Pharmacological properties
Pharmacodynamics.
Bromocriptine - the active ingredient of the drug 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 drug are discussed below for each type of indication. Endocrinological indications for use
Bromocriptine suppresses the secretion of prolactin without affecting the normal levels of other hormones released by the anterior pituitary gland.
In patients with acromegaly, bromocriptine reduces elevated levels 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 lack of dopamine. Stimulation of dopamine receptors with bromocriptine can restore neurochemical balance.
In clinical terms, bromocriptine improves symptoms of Parkinson's disease (eg, tremor, muscle rigidity, bradykinesia) and depression at all stages of the disease. Bromocriptine can be used alone or in combination with other drugs for Parkinson's disease.
Combination treatment reduces the required dose of levodopa, and therefore delays the relapse of motor abnormalities. Thus, treatment with bromocriptine may provide a reduction in the dose of other drugs used in combination with it, in particular levodopa. This may relieve patients from certain adverse effects of levodopa, such as end-of-dose worsening, on-off phenomenon, and dyskinesia.
Pharmacokinetics. Bromocriptine is rapidly and significantly 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 substance is excreted in the urine.
The binding of the drug to plasma proteins is 96%.
Cmax of the drug in the blood plasma is achieved within 1–3 hours. The effect of reducing prolactin levels appears within 1–2 hours after oral administration, reaches a maximum after approximately 5 hours and is maintained for 8–12 hours. The process of removing the original substance from the blood plasma has a two-phase character, with T½ being approximately 15 hours.
The elderly age of patients does not directly affect the pharmacokinetic properties of bromocriptine. However, in individuals with impaired liver function, delayed elimination may result in increased plasma levels of the drug, which may require dosage adjustment.
There is no evidence to support a direct effect in the elderly on the pharmacokinetic properties and tolerability of bromocriptine. However, in patients with impaired liver function, the elimination rate may be reduced and the plasma level of the drug may be correspondingly increased, requiring dose adjustment.
Biotransformation. Bromocriptine undergoes intense presystemic biotransformation in 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 exhibits high affinity for CYP3A, and the main metabolic pathway is hydroxylation of the proline ring of the cyclopeptide moiety. Therefore, inhibitors and/or potent substrates of CYP 3A4 would be expected to inhibit the elimination of bromocriptine and lead to increased bromocriptine levels. Bromocriptine is also a potent CYP3A4 inhibitor. However, given the low therapeutic concentrations of free bromocriptine in patients, significant changes in the metabolism of the second drug, the elimination of which is mediated by the CYP3A4 system, should not be expected.
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).
Indications
Menstrual irregularities and female sterility
Diseases dependent on prolactin levels and conditions with or without hyperprolactinemia. Amenorrhea (with or without galactorrhea); Oligomenorrhea. Luteal phase deficiency. Secondary hyperprolactinemia caused by other drugs (for example, some psychotropic or antihypertensive drugs).
Prolactin-independent female sterility. Polycystic ovary syndrome. Anovulatory cycles (arising under the influence of antiestrogens, such as clomiphene). Infertility associated with hyperprolactinemia. Bromocriptine has been successfully used to treat a number of sterile women without significant 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 that secrete prolactin.
Bromocriptine can be used as a first-line drug for the treatment of macroadenoma and as an alternative to surgical treatment (transsphenoidal pituitary removal) 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. 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.
Used as a special remedy, which is an alternative to radiation therapy or surgery.
Suppression of lactation. Prevention or suppression of lactation after childbirth for medical reasons, including the initial stages of postpartum mastitis. This drug is not recommended for routine suppression of lactation, for the relief of symptoms of postpartum pain, or for breast engorgement. 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 disease of the mammary glands.
Parkinson's disease. All stages of idiopathic Parkinson's disease: Bromocriptine is used either alone or in combination with levodopa to control the condition of previously untreated individuals and those severely affected by the on-off phenomenon. This remedy may help patients who do not respond to or cannot tolerate levodopa treatment, as well as individuals whose response to levodopa decreases. Postencephalitic Parkinson's disease: the drug can be used in monotherapy or in combination with other drugs for the treatment of Parkinson's disease.
Treatment of patients with cyclic benign breast disease and premenstrual syndrome (see SPECIAL INSTRUCTIONS).
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.
