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Dostinex lactation tablets. The drug "Dostinex": reviews, properties, indications and contraindications for use. Application during pregnancy and lactation

Quite often, women are faced with various diseases and disorders of the reproductive system, which occur against the background of hormonal disruptions. In addition, in some cases, it is required to stop the lactation process. In both cases, Dostinex will be effective. Reviews about him are mostly positive. Therefore, doctors often prescribe them to patients with certain disorders.

The drug "Dostinex": composition and form of release

The medicine is available in the form of white oblong tablets, which are contained in dark glass vials. Such a bottle can contain either two or eight tablets. The lid should be aluminum and have a plastic insert with porous paper and a drying agent. Each tablet contains 0.5 mg of the main active substance cabergoline. This ergoline derivative acts as a dopamine receptor agonist. Anhydrous lactose and leucine are used as auxiliary components in the production.

The main pharmacological properties of the drug

Quite a few patients are prescribed Dostinex today. The doctors' comments on this drug are extremely positive. But how does it work? It should be noted that the active substance of the drug is rapidly absorbed by the wall of the gastrointestinal tract, regardless of food intake. Approximately 41-42% of cabergoline binds to blood plasma proteins. Its maximum concentration is observed 1-4 hours after administration. Cabergoline directly stimulates the D2 receptors of lactotropic cells in the pituitary gland, while not affecting the basal secretion of other hormones in the hypothalamic-pituitary system. It should be noted that the effect of the drug persists for 1-3 weeks after administration in patients with hyperprolactinemia, as well as in healthy volunteers who participated in the study. In women in the postpartum period, the therapeutic effect lasts for 2-3 weeks, which is quite enough to completely interrupt lactation.

By the way, the effect and its duration directly depend on the dose of the drug, as well as the intensity of adverse reactions. In most women, the treatment was associated with a decrease in blood pressure, but this effect disappeared 5-6 hours after taking the pill. The body is completely cleared of the drug approximately four weeks after the start of administration. The drug and its metabolites are excreted along with urine and feces.

Indications for use

Most often, this medicine is used in order to suppress or prevent physiological lactation, which inevitably occurs after childbirth. In fact, there are many conditions in which a mother simply cannot breastfeed her baby. In such cases, Dostinex is simply irreplaceable. In addition, an indication for taking the drug is hyperprolactinemia. After all, such a disorder is associated with the occurrence of problems such as galactorrhea, amenorrhea, oligomenorrhea and anovulation. The drug is also used to treat pituitary adenoma, which is accompanied by stimulation of prolactin synthesis. Indication for use is the so-called empty Turkish saddle syndrome.

Instructions for use

In no case should you use the drug yourself. To begin with, it is imperative to consult a doctor - only a specialist can prescribe Dostinex lactation pills, as well as correctly determine the daily dose and regimen of the drug. The amount of medication directly depends on what problem needs to be eliminated. If it is necessary to prevent the appearance of lactation, then a single dose of the medication immediately after childbirth will be sufficient - the dose in this case is 1 mg. In the event that lactation has already begun, then patients are advised to take 0.25 mg every twelve hours for two days. The treatment regimen for hyperprolactinemia looks completely different. Women with a similar disease are advised to take the medicine 1-2 times a week. The initial dose should not exceed 0.5 mg at a time. With a positive reaction, the amount of the drug can be increased to 4.5 mg per week, although this depends on the tolerance of the drug and the presence of side effects. With continuous treatment with hormonal drugs, it is recommended to do tests to determine the level of prolactin every two weeks. As a rule, after discontinuation of therapy, hyperprolactinemia returns, but in some women, the therapeutic effect can last up to six months.

It is best to take pills with meals, as this reduces the intensity of side effects. Although the medicine can be used at any time of the day.

Contraindications to therapy

Of course, this drug has a number of contraindications. It should be noted right away that it is by no means used to treat patients with hypersensitivity to any ergot alkaloids. In addition, it is not recommended for girls under 16 years of age, as well as for women during pregnancy (only if the expected benefit outweighs the possible risk). Contraindications include some diseases, including peptic ulcer, severe liver failure, gastrointestinal bleeding, Raynaud's syndrome, and some diseases of the cardiovascular system. The drug is not prescribed to patients with arterial hypertension, fibrotic changes in the tissues of the heart and respiratory organs. It is not recommended to take Dostinex together with antihypertensive drugs.

Are there any side effects?

Like all hormonal medicines, this medicine can cause a number of side effects. For example, many patients complain of a drop in blood pressure. The consequences of treatment can also include increased heart rate, drowsiness, dizziness, headaches, fatigue, asthenia, depression, fainting. Many patients are interested in another important point - Dostinex and weight. After all, it's not a secret for anyone that taking hormones is often associated with a quick set of extra pounds. However, clinical studies have not found such a link. But the drug sometimes still affects the work of the digestive tract, causing nausea, vomiting, constipation, gastritis, abdominal pain, dyspepsia. Potential side effects can also include muscle cramps, vasospasm of the fingers, nosebleeds, flushing of the face, swelling, baldness, decreased hemoglobin levels in the blood, as well as the appearance of a rash and respiratory problems. In the event of severe adverse reactions, you should consult a doctor. In some cases, it is advisable to stop taking the drug, but sometimes it will be enough just to reduce a single dose.

