Assorted (Cabergoline): Treatment of hyperprolactinemia, lactation suppression. Reservations - Instructions for the application of the consequence

Agonist dopamine receptors. Cabergoline - a dopaminergic derivative of ergolin, is characterized by a pronounced and long-term prolactinous effect. The mechanism of action is associated with a direct stimulation of docking D 2-receptors of lactotropic pituitary cells. In doses exceeding those to reduce the level of prolactin in the blood plasma, it has a central dopaminergic effect due to stimulation of dopamine D 2-receptors.

The reduction in the level of prolactin in the blood plasma is observed 3 hours after the reaction of the achievement and persists within 7-28 days in healthy volunteers and patients with hyperprolactineia and until 14-21 days - in women in the postpartum period. Prolctifying effect is dose-dependent both in terms of severity and duration of action.

Cabbergoline has a strictly electoral action and, therefore, does not affect the basal secretion of other pituitary hormones, as well as cortisol.

The pharmacological effects of Cabergolin, not related to therapeutic effect, there is a decrease in blood pressure. With a single use of the drug, the maximum hypotensive effect is noted during the first 6 hours and is dose-dependent.

Pharmacokinetics

Suction

After the intake, the cabergoline is quickly absorbed from the gastrointestinal tract. C max in plasma is achieved through 0.5-4 hours. Meals do not affect the absorption and distribution of Cabergolin.

Distribution

C SS is achieved after 4 weeks of therapy due to a long T 1/2. Bonding with plasma proteins is 41-42%.

Metabolism

The main product of Cabergolin metabolism identified in the urine is 6-allyl-8β-carboxy-ergoline at a concentration of up to 4-6% of the adopted dose. The content in the urine of 3 additional metabolites does not exceed 3% of the adopted dose. Metabolism products have a significantly smaller effect on the suppression of prolctin secretion compared to Kabrigolin.

Election

T 1/2, estimated by the velocity with urine, is 63-68 hours in healthy volunteers and 79-115 hours in patients with hyperprolactineia.

10 days after the use of the drug in the urine and feces, respectively, 18% and 72% of the adopted dose are found, and the proportion of unchanged drug in the urine is 2-3%.

Form release

White tablets, flat, oblong; With the labeling "P" and "U", separated by notch, on the one hand and "700" with short notches on top and bottom of the number - on the other.

Auxiliary substances: anhydrous lactose - 75.9 mg, leucine - 3.6 mg.

2 pcs. - Dark glass vials (1) - packs cardboard.
8 pcs. - Dark glass vials (1) - packs cardboard.

Dosage

Reservable ® should be taken inward, preferably during food intake.

To prevent lactation, a drug is prescribed in a dose of 1 mg (2 tab.) One day on the first day after delivery.

To suppress the steady lactation, 0.25 mg (1/2 tab) is prescribed 2 times / day for 2 days (the total dose is 1 mg). In order to reduce the risk of developing orthostatic hypotension in lactating patients, a single dose of reaches should not exceed 0.25 mg.

For the treatment of disorders associated with hyperprolactinemia, the drug is prescribed at a dose of 0.5 mg per week in 1 (1 tab.) Or 2 reception (1/2 tab., For example, on Monday and Thursday). An increase in the weekly dose should be carried out gradually by 0.5 mg with an interval of 1 month to the achievement of an optimal therapeutic effect. The average therapeutic dose is 1 mg per week, but can fluctuate in the range from 0.25 mg to 2 mg per week. The maximum dose for patients with hyperprolactineia is 4.5 mg per week.

Depending on tolerance, the weekly dose can be taken once or divided into 2 or more techniques per week. The division of the weekly dose into several techniques is recommended when prescribing the drug at a dose of more than 1 g per week.

In patients with increased sensitivity to dopaminergic drugs, the likelihood of the development of side effects can be reduced by starting the treatment with a reachable dose (0.25 mg 1 time per week), followed by a gradual increase to it before reaching the therapeutic dose. To improve the tolerability of the drug in the occurrence of pronounced side effects, a temporary decrease in the dose is possible, followed by a gradual increase in it, for example, by 0.25 mg per week every 2 weeks.

Overdose

Symptoms: nausea, vomiting, dyspeptic disorders, orthostatic hypotension, confusion / psychosis confusion or hallucination.

Treatment: Events should be held to eliminate the drug (stomach wash) and to maintain blood pressure. The appointment of dopamine antagonists is recommended.

Interaction

There is no information on the interaction of Cabergolin and other alkaloids of the ardines; Nevertheless, the simultaneous use of these medicines during long-term therapy is not recommended.

Since the reaches ® has a therapeutic effect by direct stimulation of dopamine receptors, the drug cannot be prescribed simultaneously with drugs acting as dopamine antagonists (for example, phenothiazines, butthrofenons, thiochannel, metoclopramide), because The latter can weaken the prolact inflicting effect of the achievement.

Like other derivatives, the reaches ® cannot be used simultaneously with the antibiotics of the macrolide groups (for example, with erythromycin), as this may lead to an increase in the systemic bioavailability of Cabergolin.

Side effects

During clinical studies with the use of achievements to prevent physiological lactation (1 mg once) and to suppress lactation (0.25 mg every 12 hours for 2 days), side effects were marked at about 14% of women. When applying the reaches for 6 months at a dose of 1-2 mg per week, divided into 2 receptions, for the treatment of disorders associated with hyperprolactinemia, the frequency of side effects was 68%. The side effects arose mainly during the first 2 weeks of therapy and in most cases disappeared as therapy continues or a few days after the cancellation of the reaches. Side effects were usually transient, by severity - weakly or moderately expressed and carried a dose-dependent character. At least once, during therapy, severe side effects were observed in 14% of patients; Due to side effects, treatment was discontinued about 3% of patients.

The most frequent side effects are presented below:

From the side of the cardiovascular system: heartbeat; rarely - orthostatic hypotension (with long-term use, the drug has a hypotensive effect); Asymptomatic decrease in blood pressure during the first 3-4 days after delivery (systolic - more than 20 mm Hg, diastolic - more than 10 mm Hg).

