Bergolac tablets 0.5mg, No. 2

Prevention of physiological lactation after childbirth; suppression of already established postpartum lactation; treatment of disorders associated with hyperprolactinemia, including amenorrhea, oligomenorrhea, anovulation, galactorrhea; prolactin-secreting pituitary adenomas (micro- and macroprolactinomas); idiopathic hyperprolactinemia; syndrome of 'empty' sella turcica in combination with hyperprolactinemia.

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

Inside. The dose and the regimen of administration are set individually, depending on the indications and the clinical situation.

1 tab.

Active ingredient: cabergoline - 500 mcg

Excipients: leucine, anhydrous lactose (lactopress), magnesium stearate.

Hypersensitivity to cabergoline and ergot alkaloids; dysfunctions of the heart and respiration due to fibrotic changes in the lungs, pericardium, heart valves or retroperitoneal space, or a history of such conditions; with long-term therapy - anatomical signs of the pathology of the valve apparatus of the heart (such as thickening of the valve leaflet, narrowing of the valve lumen, mixed pathology, narrowing and stenosis of the valve), confirmed by echocardiography performed at the beginning of therapy; risk of postpartum psychosis; breastfeeding period; children under 16 years of age.

With care: arterial hypertension that developed during pregnancy, for example, preeclampsia or postpartum arterial hypertension; severe cardiovascular disease, Raynaud's syndrome; hypotension, Parkinson's disease; severe psychotic or cognitive impairment (including history); peptic ulcer, gastrointestinal bleeding; severe hepatic impairment (lower doses are recommended); renal failure; simultaneous use with drugs that have an antihypertensive effect (due to the risk of orthostatic hypotension).

Trade name: Bergolak

Description: Tablets are white, oblong, biconvex, with a risk on one side.

Composition:

1 tab.

Active ingredient: cabergoline - 500 mcg

Excipients: leucine, anhydrous lactose (lactopress), magnesium stearate.

Clinical and pharmacological group: Dopamine receptor agonist. Inhibitor of prolactin secretion

Pharmaco-therapeutic group: Dopamine receptor agonist

pharmachologic effect

Derived ergot alkaloid ergoline, dopamine D2 receptor agonist. By stimulating these receptors of the pituitary gland, it causes a pronounced and prolonged inhibition of the secretion of the hormone of the anterior lobe - prolactin. It has a therapeutic effect in hyperprolactinemia, reducing the severity of such manifestations as menstrual irregularities (oligomenorrhea, amenorrhea), infertility, galactorrhea; impotence, decreased libido. Prevents and suppresses physiological lactation.

At doses higher than those required to suppress prolactin secretion, cabergoline produces a central dopaminergic effect due to the stimulation of dopamine D2 receptors. The action is dose-dependent. Cabergoline reduces daily movement fluctuation in patients with Parkinson's disease who are being treated with a levodopa / carbidopa combination. Cabergoline is selectively active without affecting the basal secretion of other pituitary hormones and cortisol.

The pharmacodynamic effects of cabergoline, which are not associated with therapeutic activity, include only a decrease in blood pressure. With a single dose, the maximum hypotensive effect is observed during the first 6 hours and is dose-dependent.

Pharmacokinetics

After oral administration, cabergoline is rapidly absorbed from the gastrointestinal tract. Cmax in blood plasma is reached after 0.5-4 hours. Food does not affect the absorption or distribution of cabergoline. Pharmacokinetics is linear up to a dose of 7 mg / day.

The binding of cabergoline (at a concentration of 0.1-10 ng / ml) with plasma proteins is 41-42%.

The metabolites of cabergoline were found in urine: 6-allyl-8?-carboxy-ergoline in an amount of 4-6% of the dose taken, as well as three other metabolites with a total content of less than 3%. All metabolites to a much lesser extent (compared to cabergoline) inhibit the secretion of prolactin. Cabergoline has a long T1 / 2. T1 / 2 in healthy volunteers is 63-68 hours, T1 / 2 in patients with hyperprolactinemia is 79-115 hours. With this T1 / 2, the equilibrium state is achieved after 4 weeks. In urine and feces, 18% and 72% of the dose taken were found, respectively. The content of unchanged cabergoline in urine is 2-3%.

