Bromocriptine
Bromocriptine: 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. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Bromocriptine
ATX code: N.04. BC01
Active ingredient: bromocriptine (bromocriptine)
Producer: Gedeon Richter (Hungary), Kiev Vitamin Plant (Ukraine), Ozon LLC (Russia)
Description and photo update: 2019-13-08
Prices in pharmacies: from 194 rubles.
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Bromocriptine belongs to the group of inhibitors of prolactin secretion, is an antiparkinsonian drug.
Release form and composition
Bromocriptine is available in the form of 2.5 mg tablets (10, 20, 30, 40, 50, 60 or 100 pieces in blisters or polymer containers).
The active ingredient of the drug is bromocriptine.
Pharmacological properties
Pharmacodynamics
Bromocriptine is an ergot derivative and dopamine receptor agonist (D 2). The compound inhibits the production of prolactin in the anterior pituitary gland and does not affect the synthesis and release of other pituitary hormones (with the exception of patients with acromegaly, in whom bromocriptine reduces the level of growth hormone). In the postpartum period, prolactin is required for the initiation and further maintenance of lactation. In other periods of life, an increase in prolactin production causes menstrual irregularities and ovulation and / or pathological lactation (galactorrhea).
Bromocriptine, which belongs to specific inhibitors of prolactin synthesis, can be used to prevent or suppress physiological lactation, as well as in the treatment of pathological conditions provoked by prolactin hypersecretion.
In anovulatory menstrual cycles, which are accompanied or not accompanied by galactorrhea, and / or amenorrhea, bromocriptine helps to normalize ovarian function and restore endocrine regulation at the ovarian-pituitary level.
The use of bromocriptine does not lead to impaired postpartum uterine involution and does not increase the risk of thromboembolism, and also reduces the severity of clinical symptoms in polycystic ovary syndrome.
The drug inhibits the growth or reduces the size of prolactinomas (prolactin-secreting adenomas).
In patients with acromegaly, bromocriptine not only reduces the content of prolactin and growth hormone in the blood plasma, but also has a positive effect on the clinical manifestations of the disease and glucose tolerance.
In Parkinson's disease, accompanied by a dopamine deficiency in certain structures of the brain, the drug is used in higher doses than in the treatment of endocrine diseases. Bromocriptine activates dopamine receptors, ensuring the restoration of neurochemical balance in these structures. When the drug is prescribed, the severity of the symptoms of depression, which are often observed in patients with parkinsonism (gait disturbance, tremor, akinesia and rigidity at all stages of the disease), decreases.
The drug is able to lower blood pressure, but the mechanism of this action remains poorly understood. There are suggestions that this effect is due to an agonistic effect on central dopamine receptors. As a result, vascular tone decreases, and the concentration of catecholamines in the blood plasma also decreases. Thus, the drug acts as a vasodilator.
Pharmacokinetics
After oral administration, bromocriptine is absorbed from the gastrointestinal tract by 25-30%. Its maximum content in blood plasma is reached within 1-3 hours. When the drug is taken orally at a dose of 5 mg, its maximum plasma concentration is 0.465 ng / ml. The effect of decreasing prolactin is observed 1-2 hours after oral administration of the drug and reaches a peak after 5-10 hours - the concentration of prolactin decreases by about 80%, after which it remains unchanged for 8-12 hours.
Bromocriptine binds to blood plasma proteins by about 96%. It is extensively metabolized in the liver during "primary passage", forming a number of metabolites. The bioavailability of this compound is approximately 6%. In vitro studies have shown that bromocriptine has a high affinity for the CYP3A enzyme. Competing substrate and / or CYP3A4 inhibitors can inhibit metabolic processes in which bromocriptine is involved and increase its level in blood plasma. The effect of microsomal liver oxidation enzymes (CYP2C19, CYP2C8, CYP2D6) on the metabolism of the drug is not well understood. Bromocriptine is a CYP3A4 inhibitor.
The unchanged drug is excreted from the blood plasma in a biphasic manner. The final elimination half-life reaches 15 hours on average (the range is 8-20 hours). Bromocriptine and its metabolites are almost completely excreted in the feces, only 6% is excreted in the urine.
In patients with liver dysfunctions, the rate of excretion of bromocriptine may decrease, and its content in blood plasma may increase, which requires dose adjustment. The effect of gender, race and age of patients on the pharmacokinetic parameters of the active component of the drug and its metabolites has not been sufficiently studied.
