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Bromocriptine 2.5 mg (30 tablets)

$25.20

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Description

One tablet contains

active ingredient – bromocriptine 2.5 mg (as bromocriptine mesylate 2.87 mg),

excipients: anhydrous colloidal silicon dioxide, magnesium stearate, talc, povidone, microcrystalline cellulose, corn starch, lactose monohydrate.

 

Pharmacological properties

Pharmacokinetics

Absorption, distribution, excretion

Bromocriptine is rapidly and well absorbed from the gastrointestinal tract after oral administration. The parent substance and its metabolites are metabolized in the liver and excreted in the feces; only 6% of the dose is excreted in the urine. The degree of binding to plasma proteins reaches 96%. Peak plasma levels are reached 1-3 hours after ingestion. The prolactin-lowering effect develops within 1-2 hours after taking the drug, reaching a maximum after about 5 hours, and lasts for 8-12 hours. Excretion of the parent substance from blood plasma is biphasic, with a terminal half-life of about 15 hours.

There is no direct change in the pharmacokinetic properties of bromocriptine in the elderly. However, in patients with hepatic impairment, a delay in the elimination of the drug may lead to an increase in its plasma levels, requiring dose adjustment.

Biotransformation

Bromocriptine undergoes active biotransformation during the “first” passage through the liver, which is reflected in the complex profile of metabolites and the almost complete absence of the original substance in urine and feces. It shows high affinity for CYP3A, and the main metabolic pathway is hydroxylation of the proline ring of the cyclopeptide molecule. Therefore, inhibitors and/or potent substrates of CYP3A4 can be expected to inhibit the excretion of bromocriptine and lead to an increase in its plasma concentration. Bromocriptine is also a potent inhibitor of CYP3A4. However, given the low therapeutic concentrations of free bromocriptine in patients, one should not expect a significant impairment of the metabolism of the second drug, the clearance of which is mediated by CYP3A4.

 

Pharmacodynamics

The active substance of the drug Bromocriptine-Richter is bromocriptine, which suppresses the secretion of prolactin and stimulates dopamine receptors. The drug is used in endocrinological and neurological practice.

Endocrinology

The drug blocks the secretion of prolactin without affecting the normal level of other hormones of the anterior pituitary gland. Bromocriptine-Richter prevents or suppresses lactation that has already begun, restores the prolactin-dependent menstrual cycle and ovulation. Thus, it is effective in the treatment of amenorrhea and anovulation (with or without galactorrhea). Bromocriptine-Richter reduces the size of the pituitary adenoma that secretes prolactin. The drug improves the clinical picture in polycystic ovary syndrome. The drug does not increase the risk of thromboembolic diseases. In patients with acromegaly, the drug reduces the level of growth hormone in the blood plasma, thus, has a positive effect on the clinical picture of the disease and on glucose tolerance.

Neurology

Bromocriptine-Richter due to dopaminergic activity is used to treat Parkinson’s disease, but in doses higher than those prescribed in endocrinology. Parkinson’s disease is characterized by a specific nigrostrial dopamine deficiency. The drug stimulates dopamine receptors and restores neurochemical balance. Clinically, bromocriptine reduces the severity of manifestations of parkinsonism (including tremor, rigidity, bradykinesia) and depression at all stages of the disease. Bromocriptine-Richter can be administered as monotherapy or in combination with other antiparkinsonian drugs. The use of the drug allows you to reduce the doses of other antiparkinsonian drugs, (for example, levodopa) and avoid the possibility of such side effects as deterioration at the end of the dose, the “on-off” phenomenon, and dyskinesia.

 

Indications for use

– prevention or suppression of lactation solely for medical reasons (such as abortion, neonatal death, maternal HIV infection).

Bromocriptine is not recommended for the routine suppression of lactation or for the relief of symptoms of postpartum pain and breast engorgement when non-pharmacological treatments (gentle breast support, cold compresses) and/or pain relievers are effective.

– hyperprolactinemia in women and men (with or without galactorrhea)

– female infertility associated with hyperprolactinemia

– female infertility, not accompanied by hyperprolactinemia

– pituitary macroadenomas or as an alternative to surgical treatment of transsphenoidal hypophysectomy in patients with microadenomas

– acromegaly (to reduce the level of growth hormone in the blood), in combination with surgical treatment and / or radiation therapy

– Parkinson’s disease, as monotherapy or in combination with other anti-Parkinsonian drugs (levodopa).

