Description
Latin name
Bromocriptine
Packing
30 pcs
Pharmacological action of
Bromocriptine is a stimulant of central and peripheral D 2 dopamine receptors (an ergot alkaloid derivative). By inhibiting the secretion of prolactin, it suppresses physiological lactation, helps to normalize 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, stimulates the dopamine receptors of the striatum, black brain nucleus, hypothalamus, and mesolimbic system. It has an antiparkinsonian effect, inhibits the secretion of growth hormone (STH) and adrenocorticotropic (ACTH) hormones.
After taking a single dose, a decrease in blood plasma prolactin occurs after 2 hours, the maximum effect after 8 hours, the antiparkinsonian effect after 30-90 minutes, the maximum after 2 hours, the decrease in GH levels after 1-2 hours, the maximum effect achieved after 4-8 weeks. therapy.
Pharmacokinetics of
After oral administration, absorption of bromocriptine from the gastrointestinal tract is 28%. It undergoes the effect of the first passage through the liver. Bioavailability is 6%. The time to reach maximum plasma concentration is 1-3 hours. T1 / 2 is two-phase: 4-4.5 hours in the Phase, 1 hour in the terminal phase.
Binding to plasma albumin – 90-96%.
It is excreted mainly with feces – 85.6% and to a small extent with urine – 2.5-5.5%.
Contraindications
Hypersensitivity to bromocriptine and other ergot alkaloids.
gestosis.
Postpartum arterial hypertension.
Diseases of the cardiovascular system (including arterial hypertension, hypotension).
Essential, family tremor.
Psychoses.
Hepatic failure.
Chorea Gottington.
Gastrointestinal ulcer.
Children’s age.
Precautions:
Parkinsonism with symptoms of dementia.
Pregnancy.
Lactation.
Concurrent antihypertensive therapy.
Use during pregnancy and lactation
Use with caution during pregnancy and lactation.
Composition of
1 tablet contains:
Active ingredient: bromocriptine mesylate 2.87 mg
Excipients: lactose monohydrate 55.63 mg, microcrystalline cellulose 15 mg, potato starch 15 mg, carboxy methyl starchiron 3 sodium 2 starch 5 mg, magnesium stearate 1 mg.
Dosage and administration
Inside, with food, 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 day 14 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: 1 day is prescribed 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 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 milk secretion sometimes occurs. It can be eliminated 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 breast disease: 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 a satisfactory effect is achieved, a further gradual reduction in the dose of levodopa can be undertaken. In some patients, a complete abolition of levodopa is possible.
Side effects of 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.
Drug Interaction
Reduces the effectiveness of oral contraceptives.
Enhances the effect of levodopa, an antihypertensive drug.
Monoamine oxidase inhibitors, furazolidone, procarbazine, sepegillin, ergot alkaloids, haloperidol, loxapine, methyldopa, metocopramide, molindone, reserpine, thioxanthins and phenothiazines increase plasma concentrations and risk of side effects.
Erythromycin, clarithromycin, troleandomycin increase bioavailability and maximum concentration, butyrophenones decrease efficacy.
Simultaneous intake of ethanol leads to the development of disulfiram-like reactions (chest pain, hyperemia of the skin, tachycardia, nausea, vomiting, reflex cough, pulsating headache, blurred vision, weakness, cramps).
50% dose reduction is recommended when co-administered with ritonavir.
Overdose
Symptoms: headache, hallucinations, decreased blood pressure.
Treatment: parenteral administration of metoclopramide.
Storage conditions
Store in a dry, dark place at a temperature not exceeding 25 ° C.
Shelf suitability
3 Year
Deystvuyuschee substances
Bromocriptine
Dosage form
Dosage form
tablets
