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Bromocriptine 2.5 mg

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Pharmacological properties of the drug Bromocriptine 2.5 mg.

It is a specific agonist of dopamine receptors (mainly of the D2 type); the drug is a semi-synthetic derivative of the ergot alkaloid - ergocriptine. Bromocriptine suppresses the secretion of the anterior pituitary hormone - prolactin - by stimulating dopamine receptors.

Bromocriptine does not affect the normal levels of other pituitary hormones, but it can reduce the increased concentration of growth hormone in acromegaly. Prolactin is essential for the initiation and maintenance of lactation in the postpartum period. In other cases, an increase in prolactin secretion leads to abnormal lactation (galactorrhea) and / or to ovulation and menstrual disorders.

Bromocriptine prevents or suppresses physiological lactation, and can also be used in the treatment of pathological conditions caused by increased secretion of prolactin. With amenorrhea or anovulation, with or without galactorrhea, bromocriptine helps restore the menstrual cycle and ovulation.

In Stein-Leventhal syndrome, Bromocriptine 2.5 mg has a beneficial clinical effect, normalizing the secretion of luteinizing hormone. In benign breast diseases, bromocriptine helps to reduce the size and number of cysts or nodes, eliminating the imbalance between progesterone and estrogens; with prolactin-secreting pituitary adenomas (prolactinomas) - slowing their growth or decreasing their size. In acromegaly, it reduces the concentration of growth hormone and prolactin in the blood plasma, increases carbohydrate tolerance and has a beneficial clinical effect.

Bromocriptine in higher doses is used in neurology for Parkinson's disease, characterized by a specific dopamine deficiency in the striatum (corpus striatum) and black nucleus (substantia nigra) of the brain. Bromocriptine stimulates dopamine receptors, restoring neurochemical balance in these parts of the brain. The therapeutic effect of bromocriptine is manifested by a weakening of tremor, rigidity, slowing down of movements and a decrease in the severity of other symptoms of parkinsonism at all stages of the disease.

Bromocriptine retains clinical efficacy for several years of use (to date, there are reports of positive results of its use for 8 years). Bromocriptine can be prescribed as monotherapy or in combination with other antiparkinsonian drugs (eg levodopa), which can reduce their dose and avoid some side effects.

Bromocriptine has some antidepressant effect, reduces the severity of depressive symptoms in Parkinson's disease, as well as in patients with endogenous or psychogenic depression.

The maximum concentration of bromocriptine in blood plasma is reached within 1-3 hours after ingestion. Plasma protein binding of bromocriptine is 96%. Bromocriptine and its metabolites are excreted mainly in the bile and only 6% in the urine.

Indications for the use of the drug Bromocriptine.

1. Prolactin-dependent menstrual irregularities and female infertility caused by an increased and possibly normal level of prolactin secretion - amenorrhea with or without galactorrhea, oligomenorrhea, luteal phase insufficiency;

2. Violations due to increased secretion of prolactin caused by the intake of certain psychotropic, antihypertensive and other drugs;

3. Prolactin-independent female infertility - Stein-Leventhal syndrome, anovulatory cycles (an adjunct to anti-estrogen therapy, such as clomiphene);

4. Premenstrual syndrome - breast tenderness, edema associated with the phase of the cycle, flatulence, mood changes; suppression of lactation - prevention or termination of postpartum lactation for medical reasons, prevention of lactation after abortion, postpartum hypertrophy of the mammary glands;

5. Benign diseases of the mammary glands - mastalgia, benign nodular or cystic mastopathy, especially fibrocystic;

6. Prolactin-dependent hypogonadism in men - oligospermia, decreased libido, impotence;

7. Prolactinomas of the pituitary gland - conservative treatment of prolactin-secreting micro- and macroadenomas of the pituitary gland, reducing the size of the tumor before its removal, postoperative treatment while maintaining an increased level of prolactin in the blood;

8. Acromegaly - as an additional drug (sometimes alternative) in surgical or radiation treatment;

9. All stages of idiopathic Parkinson's disease and postencephalitic parkinsonism (in the form of monotherapy or in combination with other antiparkinsonian drugs).

Application of the drug Bromocriptine 2.5 mg.

In gynecological and endocrinological practice, the dose of bromocriptine depends on the specific indications for its use. In case of menstrual irregularities, female infertility appoint 1.25 mg 2-3 times a day, the dose can be gradually increased to 2.5 mg 2-3 times a day. Treatment continues until the normalization of the menstrual cycle and / or ovulation.

Several courses of treatment can be used to prevent relapse.

With premenstrual syndrome, treatment begins on the 14th day of the cycle with a dose of 1.25 mg / day, increasing the dose by 1.25 mg daily to 5 mg / day in 2 divided doses. Treatment continues until the menstrual cycle is restored.

To suppress lactation on the 1st day, 1.25 mg is prescribed 2 times a day (morning and evening), then 2.5 mg for 14 days. To prevent lactation, therapy should be started a few hours after childbirth or abortion, but only after the vital functions of the body have stabilized. 2-3 days after the abolition of bromocriptine, sometimes there is an insignificant secretion of milk, which can be eliminated by taking the drug in higher doses for another 1 week.

With postpartum hypertrophy of the mammary glands, bromocriptine is taken once in a dose of 2.5 mg, after 6 or 12 hours, the specified dose can be taken again, which will not cause undesirable suppression of lactation. With the initial manifestations of postpartum mastitis on the 1st day, 1.25 mg is prescribed 2 times a day, then 2.5 mg 2 times a day for 14 days. If necessary, treatment is carried out in combination with antibiotics.

In benign diseases of the mammary glands, Bromocriptine is prescribed at 1.25 mg 2-3 times a day, gradually increasing the dose to 5-7.5 mg / day.

