U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ABSOLUTE
Molecular Formula C26H37N5O2
Molecular Weight 451.6043
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CABERGOLINE

SMILES

CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@H]2[C@@H](CC3=CNC4=C3C2=CC=C4)N(CC=C)C1

InChI

InChIKey=KORNTPPJEAJQIU-KJXAQDMKSA-N
InChI=1S/C26H37N5O2/c1-5-11-30-17-19(25(32)31(26(33)27-6-2)13-8-12-29(3)4)14-21-20-9-7-10-22-24(20)18(16-28-22)15-23(21)30/h5,7,9-10,16,19,21,23,28H,1,6,8,11-15,17H2,2-4H3,(H,27,33)/t19-,21-,23-/m1/s1

HIDE SMILES / InChI

Description
Curator's Comment: description was created based on several sources, including: https://www.drugs.com/dosage/cabergoline.html http://www.wikidoc.org/index.php/Cabergoline http://www.rxlist.com/dostinex-drug.htm

Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D2 receptors. Results of in vitro studies demonstrate that cabergoline exerts a direct inhibitory effect on the secretion of prolactin by rat pituitary lactotrophs. It is FDA approved for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas. Common adverse reactions include constipation, nausea, dizziness, headache and fatigue. Cabergoline should not be administered concurrently with D-antagonists, such as phenothiazines, butyrophenones, thioxanthenes, or metoclopramide.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
CABERGOLINE

Approved Use

Cabergoline tablets are indicated for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas.

Launch Date

2005
Primary
CABERGOLINE

Approved Use

Cabergoline tablets are indicated for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas.

Launch Date

2005
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
33.3 ng/L
0.5 mg single, oral
dose: 0.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CABERGOLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
40.3 ng/L
1 mg single, oral
dose: 1 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CABERGOLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
67 ng/L
1.5 mg single, oral
dose: 1.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CABERGOLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1295 ng × h/L
0.5 mg single, oral
dose: 0.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CABERGOLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
1884 ng × h/L
1 mg single, oral
dose: 1 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CABERGOLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2546 ng × h/L
1.5 mg single, oral
dose: 1.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CABERGOLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
68.54 h
1 mg single, oral
dose: 1 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CABERGOLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
60%
unknown, unknown
CABERGOLINE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
20 mg 1 times / day multiple, oral
Highest studied dose
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources:
unhealthy, 41.0–73.5
Health Status: unhealthy
Age Group: 41.0–73.5
Sex: M+F
Sources:
2 mg 1 times / day multiple, oral
Overdose
Dose: 2 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2 mg, 1 times / day
Sources:
unhealthy
Other AEs: Cardiac valvulopathy...
0.5 mg 2 times / week multiple, oral
Recommended
Dose: 0.5 mg, 2 times / week
Route: oral
Route: multiple
Dose: 0.5 mg, 2 times / week
Sources:
unhealthy
Disc. AE: Headache, Nausea...
AEs leading to
discontinuation/dose reduction:
Headache (1.4%)
Nausea (0.9%)
Vomiting (0.9%)
Sources:
1 mg 2 times / week multiple, oral
Recommended
Dose: 1 mg, 2 times / week
Route: oral
Route: multiple
Dose: 1 mg, 2 times / week
Sources:
unhealthy
Disc. AE: Pleural effusion, Pulmonary fibrosis...
Other AEs: Cardiac valvulopathy, Pericardial fibrosis...
AEs leading to
discontinuation/dose reduction:
Pleural effusion
Pulmonary fibrosis
Other AEs:
Cardiac valvulopathy
Pericardial fibrosis
Retroperitoneal fibrosis
Sources:
AEs

