Bromocriptine

To prevent nausea and/or vomiting, at the beginning of treatment, a peripheral dopamine receptor antagonist, for example, domperidone, can be prescribed for several days, no later than 1 hour before taking bromocriptine.

When treating acromegaly, before prescribing the drug, the presence of gastric and duodenal ulcers should be excluded and the patient should be warned about the need to notify the doctor if gastrointestinal disorders occur.

There are reports of fatal gastrointestinal bleeding with the use of bromocriptine. There is no evidence that this is specifically related to the use of bromocriptine. Therefore, it is not recommended to use bromocriptine in patients with erosive and ulcerative lesions of the gastrointestinal tract in the acute stage.

If gastrointestinal bleeding or gastric and duodenal ulcers occur, the drug should be discontinued.

Treatment of women with prolactin-dependent dysmenorrhea leads to normalization of ovulation, and therefore the patient should be warned about the need to use contraception (except for oral contraceptives).

Bromocriptine is not recommended for use as a prophylactic agent or to reduce postpartum breast engorgement in cases where the use of antispasmodics, analgesics and wearing comfortable supportive underwear is effective.

Due to the limited amount of clinical data, the drug is not recommended for the treatment of premenstrual syndrome and benign breast diseases.

Patients are recommended to visit a gynecologist annually; for women aged before menopause - every six months.

Patients taking bromocriptine may experience symptomatic hypotension; in some cases, arterial hypotension may occur at the beginning of treatment, especially in the second week of therapy. Blood pressure should be monitored daily, especially during the first weeks of therapy. In the future, blood pressure should be monitored at regular intervals.

If arterial hypertension develops, severe persistent headaches (with or without visual disturbances) or signs of central nervous system (CNS) toxicity occur, treatment should be discontinued and the patient should be examined medically.

In some patients with acromegaly, the development of “cold” vasospasm was observed when using bromocriptine. In this case, it is necessary to reduce the dose of bromocriptine.

During long-term treatment (2-10 years) with high doses of the drug (30 mg per day), patients should be especially closely monitored for the possible appearance of signs of retroperitoneal fibrosis (for example, back pain, swelling of the lower extremities, impaired renal function), in which case it is necessary to stop treatment.

Caution should be exercised when treating patients with Parkinson's disease who may have mild dementia.

Bromocriptine, when used alone or in combination with levodopa, may cause auditory or visual hallucinations. In most cases, hallucinations can be eliminated by reducing the dose of bromocriptine; sometimes it is necessary to stop treatment.

Bromocriptine is ineffective for essential and familial tremor, as well as Huntington's chorea.

If treatment with bromocriptine is prescribed to women for pathology not associated with hyperprolactinemia, the drug should be used in the minimum effective dose necessary to relieve symptoms; this is necessary to ensure that the concentration of prolactin in the blood plasma does not decrease below the normal level, as this can cause disturbances in the development of the corpus luteum.

In patients with pituitary macroadenomas, the dynamics of tumor size should be systematically assessed.

Before initiating treatment for patients with macroprolactinoma, it is necessary to conduct a complete examination of pituitary function. In patients with secondary adrenal insufficiency, glucocorticosteroid replacement therapy has important clinical significance. It is necessary to regularly monitor the size of the pituitary tumor (macropituitary adenoma), and if its size increases, despite the therapy, it is necessary to decide on surgical treatment.

Patients who do not wish to become pregnant or who have large prolactin-secreting pituitary adenomas should be advised to use contraceptive measures other than oral contraceptives during treatment with bromocriptine. During the period of amenorrhea, it is recommended to carry out a pregnancy test at least once every 4 weeks, and, when the menstrual cycle is restored, every time there is a delay in menstruation. If pregnancy occurs during treatment with the drug in patients with a pituitary tumor, careful monitoring of the patients is necessary. Prolactin-secreting adenomas may enlarge during pregnancy. In severe cases, compression of the optic or other cranial nerves may occur, which may require emergency surgery.

