Bergolac pills 0.5 mg №8

Dosage form

Pills

Composition

1 tab. contains cabergoline 500 mcg

Packing

8 pieces

Mechanism of action

Bergolac - dopamine receptor agonist, ergolin derivative, inhibits the secretion of prolactin. Stimulates dopamine D2 receptors of lactotropic pituitary cells; in high doses has a central dopaminergic effect. Reduces the concentration of prolactin in the blood, restores the menstrual cycle and fertility. By reducing the concentration of prolactin in the blood in women, pulsating secretion of gonadotropins and release of luteinizing hormone (LH) in the middle of the cycle is restored, anovulatory cycles are eliminated and the concentration of estrogens in the body increases, the severity of hypoestrogenic (weight gain, fluid retention, osteoporosis) and hyperandrogrogrogate decreases. acne, hirsutism) symptoms. In men, it reduces the decrease in libido caused by hyperprolactinemia, impotence (with a decrease in the concentration of prolactin, the concentration of testosterone increases), gynecomastia, and lactorrhea. Subject to the reverse development of the pituitary macroadenoma and associated symptoms (headache, disruption of the fields and visual acuity, functions of the cranial nerves and the anterior pituitary gland). Reduces the concentration of prolactin in patients with prolactinoma and pseudoprolactinoma (in the latter - without reducing the size of the pituitary adenoma). A decrease in the concentration of prolactin occurs 3 hours after administration and persists for 7–28 days in patients with hyperprolactinemia and 14–21 days when suppression of postpartum lactation. A decrease in prolactin concentration occurs within 2–4 weeks of treatment.

Indications and usage

• prevention of postpartum lactation;
• suppression of already established postpartum lactation;
• treatment of disorders associated with hyperprolactinemia, including amenorrhea, oligomenorrhea, anovulation, galactorrhea;
• prolactin-secreting pituitary adenomas (micro- and macroprolactinomas);
• idiopathic hyperprolactinemia;
• empty turkish saddle syndrome combined with hyperprolactinemia.

Contraindications

Hypersensitivity (including to ergoalkaloid derivatives), uncontrolled arterial hypertension, symptoms of impaired function of the heart and respiration due to fibrotic changes, or a history of such symptoms.

When pregnancy should be used with caution if the expected benefit to the mother outweighs the potential risk to the fetus (adequate controlled studies of cabergoline in pregnant women have not been conducted). Patients should be warned about the need to inform the doctor about the planned, proposed or completed pregnancy to decide whether to continue or discontinue therapy.
Category of action on the fetus by the FDA -B.
The study of the effect of cabergoline on reproductive function was carried out on mice, rats and rabbits that received it through a stomach tube introduced through the nose. In mice treated with cabergoline at a dose of up to 8 mg / kg / day (55-fold excess of mRDC) during the period of organogenesis, a toxic effect on the maternal organism was noted; no teratogenic effect was detected. In rats treated with 0.012 mg / kg / day of cabergoline (approximately 1/7 of MFRD) during the period of organogenesis, there was an increase in post-implantation embryo-fetal loss. In rabbits, with the administration of cabergoline during the period of organogenesis at a dose of 0.5 mg / kg / day (19 mRDC), a toxic effect on the maternal organism (weight loss and depletion) was noted. At a dose of 4 mg / kg / day (150 MRDCH), the incidence of various fetal malformations increased. However, in other studies with doses of cabergoline up to 8 mg / kg / day (300 mRDC) in rabbits, developmental defects, embryo and phototoxic effects were not observed. Radiological examination of pregnant female rats showed a high concentration of cabergoline and its metabolites in the uterine wall and the absence of their accumulation in fetal tissues. When cabergoline was administered in doses of more than 0.003 mg / kg / day (1/28 MRDRH) 6 days before delivery and during the lactation period, the growth of newborns was slowed down, there were cases of death due to a decrease in milk secretion. It is not known whether cabergoline is excreted in human breast milk. Cabergoline and its metabolites are found in breast milk of lactating rats.Since many drugs are excreted with milk in women and a serious negative effect of cabergoline on the infant is possible, a decision should be made either to stop breastfeeding or to refuse to take cabergoline (taking into account the degree of need for this medicine for the mother).

Dosage and administration

Bergolac take inside, in the initial dose of 0.25 mg 2 times a week. It is possible to increase the dose to 1 mg 2 times a week (under the control of the content of prolactin in the plasma). Increase the dose no more than once every 4 weeks. If normal plasma prolactin levels are maintained for 6 months, treatment can be discontinued, but prolactin levels should be regularly monitored to resume therapy if necessary. The effectiveness of therapy with a duration of over 24 months has not been established.

Adverse reactions

The safety of cabergoline has been investigated in more than 900 patients with hyperprolactinemia; the severity of most side effects was mild or moderate. In a 4-week double-blind, placebo-controlled study, patients received cabergoline in fixed doses of 0.125, 0.5, 0.75 and 1.0 mg twice a week; doses were halved during the first week. The following side effects were noted (the percentage of occurrence of this side effect in the group of cabergoline in brackets, in the placebo group) is indicated next to the name:

From the nervous system and sensory organs: headache 26% (25%), dizziness 15% (5%), vertigo 1% (0%), paresthesia 1% (0%), drowsiness 5% (5%), depression 3% (5%), nervousness 2% (0%), asthenia 9% (10%), fatigue 7% (0%), visual impairment 1% (0%).

Since the cardiovascular system and blood (hematopoiesis, hemostasis): orthostatic hypotension 4% (0%).

From the digestive tract: dyspepsia 2% (0%), nausea 27% (20%), vomiting 2% (0%), constipation 10% (0%), abdominal pain 5% (5%).

Other: hot flashes 1% (5%), pain in the mammary glands 1% (0%), dysmenorrhea 1% (0%).

The safety of cabergoline was investigated in controlled and uncontrolled trials in approximately 1,200 patients with Parkinson's disease who received cabergoline at doses far in excess of MRDC for patients with hyperprolactinemia (up to 11.5 mg / day). In addition, side effects such as dyskinesia, hallucinations, confusion, and peripheral edema were identified in these patients.Heart failure, pleural effusion, pulmonary fibrosis, gastric or duodenal ulcer were rarely observed, and one case of constrictive pericarditis was reported.

Drug interactions

It should not be used simultaneously with dopamine antagonists D₂-receptors (derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide). Simultaneous use with drugs that have a high degree of binding to plasma proteins can with a low probability affect the association of cabergoline with plasma proteins. It should be used with caution at the same time with agents that have a hypotensive effect.

Overdosage

Symptoms: nasal congestion, fainting, hallucinations.
Treatment: symptomatic, maintenance of blood pressure.

Storage conditions

The drug is stored at a temperature not higher than 25 C. Keep out of reach of children.