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
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
DescriptionCurator'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
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.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18691132 |
1.5 nM [Ki] | ||
Target ID: CHEMBL2095169 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18691132 |
0.5 nM [Ki] | ||
Target ID: CHEMBL1833 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18691132 |
1.2 nM [Ki] | ||
Target ID: CHEMBL217 |
0.69 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | CABERGOLINE Approved UseCabergoline tablets are indicated for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas. Launch Date2005 |
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Primary | CABERGOLINE Approved UseCabergoline tablets are indicated for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas. Launch Date2005 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
33.3 ng/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7883840 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7883840 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7883840 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1295 ng × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7883840 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7883840 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7883840 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
68.54 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7884663 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
60% |
unknown, unknown |
CABERGOLINE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse 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 Health Status: unhealthy Sources: |
Other AEs: Cardiac valvulopathy... Other AEs: Cardiac valvulopathy Sources: |
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 Health Status: unhealthy Sources: |
Disc. AE: Headache, Nausea... AEs leading to discontinuation/dose reduction: Headache (1.4%) Sources: Nausea (0.9%) Vomiting (0.9%) |
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 Health Status: unhealthy Sources: |
Disc. AE: Pleural effusion, Pulmonary fibrosis... Other AEs: Cardiac valvulopathy, Pericardial fibrosis... AEs leading to discontinuation/dose reduction: Pleural effusion Other AEs:Pulmonary fibrosis Cardiac valvulopathy Sources: Pericardial fibrosis Retroperitoneal fibrosis |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 Health Status: unhealthy Sources: |
|
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
|
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 Health Status: unhealthy Sources: |
|
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 Health Status: unhealthy Sources: |
|
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/31183987/ Page: - |
likely |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: - |
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
Title | Date | PubMed |
---|---|---|
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 |
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12464354
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).
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C66884
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NCI_THESAURUS |
C38149
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WHO-VATC |
QG02CB03
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WHO-ATC |
N04BC06
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NDF-RT |
N0000007618
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LIVERTOX |
135
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QN04BC06
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NDF-RT |
N0000175827
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G02CB03
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N0000007618
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EMA VETERINARY ASSESSMENT REPORTS |
VELACTIS [SUSPENDED]
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CHEMBL1201087
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460
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C047047
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CABERGOLINE
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54746
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Cabergoline
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SUB06041MIG
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m2876
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ACTIVE MOIETY
METABOLITE (PARENT)
SALT/SOLVATE (PARENT)