From the digestive system: nausea, vomiting, pain in the epigastric area, abdominal pain, constipation, gastritis, dyspepsia.

From the CNS and the peripheral nervous system: dizziness / vertigo, headache, increased fatigue, drowsiness, depression, asthenia, paresthesia, fainting.

Others: Mastodynium, Nasal bleeding, Blood bakes to the skin of the face, transient hemiananopsy, spasms of the blood vessels, the convulsions of the muscles of the lower extremities (like other derivatives, the reaches ® can have a vesseloring effect).

With prolonged therapy with the use of the achievement, the deviation from the norm of standard laboratory indicators was rarely observed; In women with Amenorrhea, there was a decrease in the level of hemoglobin during the first few months after the restoration of menstruation.

In the post-marketing study, the following adverse reactions are registered related to the use of Kabergoline: alopecia, an increase in the activity of KFK in the blood, mania, dysnae, swelling, fibrosis, liver function disorders, deviations of the liver function, reaction of increased sensitivity, rash, respiratory disorders, respiratory failure, Walvulopathy.

Indications

prevention of physiological postpartum lactation;
suppression of the established postpartum lactation;
treatment of violations associated with hyperprolactinemia, including amenorrhea, oligomenore, annotulation and galathery;
prolactinsection adenomes of pituitary glands (micro and macroprolactinoma), idiopathic hyperprolactinemia, "empty" syndrome of the Turkish saddle in combination with hyperprolactineia.

Contraindications

children's and adolescent age up to 16 years (safety and efficiency of application are not established);
increased sensitivity to cabergoline or other components of the drug, as well as to any breath alkaloids.

Aestopera ® should be prescribed with caution in the following conditions and / or diseases:

arterial hypertension, developed against the background of pregnancy, for example, preeclampsia or postpartum arterial hypertension (the reaches ® is appointed only in cases where the potential benefit from the use of the drug significantly exceeds the possible risk);
severe cardiovascular diseases, Reina syndrome;
peptic ulcer, gastrointestinal bleeding;
heavy liver failure (it is recommended to use lower doses);
severe psychotic or cognitive disorders (including a history);
symptoms of impaired heart function and respiration due to fibrous changes or the presence of such states in history;
simultaneous use with drugs that have a hypotensive effect (due to the risk of orthostatic hypotension).

Features of application

Application in pregnancy and breastfeeding

Since controlled clinical studies with the use of achievements in pregnant women were not carried out, the use of the drug during pregnancy is possible only when the alleged benefit for the mother exceeds the potential risk to the fetus.

If pregnancy has come against the background of treatment with the achievement, it should be considered the feasibility of canceling the drug, also considering the benefit / risk ratio.

The occurrence of pregnancy should be avoided during at least 1 month after the termination of the use of the drug, given its long-lasting half-life and the presence of limited data on the effect on the fruit. According to the available data, the use of reaches in a dose of 0.5-2 mg per week about violations associated with hyperprolactineia was not accompanied by an increase in the frequency of miscarriage, premature genera, multiple pregnancies and congenital malformations.

There is no information about the release of the drug with breast milk, however, in the absence of the effect of the use of the achievement to prevent or suppress lactation, it is necessary to abandon breastfeeding. In case of violations associated with hyperprolactinemia, the reaches ® should not be prescribed mothers who do not want to stop lactation.

Application with violations of liver function

With caution, the drug is used in severe hepatic failure (lower doses are recommended).

Application in children

Contraindication: Children's and adolescent age up to 16 years (safety and efficiency is not installed).

special instructions

Before the appointment of the achievement, in order to treat violations associated with hyperprolactinemia, it is necessary to carry out a complete study of the function of the pituitary gland.

With an increase in the dose, patients must be under the supervision of a doctor in order to establish the smallest effective dose, providing the therapeutic effect. After the effective dosing mode is selected, it is recommended to carry out regular (1 time per month) determination of the concentration of prolactin in serum. Normalization of the level of prolactin is usually observed within 2-4 weeks of treatment.

After cancellation, hyperprolactinemia is usually observed, but some patients have a resistant suppression of the level of prolactin for several months. Most women have ovulatory cycles are saved for at least 6 months after the cancellation of the reaches.

Reservations ® Restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Since pregnancy may occur before the restoration of menstruation, it is recommended to carry out tests for pregnancy at least once every 4 weeks during the amenorrhea period, and after the restoration of menstruation - each time the menstruation delay is noted for more than 3 days. Women wishing to avoid pregnancy should use barrier methods of contraception during the treatment of the achievement, as well as after the cancellation of the drug before repetitions. Women who have a pregnancy should be under the supervision of a doctor for the timely identification of the symptoms of the increase in pituitary gland, since during pregnancy it is possible to increase the size of the already existing pituitary tumors.

Aestiors ® should be prescribed at lower doses to patients with severe liver failure (class with for the Child-Pugh scale), which showed long therapy with the drug. With a single application, such patients with a dose of 1 mg, an increase in AUC compared to healthy volunteers and patients with less severe liver failure was noted.

As with the use of other derivatives, after a long-term reception of Kabergolin, patients had pleural effusion / pleural fibrosis and holvulopathy. In some cases, patients received preceding therapy with ergotinine dopamine agonists. Therefore, the reaches ® should be used with caution to patients with available features and / or clinical symptoms of a heart function disorders or with such conditions as a history. After stopping the reception of the achievement in patients with a diagnosis of pleural effusion / pleural fibrosis and holvulopathy, an improvement in the symptoms was noted.

The use of Cabergolin causes drowsiness. In patients with Parkinson's disease, the use of dopamine receptor agonists can cause sudden falling asleep. In such cases it is recommended to reduce the dose of reaches or stop therapy.

Research on the use of the drug in elderly patients with disorders associated with hyperprolactinemia has not been carried out.

Use in pediatrics

The safety and efficacy of the drug in children under 16 is not installed.

Impact on the ability to driving vehicles and control mechanisms

Patients receiving the achievements ®, who have drowsiness, should be warned that it is recommended to refrain from driving a car and from performing work (for example, with mechanisms), in which reduced attention could create for them or the surrounding risk of serious damage or of death.