AEs

AESignificanceDosePopulation
Cardiac valvulopathy
2 mg 1 times / day multiple, oral
Overdose
Dose: 2 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2 mg, 1 times / day
Sources:
unhealthy
Nausea 0.9%
Disc. AE
0.5 mg 2 times / week multiple, oral
Recommended
Dose: 0.5 mg, 2 times / week
Route: oral
Route: multiple
Dose: 0.5 mg, 2 times / week
Sources:
unhealthy
Vomiting 0.9%
Disc. AE
0.5 mg 2 times / week multiple, oral
Recommended
Dose: 0.5 mg, 2 times / week
Route: oral
Route: multiple
Dose: 0.5 mg, 2 times / week
Sources:
unhealthy
Headache 1.4%
Disc. AE
0.5 mg 2 times / week multiple, oral
Recommended
Dose: 0.5 mg, 2 times / week
Route: oral
Route: multiple
Dose: 0.5 mg, 2 times / week
Sources:
unhealthy
Cardiac valvulopathy
1 mg 2 times / week multiple, oral
Recommended
Dose: 1 mg, 2 times / week
Route: oral
Route: multiple
Dose: 1 mg, 2 times / week
Sources:
unhealthy
Pericardial fibrosis
1 mg 2 times / week multiple, oral
Recommended
Dose: 1 mg, 2 times / week
Route: oral
Route: multiple
Dose: 1 mg, 2 times / week
Sources:
unhealthy
Retroperitoneal fibrosis
1 mg 2 times / week multiple, oral
Recommended
Dose: 1 mg, 2 times / week
Route: oral
Route: multiple
Dose: 1 mg, 2 times / week
Sources:
unhealthy
Pleural effusion Disc. AE
1 mg 2 times / week multiple, oral
Recommended
Dose: 1 mg, 2 times / week
Route: oral
Route: multiple
Dose: 1 mg, 2 times / week
Sources:
unhealthy
Pulmonary fibrosis Disc. AE
1 mg 2 times / week multiple, oral
Recommended
Dose: 1 mg, 2 times / week
Route: oral
Route: multiple
Dose: 1 mg, 2 times / week
Sources:
unhealthy
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
likely
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
yes
yes (co-administration study)
Comment: n healthy male volunteers, the mean of Cmax and AUC of cabergoline increased around 2.7 times by coadministration of clarithromycin.
Page: -
PubMed

PubMed

TitleDatePubMed
Prolactinomas in children and adolescents--consequences in adult life.
2001
Actigraph analysis of diurnal motor fluctuations during dopamine agonist therapy.
2001
A review of canine pseudocyesis.
2001 Dec
Tumour shrinkage and chiasmal herniation after successful cabergoline treatment for a macroprolactinoma.
2001 Jan
Comparison of the effects of cabergoline and bromocriptine on prolactin levels in hyperprolactinemic patients.
2001 Sep
Medical management of prolactin-secreting pituitary adenomas.
2002
Pregnancy termination in the bitch and queen.
2002 Aug
Switch to quetiapine in antipsychotic agent-related hyperprolactinemia.
2002 Dec
Alopecia induced by dopamine agonists.
2002 Dec 24
Macroprolactinoma associated with Cushing's disease, successfully treated with cabergoline.
2002 Feb
Restless legs syndrome: treatment with dopaminergic agents.
2002 Feb 26
Long-term studies of dopamine agonists.
2002 Feb 26
Hyperprolactinemia: etiology, diagnosis, and management.
2002 Nov
Cabergoline plasma concentration is increased during concomitant treatment with itraconazole.
2002 Nov
Effect of cabergoline on thyroid function in hyperprolactinaemia.
2002 Nov
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. III. Agonist and antagonist properties at serotonin, 5-HT(1) and 5-HT(2), receptor subtypes.
2002 Nov
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor.
2002 Nov
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
2002 Nov
Dopamine agonist monotherapy in Parkinson's disease.
2002 Nov 30
Detecting dose-response using contrasts: asymptotic power and sample size determination for binomial data.
2002 Nov 30
Combination of two different dopamine agonists in the management of Parkinson's disease.
2002 Sep
Antioxidant properties of cabergoline: inhibition of brain auto-oxidation and superoxide anion production of microglial cells in rats.
2002 Sep 13
Hyperprolactinemia in men: clinical and biochemical features and response to treatment.
2003 Feb-Mar
[Efficacy of cabergoline in the treatment of macroprolactinoma].
2003 Jan 18
Involvement of PI3'-K, mitogen-activated protein kinase and protein kinase B in the up-regulation of the expression of nNOSalpha and nNOSbeta splicing variants induced by PRL-receptor activation in GH3 cells.
2003 Mar
Gender differences in the prevalence, clinical features and response to cabergoline in hyperprolactinemia.
2003 Mar
Selective control of the estrous cycle of the dog through suppression of estrus and reduction of the length of anestrus.
2003 Mar
[Macroadenoma of the pituitary gland with moderate hyperprolactinaemia].
2003 Mar 28
Patents

