Bergolak, pills 0.5mg, 8pcs

Composition

1 tablet contains:

cabergoline 500 mcg

Auxiliary substances:

leucine,

lactose anhydrous (lactopress),

magnesium stearate.

Pharmacological action

The dopamine receptor agonist, an ergoline derivative, suppresses prolactin secretion. It stimulates dopamine_D2-receptors of lactotropic pituitary cells; in high doses, it 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 of women, the pulsating secretion of gonadotropins and the release of luteinizing hormone in the middle of the cycle are restored, anovulatory cycles are eliminated and the concentration of estrogens in the body increases, the severity of hypoestrogenic (weight gain, fluid retention, osteoporosis) and hyperandrogenic (acne, hirsutism) symptoms decreases.

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.

Pituitary macroadenomas and associated symptoms (headache, visual field and acuity disturbances, cranial nerve and anterior pituitary functions) are reversed. Reduces the concentration of prolactin in patients with prolactinoma and pseudoprolactinoma (in the latter – without reducing the size of pituitary adenoma). A decrease in prolactin concentration is observed 3 hours after use and persists for 7-28 days in patients with hyperprolactinemia and 14-21 days – with suppression of postpartum lactation. A decrease in prolactin concentration occurs during 2-4 weeks of treatment.

Pharmacokinetics

Suction and distribution

Absorption is high, independent of food intake. The time to reach_cmax in blood plasma is 0.5 – 4 hours. Binding to plasma proteins is 41-42%.

T_1/2 is 63-68 hours in healthy volunteers and 79-115 hours in patients with hyperprolactinemia. Due to prolonged T_1/2, the equilibrium concentration is reached after 4 weeks of therapy.

Metabolism and elimination

It is actively metabolized. The metabolites have a significantly lower effect on inhibiting prolactin secretion compared to cabergoline.

Approximately 18% and 72% of the cabergoline dose taken is excreted by the kidneys and through the intestines, respectively, while 2-3% is excreted as unchanged cabergoline by the kidneys.

Indications

• 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 in combination with hyperprolactinemia.

Use during pregnancy and lactation

Since no controlled clinical trials have been conducted with cabergoline in pregnant women, prescribing the drug during pregnancy is only possible if absolutely necessary, when the potential benefit of using the drug for a woman significantly exceeds the possible risk to the fetus.

Pregnancy should be avoided for at least one month after discontinuation of cabergoline, given the prolonged T_1/2 of the drug and the presence of limited data on its effects on the fetus (according to reports the use of cabergoline at a dose of 0.5-2 mg per week about the disorders associated with hyperprolactinemia, were not accompanied by an increase in the frequency of miscarriages, premature birth, multiple pregnancy and congenital malformations).

If pregnancy occurs during treatment with cabergoline, discontinuation of the drug should be considered, also taking into account the ratio of the potential benefit of using the drug for a woman and the possible risk to the fetus.

Since cabergoline suppresses lactation, the drug should not be prescribed to mothers who want to breastfeed. Breast-feeding should be discontinued during cabergoline treatment.

Use in children

It is contraindicated in patients under 16 years of age (safety and efficacy in this category of patients have not been established).

Contraindications

• age up to 16 years;
• rare hereditary forms of galactose intolerance, congenital lapp lactase deficiency or glucose-galactose malabsorption (because the drug contains lactose);
• hypersensitivity to cabergoline or other components of the drug, as well as to any ergot alkaloids.

Caution should be exercised when prescribing the drug for the following conditions and/or diseases: :

• hypertension that developed on the background of pregnancy (e. g., preeclampsia) and/or postpartum hypertension;
• severe cardiovascular disease, Raynaud’s syndrome;
• peptic ulcer; gastrointestinal bleeding;
• severe hepatic impairment;
• severe psychotic and cognitive disorders (including history);
• the presence of fibrotic changes of the heart (valvulopathy) and respiratory system (pleurisy/pleural fibrosis), including in the anamnesis;
• concomitant use with drugs that have a hypotensive effect (because of the risk of orthostatic hypotension).

Side effects

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

From the cardiovascular system: palpitations, flushes of blood to the skin of the face, spasms of the vessels of the fingers (like other ergot derivatives, cabergoline can have a vasoconstrictive effect), valvulopathy; rarely-orthostatic hypotension (with prolonged treatment with cabergoline – hypotensive effect), there was an asymptomatic decrease in blood pressure during the first 3-4 days after delivery (systolic – more than 20 mm Hg, diastolic – more than 10 mm Hg). St. ).

Nervous system disorders: dizziness/vertigo, headache, fatigue, drowsiness, depression, mania, asthenia, paresthesia, syncope.