Structure

Description of the dosage form

White flat oblong pills with the "P" and "u" marking, separated by notch on one side and "700" with short notches on top and bottom of the number - on the other hand.

pharmachologic effect

pharmachologic effect - dofamicimetic, hypopronlactinemic.

Pharmacodynamics

Cabbergoline is a dopaminergic derivative of ergolin and is characterized by a pronounced and long-term prolactinous effect, due to the direct stimulation of D 2 -Famine receptors of lactotropic cells of the pituitary. In addition, when taking higher doses compared with doses to reduce the level of prolactin in serum Cabergolin, has a central dual defaminergic effect due to the stimulation of D 2 receptors.

The decrease in the concentration of prolactin in the blood plasma is observed within 3 hours after taking the drug and persists within 7-28 days in healthy volunteers and patients with hyperprolactinemia and until 14-21 days - in women in the postpartum period.

Cabbergoline has a strictly election action, does not affect the basal secretion of other pituitary and cortisol hormones. The prolacting effect of the drug is dose-dependent, both in terms of severity and duration of action.

The pharmacodynic effects of Cabergolin, not related to therapeutic effect, only decreased blood pressure applies. With a single reception of the drug, the maximum hypotensive effect is observed during the first 6 hours and is dose-dependent.

Pharmacokinetics

Cabbergoline is quickly absorbed from the tract, C Max in the plasma is achieved in 0.5-4 hours, the connection with blood plasma proteins is 41-42%. T 1/2 Cabergolin, estimated by the speed of excavation by the kidneys, is 63-68 hours in healthy volunteers and 79-115 hours in patients with hyperprolactinemia. Due to the long T 1/2, C SS is achieved after 4 weeks. 10 days after taking the drug in the urine and feces, about 18 and 72% of the adopted dose are found, and the proportion of unchanged drug in the urine is 2-3%. The main product of Cabergolin metabolism identified in the urine is 6-allyl-8β-carboxy-ergoline at a concentration of up to 4-6% of the adopted dose. The content in the urine of 3 additional metabolites does not exceed 3% of the adopted dose. It has been established that metabolic products have a significantly smaller effect on the suppression of the prolctin secretion compared to Kabrigolin.

Meal does not affect the suction and distribution of Cabergolin.

The testimony of the preparation is reaches ®

preventing physiological lactation after childbirth;

suppression of the already established postpartum lactation;

treatment of disorders associated with hyperprolactinemia, including amenorrhea, oligomenore, annevation, galathery;

prolactinsection adenoma pituitary gland (micro and macroprolactinoma); idiopathic hyperprolactinemia; Empty Turkish saddle syndrome in combination with hyperprolactia.

Contraindications

increased sensitivity to canbergoline or other components of the drug, as well as any breath alkaloids;

impaired heart and respiration function due to fibrous changes or the presence of such states in history;

with long-term therapy: anatomical signs of the pathology of the valve apparatus of the heart (such as the thickening of the valve sash, the narrowing of the valve lumen, the mixed pathology is a narrowing and stenosis of the valve), confirmed by echocardiographic research (ECCG), carried out before the start of therapy;

lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

application in children and adolescents under the age of 16 (safety and efficacy of the drug are not installed).

Carefully

Like other derivatives, reaches ® should be prescribed with caution in the following states and / or diseases: arterial hypertension, developed against the background of pregnancy, for example, preeclampsia or postpartum arterial hypertension (Austhesk ® is appointed only in cases where the potential benefit from the use of the drug is significantly exceeds the possible risk); severe cardiovascular diseases, Reina syndrome; peptic ulcer, gastrointestinal bleeding; Heavy liver failure (it is recommended to use lower doses); severe psychotic or cognitive disorders (including a history); Simultaneous use with drugs that have a hypotensive effect (due to the risk of orthostatic anti-arterial hypotension).

Application in pregnancy and breastfeeding

Since controlled clinical studies with the use of reaches ® in pregnant women were not conducted, the appointment of the drug during pregnancy is possible only in cases of extreme necessity, taking into account the benefit / risk ratio for a woman and the fetus.

If pregnancy has come against the background of treatment with a reachable ®, it is necessary to consider the feasibility of canceling the drug, also considering the benefit / risk ratio.

According to the available data, the use of the preparation is reaches ® at a dose of 0.5-2 mg per week about violations associated with hyperprolactinemia, was not accompanied by an increase in the frequency of miscarriage, premature genera, multiple pregnancies and congenital malformations.

There is no information about the removal of the drug with breast milk, however, in the absence of the effect of the use of reaches ® to prevent or suppress lactation, mothers should be reduced to breastfeeding. In case of violations associated with hyperprolactinemia, the reaches ® is contraindicated in patients planning breastfeeding.

Side effects

During clinical studies with the use of reaches ® to prevent physiological lactation (1 mg once) and to suppress lactation (0.25 mg every 12 hours for 2 days), side effects were marked approximately 14% of women. When applying the reaches ® for 6 months in a dose of 1-2 mg / weekly divided into 2 receptions, for the treatment of disorders associated with hyperprolactinemia, the frequency of side effects was 68%. Side effects arose mainly during the first 2 weeks of therapy and in most cases disappeared as therapy continues or a few days after the cancellation of the reaches ®. Side effects were usually transient, by severity - weakly or moderately pronounced and were dose-dependent. At least once during therapy, severe side effects were observed in 14% of patients; Due to side effects, treatment was discontinued about 3% of patients.

The most frequent side effects are presented below.

From the side of the SCC: feeling of heartbeat; Rarely - orthostatic hypotension (with long-term use of the Australia ® usually has a hypotensive effect); Perhaps asymptomatic decrease in blood pressure during the first 3-4 days after delivery (garden - at least 20 mm Hg, Dad - not less than 10 mm Hg).

From the nervous system: Dizziness / Vertigo, headache, increased fatigue, drowsiness, depression, asthenia, paresthesia, fainting, nervousness, anxiety, insomnia, violation of the concentration of attention.

