Alaktin (Cabergoline) tablets 0.5 mg. N8 vial

Description

Composition

active substance: cabergoline;

1 tablet contains:

• 0.5 mg cabergoline

excipients: anhydrous lactose, leucine, magnesium stearate.

Medicinal form

Tablets.

The main physical and chemical properties:

white, oval, flat tablets with a chamfer, containing 0.5 mg of cabergoline. Each tablet is scored on one side and debossed with “CBG” on one side of the score and “0.5” on the other side of the score.

Pharmacotherapeutic group

Means used in gynecology. Prolactin inhibitors. ATX code G02C B03.

Pharmacological properties

Pharmacodynamics.

Cabergoline is a synthetic ergot alkaloid and ergoline derivative that has a pronounced and long-lasting prolactin-lowering effect. The central dopaminergic effect is achieved by stimulation of D2 receptors at doses that are higher than those that reduce the level of prolactin in the blood plasma.

The prolactin-lowering effect is dose-dependent. A decrease in the level of prolactin in the blood plasma is observed 3 hours after taking the drug and persists for 2‒3 weeks. The long-acting effect means that a single dose is enough to stop the stimulation of milk secretion. In the treatment of hyperprolactinemia, prolactin levels in the blood plasma normalize within 2‒4 weeks after reaching the optimal dose. The prolactin level may still decrease significantly for several months after treatment is stopped.

Regarding the endocrine effects of cabergoline unrelated to the antiprolactinemic effect, the available human data support the experimental results obtained in animal studies and indicate that the test substance is characterized by a highly selective effect without affecting the basal level of secretion of other pituitary hormones or cortisol .

The pharmacodynamic effect of cabergoline, which does not correlate with the therapeutic effect, concerns only the reduction of blood pressure. The maximum hypotensive effect of cabergoline when used in a single dose is usually achieved within the first 6 hours after taking the drug, and the maximum decrease in blood pressure and the frequency of such an effect are dose-dependent.

Indication

Inhibition/suppression of physiological lactation

Alactin is prescribed for the purpose of inhibiting physiological postpartum lactation immediately after childbirth or for suppression of lactation established in the following cases:

• after childbirth, if the mother has decided not to breastfeed the child or when breastfeeding is contraindicated for the mother or the child for medical reasons;
• after the birth of a dead fetus or after an abortion.

Cabergoline inhibits/suppresses physiological lactation by inhibiting prolactin secretion. In controlled clinical trials, a single dose of 1 mg of cabergoline 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 a return of breast symptoms in the third week after delivery (which were usually mild in severity).

Suppression of milk secretion and relief of breast swelling and breast pain was noted in approximately 85% of lactating women when a total dose of cabergoline 1 mg divided into four doses was used for two days. Cases of recurrence of symptoms in the chest after 10 days are infrequent (approximately 2% of cases).

Treatment of hyperprolactinemic states

Alactin is indicated for the treatment of disorders associated with hyperprolactinemia, including amenorrhea, oligomenorrhea, anovulation, and galactorrhea. The drug is indicated for the treatment of patients with prolactin-secreting adenomas of the pituitary gland (micro- and macroprolactinomas), idiopathic hyperprolactinemia, or with the syndrome of “empty” Turkish saddle with accompanying hyperprolactinemia, which are the main pathological conditions causing the above-mentioned 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 hyperprolactinemic patients.

Regular cycles resumed in 83% of women with amenorrhea. Restoration of ovulation was documented in 89% of women based on progesterone indicators, the level of which was monitored during the luteal phase. Galactorrhea, which occurred before the start of treatment, disappeared in 90% of cases.
In 50‒90% of women and men with micro- or macroprolactinoma, a decrease in the size of the tumor was found.

Contraindications of Alactin

• Hypersensitivity to cabergoline, other horn alkaloids or any component of the drug.
• History of fibrotic disease of the lungs, pericardium and retroperitoneal space.
• Simultaneous use of antipsychotic drugs.
• For long-term treatment: signs of damage to the heart valves, determined by echocardiography before the start of treatment (see the section “Particulars of use”).
• Postpartum arterial hypertension or uncontrolled arterial hypertension.
• Preeclampsia, eclampsia.
• History of psychosis or risk of postpartum psychosis.
• The drug is contraindicated in patients with liver failure and pregnant women with preeclampsia.