Bergolak, 0.5 mg tablets 2 pcs

Dopamine receptor agonist, ergoline derivative, inhibits prolactin secretion.

Stimulates dopamine D2-receptors of lactotropic pituitary cells; in high doses has a central dopaminergic effect.

Limits prolactin concentration in blood, restores menstrual cycle and fertility.

. By reducing the concentration of prolactin in blood in women, pulsatile gonadotropin secretion and release of luteinizing hormone in the middle of the cycle is restored, anovulatory cycles are eliminated and the concentration of estrogen in the body is increased; the severity of hypoestrogenic (weight gain, fluid retention, osteoporosis) and hyperandrogenic (acne, hirsutism) symptoms is reduced.

In men it decreases libido and impotence caused by hyperprolactinemia (when the concentration of prolactin decreases, the concentration of testosterone increases), gynecomastia and lactorrhea.

Pituitary macroadenomas and related symptoms (headache, disorders of visual fields and visual acuity, cranial nerve functions and anterior pituitary lobe) are reversed.

Limits the concentration of prolactin in patients with prolactinoma and pseudoprolactinoma (in the latter – without reducing the size of the pituitary adenoma).

The decrease of concentration of prolactin is noted 3 hours after intake and lasts for 7-28 days in patients with hyperprolactinemia and 14-21 days with suppression of postpartum lactation. The decrease in prolactin concentration occurs within 2-4 weeks of treatment.

Indications

Active ingredient

Composition

How to take, the dosage

The drug is taken orally, with meals.

The maximum dose for patients with hyperprolactinemia should not exceed 4.5 mg per week.

Depending on tolerance, the weekly dose of Bergolac may be taken once or divided into 2 or more doses per week. Dividing the weekly dose into multiple doses is recommended when prescribing a dose of more than 1 mg per week.

The chance of side effects can be reduced by starting Bergolac at a low dose (e.g., 0.25 mg once weekly), increasing gradually until the therapeutic dose is reached.

To improve tolerability if there are severe side effects, a temporary reduction of the dose may be appropriate, followed by a more gradual increase (e.g., 0.25 mg weekly every 2 weeks).

Interaction

The concomitant use with ergot alkaloids and their derivatives is not recommended (with long-term therapy with cabergoline).

Dopamine receptor antagonists (phenothiazine, butyrophenone, thioxanthene derivatives; metoclopramide) may weaken the effects of cabergoline when used concomitantly.

The concomitant use of cabergoline with macrolides is not recommended due to possible increased plasma concentrations of cabergoline.

The mechanism of interaction of macrolides with cabergoline is not well understood, but appears to be due to the ability of macrolides and cabergoline to competitively inhibit the cytochrome P450 system.

Special Instructions

A complete study of pituitary function should be performed before prescribing cabergoline.

If the dose of the drug is increased, patients should be monitored by a physician in order to establish the lowest dose that provides therapeutic effect. During treatment it is recommended to determine serum prolactin concentration regularly (once a month). Normalization of prolactin concentration is usually observed within 2-4 weeks of cabergoline therapy.

After withdrawal of cabergoline a recurrence of hyperprolactinemia is usually observed, but some patients have a persistent decrease in prolactin concentration for several months. In most women, ovulatory cycles persist for at least 6 months after withdrawal of cabergoline.

Cabergoline restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Because pregnancy can occur before menstruation recovers, pregnancy tests are recommended at least once every 4 weeks during the amenorrheic period, and after menstruation recovers whenever there is a delay in menstruation of more than 3 days.

Barrier methods of contraception should be used during treatment with cabergoline, as well as after discontinuation of the drug before recurrence of anovulation. If pregnancy occurs during treatment, consideration should be given to discontinuing the drug.

Women who become pregnant should be monitored by a physician for timely detection of symptoms of pituitary enlargement (pre-existing pituitary tumors may increase in size during pregnancy).

Patients with arterial hypertension developed during pregnancy (e.g. pre-eclampsia) and/or postpartum arterial hypertension should only be prescribed cabergoline when the potential benefit of the drug significantly exceeds the possible risk.

The use of cabergoline causes drowsiness. In patients with Parkinson’s disease the use of dopamine receptor agonists may cause sudden falling asleep. In such cases, it is recommended to decrease the dose of cabergoline or discontinue therapy.

Contraindications

Side effects

Side effects are usually transient, but the severity is mild to moderate and dose-dependent. They occur mostly during the first 2 weeks of therapy and in most cases disappear on their own as therapy continues or a few days after cancellation of cabergoline.

Cardiovascular system disorders: palpitations, facial flushes, finger vasospasms (like other ergot derivatives, cabergoline may have a vasoconstrictive effect), valvulopathy; rarely, orthostatic hypotension (with long-term treatment with cabergoline, hypotensive effect), asymptomatic BP reduction during the first 3-4 days after delivery (systolic by more than 20 mm Hg.sts, diastolic by more than 10 mmHg).

Nervous system disorders: dizziness/vertigo, headache, increased fatigue, somnolence, depression, mania, asthenia, paresthesias, fainting.

Digestive system disorders: nausea, vomiting, epigastric pain, abdominal pain, constipation, gastritis, dyspepsia, liver dysfunction.

Allergic reactions: hypersensitivity reactions, skin rash.

Others: mastodynia, nasal bleeding, transient hemianopsia, lower limb muscle cramps, alopecia, increased serum CPK activity, edema, pleural fibrosis, respiratory disorders (including respiratory failure).

Overdose

Symptoms:Nausea, vomiting, abdominal pain, constipation, decreased BP, orthostatic hypotension, headache, cramps of the calf muscles, severe asthenia, sweating, drowsiness, psychomotor agitation, psychosis, hallucinations.

Treatment: gastric lavage, BP control, administration of dopamine receptor antagonists (phenothiazine derivatives, butyrophenone, thioxanthene, metoclopramide).

Similarities