Indications

Prevention of physiological lactation after childbirth; suppression of already established postpartum lactation; treatment of disorders associated with hyperprolactinemia, including amenorrhea, oligomenorrhea, anovulation, galactorrhea; prolactin-secreting pituitary adenomas (micro- and macroprolactinomas); idiopathic hyperprolactinemia; syndrome of 'empty' sella turcica in combination with hyperprolactinemia.

Dosage regimen

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

Inside. The dose and the regimen of administration are set individually, depending on the indications and the clinical situation.

Side effect

From the side of the cardiovascular system: palpitations, angina pectoris; with prolonged use, cabergoline usually has a hypotensive effect, in some cases orthostatic arterial hypotension may occur; an asymptomatic decrease in blood pressure is possible during the first 3-4 days after childbirth.

From the nervous system: dizziness / vertigo, tremor, headache, increased fatigue, drowsiness, depression, asthenia, paresthesia, fainting, nervousness, anxiety, insomnia, impaired concentration, impaired impulse control (excessive passion for shopping, overeating, spending money ).

From the digestive system: nausea, vomiting, epigastric pain, abdominal pain, constipation, gastritis, dyspepsia, dryness of the oral mucosa, diarrhea, flatulence, toothache, sensation of irritation of the pharyngeal mucosa.

From the respiratory system: pleurisy.

Others: mastodynia, dysmenorrhea, nosebleeds, rhinitis, 'hot flushes' of blood to the skin of the face, transient hemianopsia, vasospasm of the fingers and muscle cramps of the lower extremities, visual impairment, flu-like symptoms, malaise, periorbital and peripheral edema, anorexia, acne, pruritus , joint pain.

With long-term therapy with cabergoline, deviations from the norm of standard laboratory parameters were rarely observed; in women with amenorrhea, a decrease in hemoglobin content was observed during the first few months after menstruation was restored.

Contraindications for use

Hypersensitivity to cabergoline and ergot alkaloids; dysfunctions of the heart and respiration due to fibrotic changes in the lungs, pericardium, heart valves or retroperitoneal space, or a history of such conditions; with long-term therapy - anatomical signs of the pathology of the valve apparatus of the heart (such as thickening of the valve leaflet, narrowing of the valve lumen, mixed pathology, narrowing and stenosis of the valve), confirmed by echocardiography performed at the beginning of therapy; risk of postpartum psychosis; breastfeeding period; children under 16 years of age.

With care: arterial hypertension that developed during pregnancy, for example, preeclampsia or postpartum arterial hypertension; severe cardiovascular disease, Raynaud's syndrome; hypotension, Parkinson's disease; severe psychotic or cognitive impairment (including history); peptic ulcer, gastrointestinal bleeding; severe hepatic impairment (lower doses are recommended); renal failure; simultaneous use with drugs that have an antihypertensive effect (due to the risk of orthostatic hypotension).

Application during pregnancy and lactation

Use during pregnancy is indicated only in cases where the intended benefit to the mother outweighs the potential risk to the fetus.

If pregnancy occurs during treatment with cabergoline, it should be discontinued immediately, also with a careful assessment of the ratio of the expected benefit to the possible risk to the woman and the fetus.

Cabergoline restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Since pregnancy can occur before menstruation is restored, it is recommended to carry out pregnancy tests at least once every 4 weeks during the period of amenorrhea, and after menstruation is restored, every time there is a delay in menstruation by more than 3 days. Women wishing to avoid pregnancy should use barrier methods of contraception during treatment with cabergoline, as well as after its cancellation until anovulation recurs. Women who have become pregnant should be under the supervision of a doctor for the timely detection of symptoms of an enlarged pituitary gland, since during pregnancy it is possible to increase the size of already existing pituitary tumors.

There is no information on the excretion of cabergoline in breast milk. If necessary, use during lactation should decide on the termination of breastfeeding.

