Bromocriptin-Richter 2.5 mg 30 tablets — Made in Hungary — Free Delivery

Pharmacological properties

Pharmacodynamics. Bromocriptine - the active ingredient of the preparation bromocriptine-richter, 2.5 mg tablets - is an inhibitor of prolactin secretion and a stimulator of dopamine receptors. The scope of application of bromocriptine includes endocrinological and neurological indications. the pharmacological properties of the preparation are discussed below for each type of indication.

Endocrinological indications for use

Bromocriptine suppresses prolactin secretion without affecting the normal levels of other hormones released by the anterior pituitary gland.

In patients with acromegaly, bromocriptine reduces the increased level of growth hormone in the blood plasma, and therefore, alleviates the clinical manifestations of the disease and improves glucose tolerance.

Bromocriptine prevents or suppresses lactation and restores the prolactin-dependent menstrual cycle and ovulation. It is an effective treatment for amenorrhea and absence of ovulation (with or without galactorrhea).

Bromocriptine does not increase the risk of thromboembolism; it has been shown to reduce the size of pituitary adenomas that secrete prolactin (prolactinomas).

Bromocriptine reduces the severity of clinical symptoms of polycystic ovary syndrome.

Neurological indications

Due to its dopaminergic activity, bromocriptine is effective in the treatment of patients with Parkinson's disease - provided that it is administered in doses exceeding those recommended for endocrinological indications. This disorder is characterized by a nigrostriatal dopamine deficiency. Stimulation of dopamine receptors with bromocriptine can restore neurochemical balance.

Clinically, bromocriptine has been shown to alleviate Parkinson's disease (eg, tremors, muscle stiffness, bradykinesia) and depression at all stages of the disease. Bromocriptine can be used alone or in combination with other preparations for Parkinson's disease.

The combined treatment reduces the required dose of levodopa and therefore delays the recurrence of motor abnormalities. Thus, treatment with bromocriptine is capable of reducing the dose of other preparations used in combination with it, in particular levodopa. This may relieve patients of certain undesirable effects of levodopa, such as aggravation at the end of the dose, on-off phenomena, and dyskinesia.

Pharmacokinetics. Bromocriptine is rapidly and significantly absorbed in the gastrointestinal tract after oral administration. The original substance and its metabolites are metabolized in the liver and excreted in the feces; only 6% of the substance is excreted in the urine.

The binding of the preparation to blood plasma proteins is 96%.

Cmax of the preparation in the blood plasma is achieved within 1-3 hours. The effect of reducing the level of prolactin appears within 1-2 hours after ingestion, reaches a maximum after about 5 hours and is maintained for 8-12 hours. The process of removing the original substance from the blood plasma has a biphasic character, and T½ is approximately 15 hours.

The advanced age of patients does not directly affect the pharmacokinetic properties of bromocriptine. However, in persons with impaired liver function, a delay in excretion can lead to an increase in the level of the preparation in the blood plasma, which may require dose adjustment.

There is no evidence for a direct effect in the elderly on the pharmacokinetic properties and tolerability of bromocriptine. However, in patients with impaired liver function, the rate of excretion may be reduced, and the level of the preparation in the blood plasma may be correspondingly increased, which requires dose adjustment.

Biotransformation. Bromocriptine undergoes intensive presystemic biotransformation in the liver, which is reflected in the complex profile of metabolites and the almost complete absence of the parent substance in urine and feces. It exhibits high affinity for CYP 3A, and the main metabolic pathway is hydroxylation of the proline ring of the cyclopeptide component. Thus, it is expected that inhibitors and / or potent substrates of CYP 3A4 will suppress the excretion of bromocriptine and lead to an increase in its level. Bromocriptine is also a potent inhibitor of CYP 3A4. Nevertheless, given the low therapeutic concentrations of free bromocriptine in patients, one should not expect significant changes in the metabolism of the second preparation, the excretion of which is mediated by the CYP 3A4 system.