From the digestive system: Nausea, vomiting, pain in the epigastric area, abdominal pain, constipation, gastritis, dyspepsia, dry oral mucosa, diarrhea, meteorism, toothache, feeling of irritation of the mucous membrane of the pharynx.

Others: Mastered, dysmenorrhea, nasal bleeding, rhinitis, blood tides to skin face, transient hemianicopsy, spasms of finger vessels and muscle cramps of the lower extremities (like other derivatives, reaches ® can have a vesseloring effect), vision, influenza-like symptoms, malaise, periorubital symptoms and peripheral edema, anorexia, acne, skin itching, pain in the joints.

With long-term therapy with the use of the drug, the reservation from the standard of standard laboratory indicators was noted rarely; In women with amenorrhea, there was a decrease in the level of HB during the first few months after the restoration of menstruation.

The following side effects associated with the reception of Cabergoline are also recorded in post-payment research: Alopecia, an increase in the activity of KFK in blood, mania, dysnae, swelling, fibrosis, liver function disorders and deviations of liver function, increased sensitivity reactions, rash, respiratory disorders, respiratory failure , Walvulopathy, pathological addiction to gaming, hypersexuality, elevated libido, aggressiveness, psychotic disorders, pericarditis, bouts of sudden fallback, decrease or increase in body weight, nasal congestion.

Interaction

There is no information on the interaction of Cabergolin and other alkaloids, therefore, the simultaneous use of these drugs during long-term therapy the preparation is not recommended.

Since Kabergolin has a therapeutic effect by direct stimulation of dopamine receptors, it cannot be prescribed simultaneously with drugs acting as dopamine antagonists (including phenothiazines, butyrofenons, thiochannels, metoclopramide), because They can weaken the action of Cabergolin, aimed at reducing the concentration of prolactin.

Like other derivatives, Cabbergoline can not be used simultaneously with macrolide antibiotics (for example erythromycin), because This can lead to an increase in the system bioavailability of Cabergolin.

Method of application and dose

Inside while eating.

Lactation prevention: 1 mg once (2 Table. 0.5 mg), on the first day after delivery.

Suppression of steady lactation: 0.25 mg (1/2 tab.) 2 times a day every 12 hours for two days (total dose - 1 mg). In order to reduce the risk of orthostatic hypotension in breastfeeding mothers, a single dose of the preparation of the reaches ® should not exceed 0.25 mg.

Treatment of disorders associated with hyperprolactinemia: The recommended initial dose is 0.5 mg per week in one reception (1 table. 0.5 mg) or in two receptions (1/2 tab. 0.5 mg, for example, on Monday and Thursday). An increase in weekly dose should be carried out gradually by 0.5 mg - with a monthly interval until the optimal therapeutic effect is achieved. The therapeutic dose is usually 1 mg per week, but may vary from 0.25 to 2 mg / week. The maximum dose for patients with hyperprolactineia should not exceed 4.5 mg per week.

Depending on tolerability, a weekly dose can be taken once or divided into 2 or more techniques per week. The division of the weekly dose into several techniques is recommended when prescribing the drug at a dose of more than 1 mg / week.

In patients with increased sensitivity to dopaminergic drugs, the likelihood of the development of side effects can be reduced by starting the treatment with the preparation of the reaches of the reaches ® at a lower dose (for example, 0.25 mg 1 time per week), followed by a gradual increase to it before reaching the therapeutic dose. To improve the portability of the drug in the occurrence of pronounced side effects, a temporary decrease in the dose is possible, followed by a more gradual increase in it (for example, an increase of 0.25 mg / weeks every 2 weeks).

Overdose

Symptoms: Development of symptoms of hyperstimulation of dopamine receptors - nausea, vomiting, dyspeptic disorders, orthostatic arterial hypotension, confusion, psychosis, hallucinations.

Treatment: Conduct auxiliary measures aimed at eliminating the drug (stomach wash), and if necessary, maintaining blood pressure. Perhaps the appointment of dopamine antagonists.

special instructions

Before the appointment of the preparation is a reaches ® in order to treat disorders associated with hyperprolactinemia, it is necessary to fully study the function of the pituitary.

In addition, an assessment of the state of the CSS, including ECOCH, should be evaluated to identify violations of the valve function of the valve apparatus flowing asymptomatic.

As with the use of other derivatives, after a long-term reception of Kabergolin, patients had pleural effusion / pleural fibrosis and holvulopathy. In some cases, patients received preceding therapy by Ergotonino dopamine agonists. Therefore, the reaches ® should not be used in patients with existing features and / or clinical symptoms of the impaired function of the heart or respiration associated with fibrous changes or such conditions as a history. An administration of the drug should be canceled in the case of the detection of signs of the appearance or deterioration of blood regurgitation, narrowing the lumen of the valves or thickening the valve sesters (see "Contraindications").

It was found that the rate of sedimentation of red blood cells increases with the development of pleural effusion or fibrosis. In case of detection of an inexplicable increase in ESO, it is recommended to perform a radiographic study of the chest. In the formulation of the diagnosis, the study of creatinine concentration in blood plasma, assessment of the renal function can also help. After discontinuation of the preparation of the preparation, the reaches ® in patients with the presence of pleural effusion / pleural fibrosis or holvulopathy there was an improvement in symptoms.

It is not known whether Cabbergoline can worsen the condition of patients with signs of blood regurgitation. Cabergoline should not be used when identifying fibrous lesions of the valve apparatus of the heart (see "Contraindications").

Fibrotic disorders can develop asymptomatic. In this regard, the state of patients receiving long-term Cabergolin therapy should be regularly monitored, and pay special attention to the following symptoms:

Pleverro-pulmonary violations: such as shortness of breath, difficulty breathing, non-cough or chest pain;

Renal failure or obstruction of vessels of ureters or abdominal organs, which may be accompanied by pain in the side or in the region of the belt and lower extremities, any swelling or soreness when touching the abdomen, which may indicate the development of retroperitoneal fibrosis;

Pericardial fibrosis and fibrosis of heart valves are often manifest with heart failure. In this regard, it is necessary to exclude fibrosis of the valve valves (and the content pericarditis) when symptoms of heart failure appear.

