Bromocriptine, pills 2.5mg, 30pcs – Ozon

Composition

1 tablet contains:

Active ingredient:

bromocriptine mesylate 2.87 mg;

Auxiliary substances:

lactose monohydrate 55.63 mg,

microcrystalline cellulose 20 mg,

potato starch 15 mg,

sodium carboxy methyl starch 2 mg,

povidone (polyvinylpyrropidone) 3.5 mg,

magnesium stearate 1 mg

Pharmacological action

Bromocriptine is a stimulator of central and peripheral D2-dopamine receptors (ergot alkaloid derivative). By inhibiting prolactin secretion, it suppresses physiological lactation, promotes normalization of menstrual function, inhibits increased secretion of growth hormone, reduces the size and number of cysts in the mammary gland (by eliminating the imbalance between progesterone and estrogens).

In high doses, it stimulates dopamine receptors in the striatum, black nucleus accumbens, hypothalamus, and mesolimbic system. It has an antiparkinsonian effect, suppresses the secretion of somatotropic (GH) and adrenocorticotropic (ACTH) hormones.

After taking a single dose, a decrease in the level of plasma prolactin occurs in 2 hours, the maximum effect-in 8 hours, the antiparkinsonian effect – in 30-90 minutes, the maximum-in 2 hours, a decrease in the level of GH – in 1-2 hours, the maximum effect is achieved in 4-8 weeks. therapy sessions.

Pharmacokinetics

After oral use, the absorption of bromocriptine from the gastrointestinal tract is 28%. Undergoes the “first pass” effect through the liver. Bioavailability – 6%. The time to reach the maximum concentration in blood plasma is 1-3 h. T1 / 2 biphasic: 4-4.5 h in the alpha phase,1 h in the terminal phase.

Binding to plasma albumins is 90-96%.

It is mainly excreted with feces-85.6% and to a small extent in the urine-2.5-5.5%.

Indications

• Menstrual disorders, female infertility:  prolactin-dependent diseases and conditions that are accompanied or not accompanied by hyperprolactinemia (amenorrhea, accompanied or not accompanied by galactorrhea; oligomenorrhea; luteal phase insufficiency; drug-induced secondary hyperprolactinemia); prolactin-independent female infertility (polycystic ovarian syndrome; anovulatory cycles – as an additional therapy to anti-estrogens).
• Premenstrual syndrome:  breast tenderness; edema associated with the cycle phase; flatulence; mood disorders.
• Hyperprolactinemia in men:  prolactin-dependent hypogonadism (oligosperimia, loss of libido, impotence).
• Prolactinomas:  conservative treatment of prolactin-secreting pituitary micro-and macroadenomas; in the preoperative period to reduce the size of the tumor and facilitate its removal; postoperative treatment if the level of prolactin remains elevated.
• Suppression of lactation:  prevention or termination of postpartum lactation for medical reasons – prevention of lactation after abortion; postpartum breast engorgement; incipient postpartum mastitis.
• Benign breast diseases:  mastalgia in isolation or in combination with premenstrual syndrome or benign nodular or cystic changes); benign nodular and/or cystic changes, especially fibrocystic mastopathy.
• Parkinson’s disease and Parkinsonism syndrome, including after encephalitis (as monotherapy or in combination with other antiparkinsonian agents).

Use during pregnancy and lactation

Use with caution during pregnancy and lactation.

Contraindications

• Hypersensitivity to bromocriptine and other ergot alkaloids.
• Gestosis.
• Arterial hypertension in the postpartum period.
• Diseases of the cardiovascular system (including arterial hypertension, hypotension).
• Essential, familial tremor.
• Psychoses.
• Liver failure.
• Gettington’s chorea.
• Ulcerative lesions of the gastrointestinal tract.
• Children’s age.

With caution:

• Parkinsonism with dementia symptoms.
• Pregnancy.
• Lactation period.
• Simultaneous antihypertensive therapy.

Side effects

From the digestive system: nausea, vomiting, dry mouth, constipation, diarrhea, liver function disorders.

From the central nervous system:  dizziness (usually occurs in the first week of treatment), headache, drowsiness, psychomotor agitation, dyskinesia, decreased visual acuity, hallucinations.

From the cardiovascular system:  orthostatic hypotension, arrhythmia; in some cases, with prolonged use – Raynaud’s syndrome (especially in predisposed patients).

Allergic reactions:  skin rash.

Other services:  nasal congestion, cramps in the calf muscles.

Interaction

Reduces the effectiveness of oral contraceptives.

Increases the effect of levodopa, antihypertensive drugs.

Monoamine oxidase inhibitors, furazolidone, procarbazine, sepegiline, ergot alkaloids, haloperidol, loxapine, methyldopa, metocpopramide, molindone, reserpine, thioxanthines and phenothiazines increase plasma concentrations and the risk of side effects.

Erythromycin, clarithromycin, and troleandomycin increase bioavailability and maximum concentration, while butyrophenones decrease efficacy.