Sample Use Guides

The recommended dosage for initiation of therapy is 0.25 mg twice a week. Dosage may be increased by 0.25 mg twice weekly up to a dosage of 1 mg twice a week according to the patient’s serum prolactin level. Dosage increases should not occur more rapidly than every 4 weeks.
Route of Administration: Oral
Tert-butylhydroperoxide caused a 42+/-4% neuronal death, which was prevented by cabergoline (2 h before) in a concentration-dependent manner (EC(50): 1.24 microM).
Name Type Language
CABASER
Preferred Name English
CABERGOLINE
EP   INN   JAN   MART.   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD  
USAN   INN  
Official Name English
FCE-21336
Code English
DOSTINEX
Brand Name English
CABERGOLINE [JAN]
Common Name English
CABERGOLINE [VANDF]
Common Name English
VELACTIS
Brand Name English
Cabergoline [WHO-DD]
Common Name English
CABERGOLINE [USP-RS]
Common Name English
ERGOLINE-8.BETA.-CARBOXAMIDE, N-(3-(DIMETHYLAMINO)PROPYL)-N-((ETHYLAMINO)CARBONYL)-6-(2-PROPENYL)-
Systematic Name English
CABERGOLINE [ORANGE BOOK]
Common Name English
FCE 21336
Code English
CABERGOLINE [USAN]
Common Name English
1-[(6-Allylergolin-8?-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea
Systematic Name English
CABERGOLINE [EP MONOGRAPH]
Common Name English
cabergoline [INN]
Common Name English
CABERGOLINE [MI]
Common Name English
CABERGOLINE [MART.]
Common Name English
CABERGOLINE [USP MONOGRAPH]
Common Name English
CABERGOLINE [EMA EPAR VETERINARY]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C66884
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
NCI_THESAURUS C38149
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
WHO-VATC QG02CB03
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
WHO-ATC N04BC06
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
NDF-RT N0000007618
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
LIVERTOX 135
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
WHO-VATC QN04BC06
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
NDF-RT N0000175827
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
WHO-ATC G02CB03
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
NDF-RT N0000007618
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
EMA VETERINARY ASSESSMENT REPORTS VELACTIS [SUSPENDED]
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
Code System Code Type Description
ChEMBL
CHEMBL1201087
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
DRUG CENTRAL
460
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
MESH
C047047
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
WIKIPEDIA
CABERGOLINE
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
CAS
81409-90-7
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
IUPHAR
37
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
NCI_THESAURUS
C47428
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
INN
5860
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
SMS_ID
100000092143
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
USAN
II-10
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
EPA CompTox
DTXSID6022719
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
RXCUI
47579
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY RxNorm
CHEBI
3286
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
RS_ITEM_NUM
1084306
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
PUBCHEM
54746
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
LACTMED
Cabergoline
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
EVMPD
SUB06041MIG
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
DRUG BANK
DB00248
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
DAILYMED
LL60K9J05T
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
FDA UNII
LL60K9J05T
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY
MERCK INDEX
m2876
Created by admin on Wed Apr 02 07:45:54 GMT 2025 , Edited by admin on Wed Apr 02 07:45:54 GMT 2025
PRIMARY Merck Index