Agalates, 0.5mg pills, 2pcs

Composition

1 tablet contains:

Active ingredient:

cabergoline 0.5 mg;

excipients:

lactose,

L-leucine,

magnesium stearate (E 572).

Pharmacological action

Cabergoline is a synthetic ergot alkaloid, an ergoline derivative, a long-acting dopamine agonist that inhibits prolactin secretion. The mechanism of action of cabergoline involves stimulation of central dopaminergic receptors in the hypothalamus. In doses higher than those required to suppress prolactin secretion, the drug causes a central dopaminergic effect due to stimulation of dopamine D2 receptors.

The effect of the drug is dose-dependent. A decrease in the prolactin content in the blood is usually observed after 3 hours and persists for 2-3 weeks, and therefore one dose of the drug is usually sufficient to suppress milk secretion. In the treatment of hyperprolactinemia, the prolactin content in the blood normalizes after 2-4 weeks of using the drug in an effective dose. Normal prolactin levels may persist for several months after discontinuation of the drug.

Cabergoline has a highly selective effect and does not affect the basal secretion of other pituitary hormones and cortisol. The only pharmacodynamic effect that is not associated with therapeutic action is a decrease in blood pressure (BP). The maximum antihypertensive effect usually develops 6 hours after a single dose of the drug; the degree of reduction in blood pressure and the frequency of development of the antihypertensive effect are dose-dependent.

Indications

• Suppression of physiological postpartum lactation (only for medical reasons).
• Suppression of already established lactation (only for medical reasons).
• Disorders associated with hyperprolactinemia (including functional disorders such as amenorrhea, oligomenorrhea, anovulation, galactorrhea).
• Prolactin-secreting pituitary adenomas (micro-and macroprolactinomas).
• Idiopathic hyperprolactinemia.

Use during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Before taking the drug, pregnancy should be excluded. It is recommended to avoid pregnancy for at least 1 month after discontinuation of treatment.. There are limited data on taking the drug during pregnancy, obtained during the first 8 weeks after conception. Cabergoline use was not associated with an increased risk of abortion, preterm birth, multiple pregnancies, or birth defects. No other data has been received so far.

In animal studies, no direct or indirect adverse effects of cabergoline on pregnancy, embryo/fetal development, delivery, or postnatal development were found.

Given the limited experience of using cabergoline during pregnancy, the drug should be discontinued when planning it. If pregnancy occurs during treatment, cabergoline is immediately discontinued. Due to the possibility of expansion of a pre-existing tumor, signs of pituitary enlargement in pregnant women should be monitored.

Since cabergoline suppresses lactation, the drug should not be prescribed to mothers who prefer to breastfeed infants. Breast-feeding should be discontinued during cabergoline treatment.

Contraindications

• Postpartum or uncontrolled arterial hypertension.
• Hypersensitivity to cabergoline, other ergot alkaloids, or any component of the drug.
• Severe liver function disorders.
• Adverse events from the lungs, such as pleurisy or fibrosis (including in the anamnesis), associated with the use of dopamine agonists.
• Psychosis (including a history of it) or the risk of developing it.
• Pregnancy and preeclampsia and eclampsia that developed on its background.
• Breast-feeding.

The efficacy and safety of cabergoline in children under 16 years of age has not been studied.

With caution: in patients with cardiovascular diseases, hypotension, Raynaud’s syndrome, peptic ulcers or gastrointestinal bleeding, in patients with end-stage renal failure or who are on hemodialysis, in elderly patients.

Side effects

the Frequency of side effects is classified in accordance with the recommendations of the world health organization: very often – not less than 10%, often at least 1% but less than 10%, infrequently – no more than 0.1% but < 1%, rare – not less than 0.01%, but less than 0.1%, very rare (including isolated cases) – less than 0.01%.

From the immune system:  infrequently – hypersensitivity reaction, skin rash.

Blood and lymphatic system disorders:  infrequently-erythromelalgia.

Nervous system disorders:  often – hallucinations, sleep disorders, confusion, dizziness, dyskinesia, increased libido, headache, drowsiness, depression, infrequently-hyperkinesis, psychotic disorder, delirium, paresthesia, transient hemianopsia, fainting, very rarely-sudden sleep attack, pathological gambling addiction.

From the cardiovascular system:  often – postural hypotension, angina pectoris, heart valve damage (including regurgitation), pericarditis, pericardial effusion, hot flashes, palpitation, peripheral edema.

From the gastrointestinal tract:  very often – nausea, abdominal pain, often-dyspepsia, vomiting, gastritis, constipation, rarely-epigastric pain, very rarely-retroperitoneal fibrosis.

Respiratory system disorders:  often-shortness of breath, infrequently-pleural effusion, pulmonary fibrosis, nosebleeds.

Other services:  often-asthenia, weakness, impaired liver function, breast pain, visual impairment, very rarely-cramps in the muscles of the lower extremities, increased creatine phosphokinase activity.

Interaction

The effect of macrolide antibiotics on the plasma content of cabergoline when used together has not been studied. Given the possibility of increasing the level of cabergoline, the drug is not recommended to be used in combination with macrolides.

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).

