Bergolak, tablets 0.5 mg 8 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. Reduces the concentration of prolactin in the blood, restores the 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. Decreases the concentration of prolactin in patients with prolactinoma and pseudoprolactinoma (in the latter – without reducing the size of pituitary adenoma). Decrease of prolactin concentration is noticed in 3 hours after treatment and lasts for 7-28 days in patients with hyperprolactinemia and 14-21 days – when we suppress postpartum lactation. Decrease of prolactin concentration occurs within 2-4 weeks of treatment.

Pharmacokinetics

Absorption and distribution

Absorption is high, not dependent on food intake. Time to reach C_max in blood plasma is 0.5-4 hours. Binding to plasma proteins is 41-42%.

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

Metabolism and excretion

Actively metabolized. Metabolites have significantly less effect in suppressing prolactin secretion compared to cabergoline.

The urinary and intestinal excretion is about 18% and 72% of the ingested dose of cabergoline, respectively, with 2-3% excretion of unchanged cabergoline in the kidneys.

Indications

Suppression of lactation

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

.

Active ingredient

Cabergoline

Composition

1 tablet contains:

cabergoline 500 mcg

Associates:

Leucine,

Lactose anhydrous (lactopress),

Magnesium stearate.

How to take, the dosage

The drug is taken orally with food.

• prevent lactation after childbirth – 1 mg once (2 tablets) on the first day after childbirth.
• reducing established lactation – 0.25 mg (1/2 tablet) 2 times/day every 12 hours for 2 days (total dose of 1 mg). To decrease the risk of orthostatic hypotension in breastfeeding mothers, the single dose of Bergolac should not exceed 0.25 mg.
• Treatment of hyperprolactinemia disorders: The recommended starting dose is 0.5 mg weekly in 1 sitting (1 tablet) or in 2 sitting (1/2 tablet, for example, on Monday and Thursday). The weekly dose should be increased gradually by 0.5 mg at monthly intervals until 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 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 may be reduced by starting therapy with Bergolac at a low dose (e.g., 0.25 mg once weekly), increasing gradually until the therapeutic dose is reached. A temporary reduction in dose followed by a more gradual increase (e.g., 0.25 mg weekly every 2 weeks) may be necessary to improve tolerance to treatment if there are severe side effects.

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 increase of plasma concentration of cabergoline. The mechanism of interaction between macrolides and 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 a pregnancy occurs during treatment, you should consider stopping the drug. Women who become pregnant should be monitored by a physician for timely detection of symptoms of pituitary enlargement (during pregnancy an increase in the size of preexisting pituitary tumors is possible).

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

Patients with arterial hypertension developed during pregnancy (e.g., preeclampsia) and/or postpartum arterial hypertension should prescribe cabergoline only 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 reduce the dose of cabergoline or discontinue therapy.

There have been no studies on the use of cabergoline in elderly patients with hyperprolactinemia-related disorders.

Impact on driving and operating machinery

At the time of treatment, it is recommended to refrain from driving and engaging in other activities requiring increased concentration and quick psychomotor reactions.

Contraindications

• age before 16 years of age
• hereditary forms of galactose intolerance, congenital lactase lapp deficiency or glucose-galactose malabsorption (because the drug contains lactose
• high sensitivity to cabergoline or other ingredients of the drug and to any ergot alkaloid.
• High sensitivity to cabergoline or other ingredients of the drug as well as to any ergot alkaloids.

The following conditions and/or diseases should be treated with caution:

• Arterial hypertension developed in pregnancy (e.g., preeclampsia) and/or postpartum arterial hypertension;
• severe cardiovascular disease, Raynaud’s syndrome;
• peptic ulcer, gastrointestinal bleeding;
• severe hepatic insufficiency;
• severe psychotic and cognitive disorders (incl.severe psychotic and cognitive impairment (including history);
• presence of fibrotic changes in heart (valvulopathy) and respiratory system (pleurisy/pleural fibrosis) including history;
• concurrent use with antihypertensive medications (due to risk of orthostatic hypotension)

.

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, prescription of dopamine receptor antagonists (phenothiazine derivatives, butyrophenone, thioxanthene, metoclopramide).

Pregnancy use

Since no controlled clinical studies have been conducted with the use of cabergoline in pregnant women, the drug may only be prescribed in pregnancy if absolutely necessary, when the potential benefit to the woman far outweighs the possible risk to the fetus.

Pregnancy should be avoided for at least one month after discontinuation of cabergoline, given the long T_1/2 drug and the limited data on its effects on the fetus (the use of cabergoline at a dose of 05-2 mg per week for hyperprolactinemia-related disorders has not been associated with an increased incidence of miscarriage, preterm birth, multiple pregnancies, and congenital malformations).

If a pregnancy occurs with cabergoline treatment, discontinuation of the drug should be considered, also considering the balance of potential benefit to the woman versus possible risk to the fetus.

Because cabergoline suppresses lactation, the drug should not be prescribed to mothers who want to breastfeed. Breastfeeding should be stopped during treatment with cabergoline.

Pediatric use

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

Similarities

Dostinex, Agalates, Lacto-Stop, Galastop