The main symptoms of an overdose

Overdose of this medication can be dangerous to the health and life of patients. Taking too much medication is usually accompanied by dizziness, confusion, and sometimes hallucinations. In addition, various digestive disorders can occur, including nausea and vomiting. In some cases, orthostatic hypotension is observed. In any case, it is best to rush a patient in this condition to the hospital. As a rule, for a start, measures are taken in order to rid the body of the drug that has not yet had time to be absorbed - most often the stomach is washed. In addition, blood pressure medications and dopamine antagonists are prescribed to patients.

The drug "Dostinex": patient reviews

In fact, many doctors prescribe this particular drug. After all, if it is necessary to correct the level of hormones or stop lactation, then sometimes the only solution is Dostinex. Most of the reviews about him are positive. Indeed, the effect of it appears quickly, especially when it comes to stopping breastfeeding. In a few days, you can completely stop lactation - this is noted by almost all patients. However, the likelihood of developing side effects is high. Many women complain that a few hours after taking the drug they feel weakness, nausea, and dizziness. On the other hand, all adverse reactions disappear over time. The advantages of the drug include the fact that it does not need to be taken often. As for the disadvantages, they include not only a large number of contraindications and side effects, but also the relatively high cost of the drug.

(DOSTINEX ®)

Registration number: P N013905 / 01-210709

Trade name of the drug: DOSTINEX ®

International non-proprietary name (INN): cabergoline

Dosage form: pills

Description: white flat oblong tablets marked “P” and “U”, separated by a notch on one side and “700” with short notches on the top and bottom of the number on the other side.

Composition: Each tablet contains:
Active substance: cabergoline 0.5 mg;
Excipients: leucine, lactose anhydrous.

Description:

Pharmacotherapeutic group: dopamine receptor agonist
ATX code G02CB03

Pharmacological properties
Pharmacodynamics
Cabergoline is a dopaminergic derivative of ergoline and is characterized by a pronounced and long-term prolactin-lowering effect due to direct stimulation of D 2 -dopamine receptors of pituitary lactotropic cells. In addition, when taken at higher doses than to reduce serum prolactin levels, cabergoline has a central dopaminergic effect due to stimulation of D 2 receptors.
A decrease in the concentration of prolactin in blood plasma is observed within 3 hours after taking the drug and persists for 7-28 days in healthy volunteers and patients with hyperprolactinemia, and up to 14-21 days in women in the postpartum period. Cabergoline has a strictly selective effect, does not affect the basal secretion of other pituitary hormones and cortisol. The prolactin-lowering effect of the drug is dose-dependent both in terms of severity and duration of action.
The pharmacodynamic effects of cabergoline, which are not associated with a therapeutic effect, include only a decrease in blood pressure (BP). With a single dose of the drug, the maximum hypotensive effect is observed within the first 6 hours and is dose-dependent.

Pharmacokinetics
Cabergoline is rapidly absorbed from the gastrointestinal tract, the maximum plasma concentration is reached after 0.5-4 hours, the connection with blood plasma proteins is 41-42%. The half-life of cabergoline, assessed by the rate of excretion in the urine, is 63-68 hours in healthy volunteers and 79-115 hours in patients with hyperprolactinemia. Due to the long half-life, the state of equilibrium concentration is reached after 4 weeks. 10 days after taking the drug in the urine and feces, about 18% and 72% of the dose taken, respectively, are found, and the proportion of the unchanged drug in the urine is 2-3%.
The main metabolic product of cabergoline, identified in urine, is 6-allyl-8ß-carboxy-ergoline at a concentration of up to 4-6% of the dose taken. The content of 3 additional metabolites in urine does not exceed 3% of the dose taken. It has been found that metabolic products have a significantly lower effect in suppressing the secretion of prolactin in comparison with cabergoline.
Food intake does not affect the absorption and distribution of cabergoline.

Indications for use

• 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" Turkish saddle in combination with hyperprolactinemia.

Contraindications

• Hypersensitivity to cabergoline or other components of the drug, as well as to any ergot alkaloids.
• The safety and efficacy of the drug in children under 16 years of age has not been established.

Carefully
Like other ergot derivatives, Dostinex ® should be prescribed with caution in the following conditions and / or diseases:

• arterial hypertension that developed during pregnancy, for example, preeclampsia or postpartum arterial hypertension (Dostinex ® is prescribed only in cases where the potential benefit of using the drug significantly outweighs the possible risk);
• severe cardiovascular disease, Raynaud's syndrome;
• peptic ulcer, gastrointestinal bleeding;
• severe hepatic impairment (lower doses are recommended);
• severe psychotic or cognitive impairment (including history);
• symptoms of dysfunction of the heart and respiration due to fibrotic changes or a history of such conditions;
• simultaneous use with drugs that have an antihypertensive effect (due to the risk of orthostatic hypotension).

