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Bromocriptine is a stimulator of the central and peripheral D 2 -dopamine receptors (a derivative of the ergot alkaloid). Inhibiting prolactin secretion, suppresses physiological lactation, helps 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 estrogen).
In high doses, it stimulates the dopamine receptors of the striatum, the black nucleus of the brain, the hypothalamus and the mesolimbic system. It has anti-Parkinsonian effect, inhibits the secretion of somatotropic (GH) and adrenocorticotropic (ACTH) hormones.
After a single dose is taken, the blood plasma prolactin level decreases after 2 hours, the maximum effect after 8 hours, the anti-parkinsonian effect after 30-90 minutes, the maximum after 2 hours, the decrease of the growth hormone level after 1-2 hours, the maximum effect is achieved in 4-8 weeks therapy.
After oral administration, the absorption of bromocriptine from the gastrointestinal tract is 28%. Exposed to the effect of "first pass" through the liver. Bioavailability - 6%. The time to reach maximum plasma concentration is 1-3 hours. T1 / 2dvhfazny: 4-4.5 h in the α-phase, 1 h in the terminal phase.
Plasma albumin binding is 90-96%.
Excreted mainly with feces - 85.6% and to a small extent with urine - 2.5-5.5%.
- Disorders of the menstrual cycle, female infertility: prolactin-related 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 anti-estrogens).
- Premenstrual syndrome: breast tenderness; swelling associated with the phase of the cycle; flatulence; mood disturbances.
- Male hyperprolactinemia: prolactin-dependent hypogonadism (oligospermia, loss of libido, impotence).
- Prolactinomas: conservative treatment of prolactin-secreting micro- and macroadenomas of the pituitary gland; in the preoperative period to reduce the size of the tumor and facilitate its removal; postoperative treatment if prolactin levels remain elevated.
- Suppression of lactation: prevention or termination of postpartum lactation for medical reasons - prevention of lactation after an abortion; postpartum breast engorgement; beginning 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, incl. after encephalitis (as monotherapy or in combination with other anti-Parkinsonian drugs).
1 tablet contains:
Active ingredient: bromocriptine mesilate 2.87 mg;
Excipients: lactose monohydrate 55.63 mg, microcrystalline cellulose 20 mg, potato starch 15 mg, carboxy methyl starch sodium 2 mg, povidone (polyvinylpyrrolidone) 3.5 mg, magnesium stearate 1 mg.
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Dosage and Administration
Inside, during meals, the maximum daily dose is 100 mg.
Violations of the menstrual cycle, 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 (the frequency of intake 2-3 times / day). Treatment continues until the normalization of the menstrual cycle and / or the restoration of ovulation. If necessary, for the prevention of recurrence, treatment can be continued for several cycles.
Premenstrual syndrome: treatment begins on the 14th day of the cycle from 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 pills per day, necessary to maintain an adequate reduction in the concentration of prolactin in the plasma.
Acromegaly: the initial dose is 1.25 mg 2-3 times a day, later, depending on the clinical effect and side effects, the daily dose is gradually increased to 10-20 mg.
Suppression of lactation: 1.25 mg is prescribed 2 times a day (with meals at breakfast and dinner), then 2.5 mg 2 times a day for 14 days. To prevent the onset of lactation, the drug should be started several hours after delivery or abortion (after stabilization of vital functions). 2-3 days after discontinuation of the drug, there is sometimes a slight secretion of milk. It can be eliminated by resuming the drug in the same dose for another 1 week.
Postpartum breast engorgement: 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).
Starting postpartum mastitis: dosing 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: for optimal tolerability, treatment should begin with a small dose of the drug: 1.25 mg 1 time per 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 occur, the daily dose can be increased further - every week at 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 can be increased again. Patients with motor impairments occurring during the administration of levodopa are advised to reduce the dose of levodopa before starting bromocriptine. After achieving a satisfactory effect, a further gradual reduction in the dose of levodopa can be undertaken. In some patients, complete elimination of levodopa is possible.
On the part of the digestive system: nausea, vomiting, dry mouth, constipation, diarrhea, abnormal liver function.
On the part of the central nervous system: dizziness (usually occur in the first week of treatment), headache, drowsiness, psychomotor agitation, dyskinesia, decreased visual acuity, hallucinations.