Simultaneous use of ethanol leads to the development of disulfiram-like reactions (chest pain, hyperemia of the skin, tachycardia, nausea, vomiting, reflex cough, throbbing headache, blurred vision, weakness, convulsions).

When co-administered with ritonavir, a 50% dose reduction is recommended.

How to take, course of use and dosage

Inside, with meals, the maximum daily dose is 100 mg.

Menstrual disorders, female infertility:  1.25 mg 2-3 times a day; if the effect is insufficient, the dose is gradually increased to 5-7.5 mg/day (multiplicity of use 2-3 times / day). Treatment is continued until the menstrual cycle is normalized and / or ovulation is restored. If necessary, to prevent relapses, treatment can be continued for several cycles.

Premenstrual syndrome:  treatment begins on the 14th day of the cycle with 1.25 mg / day. Gradually increase the dose by 1.25 mg / day to 5 mg / day (before the onset of menstruation).

Hyperprolactinemia in men:  1.25 mg 2-3 times a day, gradually increasing the dose to 5-10 mg / day.

Prolactinomas:  1.25 mg 2-3 times a day, with a gradual increase in the dose to several tablets per day, necessary to maintain an adequate decrease in the concentration of prolactin in plasma.

Acromegaly:  the initial dose is 1.25 mg 2-3 times a day, then, depending on the clinical effect and side effects, the daily dose is gradually increased to 10-20 mg.

Suppression of lactation:  on day 1,1.25 mg is prescribed 2 times (with meals for breakfast and dinner), then for 14 days-2.5 mg 2 times a day. To prevent the onset of lactation, the drug should be started several hours after delivery or abortion (after the stabilization of vital functions).2-3 days after discontinuation of the drug, sometimes there is a slight secretion of milk. It can be eliminated by resuming the drug at the same dose for another 1 week.

Postpartum breast engorgement:  assign a single dose of 2.5 mg, after 6-12 hours, if necessary, repeat the reception (this is not accompanied by undesirable suppression of lactation).

Incipient postpartum mastitis:  the dosage regimen is the same as in the case of lactation suppression. If necessary, an antibiotic is added to the treatment.

Benign breast diseases:  1.25 mg 2-3 times a day. The daily dose is gradually increased to 5-7.5 mg.

Parkinson’s disease:  to ensure optimal tolerability, treatment should begin with a small dose of the drug: 1.25 mg once a day (preferably in the evening) for 1 week. The daily dose of the drug is increased gradually, every week by 1.25 mg, the daily dose is divided into 2-3 doses. An adequate therapeutic result can be achieved within 6-8 weeks of treatment. If this does not happen, the daily dose can be increased further – every week by 2.5 mg/day. The average therapeutic dose of bromocriptine for mono-or combination therapy is 10-30 mg / day. The maximum daily dose is 30 mg. If side effects occur during dose selection, the daily dose should be reduced and maintained at a lower level for at least 1 week. If the side effects disappear, the dose of the drug can be increased again. Patients with motor disorders that occur while taking levodopa are recommended to reduce the dose of levodopa before starting the use of bromocriptine. After achieving a satisfactory effect, further gradual reduction in the dose of levodopa can be undertaken. In some patients, complete withdrawal of levodopa is possible.

Overdose

Symptoms:  headache, hallucinations, low blood pressure.

Treatment:  parenteral use of metoclopramide.

Special instructions

To prevent nausea and vomiting at the beginning of treatment, it is advisable to prescribe antiemetic medications 1 hour before taking the drug.

Periodic monitoring of blood pressure, liver and kidney function is recommended.

When using the drug in high doses for a long period of time, the risk of developing cardiac fibrosis is increased.

Treatment can cause an accelerated resumption of ovarian function after childbirth, and therefore, it is necessary to warn women about the possibility of early postpartum conception. In women taking bromocriptine, treatment is discontinued at the onset of pregnancy, except in cases where the possible positive effect of treatment outweighs the potential risk to the fetus. During therapy, it is advisable to use non-hormonal contraception.

If pregnancy occurs against the background of pituitary adenoma after withdrawal, systematic monitoring of its condition is necessary, including the study of visual fields. Before starting treatment of benign breast diseases, it is necessary to exclude the presence of a malignant tumor of the same localization.

In the treatment of acromegaly, if there is an indication of the presence of gastric ulcer in the anamnesis, it is better to refuse treatment. If treatment is necessary, pay attention to the need to inform the doctor about the occurrence of disorders of the gastrointestinal tract.

It is necessary to carefully observe oral hygiene, if the oral cavity remains dry for more than 2 weeks, it is necessary to consult a doctor.

– Influence on the ability to drive vehicles and manage mechanisms Patients taking the drug should refrain from engaging in activities that require increased attention and rapid physical and mental reactions.

Storage conditions

Store in a dry place, protected from light, at a temperature of 2-8 °C

Shelf life

3 years

Active ingredient

Bromocriptine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Infertility Treatment, Lactation suppression