Application for violations of liver function

Contraindicated in severe hepatic impairment (lower doses are recommended).

Application for impaired renal function

Use with caution in patients with renal insufficiency.

Application in children

Use in children under the age of 16 is contraindicated (the safety and effectiveness of cabergoline have not been established).

special instructions

Before prescribing cabergoline for the treatment of disorders associated with hyperprolactinemia, a complete examination of the pituitary gland is necessary.

Before prescribing cabergoline, an assessment of the state of the cardiovascular system, including echocardiography, should be performed in order to identify asymptomatic dysfunction of the valve apparatus.

Cabergoline can cause symptomatic hypotension, especially when taken together with drugs that lower blood pressure. It is recommended to regularly measure blood pressure in the first 3-4 days after starting treatment.

Long-term use of cabergoline and other ergot derivatives that are active against serotonin 5-HT2B receptors increases the risk of developing fibrotic and serous-inflammatory diseases, such as exudative pleurisy, pleural fibrosis, pulmonary fibrosis, pericarditis, damage to one or more heart valves (aortic, mitral, tricuspid), retroperitoneal fibrosis. Cancellation of cabergoline in the event of the development of this pathology led to an improvement in signs and symptoms.

Before starting long-term therapy with cabergoline, all patients should undergo a complete examination to detect lesions of the heart valves, to determine the functional state of the lungs and kidneys to prevent the worsening of the course of concomitant diseases.

When new clinical symptoms of the respiratory system appear, a fluoroscopy of the lungs is recommended. In patients with pleural effusion / fibrosis, an increase in ESR was noted, therefore, with an increased ESR without obvious clinical signs, an X-ray examination should also be performed.

With long-term therapy with cabergoline, a gradual development of fibrotic disorders is possible, therefore, during treatment, the appearance of symptoms such as shortness of breath, shortness of breath, cough, chest pain, back pain, edema of the lower extremities, signs of retroperitoneal fibrosis, heart failure should be monitored.

After starting therapy with cabergoline, in order to prevent fibrotic disorders, the condition of the heart valves should be monitored and an ECG examination should be performed within 3-6 months. Further, the frequency of ECG monitoring is set by the doctor individually for each patient, but at least once every 6-12 months. In the event of the appearance or worsening of valve regurgitation, narrowing of the lumen or thickening of the valve wall, therapy with cabergoline should be discontinued.

The patient's need for other types of clinical examination is determined by the physician on an individual basis.

It is recommended that serum prolactin levels be checked every month as after reaching an effective therapeutic regimen, the normal level of prolactin is maintained for 2-4 weeks. After withdrawal of cabergoline, hyperprolactinemia usually reoccurs. However, in some patients, a persistent decrease in prolactin concentration is observed over several months.

Influence on the ability to drive vehicles and use mechanisms

Cabergoline lowers blood pressure, which may interfere with the rate of response in some patients. Patients receiving cabergoline should refrain from driving vehicles and other activities that require high concentration of attention and speed of psychomotor reactions.

Drug interactions

It is not recommended to use cabergoline simultaneously with macrolide antibiotics (including with erythromycin), because increases the bioavailability of cabergoline and the severity of its side effects.

The mechanism of action of cabergoline is associated with direct stimulation of dopamine receptors, so it should not be used in combination with dopamine receptor antagonists (phenothiazines, butyrophenones, thioxanthenes, metoclopramide).

Combination with ergot alkaloids and their derivatives is not recommended.

Given the pharmacodynamics of cabergoline (hypotensive effect), it is necessary to take into account the interaction with drugs that lower blood pressure.

Release form:

2, 8 or 10 tablets in a blister strip packaging.
2, 8, 10 or 30 tablets in a polymer bottle with a polymer cap with first opening control.
Each bottle or 1, 4 blister packs of 2 tablets, or 1 blister pack of 8 or 10 tablets together with instructions for use in a carton pack.

Storage conditions:

List B. At a temperature not exceeding 25 ?
C. Keep out of the reach of children.