Inhibition of physiological postpartum lactation immediately after delivery or suppression of lactation established in the following cases: after delivery, if the mother has decided not to breastfeed the baby, or when breast-feeding is contraindicated to the mother or child for medical reasons; after the birth of a dead fetus or abortion. Disorders associated with hyperprolactinemia, including amenorrhea, oligomenorrhea, anovulation, and galactorrhea. Treatment of patients with prolactin-secreting pituitary adenoma (micro-and macroprolactinomas), idiopathic hyperprolactinemia or “empty” Turkish saddle syndrome with concomitant hyperprolactinemia, which are the main pathological conditions that cause the above-mentioned clinical manifestations.
active substance: cabergoline;
1 tablet contains cabergoline 0.5 mg;
Dostinex excipients: leucine, anhydrous lactose.
Dostinex Dosage form
Main physical and chemical properties: white, flat, oblong tablets with engraving “PU”, separated by a notch, on the one hand and engraving “700” and a light notch above and below the central “0” – on the other hand.
Means used in gynecology. Prolactin inhibitors. ATX code G02C B03.
Cabergoline is a dopaminergic derivative of ergot, which is characterized by strong and long-lasting prolactin-reducing activity. The drug directly stimulates D2-dopamine receptors on the surface of pituitary lactotropic cells, thus inhibiting prolactin secretion. This substance reduces the secretion of prolactin in rats when administered orally at a dose of 3‒25 μg / kg and in vitro at a concentration of 45 pg / ml. In addition, cabergoline has a central dopaminergic effect by stimulating D2 receptors at oral doses in excess of those that are effective in lowering serum prolactin levels. The long-term effect of Dostinex on prolactin levels is likely to be due to its prolonged persistence in the target organ, as indicated by the slow rate of elimination of total radioactivity from the pituitary gland after a single oral dose in rats (t½ is approximately 60 hours).
Pharmacodynamic effects have been studied in healthy volunteers, postpartum women, and patients with prolactinemia. After a single oral administration of the drug at a dose of 0.3-1.5 mg, there is a significant decrease in plasma prolactin levels in each of the studied populations. This effect develops rapidly – within 3 hours after administration of the drug and persists for 7‒28 days in healthy individuals and patients with hyperprolactinemia and for 14‒21 days – in women after childbirth. The degree of reduction in prolactin levels and duration depend on the dose.
Inhibition / suppression of physiological lactation
Inhibition of physiological postpartum lactation immediately after delivery or suppression of established lactation in the following cases:
after birth, if the mother has decided not to breastfeed or when breastfeeding is contraindicated for the mother or child for medical reasons;
after stillbirth or abortion.
Cabergoline inhibits / inhibits physiological lactation by inhibiting prolactin secretion. In controlled clinical trials, a single dose of cabergoline 1 mg on the first day after delivery was effective in inhibiting milk secretion, as well as breast swelling and pain in 70-90% of women. Less than 5% of women experienced recurrence of breast symptoms in the third week after delivery (which was usually mild in severity).
Suppression of milk secretion and relief of breast swelling and chest pain were observed in approximately 85% of lactating women with a total dose of cabregoline 1 mg in two days, divided into four doses. Cases of recurrence of symptoms in the chest after 10 days are uncommon (approximately 2% of cases).
Treatment of hyperprolactinemic conditions
Disorders associated with hyperprolactinemia, including amenorrhea, oligomenorrhea, anovulation, and galactorrhea. Treatment of patients with prolactin-secreting pituitary adenomas (micro- and macroprolactinomas), idiopathic hyperprolactinemia or “empty saddle” syndrome with concomitant hyperprolactinemia, which are the main pathological conditions that cause the above clinical manifestations.
With long-term treatment at doses of 1 to 2 mg per week, cabergoline was effective in normalizing serum prolactin levels in approximately 84% of patients with hyperprolactinemia. Regular cycles resumed in 83% of women with amenorrhea. Restoration of ovulation has been documented in 89% of women by progesterone levels, which were monitored during the luteal phase. Galactorrhea, which occurred before treatment, disappeared in 90% of cases. A decrease in tumor size was found in 50–90% of women and men with micro- or macroprolactinoma.
Hypersensitivity to cabergoline, to any of the excipients of the drug or to any ergot alkaloids.
Presence of a history of fibrotic diseases of the lungs, pericardium and retroperitoneal space.
Cabergoline is contraindicated in patients with hepatic insufficiency and pregnant women with preeclampsia. Cabergoline should not be used concomitantly with antipsychotic drugs or in women with a history of postpartum psychosis.
Cabergoline is contraindicated for long-term treatment if there are signs of heart valve damage, as determined by echocardiography before treatment (see section “Features”).