Monitor the patient's condition should be monitored for the development of fibrotic disorders. The first time ECOCH should be carried out in 3-6 months after the start of therapy. This study must be carried out depending on the clinical assessment of the patient's condition, paying particular attention to the symptoms described above, at least every 6-12 months of therapy.

The need for other methods of monitoring (for example, physical examination, including the auscultation of the heart, radiography, CT) is estimated individually for each patient.

With an increase in the dose, patients must be under the supervision of a doctor in order to establish the smallest effective dose, providing the therapeutic effect.

After the effective dosing mode is selected, it is recommended to hold regular (1 time per month) to determine the concentration of prolactin in serum. Normalization of prolactin concentration is usually observed within 2-4 weeks.

After canceling the preparation, hyperprolactinemia is usually observed, but some patients have a resistant suppression of prolactin concentration for several months. Most women have ovulatory cycles are preserved for at least 6 months after the abolition of the preparation is reaches ®.

Women wishing to avoid pregnancy should use barrier methods of contraception during treatment with the preparation of the reaches ®, as well as after the cancellation of the drug before repetitions of the annovation. Women who have a pregnancy should be under the supervision of a doctor for the timely identification of the symptoms of the increase in pituitary gland, since during pregnancy it is possible to increase the size of the already existing pituitary tumors.

Austhesk ® should be prescribed at lower doses to patients with severe hepatic insufficiency (class C according to childcare classification), which showed long therapy with the drug.

With a single application, such patients with a dose of 1 mg, an increase in AUC compared to healthy volunteers and patients with less severe liver failure was noted.

The use of Cabergolin causes drowsiness. In patients with Parkinson's disease, the use of dopamine receptor agonists can cause sudden falling asleep. In such cases, it is recommended to reduce the dose of the preparation of the reaches ® or stop therapy.

Research on the use of the drug in elderly patients with disorders associated with hyperprolactinemia has not been carried out. The safety and efficacy of the drug in children under 16 is not installed.

Breastfeeding or lactation continues, as a rule, before the child execution is 2 years. This is on WHO recommendations. But the longer this period in the life of a woman, the more difficult it is completed. Many mothers are trying to relieve it, taking "milk pills" reaches. But it is necessary, what are the pros and cons of drug therapy in this case, in which dosages do you need to drink this drug and who is it contraindicated?

How to drink reaches for termination of breast milk

Dosage and reception mode depends on whether lactation has already begun, whether it was established. If it is the first day after miscarriage in the late periods (when milk can also come) or childbirth, there will be enough one-time reception in the amount of 1 mg (2 tablets) at a time. Receiving reaches for the suppression of lactation will help to fully. With the established lactation, this dosage is divided into 4 receptions, 0.25 mg, that is, half the tablet 2 times a day for two days. After taking the drug, a long time remains in the blood and continues to act, suppressing the secretion of prolactin - lactation hormone.

If you doubt how to properly accept the achievements to stop breastfeeding, or milk after taking the drug in the dosages recommended in the manual continues to come to a reception to the gynecologist. Perhaps in your case you need a different dosage, or you take preparations or biologically active additives that reduce the efficiency of the achievement.

If you use bromocriptine to stop lactation, this is another popular drug to repay the formation of milk, then you can not wait for the result in a couple of days. It is recommended to receive for 2 weeks, and sometimes longer if the milk after the end of the drug intake reappears.

Do you need to make stopping the lactation of the achievement

It would seem that the drug is very effective and long-term action, but nevertheless, it is unlikely that it is unlikely to do without the fit. Milk will accumulate in glands and lactostasis will arise. However, plugging to the production of milk, so it is necessary to empty the mammary glands only in acute necessity - if there is strong heat and soreness.

If the reaches for lactation are already accepted and this happened, it will have to be imprisoned. Even through pain. Since it is not recommended to feed the child after taking the drug. It is not known what impact he will have on a children's body.

If it grinds the milk, you need to take an anesthetic. For example, "Nurofen". And before this procedure, hold the chest under warm water to speed up the influx of milk to the nipple. Some women are generally said that the plot is most comfortable under the warm shower. Try!

And after can be made on the mammary glands cold compress. It will remove pain and will not provoke the production of a new "party" of milk.

Application of the drug Austility: pros and cons

Since this is a rather serious medicinal product, with a number of side effects and contraindications, it is necessary to drink it only in extreme cases, if it is impossible to stop the lactation in a different time. For example, a medical support is suitable for women who have had dead children or miscarriage on a large period of pregnancy, if HIV has been detected, tuberculosis or other dangerous disease that can be converted to a child with milk.

Contraindications for stopping lactation as a reaches:

age under 16 years old;
the intolerance of Cabergolin and the alkaloids of the ardor.

With caution and in the presence of good readings, reception is possible in the following states:

heart defects;
rectal bleeding of unknown origin;
arterial hypertension;
severe liver failure;
asthma;

The last item will certainly cause questions. How then to stop breastfeeding with the help of the achievement, if it is contraindicated with lactation? This contraindication is relevant only in some cases. For example, a doctor may assign this medicine to a woman with a completely different goal than getting rid of lactation. After all, the prolctin secretion inhibitors are accepted in some diseases, for example, the pituitary microense. In this case, the woman should decide what is more important for it - to treat the main disease or feed the baby.

Pills from lactation Australia can also cause the following health problems (temporary, before the removal of the drug from the body):

fainting;
sharp decline in pressure;
feeling of nasal congestion;
dizziness;
pain in the stomach;
constipation;
convulsions;
drowsiness and fast fatigue;
nose bleed.

But all this is quite rare side effects, if the reacted tablets for stopping lactation are accepted in recommended dosages and a short time. However, it is necessary to take into account the fact that the reception of the drug is a reason to temporarily abandon travel behind the wheel of vehicles and work requiring the concentration of attention.

As you can see, there are quite a lot of nuances. If possible, the cessation of lactation with drugs is better to replace the natural way to complete breastfeeding. Or use non-drug tools to reduce lactation.

