Drug/Small Molecule:
cabergoline

2D structure

Overview

Generic Names: Cabergolina [Spanish]; Cabergolinum [Latin]
Trade Names: Cabaser; Dostinex
PharmGKB Accession Id: PA448708

Description

Cabergoline, a lysergic acid amide derivative, is a potent dopamine receptor agonist on D2 receptors. It also acts on dopamine receptors in lactophilic hypothalamus cells to suppress prolactin production in the pituitary gland. It is frequently used as a second-line agent in the management of prolactinomas when bromocriptine is ineffective. Wikipedia (source: Drug Bank)

Indication

For the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas. (source: Drug Bank)

ATC Therapeutic Categories

  • G02CB:Prolactine inhibitors
  • N04BC:Dopamine agonists

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

The secretion of prolactin by the anterior pituitary is mainly under hypothalmic inhibitory control, likely exerted through release of dopamine by tuberoinfundibular neurons. 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. Cabergoline decreased serum prolactin levels in reserpinized rats. Receptor-binding studies indicate that cabergoline has low affinity for dopamine D1, α<sub>1</sub>,- and α<sub>2</sub>- adrenergic, and 5-HT<sub>1</sub>- and 5-HT<sub>2</sub>-serotonin receptors. (source: Drug Bank)

Pharmacology

Cabergoline is a dopamine receptor agonist and uncategorized drug which suppresses the production of prolactin in pituitary gland. It is an ergot-derivative. It has at times been used as an adjunct to SSRI antidepressants as there is some evidence that it counteracts certain side effects of those drugs such as reduced libido and anorgasmia. It also has been suggested online that it has a possible recreational use in reducing or eliminating the male refractory period. (source: Drug Bank)

Food Interactions

Absorption is not affected by food.
Take with food to improve tolerance. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. Cabergoline is extensively metabolized, predominately via hydrolysis of the acylurea bond or the urea moiety. Cytochrome P-450 mediated metabolism appears to be minimal. (source: Drug Bank)

Protein Binding

Moderately bound (40% to 42%) to human plasma proteins in a concentration-independent manner. (source: Drug Bank)

Absorption

First-pass effect is seen, however the absolute bioavailability is unknown. (source: Drug Bank)

Toxicity

Overdosage might be expected to produce nasal congestion, syncope, or hallucinations. (source: Drug Bank)

Isomeric SMILES Code:

CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4c3c(c[nH]4)C[C@H]2N(C1)CC=C (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
No phenotype data No genotype data Literature annotations available Has annotations
DRD2
  • CO
  • PD
  •   
  •   
  • GN
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
DRD2 Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
erythromycin Uncurated Annotation Erythromycin increases serum levels and toxicity of cabergoline (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Heart Valve Diseases
  • CO
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Parkinson Disease
  • CO
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Pituitary adenoma
  •   
  • PD
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Prolactinoma
  • CO
  •   
  •   
  •   
  • GN
Publications

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00248
KEGG Compound ID:
C08187
KEGG Drug ID:
D00987
PubChem Compound ID:
54746
PubChem Substance ID:
10387
IUPHAR Ligand ID:
37

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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