Bromocriptine, 2.5 mg, 30 pcs.

1 tablet contains:

Active substance:

bromocriptine mesylate 2.87 mg; 

Excipients:

lactose monohydrate 55.63 mg,

microcrystalline cellulose 20 mg,

potato starch 15 mg,

carboxy methyl starch sodium 2 mg,

povidone (polyvinylpyropidone) 3.5 mg,

magnesium stearate 1 mg.

Bromocriptine is a stimulant of central and peripheral D 2 dopamine receptors (a derivative of ergot alkaloids). By inhibiting the secretion of prolactin, it suppresses physiological lactation, contributes to the 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 the dopamine receptors of the striatum, black nucleus of the brain, hypothalamus and the mesolimbic system. It has an antiparkinsonian effect, suppresses the secretion of somatotropic (STH) and adrenocorticotropic (ACTH) hormones.

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

Pharmacokinetics

After oral administration, the absorption of bromocriptine from the gastrointestinal tract is 28%. It undergoes a “first pass” effect through the liver. Bioavailability is 6%. The time to reach the maximum plasma concentration is 1-3 hours. T1 / 2 is two-phase: 4-4.5 hours in the α phase, 1 hour in the terminal phase.

Binding to plasma albumin is 90-96%.

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

• Menstrual irregularities, female infertility: prolactin-dependent diseases and conditions, accompanied or not accompanied by hyperprolactinemia (amenorrhea, accompanied and not accompanied by galactorrhea; oligomenorrhea; luteal phase insufficiency; secondary hyperprolactinemia induced by drugs); prolactin-independent female infertility (polycystic ovary syndrome; anovulatory cycles - as an additional therapy for antiestrogens).
• Premenstrual syndrome: breast tenderness; edema associated with the phase of the cycle; flatulence; mood disorders.
• Hyperprolactinemia in men: prolactin-dependent hypogonadism (oligospermia, 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 prolactin level remains elevated.
• Suppression of lactation: prevention or termination of postpartum lactation for medical reasons - prevention of lactation after abortion; postpartum engorgement of the mammary glands; beginning postpartum mastitis.
• Benign diseases of the mammary glands: mastalgia in an isolated form or in combination with premenstrual syndrome or benign nodal or cystic changes); benign nodal and / or cystic changes, especially fibrocystic mastopathy.
• Parkinson's disease and Parkinson's syndrome, incl. after encephalitis (in the form of monotherapy or in combination with other antiparkinsonian drugs).

Use with caution during pregnancy and lactation.

• Hypersensitivity to bromocriptine and other ergot alkaloids.
• Gestosis.
• Arterial hypertension in the postpartum period.
• Diseases of the cardiovascular system (including arterial hypertension, hypotension).
• Essential, family tremor.
• Psychoses.
• Liver failure .
• Gottington's chorea.
• Gastrointestinal ulcerative lesions.
• Childhood.

Carefully:

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

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

From the side of the central nervous system: dizziness (usually occur 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: nasal congestion, cramps in the calf muscles.

Reduces the effectiveness of oral contraceptives.

Enhances the effect of levodopa, antihypertensive drugs.

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

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

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

When combined with ritonavir, a 50% dose reduction is recommended.

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

Menstrual irregularities, 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 (frequency of administration 2-3 times / day). Treatment is continued until the menstrual cycle is normalized and / or ovulation is restored. If necessary for the prevention of relapse, 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 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 dose to several tablets per day, necessary to maintain an adequate decrease in plasma prolactin concentration.

Acromegaly: the initial dose is 1.25 mg 2-3 times a day, in the future, 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 at 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 birth or abortion (after stabilization of vital functions). 2-3 days after discontinuation of the drug, insignificant secretion of milk sometimes occurs. It can be eliminated by resuming taking the drug in the same dose for another 1 week.

Postpartum engorgement of the mammary glands: prescribed once in a dose of 2.5 mg, after 6-12 hours, if necessary, repeat the reception (this is not accompanied by undesirable suppression of lactation).

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

Benign diseases of the mammary glands: 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 tolerance, treatment should be started 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 side effects disappear, the dose can be increased again. Patients with motor impairment noted with levodopa are advised to reduce the dose of levodopa before using bromocriptine. After achieving a satisfactory effect, a further gradual reduction in the dose of levodopa can be undertaken. In some patients, a complete abolition of levodopa is possible.

Symptoms: headache, hallucinations, decreased blood pressure.

Treatment: parenteral administration of metoclopramide.

To prevent nausea and vomiting at the beginning of treatment, it is advisable to prescribe antiemetic drugs 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, the risk of developing cardiac fibrosis is increased.

Treatment can cause an accelerated resumption of ovarian function after childbirth, and therefore women need to be warned about the possibility of early postpartum conception. In women taking bromocriptine, pregnancy is discontinued during pregnancy, unless the possible positive effect of the treatment outweighs the potential risk to the fetus. During therapy, it is advisable to use non-hormonal contraception.

In the event of pregnancy on the background of the pituitary adenoma after cancellation, systematic monitoring of its condition, including the study of visual fields, is necessary. Before starting treatment of benign diseases of the mammary glands, 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 in the history of stomach ulcer, it is better to refuse treatment. If treatment is necessary, draw the attention of patients to the need to inform the doctor in case of disorders of the gastrointestinal tract.

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

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

Pills