Visual impairment (loss of visual fields) is a known complication of prolactinoma. Effective treatment with the drug leads to a decrease in the concentration of prolactin in the blood plasma and vision often improves. However, some patients may develop secondary visual field loss despite normal plasma prolactin concentrations and a decrease in tumor size, which may result from a displacement of the optic chiasm towards the sella turcica (formation of a hernia of the optic chiasm). Therefore, for early diagnosis of secondary visual field loss due to optic chiasm hernia, monitoring of visual fields in patients with macroprolactinoma is necessary for timely adjustment of the dose of bromocriptine.

Cerebrospinal fluid rhinorrhea has been observed in some patients with prolactin-secreting adenomas when treated with bromocriptine.

Careful oral hygiene is necessary. If dryness of the oral mucosa persists for more than 2 weeks, you should consult a doctor.

The use of bromocriptine may cause drowsiness or episodes of sudden onset of sleep (particularly in patients with Parkinson's disease) during the day, without any previous symptoms. In such cases, reducing the dose of the drug should be considered.

Use in children and adolescents

The effectiveness and safety of bromocriptine have been established in children with prolactinomas and acromegaly over 7 years of age. Given the difficult to predict sensitivity of children and adolescents, caution should be exercised when using the drug in this category of patients. The safety and effectiveness of bromocriptine in children under 7 years of age have not been confirmed.

Use in patients over 65 years of age

The number of patients aged 65 years and older in the clinical trials was insufficient to evaluate possible differences in response to treatment with bromocriptine compared with younger patients. In clinical studies and medical practice, the tolerability of the drug in patients over 65 years of age and younger patients was the same.

Given the difficult to predict tolerability of the drug in patients over 65 years of age, caution should be exercised when using the drug in this category of patients.

Use in the postpartum period

In women taking bromocriptine in the postpartum period to suppress lactation, rare cases of serious adverse events such as hypertension, myocardial infarction, seizures, stroke or mental disorders were observed, especially at the beginning of treatment.

In some patients, the development of seizures or cerebrovascular accidents was preceded by severe headaches and/or transient visual impairment.

Although the cause-and-effect relationship between the development of these phenomena and the use of bromocriptine has not been established, blood pressure should be monitored in all patients taking Bromocriptine. If arterial hypertension or severe, progressive or persistent headache (with or without visual impairment) or signs of a central nervous system disorder develop, the drug should be discontinued and immediately examined.

In patients with Parkinson's disease, when using high doses of bromocriptine, gambling addiction, increased libido and hypersexuality, compulsive shopping and spending money, and compulsive overeating are possible. Patients and their relatives should be warned about the possible development of these behavioral control disorders. In case of development of behavioral disorders, it is necessary to reduce the dose of bromocriptine or stop taking it.

There is no need for special precautions when disposing of unused drug.

Application

Doses. The drug should always be taken with food. For most indications, optimal response with minimal side effects is achieved by gradually increasing the dose.

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

Recommended dosage regimen. At the beginning of treatment, a dose of 1.25 mg is used at bedtime, with a gradual increase after 2-3 days to 2.5 mg at bedtime. Then the dose can be increased by 1.25 mg at intervals of 2-3 days until a daily dose of 2 times 2.5 mg is reached. Further increase in dose, if necessary, is carried out in a similar way.

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

Suppression of lactation. 2.5 mg on day 1, followed by increasing 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 schedule. In most patients with hyperprolactinemia, an adequate response is achieved with a dose of 7.5 mg/day (in divided doses), but doses up to 30 mg/day have been used. In sterile patients without an increase in plasma prolactin levels, the usual dose is 2.5 mg 2 times a day.

Prolactinomas. Bromocriptine is administered gradually according to the schedule. After reaching the 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. A reaction in patients was observed when using doses up to 30 mg/day.

Acromegaly. Bromocriptine is administered gradually according to the schedule. After reaching the 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:

Week 1: 1.25 mg at bedtime.