Pregnancy and lactation
Since there have been no controlled clinical trials with Dostinex® in pregnant women, prescribing the drug during pregnancy is possible only in cases of extreme necessity, taking into account the benefit / risk ratio for the woman and the fetus.
If pregnancy occurs during treatment with Dostinex ®, the advisability of discontinuing the drug should be considered, also taking into account the benefit / risk ratio.
The onset of pregnancy should be avoided for at least one month after discontinuation of Dostinex®, given the long half-life of the drug and the availability of limited data on its effect on the fetus (although, according to available data, the use of Dostinex® at a dose of 0.5-2 mg per week for disorders associated with hyperprolactinemia, was not accompanied by an increase in the frequency of miscarriages, premature births, multiple pregnancies and congenital malformations).
There is no information on the elimination of the drug in breast milk, however, in the absence of the effect of using Dostinex ® to prevent or suppress lactation, mothers should refuse breastfeeding. In case of disorders associated with hyperprolactinemia, Dostinex ® should not be prescribed to mothers wishing to breastfeed.

Method of administration and dosage
Inside, during meals.
Preventing lactation: 1 mg once (2 tablets of 0.5 mg), on the first day after childbirth.
Suppression of established lactation: 0.25 mg (1/2 tablet) twice a day every 12 hours for two days (total dose is 1 mg). In order to reduce the risk of orthostatic hypotension in breastfeeding mothers, a single dose of Dostinex® should not exceed 0.25 mg.
Treatment of disorders associated with hyperprolactinemia: The recommended starting dose is 0.5 mg per week in one dose (1 tablet 0.5 mg) or in two divided doses (1/2 tablet 0.5 mg, for example, on Monday and Thursday). The increase in the weekly dose should be carried out gradually - by 0.5 mg at monthly intervals until the optimal therapeutic effect is achieved. The therapeutic dose is usually 1 mg per week, but can range from 0.25 to 2 mg per week. The maximum dose for patients with hyperprolactinemia should not exceed 4.5 mg per week.
Depending on the tolerance, the weekly dose can be taken once or divided into 2 or more doses per week. The division of the weekly dose into several doses is recommended when prescribing the drug at a dose of more than 1 mg per week.
In patients with hypersensitivity to dopaminergic drugs, the likelihood of side effects can be reduced by starting Dostinex ® therapy at a lower dose (for example, 0.25 mg once a week), followed by a gradual increase until the therapeutic dose is reached. To improve the tolerability of the drug in the event of severe 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 per week every two weeks).

Side effect
In clinical trials with Dostinex ® for prevent physiological lactation(1 mg once) and for suppression of lactation(0.25 mg every 12 hours for 2 days) side effects were observed in approximately 14% of women. When using Dostinex ® for 6 months at a dose of 1-2 mg per week, divided into 2 doses, for the treatment of disorders associated with hyperprolactinemia, the incidence of side effects was 68%. Side effects occurred mainly during the first 2 weeks of therapy and in most cases disappeared as therapy continued or a few days after Dostinex® was discontinued. Side effects were usually transient, mild or moderate in severity and dose-dependent. At least once during therapy, severe side effects were observed in 14% of patients; due to side effects, treatment was discontinued in about 3% of patients.
The most common side effects are presented below:
On the part of the cardiovascular system: heartbeat; rarely - orthostatic hypotension (with prolonged use, Dostinex ® usually has a hypotensive effect); possible asymptomatic decrease in blood pressure during the first 3-4 days after childbirth (systolic - more than 20 mm Hg, diastolic - more than 10 mm Hg).
From the nervous system: dizziness / vertigo, headache, increased fatigue, drowsiness, depression, asthenia, paresthesia, fainting.
From the digestive system: nausea, vomiting, epigastric pain, abdominal pain, constipation, gastritis, dyspepsia.
Other: mastodynia, epistaxis, "hot flushes" of blood to the skin of the face, transient hemianopsia, vasospasm of the fingers and muscle cramps of the lower extremities (like other ergot derivatives, Dostinex ® can have a vasoconstrictor effect).
With prolonged therapy with Dostinex ®, deviation from the norm of standard laboratory parameters was rarely observed; women with amenorrhea experienced a decrease in hemoglobin levels during the first few months after menstruation was restored.
In a post-marketing study, the following side effects associated with taking cabergoline were also recorded: alopecia, increased creatinine phosphokinase activity in the blood, mania, dyspnea, edema, fibrosis, abnormal liver function and abnormal liver function indicators, hypersensitivity reactions, rash, respiratory disorders, respiratory failure, valvulopathy.

Overdose
Overdose symptoms: nausea, vomiting, dyspeptic disorders, orthostatic hypotension, confusion, psychosis, hallucinations.
In case of an overdose, auxiliary measures should be taken to remove the drug (gastric lavage) and, if necessary, maintain blood pressure. Prescription of dopamine antagonists is possible.