Indications

Menstrual irregularities and female sterility

Diseases dependent on prolactin levels and conditions with or without hyperprolactinemia. Amenorrhea (with or without galactorrhea); oligomenorrhea. Insufficiency of the luteal phase. Secondary hyperprolactinemia caused by other preparations (for example, some psychotropic or antihypertensive preparations).

Prolactin-independent female sterility. Polycystic ovary syndrome. Anovulatory cycles (caused by antiestrogens such as clomiphene). Infertility associated with hyperprolactinemia. Bromocriptine has been successfully used to treat a number of sterile women without severe hyperprolactinemia.

Premenstrual syndrome. Pain in the mammary glands; swelling of the mammary glands associated with the phase of the cycle; flatulence; mood changes.

Hyperprolactinemia in men (with or without galactorrhea). Prolactin-dependent hypogenitalism (oligospermia, loss of libido, impotence).

Prolactinomas. Conservative treatment for micro- or macroadenomas of the pituitary gland, which secrete prolactin.

Bromocriptine can be used as the first choice preparation for treatment of macroadenoma and as an alternative to surgical treatment (transsphenoidal removal of the pituitary gland) in patients with microadenoma.

Preoperative preparation to reduce the size of the tumor to limit the incision.

Postoperative treatment if prolactin levels remain elevated.

Acromegaly. It is used as an additional agent during radiation therapy or surgery to reduce the level of growth hormone in the systemic circulation of patients with acromegaly.

It is used as a special agent that is an alternative to radiation therapy or surgery.

Suppression of lactation. Prevention or suppression of lactation after childbirth for medical reasons, including the early stages of postpartum mastitis. This preparation is not recommended for routine suppression of lactation, for the relief of symptoms of postpartum pain, or for engorgement of the mammary glands. Prevention of lactation after abortion.

Benign neoplasm in the mammary gland. Mastalgia (including those associated with premenstrual syndrome or benign focal or cystic changes). Benign focal and / or cystic conditions, in particular fibrocystic breast disease.

Parkinson's disease. All stages of idiopathic Parkinson's disease: bromocriptine is used either in monotherapy or in combination with levodopa to control the condition of persons who have not been previously treated, as well as those who are severely affected by the "on-off" phenomenon. This remedy can help patients who are unresponsive to or intolerant of levodopa treatment, as well as people whose response to levodopa is decreasing. Postencephalitic Parkinson's Disease: The preparation can be used alone or in combination with other preparations to treat Parkinson's disease.

Treatment of patients with cyclic benign breast disease and premenstrual syndrome

Application

Doses. The preparation should always be taken with food. for most indications, the optimal response with a minimum of side effects is achieved by gradually increasing the dose.

Adults. The maximum dose should be limited to 30 mg / day.

Recommended regimen. At the beginning of treatment, a dose of 1.25 mg is used at bedtime, with a gradual increase in 2-3 days to 2.5 mg at bedtime. Then the dose can be increased by 1.25 mg with an interval of 2-3 days until the daily dose is 2 times 2.5 mg. A further increase in the dose, if necessary, is carried out in the same way.

Prevention of lactation. 2.5 mg on the day of delivery followed by 2.5 mg 2 times a day for 14 days. For these indications, a gradual increase in the dose of bromocriptine is not required.

Suppression of lactation. 2.5 mg on the 1st day, followed by an increase in the dose to 2.5 mg 2 times a day after 2-3 days. The course of treatment lasts 14 days; for these indications, a gradual increase in the dose of bromocriptine is not required.

Hypogenitalism / galactorrhea syndrome / sterility. Bromocriptine is administered gradually according to the scheme. In most patients with hyperprolactinemia, the proper response is achieved by using a dose of 7.5 mg / day (in divided doses), however, doses up to 30 mg / day have also been used. In patients with sterility without an increase in the level of prolactin in the blood plasma, the usual dose is 2.5 mg 2 times a day.

