Kabergovet

Pharmacotherapeutic group: Dopamine agonists, ATC code: N04BC06 Cabergoline is a dopaminergic ergoline derivative endowed with potent and long-lasting dopamine D2 receptor agonist properties.‍‍‍‍‍‍​​​‍​​​​​​ In rats the compound, acting at D2 dopamine receptors on pituitary lactotrophic cells, decreases PRL secretion at oral doses of 3-25 mcg/kg, and in vitro at a concentration of 45 pg/ml. In addition, cabergoline exerts a central dopaminergic effect via D2 receptor stimulation at doses higher than those effective in lowering serum PRL levels. Improvement of motor deficit in animal models of Parkinson's disease was present at oral daily doses of 1-2.5 mg/kg in rats and at s.c. doses of 0.5-1 mg/kg in monkeys. In healthy volunteers the administration of cabergoline at single oral doses of 0.3-2.5 mg was associated with a significant decrease in serum PRL levels. The effect is prompt (within 3 hours of administration) and persistent (up to 7-28 days). The PRL-lowering effect is dose-related both in terms of degree of effect and duration of action. The pharmacodynamic actions of cabergoline not linked to the therapeutic effect relate only to blood pressure decrease. The maximal hypotensive effect of cabergoline as a single dose usually occurs during the first 6 hours after drug intake and is dose-dependent both in terms of maximal decrease and frequency.