Interaction with other medicinal products
There is no information on the interaction of cabergoline and other ergot alkaloids, therefore, the simultaneous use of these drugs during long-term therapy with Dostinex ® is not recommended.
Since Dostinex ® has a therapeutic effect by direct stimulation of dopamine receptors, it cannot be administered simultaneously with drugs acting as dopamine antagonists (phenothiazines, butyrophenones, thioxanthenes, metoclopramide, etc.), because they can weaken the effect of Dostinex ® in reducing prolactin levels.
Like other ergot derivatives, Dostinex ® cannot be used concurrently with macrolide antibiotics (for example, erythromycin), because this can lead to an increase in the systemic bioavailability of cabergoline.

special instructions
Before prescribing Dostinex ® for the treatment of disorders associated with hyperprolactinemia, it is necessary to conduct a complete study of the pituitary gland function. When increasing the dose, patients should be under the supervision of a physician in order to establish the lowest effective dose that provides a therapeutic effect.
After an effective dosing regimen has been selected, it is recommended to carry out a regular (once a month) determination of the concentration of prolactin in the blood serum. Normalization of prolactin levels is usually observed within 2-4 weeks of treatment.
After discontinuation of Dostinex ®, a relapse of hyperprolactinemia is usually observed, however, in some patients there is a persistent suppression of prolactin levels for several months. In most women, ovulatory cycles persist for at least 6 months after discontinuation of Dostinex®.
Dostinex ® restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Since pregnancy can occur before menstruation is restored, it is recommended that pregnancy tests be performed at least once every 4 weeks during the amenorrhea period, and after menstruation is restored, whenever menstruation is delayed by more than 3 days. Women wishing to avoid pregnancy should use barrier methods of contraception during treatment with Dostinex ®, as well as after discontinuation of the drug 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, an increase in the size of already existing pituitary tumors is possible.
Dostinex ® should be prescribed in lower doses to patients with severe hepatic impairment (class C according to Child-Pugh classification), for whom long-term drug therapy is indicated. With a single dose of 1 mg to such patients, there was an increase in AUC (area under the concentration / time curve) compared with healthy volunteers and patients with less severe hepatic impairment.
As with other ergot derivatives, patients with long-term administration of cabergoline have had pleural effusion / pleural fibrosis and valvulopathy. In some cases, patients received prior therapy with ergotinine dopamine agonists. Therefore, Dostinex ® should be used with caution in patients with existing signs and / or clinical symptoms of cardiac dysfunction or with a history of such conditions. After discontinuation of Dostinex®, patients diagnosed with pleural effusion / pleural fibrosis and valvulopathy showed improvement in symptoms.
The use of cabergoline causes drowsiness. In patients with Parkinson's disease, the use of dopamine receptor agonists may induce sudden sleep. In such cases, it is recommended to reduce the dose of Dostinex ® or to stop the therapy. Studies on the use of the drug in elderly patients with disorders associated with hyperprolactinemia have not been conducted. The safety and efficacy of the drug in children under 16 years of age has not been established.

Influence on the ability to drive a car and other mechanisms
Patients taking Dostinex ® who experience drowsiness should be warned that they are advised to refrain from driving a car and from performing work (for example, with machinery), in which reduced attention could create for them or those around them the risk of serious injury or of death.

Release form
0.5 mg tablets;
2 or 8 tablets in a type I amber glass vial, closed with a screw-on aluminum cap with a plastic insert containing a drying agent and porous paper at the bottom. 1 bottle with instructions for use in a cardboard box.

Shelf life
2 years. Do not use after the expiration date.

Storage conditions
At a temperature not exceeding 25 ° C, out of the reach of children.

Conditions of dispensing from pharmacies
on prescription

Manufacturer:
Pfizer Italia S.r.l., Italy.
Legal address: Via del Comercio - 63046, Marino del Tronto, Ascoli Piceno, Italy.
Consumer claims should be sent to the address of the Representative Office.
Representative office address
Pfizer International ELS: Moscow, 109147, Taganskaya st. 21.

Dostinex is a drug for the treatment of diseases caused or combined with hyperprolactinemia: amenorrhea, galactorrhea, infertility, prolactin-secreting pituitary adenoma, acromegaly. It is used to suppress lactation.

Latin name: Dostinex / Dostinex.

Composition and release form: Dostinex tablets: in the package 2 and 8 pcs.
1 Dostinex tablet contains cabergoline 500 mcg.

Active-active substance of the drug Dostinex: Cabergoline / Cabergoline.

Pharmacological action of the drug Dostinex:

Dostinex- a dopamine-stimulating agent, an ergoline derivative, reduces hypersecretion of STH, inhibits the secretion of prolactin. Stimulates dopamine D2 receptors of pituitary lactotropic cells; in high doses has a central dopaminergic effect. Normalizes the content of prolactin in the blood, restores the menstrual cycle and fertility. By reducing the content of prolactin in women, the pulsating secretion of gonadotropins and the release of LH in the middle of the cycle are restored, anovulatory cycles are eliminated, and the concentration of estrogens in the body increases, the severity of hypoestrogenic (increased body weight, fluid retention, osteoporosis) and hyperandrogenic (acne, hirsutism, etc.) .) symptoms. A decrease in prolactin content is noted 3 hours after taking Dostinex and persists for 7-28 days in patients with hyperprolactinemia and up to 14-21 days - with suppression of postpartum lactation. Normalization of prolactin content occurs within 2-4 weeks of treatment. In men, it reduces the decrease in libido caused by hyperprolactinemia, impotence (with a drop in the level of prolactin, the level of testosterone increases), gynecomastia, reduction and softening of the testicles, lactorrhea. Macroadenomas of the pituitary gland and associated symptoms (headache, disturbance of fields and visual acuity, functions of cranial nerves and the anterior lobe of the pituitary gland) undergo reverse development. Reduces the content of prolactin in patients with prolactinoma and pseudoprolactinoma (in the latter, without reducing the size of the pituitary adenoma). Inhibits the release of STH by the pituitary adenoma and reduces visual impairment, neurological disorders and severe headaches, inhibits the progression of acromegaly. In 70–90% of patients, it causes clinical improvement, however, at the end of the course, the content of STH in the blood increases again. Stimulation of dopamine receptors restores the neurochemical balance in the striatum and the black nucleus of the brain, which helps to weaken depressive symptoms, tremors and rigidity, accelerate movements at all stages of Parkinson's disease.