 

Dosage and administration

Tablets should be taken with food (breakfast or dinner). In most cases, the drug is started with a gradual increase in dose until the optimal therapeutic effect and minimal side effects are achieved. The maximum dose should not exceed 30 mg per day.

Reception scheme

The initial dose of the drug is 1.25 mg (1/2 tablet) during meals, at dinner. After 2-3 days, the dose of Bromocriptine-Richter is increased to 2.5 mg.

In the future, the dose of the drug can be increased every 2-3 days by 1.25 mg, until a daily dose of 5 mg (2.5 mg 2 times a day) is reached. If necessary, a further increase in the dose of the drug can be carried out according to the same scheme.

lactation prevention

On the day of delivery, 2.5 mg (1 tablet) 1 time per day, and then 2 times a day, 2.5 mg of Bromocriptine-Richter for 14 days. In this case, there is no need for a gradual increase in the dose of the drug.

Suppression of lactation

On the first day, it is necessary to take 2.5 mg of the drug, and in the next 2-3 days the dose of the drug is increased to 5 mg (2.5 mg 2 times a day). The drug is continued for 14 days. In this case, there is no need for a gradual increase in the dose of the drug.

Hypogonadism/galactorrhea syndrome, infertility

It is proposed to gradually increase the dose of the drug according to the above scheme. Most patients with galactorrhea respond well to a dose of 7.5 mg of Bromocriptine-Richter per day, which is divided into several doses. If necessary, this dose can be increased to 30 mg per day. For infertility without an increase in the level of prolactin in the blood, the generally accepted dose of the drug is 5 mg per day, which is taken at 2.5 mg 2 times a day.

Prolactinomas

Gradually increase the dose of bromocriptine according to the proposed scheme. When a daily dose of 2.5 mg is reached, the dosage may be increased by 2.5 mg per day at 2-3 day intervals as follows: 2.5 mg every 8 hours, 2.5 mg every 6 hours, 5 mg every 6 hours under the control of prolactin levels. The therapeutic effect is expected when a dose of 30 mg of the drug per day is reached.

Acromegaly

Gradually increase the dose of bromocriptine according to the proposed scheme. When a daily dose of 2.5 mg is reached, the dosage may be increased by 2.5 mg per day at 2-3 day intervals as follows: 2.5 mg every 8 hours, 2.5 mg every 6 hours, 5 mg every 6 hours up to 20 mg / day (4-8 tablets).

Parkinson’s disease

It is necessary to carry out the scheme of gradual increase in a dose.

– 1 week: 1.25 mg daily at bedtime.

– Week 2: 2.5 mg daily at bedtime.

– 3 weeks: 2 times 2.5 mg per day.

– 4 weeks: 3 times 2.5 mg per day.

Subsequently, the daily dose may be increased by 2.5 mg for 3-14 days, depending on the effect noted in the patient. Increasing the dose can be continued until the optimal dose is reached; which usually ranges from 10 to 30 mg per day. At the same time, the dose of levodopa can be gradually reduced until the optimal balance is determined.

Use in elderly patients

Old age is not a particular risk group in therapy with Bromocriptine-Richter.

The use of the drug in patients with impaired liver function

In case of impaired liver function, there may be a delay in excretion and an increase in the concentration of Bromocriptine-Richter in the blood plasma. In this regard, it may be necessary to adjust the dose of the drug.

Childhood and adolescence

Bromocriptine is not recommended for use in children under 18 years of age due to limited data on the safety and efficacy of the drug, except when used on the recommendation of an endocrinologist.

 

Side effects

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

The risk of developing adverse reactions can be reduced by gradually increasing the dose and taking bromocriptine tablets with meals. If necessary, the daily dose may be reduced and treatment continued at this reduced dose for several days. After the disappearance of adverse reactions, you can try again to increase the dose.

Bromocriptine can cause orthostatic hypotension, so blood pressure in ambulatory patients should be measured in an upright position.

In patients with parkinsonism, during treatment with high doses of the drug, drowsiness, hallucinations, confusion, visual disturbances, dry mouth, leg muscle cramps and retroperitoneal fibrosis may develop. All of these side effects are dose dependent.

With prolonged treatment, there have been cases of reversible blanching or whitening of the fingers and toes in the cold, especially in patients with a history of Raynaud’s phenomenon.