Composition and release form
Bromocriptine is a single drug, the active ingredient in it is bromocriptine mesylate, a semi-synthetic substance obtained from ergot. Auxiliary components:
- silica;
- magnesium stearate;
- disodium edetate;
- starch;
- maleic acid;
- lactose;
- MCC;
- povidone.
The drug is produced in tablets and gelatin capsules by pharmaceutical companies Richter Gedeon Ltd (Hungary), Ozon (Russia) and Kiev Vitamin Plant (Ukraine). Listed as an over-the-counter product. 30 tablets of 2.5 mg each from a Russian and Ukrainian manufacturer cost from 130 to 200 rubles, the price of the same package of a Hungarian product is from 350 to 500 rubles.
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.”
Side effects
Nausea, vomiting, anorexia, headache, dizziness and fatigue may occur during the first days of treatment; however, these reactions do not usually 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 may cause orthostatic hypotension; therefore, blood pressure in outpatients should be measured in an upright position.
In patients with Parkinson's disease who use the drug in high doses, drowsiness, hallucinations, confusion, blurred vision, dry mouth, calf muscle cramps and retroperitoneal fibrosis may occur (see SPECIAL INSTRUCTIONS). All 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 postpartum women using bromocriptine to suppress lactation), serious side effects have been reported, including hypertension, myocardial infarction or stroke, although the causal relationship between these events and the use of the drug is unknown. Some patients experienced severe headache and/or temporary visual disturbances before the stroke.
Very rarely, heart valve insufficiency (including regurgitation) and associated disorders (pericarditis and pericardial effusion) have developed.
Patients with cirrhosis may develop hyponatremia and hepatic encephalopathy.
Very rarely, bromocriptine can cause sudden falling asleep during the day.
Patients using dopamine agonists, including Bromocriptine-Richter, may experience pathological gambling, increased libido, hypersexuality, impulsive spending or shopaholia, and impulsive gluttony (see SPECIAL INSTRUCTIONS).
Dopamine agonists, which belong to the group of ergot alkaloids, can 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: uncommon - 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 - blurred vision, blurred field of vision.
On the part of the organ of hearing and balance: rarely - tinnitus.
From the heart: rarely - pericardial effusion, compressive pericarditis, tachycardia, bradycardia, arrhythmia; very rarely - myocardial infarction, heart valve insufficiency.
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; uncommon - dry mouth, vomiting; rarely - abdominal pain, retroperitoneal fibrosis, gastrointestinal bleeding, gastrointestinal ulcers.
From the skin and subcutaneous tissue: uncommon - allergic skin reactions, hair loss.
From the musculoskeletal and connective tissue side: infrequently - cramps of the calf muscles.
General complications and reactions at the injection site: uncommon - increased fatigue; rarely - peripheral edema; very rarely - neuroleptic malignant syndrome (bromocriptine withdrawal syndrome).
Contraindications, side effects
Bromocriptine is contraindicated in case of individual hypersensitivity to ergot alkaloids, in the first trimester of pregnancy, after a recent myocardial infarction, as well as in the presence of the following pathologies:
- persistent hypotension (low blood pressure);
- heart rhythm disturbances;
- spastic conditions of peripheral vessels;
- gastrointestinal diseases accompanied by damage to the mucous membrane;
- endogenous psychoses;
- Huntington's disease (genetic disease of the nervous system).
Attention! While taking tablets or capsules containing Bromocriptine, it is not recommended to perform work that requires a quick reaction or increased attention, as well as combining their use with antidepressants-MAO inhibitors that have a depressant effect on the central nervous system. It is prohibited to drink alcoholic beverages.
When properly selected doses, this drug is well tolerated. In people suffering from hypertension, a dopamine receptor stimulant can cause a moderate drop in blood pressure, which, in principle, is not dangerous. During the initial period of treatment, the following side effects may develop:
- headache;
- dizziness;
- decreased visual acuity;
- fast fatiguability;
- nausea;
- constipation;
- swelling of the mucous membranes (in particular, nasal congestion);
- whitening of fingers when cooling.
special instructions
There is insufficient evidence of the effectiveness of bromocriptine in the treatment of patients with premenstrual syndrome and benign breast tumors. 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 a history of hypertension, atherosclerotic heart disease and/or severe cardiovascular disease or serious mental disorders. In postpartum women using bromocriptine, blood pressure should be carefully monitored at regular intervals, especially during the first days of treatment.