Pharmacokinetics of the drug Dostinex:

After oral administration, cabergoline is rapidly absorbed from the gastrointestinal tract. Food intake does not affect the absorption and distribution of the active substance. Cmax in plasma is reached after 0.5–4 hours; the connection with proteins - 40–42%.
The equilibrium state is achieved after 4 weeks of therapy.
Plasma protein binding is 41–42%. Withdrawal
T1 / 2 is 63–68 hours in healthy volunteers and 79–115 hours in patients with hyperprolactinemia.
The state of equilibrium concentration is achieved after 4 weeks of therapy.
Cabergoline is excreted by the kidneys.

Indications for Dostinex:

prevention of physiological postpartum lactation or suppression of established lactation (including if the mother chooses not to breastfeed the baby, or when breastfeeding is contraindicated for either the mother or the child; with stillbirth or abortion);
treatment of dysfunctions caused by or combined with hyperprolactinemia (including in women - amenorrhea, oligomenorrhea, anovulation, galactorrhea, infertility; in men - impotence, decreased libido);
treatment of prolactin-secreting pituitary adenomas (micro- and macroprolactin);
idiopathic hyperprolactinemia;
syndrome of "empty" Turkish saddle;
acromegaly (supportive care after surgery or radiation therapy).

Dosage and administration of Dostinex:

To prevent postpartum lactation, Dostinex is prescribed 1 mg once on the first day after childbirth.
To suppress established lactation, Dostinex is prescribed 250 mcg every 12 hours for 2 days. With this dosage regimen, side effects (especially arterial hypotension) are less common.
For the treatment of hyperprolactinemia, Dostinex is prescribed 1-2 times a week. The starting dose is 250 mcg per week. If necessary, the dose can be increased depending on the therapeutic effect and tolerability. The increase in the weekly dose should be carried out gradually (500 mcg with an interval of 1 month). The average therapeutic dose is 1 mg per week and can range from 250 mcg to 2 mg per week. When prescribing the drug at a dose of 1 mg per week and above, it should be divided into 2 or more doses per week, depending on tolerance.
Dostinex should be taken with meals.

Dostinex overdose:

Overdose symptoms: nausea, vomiting, abdominal pain, constipation, decreased blood pressure, headache, severe general weakness, sweating, drowsiness, psychomotor agitation, cramps in the calf muscles, impaired consciousness: psychosis, hallucinations. Treatment: gastric lavage and subsequent blood pressure control; dopamine antagonists.

Contraindications for Dostinex:

Hypersensitivity (including to other ergot derivatives); pregnancy, lactation period; postpartum psychosis (history); postpartum hypertension.
With caution - cardiovascular disease, Raynaud's syndrome, renal failure, liver failure, gastric ulcer and duodenal ulcer, gastrointestinal bleeding or mental illness in history.

Application of the drug Dostinex during pregnancy and lactation:

Dostinex should not be used during pregnancy and during breastfeeding.
A woman should be warned that if Dostinex was prescribed in order to suppress lactation, but the desired effect was not achieved, it is necessary to refrain from breastfeeding and consult a doctor.
Before starting treatment with Dostinex, it is necessary to exclude pregnancy and further use mechanical methods of contraception. If pregnancy is established during treatment with Dostinex, you must stop taking the drug.
Since the half-life of cabergoline is long, after the restoration of a regular menstrual cycle, it is recommended to stop taking the drug 1 month before the expected conception to prevent possible exposure of the fetus to the drug.

Side effects of Dostinex:

Often: lowering blood pressure, dizziness, nausea, headache, insomnia, abdominal pain.
With prolonged use - gastritis, weakness, drowsiness, constipation, vomiting, painful tension of the mammary glands, "hot flashes" of blood to the skin of the face, depression, paresthesia. These symptoms are moderate, appear within the first 2 weeks and go away on their own.

Special instructions and precautions: Dostinex is prescribed with caution in patients with cardiovascular diseases, Raynaud's syndrome, severe renal dysfunction, gastric ulcer and duodenal ulcer, gastrointestinal bleeding or mental illness in history.
Dostinex is prescribed with caution against the background of therapy with drugs that cause a hypotensive effect.

After selecting an effective dosing regimen, it is recommended to carry out a regular (1 time per month) determination of the level of prolactin in the blood serum. Normalization of prolactin levels is usually observed within 2-4 weeks of treatment.
Before starting treatment with Dostinex, pregnancy is excluded and mechanical methods of contraception are used. If pregnancy occurs during treatment, you must stop taking the drug and consult a doctor.