In male hypogonadism, Bromocriptine is prescribed at 1.25 mg 2-3 times a day, gradually increasing the dose to 5-10 mg / day.

In prolactinomas, Bromocriptine is prescribed at 1.25 mg 2-3 times a day, gradually increasing the dose until a steady suppression of prolactin secretion is achieved (depending on the level of prolactin concentration in the blood plasma), which is usually achieved by taking several tablets per day.

In acromegaly, treatment begins with a dose of 1.25 mg / day, gradually increasing the daily dose to 10–20 mg, depending on the clinical effect and the presence of side effects.

In Parkinson's disease and post-encephalitic parkinsonism, treatment with bromocriptine begins with a daily dose of 1.25 mg for 1 week, then the daily dose is gradually increased (by 1.25 mg / week) to the minimum effective dose. The daily dose is taken in 2-3 doses. The clinical effect is usually achieved within 6-8 weeks, if necessary, the daily dose is continued to increase by 1.25 mg / week.

Therapeutic doses of bromocriptine alone or in combination with other antiparkinsonian drugs are 10–40 mg / day, but higher doses may be required. If adverse reactions occur during dose selection, bromocriptine should be taken in a reduced dose for at least 1 week, and if the side effects disappear, the dose can be increased.

Before taking bromocriptine, patients with movement disorders while taking levodopa are advised to reduce the dose of the latter drug, and after achieving a therapeutic effect as a result of using bromocriptine, you can continue to gradually reduce its dose. In some cases, levodopa can be canceled.

Bromocriptine should be taken with meals, morning and evening, and with a single dose, in the evening.

Contraindications to the use of the drug Bromocriptine.

Hypersensitivity to bromocriptine or other ergot alkaloids; toxicosis of pregnant women; the presence in the early or late postpartum period of arterial hypertension, mental illness, or an indication of them in history.

Side effects of the drug Bromocriptine.

In the first days of treatment, mild nausea may appear, less often - dizziness, weakness, irritability, headache, orthostatic hypotension, vomiting, which do not require the abolition of bromocriptine. The occurrence of these phenomena can be prevented by taking a peripheral dopamine antagonist (for example, domperidone) 1 hour before taking bromocriptine for several days.

Sometimes, with long-term treatment with bromocriptine, there is a sudden, reversible blanching of the skin of the fingers and toes when exposed to cold, especially in patients with a history of Raynaud's disease.

When treating Parkinson's disease with bromocriptine in high doses, drowsiness may appear, less often - confusion, psychomotor agitation, hallucinations, dyskinesias, a feeling of dry mouth and leg muscle cramps. These side effects are dose-dependent and are usually eliminated by decreasing the dose, after which it can be carefully increased.

Special instructions for the use of the drug Bromocriptine.

Caution is needed when using bromocriptine in the postpartum period, because sometimes (about 1 in 100,000) when using bromocriptine to prevent lactation, hypertension, myocardial infarction, convulsions, stroke, or mental disorders have been observed; sometimes seizures or cerebrovascular accident preceded by severe headache or temporary visual impairment.

When prescribing bromocriptine in the early postpartum period, blood pressure should be carefully monitored, especially in the first days of treatment. Particular care is needed when treating bromocriptine in patients who have recently taken or are taking blood pressure medications. If arterial hypertension, persistent headache, or any signs of neurotoxicity occur, treatment should be discontinued immediately.

Bromocriptine should be prescribed in the minimum therapeutically effective doses (with the exception of pathology caused by increased secretion of prolactin) to prevent a decrease in the concentration of prolactin in blood plasma below normal values, which may adversely affect the function of the corpus luteum in female patients.

With mastalgia and nodular and / or cystic changes in the mammary glands, the presence of malignant neoplasms should be excluded before using bromocriptine.

In case of acromegaly, before using bromocriptine, the presence of erosive and ulcerative lesions of the digestive tract should be excluded, and if they are present, it is better to abandon the use of bromocriptine or recommend that the patient immediately consult a doctor if any disorders of the digestive system appear. Caution is needed in connection with isolated reports of gastrointestinal bleeding in patients with acromegaly during treatment with bromocriptine, despite the fact that a causal relationship has not been established.

Caution is needed when prescribing bromocriptine to patients with a history of mental or severe cardiovascular disease.

When treating with bromocriptine, especially in the first days, arterial hypotension may appear, therefore, caution is needed when working with various mechanisms.

Tolerance to bromocriptine may be impaired by alcohol consumption.

There are separate reports of the appearance of pleural effusion in patients with parkinsonism who have been receiving high doses of bromocriptine for a long time, therefore, patients with pleural and lung pathology of unknown origin should be carefully examined and, if a causal relationship is confirmed, discontinue treatment.

Interaction of the drug Bromocriptine with other drugs.

The combined use of Bromocriptine and Levodopa enhances the antiparkinsonian effect, which often reduces the dose of Levodopa. Bromocriptine is especially indicated for patients in whom the effectiveness of the use of Levodopa decreases or complications such as pathological involuntary movements (choreoathetoid dyskinesia and / or painful dystonia) occur, the effectiveness to the end of the action is sharply reduced or the effectiveness of the on-off type of bromocriptine fluctuates sharply.

Erythromycin or josamycin may cause an increase in plasma bromocriptine concentration.

Overdose with Bromocriptine.

There are no reports of life-threatening conditions following an acute overdose of bromocriptine. Until now, the highest dose taken by an adult was 225 mg, with nausea, vomiting, dizziness, orthostatic hypotension, sweating, drowsiness, and hallucinations observed. Treatment is symptomatic. Metoclopramide can be prescribed to eliminate vomiting or hallucinations.