Particular caution is required in patients who are using (or have recently used) concomitant treatment with drugs that can affect blood pressure.
Concomitant use of bromocriptine with vasoconstrictors such as sympathomimetics or ergot alkaloids, including ergometrine or methylergometrine, during labor is not recommended.
In rare cases, serious side effects, including myocardial infarction, hypertension, stroke or psychiatric disorders, have been observed in postpartum women who used bromocriptine to suppress lactation. Some patients experienced severe headache and/or temporary visual disturbances before the stroke.
In case of hypertension, severe and persistent headache with visual disturbances, or any signs of CNS toxicity, treatment should be discontinued immediately.
Patients may develop hyperprolactinemia of idiopathic or drug 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 in cases of acromegaly.
Women of reproductive age with conditions not associated with hyperprolactinemia should use the drug at the minimum effective dose. This precaution is necessary to avoid suppression of prolactin secretion to levels below normal with subsequent impairment of corpus luteum function. 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 during menopause are asked to be examined once every 6 months, and women of reproductive age are asked to be examined once a year.
Several cases of gastrointestinal bleeding and bleeding from stomach ulcers have been reported. If this occurs, bromocriptine should be discontinued immediately. Patients with a history of gastric ulcers should be carefully monitored when treated with bromocriptine.
For patients with acromegaly and a history of gastric ulcers, other treatments should be preferred if possible. If bromocriptine cannot be substituted for another agent, the patient should be advised to immediately report any gastrointestinal side effects to the physician.
Patients with severe cardiovascular or psychiatric disorders using bromocriptine for macroadenoma indications should only take it if the expected benefits outweigh the potential risks.
Because in individuals with pituitary macroadenomas the disease may be accompanied by hypofunction of the pituitary gland as a result of compression or destruction of pituitary tissue, patients should undergo a full evaluation of pituitary function before starting bromocriptine 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 if tumor growth occurs, the advisability of surgical procedures should be weighed.
If pregnancy occurs in patients with adenoma after taking bromocriptine, careful monitoring of their health condition is mandatory. Adenomas that secrete prolactin can grow during pregnancy. In these patients, treatment with bromocriptine often results in tumor shrinkage and rapid improvement of visual field defects. In severe cases of compression of the optic and other cranial nerves, emergency adrenal surgery may be necessary.
Visual field impairment is a known complication of macroprolactinoma. Effective treatment with bromocriptine leads to a reduction in tumor size and hyperprolactinemia, and often eliminates visual impairment. However, some patients may later develop secondary visual field impairment despite normalized prolactin levels and decreased tumor size. In such cases, visual field defects may improve after reducing the dose of bromocriptine, although slightly increased prolactin levels and slight tumor growth are observed. Therefore, it is recommended to monitor the visual fields in patients for the purpose of early diagnosis of secondary visual field reduction and appropriate adjustment of the drug dose.
CSF rhinorrhea has been observed in some patients with prolactin-secreting adenomas treated with bromocriptine. Evidence suggests that this may be due to a decrease in the size of proliferating tumors.
During the first few days of treatment, patients may sometimes experience arterial hypotension.
Caution is required when administering bromocriptine in high doses to patients with a history of mental disorders or severe cardiovascular disorders.
Treatment of Parkinson's disease with the drug in high doses requires caution in patients with a history of psychosis or severe cardiovascular disorders.
Pleural and pericardial effusions, pleural and pulmonary fibrosis, and constrictive pericarditis have been reported occasionally in patients using bromocriptine, especially over long periods and in high doses. Patients with pleuropulmonary disorders require careful examination to identify the causes; in such cases, discontinuation of bromocriptine treatment should be considered.
Cases of retroperitoneal fibrosis have been observed in several patients treated with bromocriptine, especially over long periods and in high doses. To ensure detection of retroperitoneal fibrosis in its early reversible stages, it is recommended to monitor its manifestations (for example, back pain, swelling of the lower extremities, impaired renal function) in this category of patients.
If fibrotic changes in the retroperitoneal space are diagnosed or suspected, treatment with bromocriptine should be discontinued.
During the treatment period, patients should be carefully monitored, paying attention to the manifestations of progressive fibrotic disorders. If retroperitoneal fibrosis is diagnosed or suspected, treatment with bromocriptine should be discontinued.