It is not always possible to complete breastfeeding natural way: the increased content of prolactin in the body of a woman gives a lot of trouble. Sometimes for some medical prescriptions, women are forced to stop breastfeeding immediately after delivery. If there is a need for a compulsory stop or suppressing the established lactation, the doctor may assign a reception of the achievement.

Principle of operation of reaches

The achievement is designed for reception by women after childbirth, which must be prevented by the production of milk, as well as for women who are successfully fed to the breast, but want to complete the lactation. The drug is produced in the form of oblong white tablets with a transverse strip for simplicity of division on the necessary doses. One tablet can be divided into two receptions.

The active substance is reached - Kabrgolin affects the lactotrophic pituitary cells responsible for the production of prolactin, thereby suppressing its secretion. Cabbergoline is quickly absorbed in the walls of the gastrointestinal tract. After receiving the prescribed dose, the decrease in the concentration of hormone in the blood occurs within 3 hours. Patients with a diagnosis of prolactinemia noted a pronounced therapeutic effect from 1 to 4 weeks. In women who took the drug after childbirth, the reduced content of the lactogenic hormone remains 2-3 weeks. During therapy, it should not be renewed to breastfeeding to the full withdrawal of the active substance from the organism (up to 5 days).

Features of the correct dosage

The reaches tablet contains:

cabergoline 0.5 mg (active ingredient);
amino acid leucine and lactose (auxiliary components).

Indications for the preparation of the drug:

completing the established lactation;
after an abortion for the forced suppression of the secretion of prolactin;
treatment of infertility, lack of menstruation, hyperprolactinemia.

It should not be prescribed a drug yourself. It is necessary to consult with the doctor.

The necessary doses are appointed by a doctor taking into account the reasons why suppressing milk production in breast glands is required:

to prevent the formation of milk in breast glands, within 24 hours after childbirth (abortion), if a woman has no opportunity or desire to start breastfeeding, a one-time reception of 1 mg of substance (2 tablets) is prescribed;
to complete the steady lactation, 1 mg (2 tablets) is received for 2 days. The tablet is divided into 2 equal parts of 0.25 mg and taken in the morning and in the evening with a break at 12 o'clock
for the treatment of over-allocation of hormone prolactin, a weekly graph of drug admission is established in strictly reserved days. Days are determined depending on the rules of treatment appointed by the doctor. A single dose takes 1 time per week (let's say on Mondays). If the dose is divided into 2 receptions, choose another schedule (for example, every Tuesday and Friday). To begin with, the reception is prescribed 0.25-0.5 mg of the drug. In the absence of a negative impact on the body, the dosage can be increased by 0.5 mg monthly. On average, 2 mg of substance per week is enough to obtain good results to the patient. The maximum allowed weekly volume should not exceed 4.5 mg. As soon as the optimal dose for treatment is found, it is necessary to regularly check the concentration of the lactogenic hormone in the blood. With a positive medical effect, the level of prolactin is normalized in 2-4 weeks.

Contraindications for use and side effects

Since the reaction of the achievement has a direct impact on the hormonal background of women, therapy should be carried out with caution. There is also a number of contraindications to which include:

increased susceptibility to the active substance Cabergolin, derivatives of the ardor;
liver, renal failure;
some diseases of the gastrointestinal tract and cardiovascular system;
mental disorders, postpartum psychosis;
pregnancy, breastfeeding;
patients up to 16 years (due to lack of research for this age group).

In case of overdose by the drug, vomiting is possible, cramps in the legs, hypotension, hallucinations

During the admission of prescribed doses, the patient does not feel significant discomfort, the effects of Cabergoline has moderate severity. Particular effects can manifest itself in sleep impaired, reduce blood pressure, pain in the abdomen, appearance of dizziness, nausea. In the treatment of hyperprolactinemia, painful sensations in the chest can be added, body weakness, embarrassed intestinal emptying, inflammation of the gastric mucous membrane, heat tilt to face. If pain symptoms do not pass independently, the dosage decrease is recommended. After cancellation, 1-2 days are required to stop negative impact on the body.

Analogs of the drug

Since the relative speed of the medicinal substance is noted, we can talk about the effectiveness of the drug. Despite the fact that the instructions indicate a good tolerance of possible side effects, nervous, cardiovascular, patient digestive systems are negative. There are analogues that have in its composition components aimed at suppressing the production of lactogenic hormone in the pituitary. Side effects also affect the well-being of a woman taking medicine. The main difference between the drugs-analogues of the achievement is lower cost.

Table: Preparations-analogues of the reaches

Name	Active substance	Side effects
Bromocriptine	bromine	Good tolerability, sometimes possible: swelling of mucous membranes; nausea, vomiting; lower pressure; constipation; the whims of the fingers and legs during supercooling.
Agalates.	cabbergoline	Sleep disorders; hallucinations; depression; headache; fainting; tides; feeling of heartbeat; stomach ache; vomiting; constipation; dyspnea; skin rashes, etc.
Bergolak	cabbergoline	Heart palpitations; spasms of finger vessels; dizziness; increased fatigue, drowsiness; mania; fainting; constipation, gastritis, dyspepsia; nose bleed; violation of liver functions, etc.
Bromomfora	bromomfora	Drowsiness; inhibition; dyspeptic phenomena.

Reviews

It turned out that I had to stop lactation on the 8th months of feeding the kid on the 2nd reasons: the milk became tasteless and bitter, the child simply does not want to drink him; And the second reason - I had to constantly join, and the time is not so much free. Given all these factors, I turned to the gynecologist, which wrote to me the achievement, drink 1/2 tablets 2 times a day 2 days, not to join and limit yourself in fluid consumption.
The process of taking tablets in all its glory:
The first drank at 8 pm, did not grit, everything was fine in the morning, the milk arrived, but the chest was still soft. Further at 8 am another half of the tablet, here it was about 30-40 minutes after 30-40 minutes ... It was terribly terribly, the good of the husband was at home, sat with the child, and I took me to the MORFOR. The hour slept, the chest was separated, I could not at all from the bed to stand up and put the hands (I was also told not to join). A few hours later I simply "existed" and reading once again reviews and forums decided to be facilitated (I really did not want to get lactostasis or mastitis). Ltd., I felt like a person). The rest of the time I also stacked the chest so that it did not become stone, and after the next tablets I was as bad and I was layer.
Result:
Gradually, the milk began to arrive less and less, 3 weeks passed and I can say that the milk almost completely blocked. Of course, I would like everything for 3 days, but apparently the "dairy" moms do not see this. For me, it is better to suffer 2 days, lie down the corpse than to tangle and earn a sore. 1 point takes off only because of the sides.

