Bergolak
Bergolak: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. For violations of liver function
- 12. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Bergolak
ATX code: G02CB03
Active ingredient: cabergoline (cabergoline)
Producer: Veropharm, JSC (Russia)
Description and photo update: 2019-19-08
Prices in pharmacies: from 291 rubles.
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Bergolak is an inhibitor of prolactin secretion, an agonist of dopamine receptors.
Release form and composition
Dosage form - tablets: oblong biconvex, white, with a dividing line on one side (2 or 8 pcs. In a polymer bottle, 1 bottle in a cardboard box).
1 tablet contains:
- active substance: cabergoline - 0.5 mg;
- auxiliary components: lactopress (anhydrous lactose), magnesium stearate, leucine.
Pharmacological properties
Pharmacodynamics
Cabergoline is a dopamine receptor agonist, an ergoline derivative that suppresses prolactin secretion. This substance stimulates the dopamine D2 receptors of the pituitary lactotropic cells. Bergolac in high doses has a central dopaminergic effect, lowers the content of prolactin in the blood, helps to restore the menstrual cycle and fertility. In women, due to a decrease in the concentration of prolactin, the pulsating secretion of gonadotropins is restored and in the middle of the cycle luteinizing hormone is released, anovulatory cycles are eliminated, the content of estrogens in the body increases, the severity of hypoestrogenic (fluid retention, osteoporosis, weight gain) and hyperandrogenic (hirsutism, acne and etc.) symptoms.
In men, cabergoline reduces factors caused by hyperprolactinemia: decreased libido, impotence (due to a decrease in prolactin concentration, testosterone concentration increases), lactorrhea, gynecomastia. There is a reverse development of pituitary macroadenomas and associated symptoms (headaches, visual acuity and visual field disorders, the function of the anterior pituitary gland and cranial nerves). Reception of Bergolak helps to reduce the concentration of prolactin in patients with prolactinoma or pseudoprolactinoma (in the latter case, without reducing the size of the pituitary adenoma). The concentration of prolactin begins to decrease 3 hours after taking the drug, remaining for 14-21 days in case of suppression of postpartum lactation and 7-28 days in patients with hyperprolactinemia. The drug provides a decrease in the concentration of prolactin at 2–4 weeks of therapy.
Pharmacokinetics
Cabergoline is characterized by high absorption, independent of food intake. The maximum concentration of the drug in blood plasma is reached within 0.5-4 hours. Approximately 41-42% of the dose taken binds to plasma proteins. The half-life in healthy volunteers is 63 to 68 hours, and in patients with hyperprolactinemia, from 79 to 115 hours. Due to the long half-life, the state of equilibrium concentration is achieved 4 weeks after the start of treatment.
Cabergoline is extensively metabolized. Its metabolites provide a significantly smaller effect in terms of suppressing the secretion of prolactin in comparison with the active substance itself. It is excreted by the kidneys (about 18%) and through the intestines (about 72%), while the kidneys are excreted from 2 to 3% of unchanged cabergoline.
Indications for use
- prevention or suppression of postpartum lactation;
- treatment of conditions associated with hyperprolactinemia, including anovulation, amenorrhea, oligomenorrhea, galactorrhea;
- syndrome of "empty Turkish saddle", combined with hyperprolactinemia;
- idiopathic hyperprolactinemia, prolactin-secreting pituitary adenomas (macro- and microprolactinomas).
Contraindications
- age under 16;
- syndrome of glucose-galactose malabsorption, galactose intolerance, lactase deficiency;
- hypersensitivity to all ergot alkaloids;
- individual intolerance to cabergoline and other components of the drug.
According to the instructions, Bergolak should be prescribed with caution for severe pathologies of the cardiovascular system (including Raynaud's syndrome), arterial hypertension that occurs during pregnancy (including preeclampsia) and / or after childbirth, while taking drugs that have an antihypertensive effect (risk of orthostatic hypotension), severe liver failure, gastrointestinal bleeding, peptic ulcer, severe forms of psychotic and cognitive impairment (including history), in the presence (including history) of fibrotic changes in the heart and respiratory system (valvulopathy and pleurisy or pleural fibrosis).
The appointment of cabergoline during pregnancy is indicated only in the exceptional case when, according to the doctor's opinion, the potential benefit of therapy for the mother significantly exceeds the possible threat to the fetus.
After the preliminary administration of Bergolak, conception can begin no earlier than one month later.
If a woman becomes pregnant during treatment, it is necessary to consider the feasibility of discontinuing the drug, taking into account the balance of benefits and risks of therapy.
Bergolac should not be prescribed to women wishing to breastfeed, therefore, if treatment with cabergoline is necessary, breastfeeding should be discontinued.
Instructions for the use of Bergolak: method and dosage
Bergolac tablets are intended for oral administration with meals.
Recommended dosage:
- prevention of postpartum lactation: after childbirth on the first day - 1 mg once;
- suppression of established breastfeeding: 0.25 mg 2 times a day with an interval of 12 hours. Duration of admission is 2 days. Due to the risk of orthostatic hypotension, a single dose should not exceed 0.25 mg;
- treatment of conditions associated with hyperprolactinemia: the initial dose is 0.5 mg per week, can be taken once or divided into 2 doses of 0.25 mg with an interval of 3 days. An increase in the weekly dose should be made gradually, no more than 1 time per month by 0.5 mg. The increase is continued until the dose reached provides the optimal therapeutic effect, usually up to 1-2 mg per week, but not more than 4.5 mg. A dose of more than 1 mg per week is recommended to be divided into 2 or more doses per week in equal shares. To reduce the risk of side effects, treatment can be started with a weekly dose of 0.25 mg. If severe side effects appear, the dose can be temporarily reduced until the patient's tolerance for Bergolak improves. Then it should be gradually increased by 0.25 mg per week with an interval of 2 weeks.