Week 2: 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 over 3–14 days depending on the patient's response. Dose increases can be continued until the optimal dose is achieved; 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 elderly people. There is no evidence that bromocriptine poses a particular risk to older people.

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

Overdose

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

There have been isolated reports of accidental administration of bromocriptine to children. They reported side effects such as vomiting, drowsiness and fever. Normalization of the patients' condition occurred spontaneously within a few hours or after proper treatment.

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

Contraindications

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

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

Toxemia of pregnant women, postpartum and childbirth hypertension, uncontrolled hypertension, idiopathic or hereditary tremors, Huntington's chorea.

Bromocriptine is contraindicated for use to suppress 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 outweigh the potential risks (see PRECAUTIONS).

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 evidence of cardiac valve insufficiency on echocardiography performed before starting treatment.

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

Synonyms and analogues

Drug synonyms are drugs with identical active ingredients. Pharmaceutical companies in Russia, Ukraine, Kazakhstan, Hungary, Italy, the USA, and Canada produce tablets and capsules with Bromocriptine under the names:

Apo-Bromocriptine;
Bromocriptine-K;
Bromocriptine-KB;
Bromocriptine Poly;
Abergeen;
Bromergon;
Laktodel;
Lactodel;
Parlodel;
Serocriptine;
Ronalyn.

Analogue drugs have the same code according to the International Therapeutic Chemical Classification (ATC code), but are made on the basis of other active ingredients. The most commonly used Bromocriptine analogues in weight loss programs are:

"Alactin" is the active component of the prolactin inhibitor cabergoline, (Czech Republic).
“Dostinex” is the active substance cabergoline, manufactured by Pfizer (Italy).
“Norprolac” is the main component of quinagolide hydrochloride, a product of GmbH Ferring (Germany).

Note!

Description of the drug Bromocriptine-Richter table. 2.5 mg No. 30 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.

Mechanism of action

Bromocriptine is a prolactin inhibitor and dopamine antagonist. The first of these enzymes slows down the rate of metabolic processes and increases appetite, the second causes an increase in motor activity, and its deficiency contributes to the deposition of subcutaneous fat.

Similar in structure to dopamine, Bromocriptine imitates its action by stimulating the corresponding receptors in the brain. Reduces the amount of prolactin in the blood, due to which it acts as a fat burner and hunger suppressant. This dopamine also prevents metabolic slowdown, which is important when losing weight. And since dopamine is considered a pleasure hormone, Bromocriptine psychologically makes it easier to cope with a low-calorie diet.

This is interesting! The famous nutritionist and physiologist Lyle MacDonald, in his book on diets, cites the results of studies conducted in 1997 in one of the American clinics. Women with excess body weight gained during menopause were given Bromocriptine for 6 weeks in the dosages prescribed in the instructions. Without changing the degree of physical activity and diet, the amount of body fat decreased by an average of 3.8 kg, and the volume of subcutaneous fat folds by 25%.

One of the additional properties of this hormone-like substance is its ability to increase the level of hormones in the body that affect reproductive function. In men, taking this dopamine receptor stimulant causes an increase in libido and potency due to an increase in testosterone levels; in women, libido increases due to estrogens converted from the same testosterone.

Interactions

Tolerance to bromocriptine may be reduced by alcohol.

Caution is required when using the drug simultaneously with antihypertensive drugs (see SPECIAL INSTRUCTIONS).

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 reducing prolactin levels and treating Parkinson's disease.

Metoclopramide and domperidone may reduce the prolactin-lowering effect of bromocriptine.

Sympathomimetic drugs, such as phenylpropanolamine, isometheptene, increase the risk of toxicity.

Concomitant use with other ergot alkaloids should be avoided.

Bromocriptine should be used with caution in combination with CYP3A4 inhibitors (for example, azole fungicides, HIV protease inhibitors) (see PHARMACOLOGICAL PROPERTIES).