Prolactinomas. Bromocriptine is administered gradually according to the scheme. After reaching a daily dose of 2.5 mg, the dose can be increased by 2.5 mg / day at intervals of 2-3 days as follows: 2.5 mg every 8 hours, 2.5 mg every 6 hours, 5 mg - every 6 hours. The reaction in patients was observed at doses up to 30 mg / day.

Acromegaly. Bromocriptine is administered gradually according to the scheme. After reaching a daily dose of 2.5 mg, the dose can be increased by 2.5 mg / day at intervals of 2-3 days as follows: 2.5 mg every 8 hours, 2.5 mg every 6 hours, 5 mg - every 6 hours

Parkinson's disease. Bromocriptine is administered gradually as follows:

1st week: 1.25 mg at bedtime.

2nd week: 2.5 mg at bedtime.

3rd week: 2.5 mg 2 times a day.

4th week: 2.5 mg 3 times a day.

Later, the daily dose may be increased by 2.5 mg for 3-14 days, depending on the patient's response. Increasing the dose can be continued until the optimal dose is reached; as a rule, this dose is 10-30 mg / day. At the same time, the dose of levodopa can be gradually reduced until an optimal balance is achieved.

Use in the elderly. There is no evidence that bromocriptine is a particular hazard to the elderly.

Patients with impaired liver function. In patients with impaired liver function, the rate of elimination of the preparation may decrease, and, accordingly, the level of the preparation in the blood plasma may increase, which requires dose adjustment.

Contraindications

Hypersensitivity to the active ingredient, other ergot alkaloids, or any of the excipients.

In the case of long-term treatment: signs of heart valve insufficiency obtained during echocardiography performed before starting treatment.

Toxemia of pregnancy, postpartum and birth hypertension, uncontrolled hypertension, idiopathic or hereditary tremors, Huntington's chorea.

Bromocriptine is contraindicated for use in suppressing lactation in patients with a history of atherosclerotic heart disease or other severe cardiovascular disease or symptoms / history of severe mental disorders. Patients with these conditions, requiring the use of bromocriptine for macroadenoma indications, should only take it if the expected benefits are greater than the potential risks.

Bromocriptine should not be taken at the same time as other ergot alkaloids.

Bromocriptine should not be prescribed to patients with a history of fibrotic disorders or signs of heart valve insufficiency obtained by echocardiography performed before starting treatment.

Treatment during pregnancy is described in the section "Use during pregnancy and lactation."

Side effects

Nausea, vomiting, anorexia, headache, dizziness and fatigue may occur during the first days of treatment; however, these reactions usually do not require discontinuation of bromocriptine.

The risk of adverse reactions can be reduced by gradually increasing the dose and taking bromocriptine tablets with food. If necessary, the daily dose can be reduced and maintained at this level for several days. After the side effects disappear, you can try to gradually increase the dose.

Bromocriptine can cause orthostatic hypotension; therefore, BP should be measured in an upright position in outpatients.

In patients with Parkinson's disease who use the preparation in high doses, drowsiness, hallucinations, confusion, blurred vision, dry mouth, calf muscle cramps and retroperitoneal fibrosis are possible (see SPECIAL INSTRUCTIONS). All of these undesirable effects are dose-dependent.

During long courses of treatment, especially in patients with a history of Raynaud's phenomenon, reversible cold-induced pallor of the fingers and toes was noted.

In extremely rare cases (in women after childbirth who used bromocriptine to suppress lactation), serious side effects have been identified, including hypertension, myocardial infarction or stroke, although the existence of a causal relationship between these phenomena and the use of the preparation is unknown. Some patients have had severe headache and / or temporary visual impairment before stroke.

Very rarely, heart valve insufficiency (including regurgitation) and related disorders (pericarditis and pericardial effusion) have developed.

Patients with cirrhosis of the liver may develop hyponatremia and hepatic encephalopathy.

Very rarely, bromocriptine can cause sudden sleep during the day.