Indications for use
According to the instructions, Bromocriptine is advisable to use for female infertility and menstrual irregularities:
- Prolactin-dependent conditions and diseases that are accompanied or not accompanied by hyperprolactinemia (oligomenorrhea; secondary hyperprolactinemia induced by drugs; amenorrhea, accompanied and not accompanied by galactorrhea; luteal phase failure);
- Prolactin-independent female infertility (polycystic ovary syndrome, anovulatory cycles - as an additional treatment to antiestrogens).
Also indications for prescribing the drug are:
- Hyperprolactinemia in men: prolactin-dependent hypogonadism (loss of libido, oligospermia, impotence);
- Benign breast diseases: benign cystic and / or nodular changes, especially fibrocystic breast disease; mastalgia in isolation or in combination with benign cystic or nodular changes or with premenstrual syndrome;
- Premenstrual syndrome: edema associated with the phase of the cycle; soreness of the mammary glands; flatulence; mood disorders;
- Prolactinomas: as a conservative treatment for prolactin-secreting micro- and macroadenomas of the pituitary gland; in order to reduce the size of the tumor and facilitate its removal (in the preoperative period of therapy); as a postoperative therapy if the prolactin level remains elevated;
- Parkinson's disease, parkinsonism syndrome, including after encephalitis (as monotherapy, or as part of a combination treatment with other antiparkinsonian drugs).
Also, Bromocriptine is prescribed to stop lactation or prevent it after childbirth if there is a medical indication (postpartum engorgement of the mammary glands, prevention of lactation after abortion, postpartum mastitis that begins).
Contraindications
- Chorea of Huntington;
- Arterial hypotension / hypertension;
- Essential and familial tremors;
- Severe forms of cardiovascular disease;
- Endogenous psychoses;
- Pregnancy toxicosis;
- Hypersensitivity of the patient to ergot alkaloids.
Instructions for the use of Bromocriptine: method and dosage
The exact dosage and duration of therapy are determined individually.
Tablets are taken orally at 1.25-2.5 mg 2-3 times a day.
The daily dose of the drug may be gradually increased:
- With prolactinoma, male hypogonadism, acromegaly, benign diseases of the mammary glands - up to 5-20 mg;
- With parkinsonism - up to 10-40 mg.
In the event that side reactions appear during the selection of the dose, it is necessary to reduce the daily dose of Bromocriptine and maintain it at this level for a week. When the side effects disappear, you can increase the dose again.
Side effects
In some cases, the use of Bromocriptine can cause the following side effects:
- From the side of the central nervous system: headaches, dizziness (usually occurs in the first week of therapy), psychomotor agitation, decreased visual acuity, drowsiness, dyskinesia, hallucinations;
- From the digestive system: diarrhea, nausea and vomiting, constipation, liver dysfunction, dry mouth;
- On the part of the cardiovascular system: arrhythmia, orthostatic hypotension; with prolonged use, in some cases - Raynaud's syndrome (especially in patients with a predisposition);
- Allergic reactions: skin rash;
- Others: cramps in the calf muscles, nasal congestion.
Overdose
Overdose symptoms include hallucinations, blurred consciousness, headache, drowsiness, nausea, vomiting, chest pain, cold extremities, heart palpitations, weak pulse, changes in blood pressure (most often a decrease).
In this case, symptomatic therapy is recommended. During the first 3 hours after taking Bromocriptine, it is necessary to flush the stomach and take activated charcoal in order to reduce the absorption of the drug from the gastrointestinal tract.
special instructions
Bromocriptine is prescribed with caution with concurrent antihypertensive therapy, as well as if the patient has:
- Parkinsonism with signs of dementia;
- A history of gastrointestinal bleeding;
- Erosive and ulcerative lesions of the gastrointestinal tract.
During therapy, it is necessary to regularly monitor the patient's condition and blood pressure due to the possibility (especially in the first days of treatment) of the occurrence of hypotensive reactions.
As the dose is reduced, most of the side effects of Bromocriptine tend to decrease. At the initial stages of treatment, it is recommended to prescribe an antiemetic agent one hour before taking the drug.
With prolonged use of Bromocriptine by women with a regular monthly cycle, it is necessary to undergo a gynecological examination once a year, preferably with a cytological examination of the tissues of the cervix and endometrium. When menopause occurs within six months, diagnostics are carried out every month.
