Bergolak - instructions for use, dose, side effects, contraindications

Active substanceCabergolineCabergoline

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OBNINSKAYA CHEMICAL - PHARMACEUTICAL COMPANY, CJSC Russia

Dosage form: & nbsppills

Composition:

1 tablet contains:

active substance: cabergoline - 0.5 mg;

auxiliary substances: leucine, lactose (lactose anhydrous), magnesium stearate.

Description:Tablets are white, oblong, biconvex with a risk on one side.

Pharmacotherapeutic group:Dopamine receptor agonist

ATX: & nbsp

G.02.C.B.03 Cabergoline

Pharmacodynamics:

The dopamine receptor agonist, the ergoline derivative, inhibits the secretion of prolactin. Stimulates dopamine D2 receptors of lactotrophic cells of the pituitary gland; 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, the pulsating secretion of gonadotropins and the release of luteinizing hormone (LH) in the middle of the cycle are restored, the anovulatory cycles are eliminated and the concentration of estrogens in the body is increased,decreases the severity of hypoestrogen (weight gain, fluid retention, osteoporosis) and hyperandrogenic (acne, hirsutism, etc.) symptoms.

In men, reduces the hyperprolactinemia-related decrease in libido, impotence (with a decrease in the concentration of prolactin increases the concentration of testosterone), gynecomastia, lactorrhea. The macroadenoma of the pituitary gland and the associated symptoms (headache, disturbance of the fields and visual acuity, functions of the cranial nerves and the anterior lobe of the pituitary gland) are reversed. Reduces the concentration of prolactin in patients with prolactinoma and pseudoprolactinoma (in the latter - without reducing the size of the pituitary adenoma). Reduction in the concentration of prolactin is observed 3 hours after administration and persists for 7-28 days in patients with hyperprolactinaemia and 14-21 days - with suppression of postpartum lactation. Reduction in the concentration of prolactin occurs within 2-4 weeks of treatment.

Pharmacokinetics:

Absorption is high, it does not depend on food intake. Time to reach the maximum concentration in the blood plasma (Tc_m_Oh) - 0.5-4 hours. The connection with plasma proteins is 41-42%. The half-life (T_1/2) is 63-68 hours in healthy volunteers and 79-115 hours in patients with hyperprolactinaemia. Because of the long T_1/2 state of equilibrium concentration (C_ss) is achieved after 4 weeks of therapy. It is actively metabolized, metabolites have a much smaller effect on the inhibition of prolactin secretion compared to cabergoline. It is excreted by the kidneys and through the intestine about 18% and 72% of the dose of cabergoline, respectively, while in the form of unchanged cabergoline, 2-3% are excreted by the kidneys.

Indications:

- Prevention of postpartum lactation.

- Suppression of already established postpartum lactation.

- Treatment of disorders associated with hyperprolactinemia, including amenorrhea, oligomenorrhoea, anovulation, galactorrhea.

- Prolactin-secreting adenomas of the pituitary gland (micro- and macro-prolactinomas); idiopathic hyperprolactinaemia; syndrome of the "empty" Turkish saddle in combination with hyperprolactinemia.

Contraindications:

Hypersensitivity to cabergoline or other components of the drug, as well as to any ergot alkaloids.

Age to 16 years (safety and efficacy in this category of patients not established).

The preparation contains lactose.Do not take patients with rare hereditary forms of intolerance to galactose, a congenital deficiency of Lapp's lactase, or a violation of absorption of glucose-galactose.

Carefully:

Like other ergot derivatives, cabergoline should be administered with caution in the following conditions and / or diseases:

- arterial hypertension, developed against a background of pregnancy (eg, pre-eclampsia) and / or postpartum arterial hypertension;

-heavy diseases of the cardiovascular system, Raynaud's syndrome;

- Peptic ulcer, gastrointestinal bleeding;

severe liver failure;

-heavy psychotic and cognitive impairment (including in the anamnesis);

- the presence of fibrotic changes in the heart (valvulopathy) and the respiratory system (pleurisy / pleural fibrosis), including in history;

- simultaneous reception with drugs that have an antihypertensive effect (due to the risk of developing orthostatic hypotension).

Pregnancy and lactation:Since controlled clinical studies with the use of cabergoline in pregnant women were not performed, the appointment of the drug during pregnancy is possible only in case of emergency,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 cessation of cabergoline, given the long half-life of the drug and the availability of limited data on its effects on the fetus (according to available data, the use of cabergoline in a dose of 0.5-2 mg per week for violations , associated with hyperprolactinemia, was not accompanied by an increase in the frequency of miscarriages, premature birth, multiple pregnancies and congenital malformations). If the pregnancy occurred against the background of treatment with cabergoline, should consider the feasibility of discontinuing the drug, also considering the ratio of the potential benefits of using the drug for a woman and the possible risk to the fetus.

Because the cabergoline suppresses lactation, the drug should not be given to mothers who want to breast-feed. During treatment with cabergoline, breastfeeding should be discontinued.

Dosing and Administration:

Inside, with food.