Patients using dopamine agonists, including the preparation Bromocriptine-Richter, may experience pathological gambling, increased libido, hypersexuality, a tendency to impulsive spending of money or shopaholia, and impulsive binge eating.

Dopamine agonists, which are ergot alkaloids, may increase the risk of heart valve regurgitation.

Side effects, grouped by systemic organ class, are listed below.

Metabolic and nutritional disorders: often - anorexia.

Mental disorders: infrequently - confusion, hallucinations, psychomotor agitation; rarely - insomnia, mental disorders; very rarely - hypersexuality, increased libido, pathological attraction to gambling.

From the nervous system: often - headache, drowsiness; infrequently - dizziness, dyskinesia; rarely - drowsiness, paresthesia; very rarely - sudden falling asleep, CSF rhinorrhea.

From the side of the organ of vision: very rarely - visual impairment, blurred field of vision.

On the part of the organ of hearing and balance: rarely - tinnitus.

From the side of the heart: rarely - pericardial effusion, compressing pericarditis, tachycardia, bradycardia, arrhythmia; very rarely - myocardial infarction, heart valve failure.

Vascular disorders: infrequently - orthostatic hypotension; very rarely - hypertension, pallor.

From the respiratory system, chest and mediastinal organs: often - nasal congestion; rarely - pleural effusion, pleural fibrosis, pulmonary fibrosis, pleurisy, difficulty breathing.

From the digestive system: often - nausea, constipation; infrequently - dry mouth, vomiting; rarely - abdominal pain, retroperitoneal fibrosis, bleeding from the gastrointestinal tract, ulcers in the gastrointestinal tract.

On the part of the skin and subcutaneous tissue: infrequently - allergic skin reactions, hair loss.

Musculoskeletal and connective tissue disorders: infrequently - cramps of the calf muscles.

Complications of a general nature and reactions at the injection site: infrequently - increased fatigue; rarely - peripheral edema; very rarely - neuroleptic malignant syndrome (bromocriptine withdrawal syndrome).

Special instructions

There is insufficient evidence for the efficacy of bromocriptine in the treatment of patients with premenstrual syndrome and benign breast neoplasms. therefore, the use of bromocriptine-richter for the treatment of patients with these diseases is not recommended.

Bromocriptine is not recommended for use after or during childbirth in women with hypertension, atherosclerotic heart disease and / or severe cardiovascular disease or a history of severe mental illness. In postpartum women who use bromocriptine, blood pressure should be carefully monitored at regular intervals, especially during the first days of treatment.

Particular care is needed in patients who are using (or have recently used) concomitant treatment with preparations that can affect blood pressure.

The concomitant use of bromocriptine with vasoconstrictors such as sympathomimetics or ergot alkaloids, including ergometrine or methylergometrine, during labor is not recommended.

In rare cases, postpartum women who have used bromocriptine to suppress lactation have experienced serious side effects, including myocardial infarction, hypertension, stroke, or mental illness. Some patients have had severe headache and / or temporary visual impairment before stroke.

In the case of hypertension, severe and persistent headache with visual impairment or any signs of toxicity to the central nervous system, treatment should be stopped immediately.

Patients may develop hyperprolactinemia of idiopathic or preparation origin, or due to diseases of the hypothalamus or pituitary gland. Bromocriptine effectively reduces prolactin levels in patients with pituitary tumors; however, it does not obviate the need for radiation therapy or surgery for acromegaly.

Women of reproductive age with conditions not associated with hyperprolactinemia should use the preparation in the minimum effective dose. This caution is necessary to avoid suppression of prolactin secretion to levels below normal with subsequent dysfunction of the corpus luteum. During treatment, such patients should use a reliable non-hormonal method of contraception, since oral contraceptives are known to increase plasma prolactin levels.

Women who need to use bromocriptine for a long period require a gynecological examination (including cytological examination). Women in the period of menopause are offered to undergo an examination once every 6 months, and women of reproductive age - to be examined once a year.