In extremely rare cases (in women in the postpartum period who received bromocriptine to prevent lactation), serious side effects may develop, including arterial hypertension, myocardial infarction or stroke, although their causal relationship with the use of the drug has not been established. In some cases, the development of stroke was preceded by severe headache and/or transient visual impairment.

In very rare cases, valvular heart disease (including regurgitation) and associated disorders (pericarditis and pericardial effusion) have been reported.

Patients with cirrhosis of the liver may experience hyponatremia and portosystemic encephalopathy.

In extremely rare cases, bromocriptine can provoke cases of sudden falling asleep during the day.

Patients treated with dopamine agonists, including Bromocriptine-Richter, may experience pathological gambling, increased sex drive, hypersexuality, compulsive spending or shopping habits, constant need for food, and compulsive binge eating.

Dopamine agonists, belonging to the group of ergot alkaloids, may increase the risk of developing regurgitation of the heart valves.

Undesirable effects are summarized by their frequency of occurrence:

Common (≥1/100 to <1/10)

– headache
– loss of appetite
– nausea, constipation
– drowsiness
– nasal congestion

Uncommon (≥1/1000 to <1/100)

– confusion, hallucinations
– dyskinesia, psychomotor agitation
– dizziness, orthostatic hypotension
– dry mouth, vomiting
– skin allergic reaction, allergic dermatitis, alopecia
– muscle spasms, weakness

Rare (≥1/10000 to <1/1000)

– insomnia, psychotic disorders, paresthesias
– noise in ears
– pericardial effusion, constrictive pericarditis, tachycardia, bradycardia, arrhythmia
– pleural effusion, pleural fibrosis, pulmonary fibrosis, pleurisy, dyspnea
– retroperitoneal fibrosis, gastrointestinal bleeding, ulcers on the mucous membrane of the gastrointestinal tract
– peripheral edema

Very rare (< 1/10000)

– blurred vision, blurred vision
– acute cerebrovascular accident, neuroleptic malignant syndrome (bromocriptine withdrawal syndrome)
– sudden onset of sleep in the middle of the day
– rhinorrhea of ​​cerebrospinal fluid
– pathological gambling, increased libido and hypersexuality
– myocardial infarction, diseases of the valvular apparatus of the heart
– arterial hypertension
– pallor of the skin
– hyponatremia

 

Contraindications

– hypersensitivity to bromocriptine or other ergot alkaloids (ergocriptine derivatives), as well as to excipients of the drug

– hypertensive conditions associated with pregnancy: preeclampsia of pregnancy, preeclampsia or gestational arterial hypertension

– arterial hypertension in childbirth or in the postpartum period

– uncontrolled arterial hypertension

– peptic ulcer of the stomach and duodenum

– idiopathic or familial tremor

– chorea of ​​Huntington (Huntington)

– with non-life-threatening indications in patients (including suppression of lactation) with cardiovascular diseases (including coronary heart disease) or other cardiovascular pathology at present and in history

– for long-term treatment in the presence of diseases of the valvular apparatus of the heart

– connective tissue diseases, including history

– severe mental illness at present or in history

– hereditary intolerance to galactose, lactose, lactase deficiency, malabsorption of glucose, galactose

– combined use with oral contraceptives

– simultaneously with other ergot alkaloids

– period of breastfeeding

 

Drug Interactions

With the joint use of the drug Bromocriptine-Richter with

– 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, convulsions), the tolerability of Bromocriptine-Richter is reduced

– antihypertensive drugs: enhances the effect of antihypertensive drugs

– erythromycin, clarithromycin, troleandomycin concentration and bioavailability of the drug Bromocriptine-Richter in blood plasma may increase

– dopamine antagonists (for example: butyrophenones, phenothiazines) – may reduce the prolactin-lowering and antiparkinsonian effects of bromocriptine.

– metoclopramide and domperidone – can reduce the severity of the prolactin-reducing effect of bromocriptine.

– sympathomimetic drugs, including phenylpropanolamine and isometheptene – increase the risk of toxicity.

The simultaneous use of the drug with other ergot alkaloids should be avoided.

Caution should be exercised when bromocriptine is co-administered with CYP3A4 inhibitors (eg, azole antifungals, HIV protease inhibitors).

 

Special instructions

The use of Bromocriptine-Richter in patients with premenstrual syndrome and benign breast tumors is not recommended due to insufficient evidence of efficacy in the treatment.

