Bromocriptine, tablets 2.5mg 30 pcs

Bromocriptine is a stimulator of central and peripheral D 2 -dopamine receptors (ergot alkaloid derivative). By inhibiting prolactin secretion, it suppresses physiological lactation, promotes normalization of menstrual function, suppresses increased secretion of growth hormone, and reduces the size and number of cysts in the breast (due to elimination of an imbalance between progesterone and estrogens).

In high doses it stimulates dopamine receptors of the striatum, black nucleus of the brain, hypothalamus and mesolimbic system. It has antiparkinsonian effect, inhibits secretion of somatotropic (STH) and adrenocorticotropic (ACTH) hormones.

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

Pharmacokinetics

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

Binding with plasma albumin is 90-96%.

Extracted mainly with feces – 85.6% and to a small extent with urine – 2.5-5.5%.

Indications

Active ingredient

Composition

One tablet contains:

Active substance:

bromocriptine mesylate 2.87 mg;

Associates:

Lactose monohydrate 55.63 mg,

microcrystalline cellulose 20 mg,

potato starch 15 mg,

carboxy methyl starch sodium 2 mg,

povidone (polyvinylpyrropidone) 3.5 mg,

magnesium stearate 1 mg.

How to take, the dosage

Overly, 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 (number of times 2-3 times/day). Treatment is continued until normalization of the menstrual cycle and/or restoration of ovulation. If necessary to prevent recurrences, treatment may be continued for several cycles.

Premenstrual syndrome: treatment is started 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 daily, with gradual increase in dose to several tablets per day needed to maintain adequate reduction of plasma prolactin concentrations.

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

Lactation suppression: on the first day, 1.25 mg 2 times (with meals at breakfast and dinner), then for 14 days, 2.5 mg 2 times a day. To prevent the beginning of lactation the drug should be started a few hours after childbirth or abortion (after stabilization of vital functions). Sometimes a small amount of milk secretion occurs 2 to 3 days after withdrawal of the drug. It can be eliminated by resuming the drug in the same dose for another 1 week.

Postpartum engorgement of the mammary glands: it is prescribed once in a dose of 2.5 mg and repeated 6-12 hours later if necessary (this is not accompanied with undesirable suppression of lactation).

Incoming postpartum mastitis: the dosing regimen is the same as for lactation suppression. If necessary, an antibiotic is added to the treatment.

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

Parkinson’s disease: for optimal tolerability, treatment should be started with a small dose of the drug: 1.25 mg once daily (preferably in the evening) for 1 week. The daily dose of the drug is increased gradually, weekly by 1.25 mg, and the daily dose is divided into 2-3 doses. Adequate therapeutic results 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 doses of bromocriptine for mono- or combination therapy are 10-30 mg/day. The maximum daily dose is 30 mg. If side effects occur when adjusting the dose, the daily dose should be reduced and maintained at a lower level for at least 1 week. If the side effects disappear, the dose can be increased again. Patients with motor disturbances observed against the background of levodopa administration are recommended to reduce the dose of levodopa before starting bromocriptine. After a satisfactory effect has been achieved, further gradual reduction of the levodopa dose may be undertaken. Complete withdrawal of levodopa is possible in some patients.

Interaction

Decreases the effectiveness of oral contraceptives.

Enhances the effect of levodopa , hypotensive drugs.

Moamine oxidase inhibitors, furazolidone, procarbazine, sepegiline, ergot alkaloids, haloperidol, loxapine, methyldopa, metocopramide, molindone, reserpine, thioxantins and phenothiazines increase plasma concentrations and risk of side effects.

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

The concomitant administration of ethanol results in disulfiram-like reactions (chest pain, skin hyperemia, tachycardia, nausea, vomiting, reflex cough, pulsatile headache, blurred vision, weakness, seizures).

In co-administration with ritonavir, a 50% dose reduction is recommended.

Special Instructions

In order to prevent nausea and vomiting at the beginning of treatment, it is reasonable to administer antiemetic medication 1 hour before taking the drug.

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

The risk of cardiac fibrosis increased when the drug is used in high doses for a prolonged period.

The treatment may cause accelerated resumption of ovarian function after childbirth; therefore, women should be warned about the possibility of early postpartum conception. In women taking bromocriptine treatment is discontinued at the onset of pregnancy, unless the possible positive effect of treatment outweighs the potential risk to the fetus. During therapy it is reasonable to use non-hormonal contraception.

In case of pregnancy against adenoma of the pituitary gland after withdrawal, systematic monitoring of her condition, including examination of the visual fields, is necessary. Before starting treatment of benign breast diseases it is necessary to rule out the presence of a malignant tumor of the same localization.

When treating acromegaly, if there is a history of peptic ulcer disease, it is better to refuse treatment. If treatment is necessary, patients should be advised to tell their physician if they have any gastrointestinal problems.

Monitoring and oral hygiene should be performed carefully; if dry mouth persists for more than 2 weeks, a physician should be consulted.

– Effect on the ability to drive and operate machinery Patients taking the drug should refrain from engaging in activities requiring increased attention and rapid physical and mental reactions.

Contraindications

With caution:

Side effects

Digestive system disorders: nausea, vomiting, dry mouth, constipation, diarrhea, liver function disorders.

CNS disorders: dizziness (usually occurs in the first week of treatment), headache, somnolence, psychomotor agitation, dyskinesia, decreased visual acuity, hallucinations.

Cardiovascular system disorders: orthostatic hypotension, arrhythmia; in single cases, with long-term use – Raynaud’s syndrome (especially in predisposed patients).

Allergic reactions: skin rash.

Others: nasal congestion, cramps in the calf muscles.

Overdose

Symptoms: headache, hallucinations, decreased blood pressure.

Treatment: parenteral administration of metoclopramide.

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Pregnancy use

Use with caution during pregnancy and lactation.