Several cases of gastrointestinal bleeding and bleeding from stomach ulcers have been reported. If this occurs, bromocriptine must be discontinued immediately. Patients with a history of gastric ulcer should be closely monitored during treatment with bromocriptine.

For patients with acromegaly and a history of gastric ulcer, other treatments should be preferred whenever possible. If bromocriptine cannot be substituted by another agent, the patient should be advised to immediately report any side effects of the gastrointestinal tract to the doctor.

Patients with severe cardiovascular or psychiatric disorders using bromocriptine for a macroadenoma indication should only take it if the expected benefits are greater than the potential risks.

Since in individuals with macroadenomas of the pituitary gland, the disease may be accompanied by hypofunction of the pituitary gland as a result of compression or destruction of the pituitary tissue, before using bromocriptine, patients should undergo a complete examination of the function of the pituitary gland and begin appropriate replacement therapy, if necessary. For patients with secondary adrenal insufficiency, GCS replacement therapy is important.

Changes in tumor size in patients with pituitary macroadenomas should be carefully monitored, and in the event of tumor growth, the advisability of using surgical procedures should be weighed.

If patients with adenoma become pregnant after taking bromocriptine, careful monitoring of their health is imperative. Adenomas that secrete prolactin can grow during pregnancy. In these patients, treatment with bromocriptine often leads to a decrease in the size of tumors and a rapid decrease in visual field defects. In severe cases of compression of the optic and other cranial nerves, urgent adrenal surgery may be necessary.

Visual field impairment is a known complication of macroprolactinoma. Effective treatment with bromocriptine leads to a decrease in tumor size and hyperprolactinemia, and often also to elimination of visual impairment. However, some patients may later develop secondary visual field impairment despite normalized prolactin levels and tumor shrinkage. In such cases, visual field defects may decrease after lowering the dose of bromocriptine, although there are slightly increased prolactin levels and slight tumor growth. Therefore, it is recommended to monitor the visual fields in patients with the aim of early diagnosis of secondary reduction of the visual field and appropriate dose adjustment of the preparation.

In some patients with prolactin-secreting adenomas who used bromocriptine, CSF rhinorrhea was observed. Available evidence suggests that this may be due to a decrease in the size of proliferating tumors.

During the first few days of treatment, patients sometimes experience arterial hypotension.

Caution is needed in the case of high doses of bromocriptine in patients with a history of mental disorders or severe cardiovascular disorders.

Treatment of Parkinson's disease with a high-dose preparation requires caution in patients with a history of psychosis or severe cardiovascular disorders.

In patients using bromocriptine, especially for long periods and at high doses, pleural and pericardial effusion, pleural and pulmonary fibrosis, and compressive pericarditis have been noted from time to time. Patients with pleural-pulmonary disorders require careful examination to identify the causes; in such cases, the feasibility of discontinuing treatment with bromocriptine should be considered.

Cases of retroperitoneal fibrosis have been observed in several patients using bromocriptine, especially for long periods and at high doses. To ensure the detection of retroperitoneal fibrosis in its early reversible stages, it is recommended to monitor its manifestations (for example, back pain, edema of the lower extremities, impaired renal function) in this category of patients.

In case of diagnosis or suspicion of fibrotic changes in the retroperitoneal space, treatment with bromocriptine preparations should be discontinued.

During the period of treatment, the patient's health should be carefully monitored, paying attention to the manifestations of progressive fibrotic disorders. In case of diagnosis or suspicion of the presence of retroperitoneal fibrosis, treatment with bromocriptine should be discontinued.

Treatment with bromocriptine may be associated with drowsiness and falling asleep, especially in individuals with Parkinson's disease. Sudden falling asleep during daily activities, in some cases even without the patient's awareness and without warning signs, was observed very rarely. Patients should be informed of this possibility, and they should be advised to exercise caution when driving and operating machinery during treatment with bromocriptine. Patients who have experienced drowsiness and / or cases of sudden falling asleep should refrain from driving or operating machinery. Moreover, in this case, the possibility of reducing the dose or discontinuing treatment should be considered.