There is no information about the interactions of cabergoline with other ergot alkaloids, however, long-term use of such combinations is not recommended.

Considering the Pharmacodynamics of cabergoline (hypotensive effect), it is necessary to take into account the interaction with drugs that reduce blood pressure.

In clinical studies in patients with Parkinson’s disease, no pharmacokinetic interaction with levodopa or selegiline was found. Pharmacokinetic interactions with other drugs cannot be predicted based on the available information on cabergoline metabolism.

How to take, course of use and dosage

Inside, preferably with a meal.

Adults

Treatment of disorders associated with hyperprolactinemia:  The recommended starting dose is 0.5 mg per week in 1 or 2 divided doses (for example, on Monday and Thursday). The dosage is increased gradually, usually by 0.5 mg / week with an interval of 1 month until the optimal therapeutic effect is achieved. The maximum daily dose should not exceed 3 mg.

The maintenance dose is 1 mg / week (0.25-2 mg / week); in some cases, in patients with hyperprolactinemia, up to 4.5 mg/week.

When using Agalates in doses higher than 1 mg/week, it is recommended to divide the weekly dose into 2 or more doses, depending on tolerability.

To suppress physiological postpartum or already established lactation:  The recommended dose is 1 mg once within the first 24 hours after birth.

Use in patients with impaired liver or kidney function:  For more information, see the sections ” Contraindications “and”Special Instructions”.

Use in patients over 65 years of age:  given the indications for use, the experience of using cabergoline in patients over 65 years of age is limited. The available data indicate that there is no specific risk.

Overdose

Symptoms:  There is no information about an overdose of the drug. Based on the results of animal experiments, we can expect the appearance of symptoms due to hyperstimulation of dopamine receptors: nausea, vomiting, decreased blood pressure, impaired consciousness/psychosis or hallucinations.

Treatment:  if indicated, measures should be taken to restore blood pressure. In addition, with severe symptoms from the central nervous system (hallucinations), the use of dopamine antagonists may be required.

Special Instructions

To open the bottle, first press the cap, then turn it as shown on the cap. Do not remove the silica gel capsule from the bottle and do not use it inside.

Data on the efficacy and safety of Agalates in patients with impaired liver or kidney function are limited. The pharmacokinetics of cabergoline do not change significantly in patients with moderate or severe renal insufficiency. It has not been studied in patients with end-stage renal failure or hemodialysis. Therefore, Agalates should be used with caution in these patients. The effect of alcohol on the overall tolerability of Agalates has not been established.

The use of Agalates may cause symptomatic hypotension, especially when combined with drugs that reduce blood pressure. It is recommended to regularly measure blood pressure in the first 3-4 days after the start of treatment.

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

Before starting long-term therapy with Agalates, all patients should undergo a full examination to detect damage to the heart valves, determine the functional state of the lungs and kidneys to prevent the deterioration of concomitant diseases.

If new clinical symptoms from the respiratory system appear, a lung X-ray is recommended. In patients with pleural effusions/fibrosis, an increase in ESR was noted, and therefore, if there is an increased ESR without obvious clinical signs, an X-ray examination should also be performed.

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

After starting therapy with Agalates for the prevention of 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. If valvular regurgitation appears or worsens, narrowing of the lumen, or thickening of the valve wall, Agalates therapy should be discontinued.

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

When using Agalates, drowsiness and episodes of sudden falling asleep may occur, especially in patients with Parkinson’s disease (see “Effects on the ability to drive vehicles and mechanisms”).

When using the drug Agalates, there was an increase in libido, hypersexuality, and a pathological desire for gambling. These symptoms were reversible and disappeared with dose reduction or discontinuation of Agalates.

Hyperprolactinemia in combination with amenorrhea and infertility may be associated with pituitary tumors, so before starting therapy with Agalates, it is necessary to find out the cause of hyperprolactinemia.

It is recommended to check the prolactin content in the blood serum every month, because after achieving an effective therapeutic regimen, the normal concentration of prolactin remains for 2-4 weeks.

After discontinuation of Agalates, hyperprolactinemia usually occurs again. However, in some patients, there is a persistent decrease in prolactin concentration for several months.

The use of Agalates restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Since pregnancy can occur before the resumption of menstruation, pregnancy tests are recommended to be performed during amenorrhea, and after the restoration of the menstrual cycle-in all cases of their delay by more than 3 days. Women who are not planning pregnancy are advised to use effective non-hormonal contraceptives during and after treatment with Agalates. For women planning pregnancy, conception is recommended no earlier than 1 month after discontinuation of Agalates.

Influence on the ability to drive vehicles and mechanisms

Patients should be informed about the need to exercise caution when driving a car or operating mechanisms. Patients who have already experienced drowsiness and / or episodes of sudden falling asleep during treatment with Agalates should refrain from driving a car or other activities that require increased concentration and speed of psychomotor reactions.

Storage conditions

In a dry place, at a temperature not exceeding 30 °C. In a tightly closed original bottle. Keep out of reach of children.

Shelf

life is 2 years.

Active ingredient

Cabergoline

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For women, Adults as prescribed by a doctor

Indications

To suppress lactation