In the case of prolonged use of Dostinex, a regular gynecological examination is necessary, including a cervical histological examination and a histological examination of the endometrium. After the restoration of a regular menstrual cycle 1 month before the expected conception, you should stop taking the drug.

Monitoring of blood pressure, gastrointestinal tract functions is required (potential risk of bleeding). If blood pressure rises, persistent headaches or any signs of neurotoxicity occur, Dostinex should be stopped immediately. To reduce nausea, reduce the dose, prescribe domperidone or cisapride.

The ineffectiveness of cabergoline indicates the presence of other causes of hyperprolactinemia (decreased clearance of prolactin in liver diseases, chronic renal failure, especially in patients on hemodialysis).

Influence on the ability to drive vehicles and control mechanisms:
Patients taking the drug should refrain from engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Drug interactions: With the simultaneous use of Dostinex with antibiotics from the macrolide group, the risk of side effects increases.
Derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide reduce the effectiveness of Dostinex.
A combination with ergot alkaloids and their derivatives, as well as with antihypertensive drugs, is not recommended.

Storage conditions: The drug should be stored at a temperature not exceeding 25 ° C.
Shelf life is 2 years.
Dispensing the drug from the pharmacy is a prescription.

The description of the drug Dostinex is not an instruction for self-medication, a doctor's consultation is necessary.

In this article, you can read the instructions for using the medicinal product. Dostinex... Reviews of website visitors - consumers of this medicine, as well as opinions of doctors of specialists on the use of Dostinex in their practice are presented. A big request is to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, which may not have been declared by the manufacturer in the annotation. Dostinex's analogs in the presence of available structural analogs. Use for the termination of lactation and the treatment of hyperprolactinemia in adults, children, as well as during pregnancy and lactation.

Dostinex- a dopamine receptor agonist. Cabergoline (the active substance of Dostinex) is a dopaminergic derivative of ergoline, characterized by a pronounced and prolonged prolactin-lowering effect. The mechanism of action is associated with direct stimulation of dopamine D2 receptors of pituitary lactotropic cells. In doses exceeding those for lowering the level of prolactin in the blood plasma, it has a central dopaminergic effect due to the stimulation of dopamine D2 receptors.

A decrease in the level of prolactin in blood plasma is noted 3 hours after taking Dostinex and persists for 7-28 days in healthy volunteers and patients with hyperprolactinemia and up to 14-21 days in women in the postpartum period. Prolactin-lowering action is dose-dependent both in terms of severity and duration of action.

Cabergoline has a strictly selective effect and, therefore, does not affect the basal secretion of other pituitary hormones, as well as cortisol.

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

Pharmacokinetics

After oral administration, Dostinex is rapidly absorbed from the gastrointestinal tract. Food intake does not affect the absorption and distribution of cabergoline. Metabolic products have a significantly less effect in terms of suppressing the secretion of prolactin compared to cabergoline. 10 days after the application of the drug in urine and feces, 18% and 72% of the dose taken, respectively, are found, and the proportion of the unchanged drug in the urine is 2-3%.

Indications

• prevention of physiological postpartum lactation;
• suppression of established postpartum lactation;
• treatment of disorders associated with hyperprolactinemia, including functional disorders such as amenorrhea, oligomenorrhea, anovulation and galactorrhea;
• prolactin-secreting pituitary adenomas (micro- and macroprolactinomas), idiopathic hyperprolactinemia or the syndrome of "empty" Turkish saddle in combination with hyperprolactinemia.

Forms of issue

Tablets 0.5 mg.

Instructions for use and reception scheme

Dostinex should be taken orally, preferably with meals.

To prevent lactation, the drug is prescribed in a dose of 1 mg (2 tablets) once on the first day after childbirth.

To suppress the established lactation, 0.25 mg (1/2 tablet) is prescribed 2 times a day for 2 days (the total dose is 1 mg). In order to reduce the risk of orthostatic hypotension in lactating patients, a single dose of Dostinex 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 or 2 doses (1/2 tablet, 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 until the optimal therapeutic effect is achieved. The average therapeutic dose is 1 mg per week, but can range from 0.25 mg to 2 mg per week. The maximum dose for patients with hyperprolactinemia is 4.5 mg per week.

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

In patients with hypersensitivity to dopaminergic drugs, the likelihood of side effects can be reduced by starting Dostinex therapy at a lower dose (0.25 mg once a week), followed by its gradual increase until the therapeutic dose is reached. To improve the tolerance of the drug in the event of severe side effects, it is possible to temporarily reduce the dose, followed by a gradual increase, for example, by 0.25 mg per week every 2 weeks.

Side effect

• palpitations;
• orthostatic hypotension (with prolonged use, hypotensive effect);
• nausea, vomiting;
• abdominal pain;
• constipation;
• gastritis;
• dyspepsia;
• dizziness;
• headache;
• increased fatigue;
• drowsiness;
• depression;
• asthenia;
• paresthesia;
• fainting;
• mammalgia;
• nose bleed;
• "hot flushes" of blood to the skin of the face;
• transient hemianopsia;
• spasms of the vessels of the fingers;
• muscle cramps of the lower extremities;
• alopecia;
• swelling;
• liver dysfunction;
• hypersensitivity reactions;
• rash;
• respiratory disorders;
• respiratory failure;
• valvulopathy.

