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.
Cabergoline's dopamine-like effects inhibit prolactin production in the pituitary gland.

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.
The estimated half-life is up to 69 hours. The drug is excreted mainly in the feces.

Drug Interactions

Because of its dopamine receptor-stimulating effects, cabergoline should not be used together with dopamine receptor-inhibiting drugs (e.g., metoclopramide, phenothiazines, butyrophenones, thioxanthenes).
To avoid elevated cabergoline plasma levels, the drug should not be combined with macrolide antibiotics, such as erythromycin.

Side effects

Often treatment with Cabergoline leads to swelling of arms and/or legs, valvular changes resulting in inflammation or fluid accumulation in the pericardium.
Furthermore, side effects such as nausea, headache or dizziness may occur.

Toxicological data

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