Since the cardiovascular system: orthostatic hypotension, arrhythmia; in some cases, with long-term use - Raynaud's syndrome (especially in susceptible patients).
Allergic reactions: skin rash.
Other: nasal congestion, cramps in the calf muscles.
- Parkinsonism with symptoms of dementia.
- Lactation period.
- Simultaneous antihypertensive therapy.
Reduces the effectiveness of oral contraceptives.
Enhances the effect of levodopa, antihypertensive drugs.
Monoamine oxidase inhibitors, furazolidone, procarbazine, sepegyline, ergot alkaloids, haloperidol, loxapine, methyldopa, metocopopramide, molindone, reserpine, thioxanthines and phenothiazines increase plasma concentration and the risk of side effects.
Erythromycin, clarithromycin, troleandomycin increase bioavailability and maximum concentration, butyrophenones reduce effectiveness.
Simultaneous use of ethanol leads to the development of disulfiram-like reactions (chest pain, skin hyperemia, tachycardia, nausea, vomiting, reflex cough, pulsating headache, blurred vision, weakness, cramps).
When administered jointly with ritonavir, a 50% dose reduction is recommended.
Pregnancy and Lactation
Use with caution during pregnancy and lactation.
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 function 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, it is necessary to warn women about the possibility of early postpartum conception. In women taking bromocriptine, treatment is stopped when the pregnancy occurs, unless the potential positive effect of treatment outweighs the potential risk to the fetus. During therapy, the use of non-hormonal contraception is advisable.
In the event of pregnancy on the background of pituitary adenoma after cancellation, 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 in the history of the presence of gastric ulcer, it is better to refuse treatment. If treatment is necessary, pay attention of patients to the need to notify the doctor in the event of disorders of the gastrointestinal tract.
It is necessary to carefully observe the oral hygiene, with the continued dryness of the oral cavity for more than 2 weeks, you should consult with your 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.
Symptoms: headache, hallucinations, low blood pressure.
Treatment: parenteral administration of metoclopramide.
- Comparison of the effect of levodopa and bromocriptine on naloxone-precipitated morphine withdrawal symptoms in mice
- Comparative effects of tamoxifen and bromocriptine on prolactin and pituitary weight in estradiol-treated male rats
- Effects of bromocriptine on prolactin-secreting pituitary adenomas. Mechanism of reduction in tumor size evaluated by light and electron microscopic, immunohistochemical, and morphometric analysis
- Cytocidal effects of bromocriptine, somatostatin analog, and heat on growth hormone-secreting pituitary adenoma in vitro
- Cortical effects of bromocriptine, a D-2 dopamine receptor agonist, in human subjects, revealed by fMRI
- Efficacy and tolerability of tolcapone compared with bromocriptine in levodopa-treated parkinsonian patients
- The efficacy and safety of adjunct bromocriptine therapy for levodopa-induced motor complications: A systematic review
- Time course of loss of clinical benefit following withdrawal of levodopa/carbidopa and bromocriptine in early Parkinson's disease
- A clinical trial of bromocriptine for treatment of primary progressive aphasia
- Comparison between lergotrile and bromocriptine in parkinsonism
- Brain dopamine receptor stimulation and the relief of parkinsonism: Relationship between bromocriptine and levodopa
- Incontinence of urine with long-term bromocriptine therapy
- Bromocriptine and lisuride in Parkinson disease
- Hypothalamic mass and gigantism in neurofibromatosis: Treatment with bromocriptine
- Diencephalic seizures: Responsiveness to bromocriptine and morphine
- A crossover trial of bromocriptine in the treatment of vascular dementia
- A double-blind randomized crossover trial of bromocriptine and placebo in restless legs syndrome
- The role of prolactin in autoimmune demyelination: Suppression of experimental allergic encephalomyelitis by bromocriptine
- The therapeutic effect of bromocriptine on acute and chronic experimental allergic encephalomyelitis
- Effect of Prolactin and Bromocriptine on the Population of Prostate Neuroendocrine Cells from Intact and Cyproterone Acetate-Treated Rats: Stereological and Immunohistochemical Study
- Bromocriptine suppresses postpartum exacerbation of collagen-induced arthritis
- Bromocriptine and cyclosporin a combination therapy in rheumatoid arthritis
- Pharmacokinetics and pharmacodynamics of bromocriptine in the rat