Violation of control over drives. The condition of patients should be regularly monitored for the development of impaired control over drives. Patients and their caregivers should be informed about the possibility of development in patients using dopamine agonists, including the preparation Bromocriptine-Richter, behavioral symptoms of impairment control over cravings, including pathological craving for gambling, increased libido, hypersexuality, tendencies to impulsive spending of money or shopaholism, as well as impulsive gluttony. In case of such symptoms, the possibility of reducing the dose / gradual discontinuation of the preparation should be considered.

The preparation contains 41 mg of lactose monohydrate. Patients with rare hereditary complications such as galactose intolerance, lactose intolerance or glucose-galactose malabsorption should not take this preparation.

Use during pregnancy and lactation. Pregnancy. In patients planning a pregnancy, bromocriptine, like all other preparations, must be canceled when pregnancy is confirmed, unless there are medical contraindications for continuing therapy. No increase in the number of abortions was observed after discontinuation of bromocriptine during this period. Clinical experience has shown that the use of bromocriptine during pregnancy does not adversely affect its course or outcome.

If pregnancy occurs in a patient with pituitary adenoma and treatment with bromocriptine has been stopped, close medical supervision throughout the pregnancy is essential. In patients who develop signs of a pronounced increase in prolactinoma, such as headache or deterioration of the visual field, treatment with bromocriptine may be resumed or surgery may be appropriate.

Lactation. Because bromocriptine suppresses lactation, it should not be used by breastfeeding women.

Children. The preparation Bromocriptine-Richter, tablets, is not recommended for use in children under the age of 7 years due to insufficient data on safety and efficacy.

Bromocriptine has been used to treat prolactinoma and gigantism (acromegaly) in patients ≥7 years of age, as described in the literature. There are some data on the use of bromocriptine in pediatric practice in patients under the age of 7 years. Safety data are limited, especially with long term use.

The ability to influence the reaction rate when driving or working with other mechanisms. In the first few days of treatment, patients may experience arterial hypotension, visual impairment and dizziness, therefore, they should be especially careful when driving or operating machinery.

Patients who develop drowsiness and / or fall asleep suddenly should be advised to avoid driving or engaging in activities that may endanger others with reduced attention.

Interactions

Tolerance to bromocriptine may be impaired by alcohol.

Caution is needed while using the preparation with antihypertensive preparations.

The simultaneous use of erythromycin, other macrolide antibiotics and octreotide can increase the level of bromocriptine in the blood plasma.

Dopamine antagonists (for example, butyrophenones, phenothiazines) can reduce the severity of the effects of bromocriptine, aimed at lowering prolactin levels and treating Parkinson's disease.

Metoclopramide and domperidone may weaken the effect of bromocriptine in reducing prolactin levels.

Sympathomimetic preparations, such as phenylpropanolamine, isomeptene, increase the risk of toxicity.

Simultaneous use with other ergot alkaloids should be avoided.

Bromocriptine must be used with caution in combination with CYP 3A4 inhibitors (eg, azole fungicides, HIV protease inhibitors).

Overdose

Signs and symptoms. an overdose of bromocriptine is likely to cause symptoms of overstimulation of dopaminergic receptors and may include vomiting, nausea, dizziness, arterial hypotension, orthostatic hypotension, tachycardia, drowsiness, drowsiness, lethargy, hallucinations, and confusion.

There have been separate reports of accidental use of bromocriptine in children. They reported side effects such as vomiting, drowsiness, and fever. Patients normalized their condition spontaneously after a few hours or after proper treatment.

Treatment. It is necessary to apply general supportive measures aimed at removing any part of the preparation that has not had time to be absorbed, and maintaining blood pressure if necessary.

Storage conditions

At a temperature not exceeding 30 ° C in a dark place.