The active substance of Dostinex is cabergoline, a dopaminergic agent, an ergoline derivative. Has a long and pronounced effect of reducing prolactin. Effects due to blockade of prolactin secretion as a result of direct stimulation in lactotrophic cells of the pituitary D2-dopamine receptors. When using high doses, there is also a central stimulating dopaminergic effect on D2 receptors. This property of the drug differs from other prolactin-lowering agents.
Just 3 hours after taking Dostinex in the blood, a decrease in the level of prolactin is observed, which persists for 7 to 28 days in healthy individuals and patients with increased prolactin levels. The effect of Dostinex when used in the period of postpartum lactation lasts up to 2-3 weeks. From the digestive tract is absorbed quickly. The maximum plasma concentration is reached in 0,5-4 hours after internal reception of a preparation. The half-life was evaluated by the rate of elimination of cabergoline in the urine – it was 63-68 hours in healthy individuals, in patients with hyperprolactinaemia – 79-115 hours. Due to the significant half-life of cabergoline, the equilibrium concentrations of the drug are reached after 28 days. About 41-42% of cabergoline binds plasma proteins.