In rare cases, serious adverse events have been reported, including arterial hypertension, myocardial infarction, stroke, or psychiatric disorders in women in the postpartum period who received bromocriptine to suppress lactation. The development of epileptic seizures or stroke in some patients was preceded by severe headache and/or transient visual disturbances.

When using the drug after childbirth, especially in the first days of admission, it is necessary to regularly and carefully monitor blood pressure. It is especially necessary to monitor patients who are taking or have taken drugs that affect blood pressure in the near future.

In the event of the development of arterial hypertension, chest pain, severe and unrelenting headache with or without visual impairment, as well as any signs of toxic effects on the central nervous system, treatment with the drug should be stopped immediately and the patient should be examined immediately.

The simultaneous use of bromocriptine with vasoconstrictors, such as sympathomimetics or ergot alkaloids, including ergometrine or methylergometrine, during the postpartum period is not recommended.

Idiopathic hyperprolactinemia may be observed, caused by taking drugs or associated with a disease of the hypothalamic-pituitary system. Bromocriptine-Rich effectively reduces prolactin levels in patients who suffer from a pituitary tumor, but in acromegaly this does not eliminate the need for radiation therapy or surgery.

When treating women of childbearing age without symptoms of hyperprolactinemia, the drug should be prescribed at the lowest effective dose to prevent a decrease in the level of prolactin in the blood below the normal value and to prevent dysfunction of the corpus luteum. During the course of therapy with Bromocriptine-Richter, it is necessary to use reliable, non-hormonal methods of contraceptive protection, since oral hormonal contraceptives increase the level of prolactin in the blood serum.

With prolonged use of the drug, it is necessary to conduct a gynecological examination of a woman with a collection of cytological material. This examination should be performed every 6 months in the treatment of postmenopausal women and annually in the treatment of women of childbearing age.

Patients with acromegaly who have a history of gastric ulcer should be treated by other methods if possible. If treatment with bromocriptine is necessary, the patient should be instructed to notify the physician immediately of adverse gastrointestinal effects.

Patients with severe cardiovascular disease or psychiatric disorders taking bromocriptine for macroadenomas should only receive it if the expected benefit of treatment outweighs the potential risks associated with it.

Since patients with pituitary macroadenomas may have concomitant hypopituitarism due to compression or destruction of pituitary tissue, it is necessary to conduct a full assessment of the functional state of the pituitary gland and prescribe adequate replacement therapy before prescribing bromocriptine. In patients with secondary adrenal insufficiency, corticosteroid replacement therapy is mandatory.

Changes in tumor size should be carefully monitored in patients with pituitary macroadenomas, and surgery should be considered if there are signs of tumor growth.

Prolactin-secreting adenomas may increase in size during pregnancy. In such cases, it is necessary to monitor patients with macroadenoma. In these patients, treatment with bromocriptine often results in tumor shrinkage and rapid recovery of narrowed visual fields. In severe cases, compression of the optic or other cranial nerves may require emergency pituitary surgery.

Visual field impairment is a known complication of prolactinoma. Effective treatment with bromocriptine leads to a reduction in the size of the tumor and the severity of hyperprolactinemia, and often to the disappearance of visual impairment. However, some patients may subsequently develop secondary visual field impairment despite normalization of prolactin levels and shrinkage of the tumor. In these cases, the visual field defect may improve with a reduced dose of bromocriptine, despite some increase in prolactin levels and some re-enlargement of the tumor. Thus, monitoring of the visual fields is recommended for early detection of secondary visual field loss and individual selection of the dose of bromocriptine.

Some patients with prolactin-secreting adenomas treated with bromocriptine experienced rhinorrhea of ​​the cerebrospinal fluid, which may be due to tumor shrinkage with invasive growth.

During the first few days of treatment, in isolated cases arterial hypotension may develop.

Caution should be exercised when prescribing high doses of bromocriptine to patients with a history of psychotic disorders or severe cardiovascular disease.

Treatment with the drug in high doses in parkinsonism requires caution in patients with a history of psychosis or severe cardiovascular disease.

In patients treated with bromocriptine, especially at high doses or for a long time, isolated cases of effusion into the pleural cavity and into the pericardial cavity, as well as fibrosis of the pleura and lungs and constrictive pericarditis have been reported. Patients with unexplained pleuropulmonary disorders should be carefully evaluated and, if necessary, discontinue bromocriptine therapy.