Contraindications

• children and adolescents under 16 years of age (safety and efficacy have not been established);
• hypersensitivity to cabergoline or other components of the drug, as well as to any ergot alkaloids.

Application during pregnancy and lactation

Since no controlled clinical trials have been conducted with Dostinex in pregnant women, the use of the drug during pregnancy is possible only when the intended benefit to the mother outweighs the potential risk to the fetus.

If pregnancy occurs during treatment with Dostinex, the advisability of discontinuing the drug should be considered, also taking into account the benefit / risk ratio.

Pregnancy should be avoided for at least 1 month after discontinuation of the drug, given its long half-life and limited data on fetal exposure. According to the available data, the use of Dostinex at a dose of 0.5-2 mg per week for disorders associated with hyperprolactinemia was not accompanied by an increase in the frequency of miscarriages, premature births, multiple pregnancies and congenital malformations.

There is no information on the release of the drug in breast milk, however, in the absence of the effect of Dostinex to prevent or suppress lactation, breastfeeding should be abandoned. For disorders associated with hyperprolactinemia, Dostinex should not be prescribed to patients who do not want to stop lactation.

special instructions

Before the appointment of Dostinex for the treatment of disorders associated with hyperprolactinemia, it is necessary to conduct a complete study of the function of the pituitary gland.

When increasing the dose, the patient should be under the supervision of a physician in order to establish the lowest effective dose that provides a therapeutic effect. After selecting an effective dosing regimen, it is recommended to carry out regular (once a month) determination of the level of prolactin in the blood serum. Normalization of prolactin levels is usually observed within 2-4 weeks of treatment.

Orthostatic hypotension may develop after Dostinex is applied. Dostinex is prescribed with caution against the background of therapy with drugs that have an antihypertensive effect.

With long-term therapy, Dostinex should be prescribed in lower doses to patients with severe hepatic impairment (class C on the Child-Pugh scale), for whom long-term Dostinex therapy is indicated. With a single use in such patients of the drug at a dose of 1 mg, there was an increase in AUC compared to healthy volunteers and patients with less severe hepatic impairment.

Pleural effusion / pleural fibrosis and valvulopathy were observed after long-term use of cabergoline. In some cases, patients have received prior therapy with ergotinine dopamine agonists. Therefore, Dostinex should be used with caution in patients with existing signs and / or clinical symptoms of cardiac dysfunction (including a history). After discontinuation of the drug, patients showed an improvement in the above symptoms.

After discontinuation of Dostinex, a relapse of hyperprolactinemia is usually observed. However, a number of patients show persistent suppression of prolactin levels for several months. Most women have ovulatory cycles for at least 6 months after discontinuation of Dostinex.

Dostinex restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Since pregnancy can occur even 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 who want to avoid pregnancy should use non-hormonal methods of contraception for the period of treatment with Dostinex, as well as after discontinuation of Dostinex and before the return of anovulation.

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, an increase in the size of already existing pituitary tumors is possible.

The use of cabergoline causes drowsiness. In patients with Parkinson's disease, the use of dopamine receptor agonists may induce sudden sleep. In such cases, it is recommended to reduce the dose of Dostinex or discontinue therapy.

Studies on the use of the drug in elderly patients with disorders associated with hyperprolactinemia have not been conducted.

Influence on the ability to drive vehicles and control mechanisms

Patients taking Dostinex who experience drowsiness should be warned that they are advised to refrain from driving a car and performing work in which low attention can create a risk of serious injury or death for them or those around them.

Drug interactions

There is no information on the interaction of cabergoline and other ergot alkaloids; however, the simultaneous use of these drugs during long-term therapy with Dostinex is not recommended.

Since Dostinex has a therapeutic effect by directly stimulating dopamine receptors, the drug should not be administered concurrently with drugs acting as dopamine antagonists (for example, phenothiazines, butyrophenones, thioxanthenes, metoclopramide). the latter can weaken the prolactin-lowering effect of Dostinex.

Like other ergot derivatives, Dostinex should not be used concomitantly with macrolide antibiotics (for example, with erythromycin), since this can lead to an increase in the systemic bioavailability of cabergoline.

Analogues of the drug Dostinex

Structural analogues for the active substance:

• Agalates;
• Bergolak;
• Cabergoline.

In the absence of analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and see the available analogues for the therapeutic effect.

Every woman at a certain moment in her life begins to understand that she is already ready to become a mother and that her whole nature is striving for this more and more. But not every representative of the beautiful half of humanity, unfortunately, from the first attempts can realize what she wants. It happens that pregnancy does not occur for some reason. In some cases, hormonal "problems" are to blame for this state of affairs. Often, an increased amount of the hormone prolactin in a woman's body leads to the inability to become pregnant. If this is confirmed after a thorough examination and tests performed, the woman is prescribed a course of treatment. As a rule, dostinex is prescribed to reduce the amount of prolactin in the body.