Side effects
- from the nervous system: headache, drowsiness, vertigo (dizziness), fainting, fatigue, asthenia, paresthesia, mania, depression;
- on the part of the cardiovascular system: flushing of the skin of the face, palpitations, valvulopathy, spasms of the vessels of the fingers; rarely - orthostatic hypotension (with long-term treatment), asymptomatic decrease in blood pressure (BP) in the first 3-4 days after delivery;
- from the digestive system: pain in the epigastric region, nausea, vomiting, constipation, abdominal pain, dyspepsia, gastritis, functional liver disorder;
- allergic reactions: skin rash, hypersensitivity reactions;
- others: nosebleeds, muscle cramps of the lower extremities, mastodynia, transient hemianopsia, alopecia, edema, respiratory disorders (including respiratory failure), pleural fibrosis, increased serum creatine phosphokinase (CPK) activity.
Adverse effects are dose-dependent, usually transient, and may be mild or moderate in severity.
Overdose
Symptoms: nausea, vomiting, constipation, abdominal pain, low blood pressure, headache, orthostatic hypotension, calf muscle cramps, sweating, drowsiness, severe asthenia, psychomotor agitation, hallucinations, psychosis.
Treatment: gastric lavage, ensuring blood pressure control, the use of dopamine receptor antagonists (derivatives of butyrophenone, phenothiazine, thioxanthene, metoclopramide).
special instructions
The appointment of cabergoline is based on the results of a complete study of the function of the pituitary gland.
To establish the lowest effective dose of Bergolak, its selection should be carried out under the supervision of a physician. It is necessary to monitor the level of prolactin concentration in the blood serum regularly (once a month) during the entire period of treatment. Usually, its normalization occurs after 2-4 weeks of using cabergoline.
The appearance of a relapse of hyperprolactinemia after Bergolak's discontinuation is possible; a steady decrease in the concentration of prolactin in some patients persists for several months. Ovulatory cycles after drug withdrawal in most cases persist for 6 months.
Side effects of Bergolak often occur during the first weeks of therapy and usually go away on their own with continued therapy or after drug withdrawal.
With arterial hypertension that develops during pregnancy and / or after childbirth, the appointment of cabergoline is possible only if the potential benefit of therapy exceeds the likely risk.
It is necessary to use barrier methods of contraception both during the period of treatment and after the cancellation of Bergolak before the recurrence of anovulation. Women who become pregnant while taking the pills need close medical supervision. This will promptly identify the symptoms of an enlarged pituitary gland.
Bergolak restores fertility and ovulation in women with hyperprolactinemic hypogonadism. Because of the possible conception before the menstruation is restored, it is recommended to carry out pregnancy tests at least 1 time per month during the period of amenorrhea; after the menstrual cycle is restored, the test is carried out at each delay of menstruation for more than 3 days.
Because the drug causes drowsiness, patients with Parkinson's disease need to reduce their usual dose or stop taking the pills if Bergolac makes them fall asleep suddenly.
You should refrain from driving vehicles and mechanisms during the entire period of treatment.
Application during pregnancy and lactation
Bergolac is contraindicated for the treatment of pregnant women, since no controlled clinical trials have been conducted with cabergoline in this group of patients. During pregnancy, it is allowed to prescribe the drug only in cases of extreme necessity, if the potential risk to the fetus is lower than the expected benefit to the mother. Pregnancy should be avoided for at least 1 month after the termination of cabergoline therapy, since the drug has a long half-life, and there is no sufficient data on the effect of the active substance on the fetus (according to available information, the use of cabergoline at a dose of 0.5–2 mg for a week for disorders caused by hyperprolactinemia were not accompanied by an increase in the incidence of preterm birth, miscarriages, congenital malformations or multiple pregnancies). If pregnancy occurs on the background of cabergoline therapy, the possibility of discontinuing Bergolak should be considered based on an analysis of the ratio of the potential risk to the fetus and the expected benefit to the mother.
Since cabergoline suppresses lactation, Bergolac tablets should not be prescribed to patients who intend to breastfeed. During treatment with cabergoline, breastfeeding should be discontinued.
Pediatric use
It is forbidden to use Bergolac for the treatment of patients under the age of 16 years.
For violations of liver function
In severe hepatic impairment, Bergolac should be used with caution.
Use in the elderly
Studies of the use of cabergoline in elderly patients with disorders caused by hyperprolactinemia have not been conducted.
Drug interactions
It is not recommended to prescribe ergot alkaloids and their derivatives during prolonged therapy with Bergolac.
The combination with antagonists of dopamine receptors (derivatives of butyrophenone, phenothiazine, metoclopramide, thioxanthene) can weaken the effect of Bergolac.
Due to the risk of increasing the concentration of cabergoline in blood plasma, it is not recommended to use macrolides at the same time.
Analogs
Bergolak's analogues are Cabergoline, Agalates, Dostinex.
Terms and conditions of storage
Store at temperatures up to 25 ° C out of reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Bergolak
Reviews of Bergolak as a means of stopping lactation are predominantly positive. Some users report that side effects may develop in the first weeks of therapy.
Price for Bergolak in pharmacies
The approximate price for Bergolac is: 2 tablets of 0.5 mg - 290 rubles, 8 tablets of 0.5 mg - 860 rubles.
Bergolak: prices in online pharmacies
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Drug name Price Pharmacy |
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Bergolak 0.5 mg tablets 2 pcs. RUB 291 Buy |
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Bergolac 0.5 mg tablets 8 pcs. RUB 936 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