Retroperitoneal fibrosis has been reported in several patients treated with bromocriptine, especially at high doses or for a long time. For timely recognition of retroperitoneal fibrosis at an early reversible stage, it is recommended to monitor its manifestations (such as back pain, swelling of the lower extremities, impaired renal function).

Bromocriptine should be discontinued in cases of diagnosed or suspected retroperitoneal fibrosis.

Look out for the following signs and symptoms:

– lung disease, manifested by shortness of breath, choking, persistent cough or chest pain;

– impaired renal function or obstruction of the urethra / abdominal vessels, which may be accompanied by pain in the lumbar region / lateral sections of the abdomen and swelling of the lower extremities, as well as the presence of any mass formations in the abdominal cavity or its tenderness on palpation, which may indicate retroperitoneal fibrosis;

– heart failure caused by pericardial fibrosis (if such symptoms occur, constrictive pericarditis should be excluded).

In the diagnosis of fibrosing disorder, it is useful to determine the erythrocyte sedimentation rate (ESR) and the concentration of creatinine in the blood, as well as an x-ray examination of the chest. In addition, it is advisable to determine the baseline levels of other inflammatory markers and indicators of kidney function before starting treatment.

During treatment, patients should be closely monitored for manifestations of progressive fibrosing disorders. If retroperitoneal fibrosis is diagnosed or suspected, treatment with bromocriptine should be discontinued.

The use of bromocriptine may be accompanied by drowsiness and episodes of sudden falling asleep, especially in patients with Parkinson’s disease. Sudden falling asleep during daytime activities, in some cases without any warning or warning signs, has been reported extremely rarely. Patients should be informed of the possibility of this phenomenon and should be careful when driving vehicles or operating machinery during treatment with bromocriptine. Patients who experience drowsiness and / or episodes of sudden falling asleep should refrain from driving vehicles or working with mechanisms. In addition, consideration should be given to reducing the dose or stopping treatment.

impulse control disorder

Patients should be monitored regularly for the development of an impulse control disorder. Patients and their caregivers should be aware of the possibility that patients treated with dopamine agonists (including Bromocriptine-Richter) may develop behavioral symptoms of impulse control disorder, including pathological gambling, increased sexual desire, hypersexuality , compulsive spending or shopping habits, constant need for food and compulsive overeating. In the event of the development of such symptoms, the advisability of dose reduction / gradual withdrawal of the drug should be considered.

In clinical studies of cabergoline and pergolide, an increased risk of developing valvular pathology was noted. It can be assumed that this effect may be characteristic of other derivatives of ergot alkaloids, such as bromocriptine.

The drug contains 41.0 mg of lactose monohydrate. Patients with rare hereditary problems of galactose intolerance, lactose intolerance or glucose-galactose malabsorption should not take this medicine.

Pregnancy and lactation

In case of pregnancy, the drug should be discontinued.

In pregnant patients with pituitary adenoma after discontinuation of the drug, careful follow-up is necessary (including re-determination of visual fields) throughout pregnancy.

In the case of growth of prolactinoma, it is necessary to start therapy again. Based on data obtained from more than 2,000 pregnant women, the use of Bromocriptine-Richter did not increase the number of spontaneous abortions, preterm births and neonatal anomalies. According to these data, Bromocriptine-Richter does not have an embryotoxic or teratogenic effect.

Since bromocriptine suppresses lactation and passes into breast milk, it should not be given to women who are breastfeeding.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

The use of the drug can cause hypotension, blurred vision, dizziness, especially in the first days of therapy, so care must be taken when driving vehicles or when working in conditions of increased injury.

The use of Bromocriptine-Richter may cause drowsiness or a symptom of sudden falling asleep, which may occur during the daytime without warning signs. This should be paid attention to persons driving vehicles or working in conditions of increased injury. Those patients who have such symptoms are prohibited from driving vehicles.

 

Overdose

Symptoms: nausea, vomiting, lowering blood pressure, headache, hallucinations, confusion.

Treatment: removal of all unabsorbed drug, in maintaining blood pressure, if necessary.

 

Storage conditions

Store in the original packaging, in a place protected from light at a temperature not exceeding 25 C.
Keep out of the reach of children!
Shelf life 3 years
Do not use after the expiration date.

Additional information

Ingredient

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