Dostinex, pills 0.5mg, 2pcs

Composition

1 tablet contains:

Active ingredient:

cabergoline 500 mcg;

Auxiliary substances:

leucine;

lactose anhydrous.

Pharmacological action

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 lactotropic pituitary cells. In doses higher than those for reducing the level of prolactin in 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 ingestion 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. The prolactin-lowering effect is dose-dependent both in terms of the 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 related to the therapeutic effect, include a decrease in blood pressure. With a single application of the drug, the maximum antihypertensive effect is noted during the first 6 hours and is dose-dependent.

Pharmacokinetics

  Suction

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

Css distribution is achieved after 4 weeks of therapy due to prolonged T1 / 2. Binding to plasma proteins is 41-42%.

Metabolism

The main product of cabergoline metabolism identified in the urine is 6-allyl-8β-carboxy-ergoline in concentrations up to 4-6% of the dose taken. The content of 3 additional metabolites in the urine does not exceed 3% of the dose taken. Metabolic products have a significantly lower effect on inhibiting prolactin secretion compared to cabergoline.

Elimination

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

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

Indications

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

Use during pregnancy and lactation

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 0.5-2 mg per week in diseases associated with hyperprolactinemia is not accompanied by an increased risk of miscarriage, premature birth, various pregnancy anomalies and congenital malformations of the fetus.

Contraindications

• postpartum arterial hypertension;
• preeclampsia;
• hypersensitivity.

Side effects

From the CCC side:  palpitations; rarely-orthostatic hypotension (with prolonged use of Dostinex® usually has a hypotensive effect); possibly an asymptomatic decrease in blood pressure. Blood pressure during the first 3-4 days after delivery (sBP-more than 20 mm Hg, dBP-more than 10 mm Hg).

Nervous system disorders:  dizziness/vertigo, headache, fatigue, drowsiness, depression, asthenia, paresthesia, fainting.

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

Other services:  mastodynia, nosebleeds, flushes of blood to the skin of the face, transient hemianopsia, vascular spasms of the fingers and muscle spasms of the lower extremities (like other ergot derivatives, Dostinex® can have a vasoconstrictive effect).

Interaction

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

When used concomitantly with derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide, the effect of Dostinex is weakened.

Concomitant use of Dostinex with macrolide antibiotics increases the risk of side effects, as this may lead to an increase in the systemic bioavailability of cabergoline.

How to take, course of use and dosage

Dostinex should be taken orally, preferably with a meal.

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

To suppress 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 tablets, for example, on Monday and Thursday). Increasing the weekly dose should be carried out gradually-by 0.5 mg at intervals 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 or higher, the drug intake should be divided into 2 or more doses per week, depending on tolerability.

Overdose

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

Treatment:  measures should be taken to remove the non-absorbed drug (gastric lavage) and maintain blood pressure. Dopamine antagonists are recommended.

Special instructions

After selecting an effective dosage regimen, it is recommended to regularly (1 time per month) determine the level of prolactin in the blood serum. Normalization of prolactin levels is usually observed within 2-4 weeks of treatment.

Dostinex should be used with caution in patients with cardiovascular diseases, Raynaud’s syndrome, peptic ulcer or gastrointestinal bleeding, as well as in patients with a history of severe mental illness, especially psychosis. With caution, Dostinex is prescribed against the background of therapy with drugs that have a hypotensive effect.

During long-term therapy, Dostinex should be administered in lower doses to patients with severe hepatic insufficiency.

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 report ovulatory cycles for at least 6 months after the withdrawal 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 the occurrence of orthostatic hypotension.

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

Dostinex restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Since pregnancy can occur even before the recovery of menstruation, it is recommended to conduct pregnancy tests at least once every 4 weeks during the period of amenorrhea, and after the recovery of menstruation – every time there is a delay in menstruation for more than 3 days. Women who want to avoid pregnancy should use non-hormonal methods of contraception during treatment with Dostinex, as well as after the withdrawal of Dostinex and before the return of anovulation.

Women who are pregnant should be monitored by a doctor to detect symptoms of pituitary gland enlargement in a timely manner, since pre-existing pituitary tumors may increase in size during pregnancy.

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

Long-term treatment with Dostinex is not characterized by a deviation from the norm of standard laboratory tests; in women with amenorrhea, a decrease in hemoglobin levels was noted during the first few months after menstrual recovery.

Form of production

Tablets

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Cabergoline

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For women, For adults as prescribed by a doctor

Indications

Lactation Suppression