Prolactin - pregnancy hormone

The hormone prolactin, produced mainly by the pituitary gland, cannot be called secondary. He plays a rather important role, participates in the work of many systems of the body, primarily the reproductive. If prolactin in a woman's blood rises significantly, a hormonal failure occurs, which leads to unpleasant consequences, namely, infertility. Women with elevated prolactin levels always have menstrual irregularities.

Normally, prolactin levels increase if pregnancy occurs, as well as during breastfeeding. If a woman is actively involved in sports, then the level of this hormone in her blood will also be increased. Prolactin can be elevated for a short period from stress or after positive emotions, as well as as a result of intercourse.

Doctors also note the pathological reasons for the increase in prolactin in the blood. These include various diseases, including diseases, liver cirrhosis, renal failure, polycystic ovary syndrome), as well as pituitary tumors.

In non-pregnant women with increased prolactin, the following symptoms are noted: menstrual irregularities (scanty periods, anovulation), discharge or milk from the breast, infertility, excessive hair growth, and even decreased libido.

What is Dostinex?

Dostinex (Dostinex) - a medical drug that is prescribed to women to reduce the level of prolactin produced. The active substance of dostinex is cabergoline, the inactive ones are leucine and lactose. The drug is produced in the form of tablets of 0.5 mg each. There are 8 tablets in the package. This medication is available only in pharmacies and with a prescription.

Dostinex acts by blocking the production of this hormone, which, in turn, contributes to the normal and timely maturation of follicles in the ovaries and restores the menstrual cycle. All this leads to the fact that normal ovulation occurs in a woman's body.

A decrease in the level of prolactin occurs on average after 3 hours after a single dose of Dostinex. The drug works from 7 to 28 days. Dostinex is absorbed from the digestive tract quickly.

How much dostinex is taken?

Dostinex is taken one (maximum two) times a week. For the first time, take a dose equal to 0.5-1 tablet of the drug. If dostinex is well tolerated, and the therapeutic effect has not yet been achieved, the dose is gradually increased. In the case of hyperprolactinemia (an increased amount of the hormone prolactin in the blood), the maximum dose of the drug should not exceed 4.5 mg per week. After starting treatment, a woman must monitor the level of this hormone in the body every month, for which it is necessary to take appropriate tests. As a rule, the indicators return to normal within 2-4 weeks after the start of taking dostinex.

Side effects of dostinex

As a rule, the drug is well tolerated by patients. If the drug is used to normalize the level of prolactin, then such "side effects" as headache and dizziness, nausea, constipation, abdominal pain, gastritis, dyspeptic symptoms, and general weakness are possible. Also, the mammary glands become hypersensitive and painful, the patient may become depressed, feel hot flashes in the face, and suffer from low blood pressure. True, all these signs are rarely strongly pronounced. As a rule, they are weak and go away rather quickly. Side effects are especially common at the very beginning of treatment - in the first two weeks. By the way, if the dosage is reduced, the symptoms will disappear. Gradually, the amount of medication taken can be increased again to the original dose. When Dostinex is canceled, absolutely all symptoms disappear after one or two days (but this can be done only with the consent of the attending physician and in no case should one engage in arbitrariness!).

Are these two concepts compatible? This question worries many women, since it often happens that conception occurs against the background of treatment with dostinex. Then the expectant mother has a natural question: does the drug harm a tiny embryo and shouldn't it be canceled altogether?

The answer is: Dostinex and pregnancy are absolutely incompatible. Since many women with an increased amount of prolactin and, as a result, hormonal infertility begin treatment in order to prepare the body for pregnancy. By taking dostinex, they are trying to significantly reduce prolactin, and if pregnancy has begun, then this is absolutely impossible. After all - the main hormone of pregnancy, preserving and supporting it. Therefore, as soon as a woman found out that a new life had arisen under her heart, she should immediately inform her gynecologist about this and stop taking the drug. Moreover, women planning a pregnancy are advised to wait for a pause of one month after the end of the course of treatment, and only after that start realizing their dreams. This is due to the fact that the drug is excreted from the body for a very long time, and the effect of cabergoline (the active substance of dostinex) on the developing fetus is highly undesirable.

Specially for Olga Rizak

From the guest

I, too, could not get pregnant for a long time, after Dostinex I immediately became pregnant in the second cycle, we are planning a second for our 4.5-year-old daughter now, Prolactin is increased again, on Monday I go to the doctor I will drink Dostinex again, I hope that this will help me

From the guest

Here, too, the doctor prescribed Dostinex for me. Since prolactin is high and hence all the consequences: fullness, thyroid gland, menstrual cycle is disrupted and there is no ovulation. She says that she urgently needs to get pregnant in order for everything to recover. I don’t know whether this is really so or not .. I drink 2 r a week, half a pill, I said after 45 days repeated tests of prolactin, and if it returns to normal, we will reduce the dose. The drug should not be abruptly canceled in any case.

From the guest

The doctor prescribed dostinex to me so that my periods would come, since they had not been there for 4 months. After drinking two pills, I made an ultrasound scan and found that I was pregnant. In terms of time, I became pregnant before dostinex, without menstruation. She gave birth to a healthy daughter. I want to say that dostinex did not cause any harm to the fetus.