Cabergoline

Cabergoline
ATC Code G02CB03, N04BC06
Formula C26H37N5O2
Molar Mass (g·mol−1) 451,6043
Physical State solid
Melting Point (°C) 102-204
CAS Number 81409-90-7
PUB Number 54746
Drugbank ID DB00248

Basics

Cabergoline is a dopamine receptor agonist, which means that it mimics the effect of the neurotransmitter dopamine. In human medicine, the drug is used on the one hand to treat neurological diseases such as Parkinson's disease or restless legs syndrome, and on the other hand to treat gynecological diseases involving weaning or prolactin excess (hormone that forms breast milk).

Pharmacology

Pharmacodynamics

The drug stimulates centrally located dopamine receptors, mainly the D2 and D3 receptor subtypes, with postsynaptic D2 stimulation (downstream of the synaptic cleft) responsible for the antiparkinsonian effects and presynaptic D2 stimulation (upstream of the synaptic cleft) responsible for the neuron-protective effects.
Durch die Dopamin-ähnliche Wirkung des Cabergolins wird in der Hirnanhangsdrüse die Prolaktin-Produktion gehemmt.

Pharmacokinetics

Cabergoline is metabolized primarily in the liver by cleavage of the acylurea bond. The enzyme responsible for metabolism has not yet been identified; the cytochrome P450 enzyme plays only a minimal role.
Die geschätzte Halbwertszeit beträgt bis zu 69 Stunden. Der Wirkstoff wird hauptsächlich mit dem Fäzes ausgeschieden.

Interactions

Due to its dopamine receptor-stimulating effect, cabergoline should not be used together with dopamine receptor-inhibiting drugs (e.g., metoclopramide, phenothiazines, butyrophenones, thioxanthenes).
Um erhöhte Cabergolin-Plamaspiegel zu vermeiden, sollte der Wirkstoff nicht mit Makrolidantibiotika, wie z.B. Erythromycin, kombiniert werden.

Toxicity

Side effects

Frequently, treatment with cabergoline results in swelling of the arms and/or legs, valvular changes, and consequent inflammation or fluid accumulation in the pericardium.
Weiters können Nebenwirkungen wie Übelkeit, Kopfschmerzen oder Schwindel auftreten.

Toxicological data

In case of overdose, nasal congestion, circulatory collapse, or hallucinations may be expected.
LD50 (Ratte, oral): 420 mg/kg

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

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