Dostinex 0.5 mg

1 tablet contains:

Active substance :

cabergoline 500 mcg;

Excipients:

 leucine;

anhydrous lactose.

Dostinex is a dopamine receptor agonist. Cabergoline 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

  Suction

After oral administration, cabergoline is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached after 0.5-4 hours. Food intake does not affect the absorption and distribution of cabergoline.

Distribution

Css is achieved after 4 weeks of therapy due to prolonged T1 / 2. Plasma protein binding is 41-42%.

Metabolism

The main metabolic product of cabergoline identified in urine is 6-allyl-8β-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. Metabolic products have a significantly lower effect in terms of suppressing the secretion of prolactin compared to cabergoline.

Withdrawal

T1 / 2, assessed by the rate of excretion in the urine, is 63-68 hours in healthy volunteers and 79-115 hours in patients with hyperprolactinemia.

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%.

• menstrual irregularities
• female infertility
• to suppress lactation (after childbirth or abortion)
• pituitary tumors.

Pregnancy should be avoided for at least 1 month after stopping treatment with Dostinex, since it is characterized by a long half-life, and in addition, there are only limited data on the effect of the drug on the fetus, although the use of Dostinex at 0.5-2 mg per week for diseases associated with hyperprolactinemia, is not accompanied by an increased risk of miscarriage, premature birth, various abnormalities of pregnancy and congenital malformations of the fetus.

• postpartum arterial hypertension;
• preeclampsia;
• hypersensitivity.

From the CCC: palpitations; 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 (SBP - more than 20 mm Hg, DBP - more than 10 mm Hg).

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

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

Others: mastodynia, epistaxis, flushing 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).

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

With simultaneous use with derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide, a weakening of the Dostinex effect is observed.

With the simultaneous use of Dostinex with antibiotics from the macrolide group, the risk of side effects increases, since this can lead to an increase in the systemic bioavailability of cabergoline.

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). 

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. In patients with hyperprolactinemia, doses of up to 4.5 mg per week are used.

When prescribing the drug at a dose of 1 mg per week and above, the drug intake should be divided into 2 or more doses per week, depending on the tolerance.

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

Treatment: measures should be taken to eliminate the unabsorbed drug (gastric lavage) and to maintain blood pressure. Dopamine antagonists are recommended.

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.

Dostinex is prescribed with caution to patients with cardiovascular diseases, Raynaud's syndrome, peptic ulcers or gastrointestinal bleeding, as well as to patients with a history of severe mental illness, especially psychosis.
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.

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.

Do not exceed a single dose of Dostinex, equal to 0.25 mg, in nursing mothers who are undergoing treatment aimed at suppressing already established lactation in order to prevent orthostatic hypotension.

Before starting therapy with Dostinex, a complete study of the function of the pituitary gland is indicated.

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 it is possible to increase the size of already existing pituitary tumors.

Side effects associated with taking the drug are dose-dependent. The likelihood of side effects can be reduced if Dostinex therapy is started at lower doses (for example, 0.25 mg once a week), followed by a gradual increase in the dose until the therapeutic dose is reached. If persistent or severe side effects occur, then a temporary decrease in the dose, and then a more gradual increase in it (for example, an increase of 0.25 mg per week every 2 weeks) will help to better tolerate the drug.

With prolonged therapy with Dostinex, a deviation from the norm of the indicators of standard laboratory tests is not characteristic; women with amenorrhea had a decrease in hemoglobin levels during the first few months after menstruation was restored. 

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