To prevent lactation after childbirth: 1 mg once (2 tablets), on the first day after childbirth.

To suppress the established lactation: 0.25 mg (1/2 tablets) 2 times a 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.

For the treatment of violations associated with hyperprolactinemia: the recommended initial dose is 0.5 mg per week in 1 dose (1 tablet) or in 2 divided doses (1/2 tablet, for example, on Monday and Thursday). An increase in the weekly dose should be carried out gradually - by 0.5 mg with a monthly interval 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 tolerability, a weekly dose of Bergolak can be taken once or divided into 2 or more receptions per week. The division of the weekly dose into several doses is recommended when the drug is administered at a dose of more than 1 mg per week. The likelihood of developing side effects can be reduced by starting therapy with Bergolac from a low dose (for example, 0.25 mg once a week), then gradually increasing it until a therapeutic dose is reached.To improve the tolerability of the drug in the occurrence of severe side effects, a temporary dose reduction may be possible, followed by a more gradual increase (for example, an increase of 0.25 mg per week every 2 weeks).

Side effects:

Adverse events are usually transient, in severity - weak or moderately expressed and are dose-dependent. Occur, mainly, during the first 2 weeks of therapy and in most cases disappear on their own as they continue

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

From the nervous system: dizziness / vertigo, headache, increased fatigue, drowsiness, depression, mania, asthenia, paresthesia, fainting.

From the digestive system: nausea, vomiting, pain in the epigastric region, abdominal pain, constipation, gastritis, dyspepsia, impaired liver function.

Allergic reactions: reactions of hypersensitivity, skin rash.

Other: mastodonia, epistaxis, transient hemianopia, muscle cramps lower extremities, alopecia, increased activity of serum creatinine phosphokinase, edema, pleural fibrosis, respiratory disorders (including respiratory failure).

Overdose:Symptoms: nausea, vomiting, abdominal pain, constipation, lowering blood pressure, orthostatic hypotension, headache, calf muscle cramps, severe asthenia, sweating, drowsiness, psychomotor agitation, psychosis, hallucinations. Treatment: gastric lavage, control of blood pressure, administration of dopamine receptor antagonists (derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide).

Interaction:

It is not recommended simultaneous use with ergot alkaloids and their derivatives (with prolonged therapy with cabergoline).

With simultaneous use of antagonists of dopamine receptors (derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide, etc.) can weaken the action of cabergoline.

It is not recommended simultaneous use of cabergoline with macrolides in connection with a possible increase in the concentration of cabergoline in the blood plasma. The mechanism of interaction of macrolides with cabergoline is not sufficiently studied, but, apparently, due to the ability of macrolides and cabergoline to competitively inhibit the cytochrome P450 system.

Special instructions:

Before the appointment of cabergoline, a complete examination of the pituitary gland function is necessary.

With an increase in the dose of the drug, patients should be under the supervision of a physician in order to establish the lowest dose providing a therapeutic effect. During the period of treatment, it is recommended that the concentration of prolactin in the blood serum be determined regularly (once a month). Normalization of prolactin concentration is usually observed within 2-4 weeks of therapy with cabergoline.

After the withdrawal of cabergoline, a relapse of hyperprolactinemia is usually observed, but in some patients persistent decreases in prolactin concentrations persist for several months. In most women, ovulatory cycles persist for at least 6 months after the abolition of cabergoline.

Cabergoline restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Since pregnancy can occur before the recovery of menstruation, it is recommended that pregnancy tests be performed at least once every 4 weeks during the amenorrhea period, and after the recovery of menstruation, whenever there is a delay in menstruation for more than 3 days. It is necessary to use barrier methods of contraception in the burden of treatment with cabergoline, as well as after drug discontinuation before the recurrence of anovulation. If pregnancy occurred during treatment should consider the feasibility of drug discontinuation (see the section "Pregnancy and lactation"). Women who have become pregnant should be under the supervision of a doctor to promptly detect symptoms of an increase in the pituitary gland (during pregnancy, an increase in the size of pre-existing pituitary tumors may be possible).

After prolonged administration of cabergoline, patients 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, incl. in the anamnesis.

Patients with arterial hypertension that developed on a background of pregnancy (eg, pre-eclampsia) and / or postpartum arterial hypertension cabergoline appoint only in those cases when the potential benefit from the use 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 discontinue therapy. Studies on the use of cabergoline in elderly patients with disorders associated with hyperprolactinemia have not been conducted.

Effect on the ability to drive transp. cf. and fur:

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

Form release / dosage:

Tablets of 0.5 mg.

Packaging:2, 8 or 10 tablets into a contiguous cell package. By 2, 8, 10 or 30 tablets in a polymer bottle with a polymeric cover with control of the first dissection.Each vial or 1, 4 contourcell packs of 2 tablets, or 1 outline cell pack of 8 or 10 tablets together with instructions for use in a pack of cardboard.

Storage conditions:List B. At a temperature not higher than 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006647/10

Date of registration:09.07.2010/02.10.2015

Expiration Date:Unlimited

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp23.01.2017

Illustrated instructions

Instructions

Bergolak (Bergolak)