The issue of cessation of breastfeeding is often concerned about young mothers. And you do not need to condemn me for it, I had to interrupt the GW because of health problems, or rather because of the reception of antibiotics. The main thing to choose a simple and safe way to not harm your body. It is good that now there is such a modern way - a tablet for stopping lactation is a reaches based on Cabergolin. Its action is based on the fact that it suppresses the production of a hormone prolactin in the pituitary gland, and thus lactation stops. This drug was advised to me in the pharmacy, it is of course it is not cheap, but it eliminates milk for 2-3 days. I took it on ½ tablet 2 times a day (every 12 hours), and for 2 days. On the first day of reception, milk was still abide, accounted for a little to relieve, there was no strong tide on the second day. Literally after 3-4 days, milk completely passed. I did not cause any side effects this drug, no headache or nausea. I also heard that the achievement contributes to conception, but I can't argue. In any case, every woman herself decides which way to interrupt lactation, but I am for a modern and affordable method. I advise you to achieve

Completion of breastfeeding occurs in each mother individually, in different times and for various reasons. The most secure and easy for mom and child The method is a natural gradual refusal to the GW with an increase in the supplies. However, it is far from every woman, and often lactation has to be interrupted by artificially on medical testimony (diseases, antibiotics) or in life circumstances (the need to go to work). In such cases, the doctor may assign tablets to suppress lactation, for example, the achievek.

We will analyze in detail when they use the achievements to stop lactation, how to apply it correctly and what consequences should be feared. We also collected the most interesting feedback for you (both negative and positive) from the expanses of the Internet. It is also important to know that this medication has a huge number of side effects, in connection with which we also discuss how it can be safely complete with a sage and gradually reduce feeds.

Brief description of the drug according to the instructions

The reaches refers to the group of inhibitors (suppressors) of the secretion of the hormone of prolactin, the second name of which is a lactogenic hormone - indicates its main purpose: stimulation of the development of dairy glasses, an increase in the number of ducts in them, forming the poles first, and then milk. Inhibiting prolactin, the achievement opposes lactation, gradually stopping it.

The drug is produced in the form of white tablets with a notch for the convenience of dividing, packaged in vials of 2 (approximate price - about 690 rubles) and 8 (about 1,700 rubles) tablets. The active substance of the achievement is canbergoline, auxiliary only two: lactose anhydrous (milk sugar) and leucine (one of the essential amino acids).

The drug is released only by prescription.

Indications for application

In accordance with the instructions, the reaches are assigned at:

the need to fully prevent postpartum lactation;
the need to stop already established lactation;
prolactinsection adenomas of pituitary
"empty" syndrome of the Turkish saddle together with hyperprolactinemia;
idiopathic hyperprolactinemia;
other disorders associated with hyperprolactineia (Galactere, Annovulation, Amenorrhea, oligomenorrhea).

Contraindications

Although this drug is not in the full sense of the word hormonal, it significantly changes the hormonal background of women. Stimulation of the neurotransmitter of dopamine, overwhelming prolactin, is a serious intervention in the physiology of a person, in connection with which the achievement has some contraindications.

In addition to accounting by major contraindications, negative consequences can cause the use of reaches with:

severe form of liver failure;
peptic ulcers and gastric or intestinal bleeding;
severe diseases of the cardiovascular system, Raino disease;
violation of normal respiration and heart work due to fibrous changes (even in the past);
severe cognitive and mental disorders;
the arterial hypertension used during pregnancy - both preeclampsia and postpartum arterial hypertension (the achievers can only be taken only when the benefit of treatment with them significantly exceeds the risk of possible negative consequences).

Operating principle

After receiving the reaches of Cabergolin, in the shortest possible time is absorbed by the intestinal walls and enters the blood, reaching its maximum concentration after 0.5-4 hours. Meal does not have any influence on the assimilation and concentration of Cabergolin. Cabergoline causes the response of dopamine receptors in the lactotropic cells of the pituitary gland and increase the level of dopamine - neurotiator, which strongly slows down the secretion of prolactin.

The level of prolactin begins to decline 3 hours after taking a tablet and remains unchanged quite a long time: healthy women and hyperprolactinemia suffering from 7 to 28 days, in women during breastfeeding period - from 14 to 21 days. There is a direct relationship between the dose of the drug and the duration / severity of the reduction in the level of prolactin.

Cabergoline acts selectively and does not affect the synthesis of other hormones, but it can reduce blood pressure. After a single use of the drug, hell remains reduced for the first 6 hours, and the reduction force depends on the dose.

If you need to stop breastfeeding, it is necessary only for a while, it is possible to restore lactation only after fully eliminating the reasons forced it to interrupt. It should be remembered that the longer the drug was taken, the harder it is to restore the production of milk.

Dosage

The dosage is determined by the reason for the use of the achievement. Against the continuation of the already established lactation take half a tablet twice a day for two days (i.e., in the total amount of 1 mg). At the risk of development of the hypotension, a single dose should not exceed 0.25 mg (half of the tablet).

To prevent yet lactation, a single dose of 1 mg (2 tablets) is taken to the next day after childbirth.

Against the hyperprolactinemia (over-secretion of prolactin), drink 1 tablet per week or make a reception to two approaches - for example, half the chalks on Monday and half the chalk tracks on Thursday. Raise a weekly dose of reaches should be carefully 0.5 mg times a month until the required therapeutic effect is achieved. The maximum dose for patients with hyperprolactinemia is 9 tablets per week (4.5 mg).

Since the portability of the drug in each woman is individual, the doctor may advise drinking one dose into several techniques. It is usually recommended that if the dose exceeds 2 tablets per week.

