL
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	AGONIST	Ki	6.20	IUPHAR
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN	ANTAGONIST	Ki	6.50	IUPHAR
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN	ANTAGONIST	Ki	7.10	IUPHAR
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN	AGONIST	Ki	9.10	IUPHAR
D(1B) dopamine receptor	GPCR	P21918	DRD5_HUMAN	AGONIST	Ki	7.70	IUPHAR

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External reference:

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ID	Source
005446	NDDF
109139002	SNOMEDCT_US
134895	RXNORM
37	IUPHAR_LIGAND_ID
386979007	SNOMEDCT_US
4021014	VUID
4021014	VANDF
4317	MMSL
54746	PUBCHEM_CID
5860	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Cabergoline	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5420	TABLET	0.50 mg	ORAL	ANDA	25 sections
Cabergoline	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5420	TABLET	0.50 mg	ORAL	ANDA	25 sections
Cabergoline	HUMAN PRESCRIPTION DRUG LABEL	1	23155-823	TABLET	0.50 mg	ORAL	ANDA	11 sections
Cabergoline	HUMAN PRESCRIPTION DRUG LABEL	1	23155-823	TABLET	0.50 mg	ORAL	ANDA	11 sections
Cabergoline	HUMAN PRESCRIPTION DRUG LABEL	1	49884-673	TABLET	0.50 mg	ORAL	ANDA	21 sections
Cabergoline	HUMAN PRESCRIPTION DRUG LABEL	1	50090-3157	TABLET	0.50 mg	ORAL	ANDA	25 sections
Cabergoline	HUMAN PRESCRIPTION DRUG LABEL	1	50090-3951	TABLET	0.50 mg	ORAL	ANDA	21 sections
Cabergoline	HUMAN PRESCRIPTION DRUG LABEL	1	50090-5834	TABLET	0.50 mg	ORAL	ANDA	22 sections
Cabergoline	HUMAN PRESCRIPTION DRUG LABEL	1	50090-5834	TABLET	0.50 mg	ORAL	ANDA	22 sections
Cabergoline	HUMAN PRESCRIPTION DRUG LABEL	1	50090-6596	TABLET	0.50 mg	ORAL	ANDA	11 sections

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