From the digestive system: nausea, vomiting, epigastric pain, abdominal pain, constipation, gastritis, dyspepsia, liver dysfunction.

Allergic reactions: hypersensitivity reactions, skin rash.

Others: mastodynia, nosebleeds, transient hemianopsia, lower limb muscle spasms, alopecia, increased serum creatinine clearance, edema, pleural fibrosis, respiratory disorders (including respiratory failure).

Interaction

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

Concomitant use of dopamine receptor antagonists (derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide) may weaken the effect of cabergoline.

Concomitant use of cabergoline with macrolides is not recommended due to the possible increase in the concentration of cabergoline in blood plasma. The mechanism of interaction of macrolides with cabergoline is not sufficiently studied, but, most likely, it is explained by the ability of macrolides and cabergoline to competitively inhibit the cytochrome P 450 system.

How to take, course of use and dosage

The drug is taken orally, with meals.

• prevention of lactation after delivery – 1 mg once (2 tablets) on the first day after delivery.
• suppression of established lactation – 0.25 mg (1/2 tab. ) 2 times / day every 12 hours for 2 days (total dose-1 mg). In order to reduce the risk of orthostatic hypotension in breast-feeding mothers, a single dose of Bergolak should not exceed 0.25 mg
• . treatment of disorders associated with hyperprolactinemia: the recommended starting dose is 0.5 mg per week in 1 dose (1 tab. ) or in 2 doses (1/2 tab., for example, on Monday and Thursday). The weekly dose should be increased gradually by 0.5 mg at monthly intervals until the optimal therapeutic effect is achieved. The therapeutic dose is usually 1 mg per week, but can range from 0.25 to 2 mg per week.

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

Depending on the tolerance, the weekly dose of Bergolak can be taken once or divided into 2 or more doses per week. Dividing the weekly dose into several doses is recommended when prescribing the drug at a dose of more than 1 mg per week.

The likelihood of side effects can be reduced by starting therapy with Bergolak with a low dose (for example,0.25 mg once a week), followed by a gradual increase until the therapeutic dose is reached. To improve the tolerability of the drug, if severe side effects occur, a temporary dose reduction is possible, followed by a more gradual increase (for example, an increase of 0.25 mg per week every 2 weeks).

Overdose

Symptoms: nausea, vomiting, abdominal pain, constipation, decreased blood pressure, orthostatic hypotension, headache, calf muscle cramps, severe asthenia, sweating, drowsiness, psychomotor agitation, psychosis, hallucinations.

Treatment: gastric lavage, blood pressure control, use of dopamine receptor antagonists (phenothiazine, butyrophenone, thioxanthene, metoclopramide derivatives).

Special instructions

Before prescribing cabergoline, a complete pituitary function study should be performed.

When increasing the dose of the drug, patients should be under the supervision of a doctor in order to determine the lowest dose that provides a therapeutic effect. During treatment, it is recommended to regularly (once a month) determine the concentration of prolactin in the blood serum. Normalization of prolactin concentrations is usually observed during 2-4 weeks of cabergoline therapy.

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

Cabergoline restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Since pregnancy can occur before menstruation recovers, it is recommended to perform pregnancy tests at least once every 4 weeks during the amenorrhea period, and after menstruation recovers – every time there is a delay in menstruation for more than 3 days.

Barrier methods of contraception should be used during treatment with cabergoline, as well as after discontinuation of the drug before repeating anovulation. If pregnancy occurs during treatment, discontinuation of the drug should be considered. Women who are pregnant should be monitored by a doctor for timely detection of symptoms of pituitary gland enlargement (during pregnancy, an increase in the size of pre-existing pituitary tumors may occur).

After long-term use of cabergoline, patients have experienced pleural effusion/pleural fibrosis and valvulopathy, so cabergoline should be used with caution in patients with current manifestations and / or clinical symptoms of cardiac dysfunction, including in the anamnesis.

Patients with arterial hypertension that developed during pregnancy (for example, preeclampsia) and/or postpartum arterial hypertension cabergoline is prescribed only in cases where 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 can cause sudden falling asleep. In such cases, it is recommended to reduce the dose of cabergoline or stop therapy.

Studies on the use of cabergoline in elderly patients with disorders associated with hyperprolactinemia have not been conducted.

Influence on the ability to drive motor vehicles and manage mechanisms

During the treatment period, it is recommended to refrain from driving vehicles and performing other activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Bergolak. Pills.

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Cabergoline

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For women, For adults as prescribed by a doctor

Indications

Lactation Suppression