Overviews are observed:

vomiting;
nausea;
ortostatic hypotension (sharp decrease in blood pressure);
dyspeptic disorders (stomach pain, difficult digestion);
hallucinations, psychosis, confused.

Symptoms of overdose are eliminated by keeping blood pressure, washing the stomach. Sometimes a dopamine antagonists are required.

Side effects

They are found at a significant percentage of women. So, in the course of studies with a single dose of 1 mg (to prevent lactation) and a dose of 0.25 mg twice a day for two days (for lactation suppression), side effects were observed in 14% of the subjects. With an increase in the study of the study until six months (2-4 tablets weekly), 68% of women began to disturb the side effects.

The list of basic side effects is large and can be divided into four groups:

From the nervous system: headaches, drowsiness, asthenia, paresthesia, dizziness, severe fatigue, fainting, depression.
From the digestive system: gastritis, dyspepsia, pain in the abdomen and / or epigastric area, nausea, vomiting, constipation.
From the side of the cardiovascular system: decreased blood pressure during the first 3-4 days after delivery, orthostatic hypotension.
Others: Foot cramps (due to vasoconstrictor effect), spasms of blood vessels in the fingers, blood tides to face, nasal bleeding, hemianopsy, medianity, alopecia, holvulopathy, dysnae, fibrosis, swelling, liver function, rash, respiratory failure, other respiratory disorders , improving the level of creatinophosphokinease, mania.

Against the background of such an impressive list of side effects should not be continued to feed the child when receiving the drug, so as not to expose the faster organism at unemployed risk. BUT The best option will be an attempt to overcome the baby from the breast with natural and safe methods.

Mom's reviews about reaches

Natalia: "In the evening she took half the chalk. Today I almost lost consciousness. The state is terrible, the pressure fell to 90 to 53, the temperature is about 38, nausea, difficulty breathing.

Oksana: "Saw a reaches on the instructions - four times a quarter of a pill. Milk has become less, but not at all. Now the 10th day after the start of the course. Milk still has and disappear, it seems not going to ".

Catherine: "Alas, the" miraculous "effect of the tablets will grow strongly. While I drank them, milk, of course, was smaller, but it did not disappear anywhere. Price of tablets at the same time cosmic. When I was advised by the achievements in a pharmacy, I first thought that the milk should be a gap because of the price of him. The same bromocophora is much cheaper, and the result was visible on the second day of the course. "

Lyudmila: "I was sold even to me without a recipe, but about the reception still it is worth consulted with a doctor. Saw sam 3 weeks after childbirth. There were almost no pauses: the pressure slightly decreased, and it was recovered several days later. Milk stacked, and completely left the week after a half. "

Svetlana: "Side effects he has so much as possible in the hospital. I, fortunately, carried me, but my sister was bad. I had to stop breastfeeding. Ensure: For several days, milk jumped, and after two weeks it was still a little more developed. For the planned ending of the GW, the achievek is not suitable, it is better to choose less risky options. "

Summarizing these and a few more tens of reviews, suggests the following conclusion: the achievement acts on every woman extremely individual. Someone's side effects are limited to a slight decrease in blood pressure, other consequences reach a pre-industrous state. The price of the drug does not correspond to its effectiveness and significantly exceeds more secure analogs.

Relief from GW by non-drug methods

With an ideal scenario, self-dedication occurs - a voluntary refusal of a child from the chest, most often the coming age of 2-3 years.

However, in most cases, even on the occurrence of cherished age, the attachment of the child to breastfeeding does not weaken, and then the mother can come to the rescue, which are not associated with the reception of prolactin inhibitors of the GW interruption methods.

Video consultant for HB: how and when to teach a child

We offer you a wonderful video of Nina Zheninko.

Instructions for smooth excavation

First of all, you should try the following instructions tested by millions of women:

One of the feedings should be replaced with a mixture of a bottle, other food or released milk. If the child flatly refuses this food, try to feed the baby can father or any of the familiar child of relatives. Baby must realize that in addition to the chest there is another food. The first such feeding cannot be carried out immediately after sleep or before it.
Three days later, you can replace another meal. A few days later, one more, gradually changing all day feeding on the "adult" food.
After that, you can replace meals, adjacent to the sleep of the child: first only day or night, then the remaining. It is better to start with the replacement of night feedings, because at night the baby is easier to go to bed. The break from the breast day can provoke a complete refusal of a child from day sleep, which, according to pediatricians, is unacceptable.
If the child sleeps near the mother, she follows immediately after awakening to rise: the usual for the morning "five more minutes" will give a child time to make a breast.

Speaking about another concomitant problem - the ongoing production of milk, it is worth listening to several useful advice of the famous children's doctor E.O. Komarovsky. To reduce the volume of milk it follows:

actively play sports;
eliminate complaining;
reduce sucking time;
temporarily drink less fluid;
monitor the lack of products in the diet stimulating lactation.

There are also a number of people's ways to suppress lactation. Safe alternatives to the reaches and such drugs can be infusions of basilica, lingers, mints, parsley, tocheries and sage.

Herbs to complete breastfeeding

Sage is considered the most efficient natural means to complete the GW. The recipe rate of the brave is simple: two tablespoons of the sage must be pouring a glass of boiling water, insist, skip through the siete and drink several sips three times a day. An even more effective use of the alcohol tincture of sage, its extract and finally essential oil. When using the latter, the volume of milk is significantly reduced after 3-4 days.

If it should be remembered that it is simply because to interrupt breastfeeding because the child has marks or a half, there is no need. The myth that after the year GV milk is deprived of most of its useful properties, was debunk by the research of the World Health Organization. WHO recommends continuing to feed the child with breasts at least to two years, and if it does not cause inconvenience, neither mother nor her choa, then longer.

Conclusion

Aestopera - far from the safest drug with a lot of side effects and unpredictable consequences. Its use is justified only if the need for an emergency suppression of lactation and, moreover, should be carried out only on the prescription of the doctor and in accordance with the instructions. The planned interruption of the GW is better to spend with the help of softer methods: vegetable infusions, decoctions and lifestyle adjustments.