Bromocriptine therapy can normalize reproductive function. In order to prevent unwanted pregnancy, you should use reliable contraception (with the exception of hormonal contraceptives).
With pituitary adenoma, accompanied by a significant increase in the size of the sella turcica and impaired visual fields, the appointment of the drug is possible only in cases of ineffectiveness of surgical treatment and radiation therapy.
In the case of the appointment of Bromocriptine for mastopathy, the presence of a malignant tumor should be completely excluded.
Combination therapy with bromocriptine and levodopa in Parkinson's disease and parkinson's syndrome can increase the clinical effect, which allows you to reduce the dose of levodopa or cancel it completely. This is especially important in the treatment of patients in whom levodopa therapy does not lead to a stable therapeutic effect, or causes the development of motor disorders.
Patients taking Bromocriptine are advised to refrain from carrying out potentially hazardous activities that require psychomotor speed and increased concentration.
Application during pregnancy and lactation
When pregnancy occurs, Bromocriptine should be stopped immediately unless the potential benefit of therapy to the mother significantly outweighs the potential risks to the fetus (with large pituitary tumors showing a tendency to grow). Taking the drug in the first 8 weeks of pregnancy does not have a negative effect on the course and outcome of pregnancy. After the abolition of bromocriptine, the risk of spontaneous miscarriage does not increase.
The drug reduces the production of breast milk, so it should not be used during lactation.
To stop lactation, Bromocriptine may be prescribed if medically indicated.
Drug interactions
With the simultaneous use of bromocriptine with oral contraceptives, the level of prolactin in the blood plasma increases. The drug should not be administered together with other ergot alkaloids.
Bromocriptine enhances the effect of antihypertensive drugs and levodopa. The effectiveness of their treatment may decrease when combined with tricyclic antidepressants (amitriptyline, imipramine) or dopamine agonists (butyrophenones, phenothiazines).
Phenothiazines, monoamine oxidase inhibitors, thioxanthines, furazolidone, reserpine, loxapine, metoclopramide, methyldopa increase the content of bromocriptine in the blood plasma and increase the risk of side effects.
When bromocriptine is combined with ritonavir, it is recommended to reduce the dose of the former by 50%. The combination of the drug with sympathomimetics can provoke attacks of severe headaches and increased blood pressure. With the simultaneous administration of bromocriptine and sumatriptan, the risk of a vasospastic reaction increases due to the additive action of these compounds.
The maximum concentration of bromocriptine in blood plasma and its bioavailability increase when the drug is combined with octreotide, erythromycin, clarithromycin and josamycin.
Bromocriptine increases the concentration in the blood of drugs that are metabolized by the isoenzyme CYP3A4. Caution should be exercised when combining bromocriptine with drugs with a narrow therapeutic index, especially those provoking a prolongation of the QT interval (for example, terbinafine, imipramine, amiodarone).
The combination of ethanol with bromocriptine can lead to the development of disulfiram-like reactions, expressed in convulsive seizures, weakness, chest pain, decreased visual acuity, hyperemia, throbbing headache, reflex cough, nausea, vomiting.
Analogs
Bromocriptine analogs are: Abergin, Parlodel, Bromergon, Bromocriptine-KB, Bromocriptine-Richter.
Terms and conditions of storage
Shelf life - 3 years, store in a dry, dark place at a temperature of 2-8 ° C. Keep out of the reach of children.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Bromocriptine
Numerous reviews of Bromocriptine prove the effectiveness of the drug. Patients report a decrease in prolactin levels, a rapid cessation of lactation, and the disappearance of breast lumps. The drug has helped to stop the production of breast milk for many breastfeeding women, but there are reports that not all patients have been helped. Some patients speak negatively about Bromocriptine due to frequent and severe side effects.
The price of Bromocriptine in pharmacies
The approximate price of Bromocriptine in pharmacies is 188-287 rubles (the package includes 30 tablets).
Bromocriptine: prices in online pharmacies
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Drug name Price Pharmacy |
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Bromocriptine 2.5 mg tablets 30 pcs. 194 r Buy |
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Bromocriptine tab. 2.5mg can # 30 RUB 300 Buy |
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Bromocriptine Richter 2.5mg tablets 30 pcs. 346 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
