Dostineks - instructions for use, reviews, analogs and formulations (tablets 0.5 mg) drugs for stopping lactation and treating hyperprolactinemia in adults, children and in pregnancy

In this article, you can read the instructions for using the drug Dostinex. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Dostinex in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Dostinex in the presence of existing structural analogues. Use to stop lactation and treat hyperprolactinemia in adults, children, as well as during pregnancy and lactation.

Dostinex dopamine receptor agonist.Cabergoline (active ingredient of the drug 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 lactotrophic pituitary cells. In doses exceeding those for reducing the level of prolactin in the blood plasma, it has a central dopaminergic effect due to the stimulation of dopamine D2 receptors.

Reduction in the level of prolactin in the blood plasma is observed 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, not associated with the therapeutic effect, include a decrease in blood pressure. With a single application of the drug, the maximum hypotensive effect is noted within the first 6 hours and is dose-dependent.

Pharmacokinetics

After oral administration, Dostinex is rapidly absorbed from the digestive tract. The intake of food does not affect the absorption and distribution of cabergoline. Metabolism products have a significantly lower effect on the inhibition of prolactin secretion compared to cabergoline. After 10 days after application of the drug, 18% and 72% of the dose are detected in urine and feces, the proportion of unchanged drug in urine being 2-3%.

Indications

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

Forms of release

Tablets 0.5 mg.

Instructions for use and reception scheme

Dostinex should be taken orally, preferably during meals.

To prevent lactation appoint the drug 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). To reduce the risk of orthostatic hypotension in lactating patients, a single dose of Dostinex should not exceed 0.25 mg.

To treat 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 at intervals of 1 month to achieve the optimal therapeutic effect. 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, a weekly dose can be taken once or divided into 2 or more receptions per week. Separation of a weekly dose for 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 developing side effects can be reduced by starting with Dostinex at a lower dose (0.25 mg once a week), then gradually increasing it until a therapeutic dose is reached.To improve the tolerability of the drug in the occurrence 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

• palpitation;
• Orthostatic hypotension (with prolonged use of hypotensive effect);
• nausea, vomiting;
• abdominal pain;
• constipation;
• gastritis;
• dyspepsia;
• dizziness;
• headache;
• increased fatigue;
• drowsiness;
• depression;
• asthenia;
• paresthesia;
• fainting;
• mammalgia;
• nose bleed;
• "tides" of blood to the skin of the face;
• transient hemianopsia;
• spasms of the vessels of the fingers;
• cramps in the muscles of the lower limbs;
• alopecia;
• edema;
• impaired liver function;
• hypersensitivity reactions;
• rash;
• respiratory disorders;
• respiratory insufficiency;
• valvulopathy.

Contraindications

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

Application in pregnancy and lactation

Since controlled clinical studies using Dostinex in pregnant women have not been conducted, the use of the drug in pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

If the pregnancy occurred against the background of treatment by Dostinex, one should consider the desirability of drug discontinuation, also considering the benefit / risk ratio.

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

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

special instructions

Before the appointment of Dostinex to treat violations associated with hyperprolactinemia, it is necessary to conduct a full study of the pituitary gland function.

When the dose is increased, the patient should be under the supervision of a physician in order to establish the lowest effective dose providing a therapeutic effect. After choosing an effective dosing regimen, it is recommended to conduct 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.

After using Dostinex, orthostatic hypotension may develop. With caution appoint Dostinex on the background of therapy with drugs that have hypotensive effect.

With prolonged therapy, Dostinex should be administered at lower doses to patients with severe hepatic insufficiency (class C on the Child-Pugh scale), which shows prolonged therapy with Dostinex. With a single use in such patientsof the drug at a dose of 1 mg there was an increase in AUC compared with healthy volunteers and patients with less severe hepatic insufficiency.

After prolonged use of cabergoline, patients experienced pleural effusion / pleural fibrosis and valvulopathy. In some cases, patients received previous therapy with ergotin agonists of dopamine. Therefore, Dostinex should be used with caution in patients with existing signs and / or clinical symptoms of cardiac dysfunction (including history). After the drug was discontinued, the symptoms described above improved in patients.

After the abolition of Dostinex, a relapse of hyperprolactinemia is usually observed. However, in a number of patients, persistent suppressive levels of prolactin have been observed for several months. Most women register ovulatory cycles for at least 6 months after the abolition of Dostinex.

Dostineks restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Since pregnancy can occur before the recovery of menstruation, it is recommended that pregnancy tests be performed at least once every 4 weeks during the amenorrhea period, and after the recovery of menstruation,when there is a delay in menstruation for more than 3 days. For women who want to avoid pregnancy, for the period of treatment with Dostinex, and after the abolition of Dostinex and before the return of anovulation, nonhormonal methods of contraception should be used.

Women who have become pregnant should be under the supervision of a doctor to detect symptoms of pituitary gland enlargement in time, since during pregnancy it is possible to increase the size of pre-existing pituitary tumors.

The use of cabergoline 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 Dostinex or to stop therapy.

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

Impact on the ability to drive vehicles and manage mechanisms

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

Drug Interactions

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

Since Dostinex exerts therapeutic effects through direct stimulation of dopamine receptors, the drug can not be administered simultaneously with drugs acting as dopamine antagonists (e.g., phenothiazines, butyrophenones, thioxanthenes, metoclopramide) since The latter can weaken the prolactin-reducing effect of Dostinex.

Like other ergot derivatives, Dostinex can not be used concurrently with the macrolide antibiotic (e.g., erythromycin), as this may result in increased systemic bioavailability of cabergoline.

Analogues of the drug Dostinex

Structural analogs for the active substance:

• Agalates;
• Bergolak;
• Cabergoline.

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