Cabergoline

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).

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.

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