Treatment with bromocriptine may be associated with drowsiness and episodes of sudden sleep onset, especially in individuals with Parkinson's disease. Sudden falling asleep during daily activities, in some cases without the patient even realizing it and without warning signs, has been very rare. Patients should be informed of this possibility and should be advised to exercise caution when driving or operating machinery during treatment with bromocriptine. Patients who have experienced drowsiness and/or cases of sudden falling asleep should refrain from driving vehicles or operating machinery. Moreover, in this case, the possibility of reducing the dose or stopping treatment should be considered.
Impaired impulse control. Patients should be regularly monitored for the development of impulse control disorders. Patients and caregivers should be informed of the possibility that patients using dopamine agonists, including Bromocriptine-Richter, may develop behavioral symptoms of impulse control disorders, including pathological gambling, increased libido, hypersexuality, a tendency to impulsively spend money or shopaholia, as well as impulsive gluttony. If such symptoms occur, consider reducing the dose of the drug/gradually stopping its use.
The drug 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 drug.
Use during pregnancy and lactation. Pregnancy. In patients planning pregnancy, bromocriptine, like all other drugs, should be discontinued when pregnancy is confirmed, unless there are medical contraindications to continue therapy. No increase in abortion rates was observed after bromocriptine was discontinued during this period. Clinical experience has shown that the use of bromocriptine during pregnancy does not have a negative effect on its course or outcome.
If pregnancy occurs in a patient with a pituitary adenoma and treatment with bromocriptine has been stopped, careful medical supervision throughout the pregnancy is essential. In patients who experience signs of significant enlargement of the prolactinoma, such as headache or blurred visual field, bromocriptine treatment may be restarted or surgery may be appropriate.
Lactation. Because bromocriptine suppresses lactation, it should not be used by breastfeeding women.
Children. Bromocriptine-Richter tablets are not recommended for use in children under 7 years of age due to insufficient data on safety and effectiveness.
Bromocriptine has been used for the treatment of prolactinoma and gigantism (acromegaly) in patients aged ≥7 years, such cases have been described in the literature. There is some data on the use of bromocriptine in pediatric practice in patients under the age of 7 years. Safety data are limited, especially for long-term use.
The ability to influence reaction speed when driving vehicles or working with other mechanisms. In the first few days of treatment, patients may experience hypotension, visual disturbances and dizziness; therefore, they should be especially careful when driving or operating machinery.
Patients who experience drowsiness and/or sudden sleep onset should be advised not to drive or engage in activities where decreased alertness could endanger others.
Reviews and results of losing weight
Natalya, 25 years old
I read a book by the American physiologist McDonald, the author of popular publications on the topics of dietary nutrition and weight loss. He advises taking low doses of Bromocriptine when dieting to speed up and enhance its effect. The very convincing arguments presented in the book prompted me to try these pills. I take them for 1.5 weeks, 1 before bed. The first few days I felt a little dizzy and nauseous in the mornings. Now I feel great and even feel more optimistic. Maybe this is a side effect? But there is an effect. My weight dropped by 2 kg, although I didn’t make any changes to my diet, and I go to the gym, as before, only 2 times a week.
Tatyana Ivanovna, 42 years old
I have always had problems with excess weight, but after 40 it became more difficult to get rid of it. Through trial and error, I'm trying to find pills that really help with weight loss. I came to the conclusion that almost all so-called fat burners work exclusively under the condition of a constant calorie deficit. And it’s also good if they have an effect and are not too harmful to health. For example, Bromocriptine, which I tried to take, causes severe nausea, weakness and dizziness. I withstood such torture for only 3 days.
Nadezhda, 24 years old
An endocrinologist prescribed me bromocriptine. I have been unsuccessfully trying to lose weight, and upon examination it turned out that, among other things, my prolactin levels are elevated, but this hormone increases appetite, promotes fat deposition and slows down metabolism. This medicine is probably tolerated individually, at least for me at first it was difficult. In the evening I took a pill and slept like a log. And in the morning I went to work and thought that I wouldn’t be able to work: weakness, exhaustion, headache, chills. But she endured it and continued taking it. This side effect lasted for exactly two days, and now I feel great. I’ll finish the course of treatment soon - I’ve been taking the pills for more than a month, during which time I’ve lost 4 kg.
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).
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.
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.
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.