Cabergoline (Dostinex): instructions for use, purchase from an online pharmacy

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Сabergoline (Dostinex): instructions for use

Pharmachologic effect:

The active substance of Dostinex is cabergoline, a dopaminergic agent, an ergoline derivative. The substance has a long-term and pronounced effect of reducing prolactin. It acts by blocking prolactin secretion as a result of direct stimulation of dopamine D2 receptors in the lactotrophic cells of the pituitary gland. When high doses are used, there is also a central stimulatory dopaminergic effect on D2 receptors. This property differs the drug from other prolactin-lowering drugs.

Already 3 hours after taking Сabergoline (Dostinex), a decrease in the level of prolactin is observed in the blood, which persists for 7 to 28 days in healthy individuals and patients with an increased content of prolactin. The effect when used in the postpartum lactation period lasts up to 2-3 weeks. The substance is absorbed quickly from the digestive tract.

The maximum plasma concentration of the drug is achieved within 0.5-4 hours after internal administration of the drug. The half-life was assessed by the scientists by the rate of elimination of cabergoline in the urine - it was 63–68 hours in healthy individuals, and 79–115 hours in patients with hyperprolactinemia. Due to the significant half-life of cabergoline, equilibrium drug concentrations are reached after 28 days. In this case, approximately 41–42% of cabergoline binds to plasma proteins.

Indications for use:

• In women - treatment of hyperprolactinemia, which is manifested by infertility, menstrual irregularities (oligomenorrhea, amenorrhea, anovulatory menstrual cycles), galactorrhea;

• in men - treatment of hyperprolactinemia, which is manifested by decreased libido or impotence;

• prolactin-secreting pituitary adenoma (micro- or macroprolactinoma);

• idiopathic hyperprolactinemia;

• syndrome of an empty Turkish saddle;

• to suppress physiological lactation after childbirth if a woman is unwilling or unable to breastfeed, or there are contraindications to feeding on the part of the child or mother;

• to prevent postpartum lactation in case of abortion or stillbirth.

Mode of application:

To suppress lactation after childbirth, 0.5 tablets (0.25 mg) should be used every 12 hours for 2 days.

To prevent lactation, Cabergoline (Dostinex) is administered once in a dose of 1 mg on the first day after childbirth.

In the therapy of hyperprolactinemia. The regimen for taking the prescribed dosage is 1-2 times a week on certain days (for example, every Tuesday with the 1 time per week regimen or every Tuesday-Friday with the 2 times a week regimen). At first, it is recommended to take lower doses of the drug Cabergoline (Dostinex) - 0.5-1 tablet (0.25-0.5 mg) once a week. If necessary, the dose can be gradually increased depending on the tolerance and therapeutic response. Dosage increase regimen: 0.5 mg every month of admission.

The average therapeutic dose of Dostinex is 1 mg / week. Usually, for the treatment of hyperprolactinemia, the maximum dose of the drug is 4.5 mg / week. If a dose of more than 2 mg / week is used, then it is divided into 2 doses. As soon as the optimal dosing regimen is selected, it is necessary to determine the prolactin content in the blood once a month. On average, the normalization of prolactin levels is observed after 0.5-1 months of treatment.

Side effects:

The drug is usually well tolerated. When Cabergoline (Dostinex) is prescribed to prevent or suppress lactation, dizziness, hypotension, insomnia, headache, nausea, and abdominal pain are common. These signs are mild and pass quickly.

If the drug is used to treat hyperprolactinemia, then dizziness, headache, nausea, dyspeptic symptoms, abdominal pain, gastritis, constipation, general weakness, breast tenderness, depression, hot flashes, hypotension, paresthesia are possible. These signs are mild or moderate and pass quickly. The most common side effects appear during the first 14 days of taking Dostinex.

Side effects of the drug Сabergoline (Dostinex) are pre-dose-dependent, therefore, with the development of strong effects, it is recommended to first reduce the dosage, and then try to increase it again, if necessary (by 0.25 mg per week for 2 weeks). If the side effects are severe, which requires discontinuation of the drug, the symptoms disappear after 1-2 days.

Contraindications:

• Liver failure;

• late gestosis;

• hypersensitivity to ergot alkaloids, cabergoline or other components of Dostinex;

• anamnestic indication of postpartum psychosis.

Pregnancy:

Cabergoline (Dostinex) is not intended for use in pregnant women. Before prescribing the drug, it is recommended to exclude the presence of pregnancy. After the end of the drug intake, adequate contraception is required for 1 month, after which you can become pregnant. If the drug Cabergoline (Dostinex) is ineffective for suppressing lactation, breastfeeding is discontinued. If conception occurs against the background of the drug, Dostinex is canceled.

Interaction of the drug with other drugs:

Interactions between Dostinex and methylergonovine maleate have not been identified. However, you should refrain from using a combination of cabergoline and ergot alkaloids. While taking the drug, dopamine antagonists (butyrophenones, phenothiazines, metoclopramide, thioxanthenes) should not be prescribed.

Because cabergoline stimulates dopamine receptors, dopamine antagonists can cause clinical ineffectiveness of the drug.

A side effect of cabergoline is arterial hypotension, therefore it is not recommended to prescribe other drugs with an antihypertensive effect while taking the drug.

Overdose:

In case of an accidental overdose of the drug Cabergoline (Dostinex), vomiting, nausea, dyspeptic symptoms, impaired consciousness (hallucinations, psychosis), arterial hypotension are possible. For treatment, it is recommended to carry out generally accepted measures to remove unabsorbed cabergoline from the digestive tract. Dopamine antagonists may be used. In the future, symptomatic therapy (normalization of blood pressure).

Release form of the drug:

0.5 mg tablets. The package contains 8 tablets.

Storage conditions:

Storage - at room temperature. Prescription dispensing from pharmacies.

Structure:

Active ingredient: cabergoline.

Inactive substances: leucine and lactose.

Additional Information.

Scientists have not studied the efficacy and safety of the drug Сabergoline 0.5 mg in patients with renal or hepatic insufficiency. The main way of elimination of cabergoline is excretion with bile, therefore, it is not recommended to use the drug in severe liver dysfunctions.

With caution, the drug is prescribed to patients with pathology of the cardiovascular system, with liver diseases, Raynaud's syndrome, duodenal ulcer or stomach ulcer, renal failure, mental illness (including diseases in the past), bleeding from the gastrointestinal tract.

If Сabergoline 0.5 mg is used in a long-term mode, it is necessary to periodically conduct a gynecological examination, which includes a histological examination of the endometrium and mucous membrane of the cervical canal. Cabergoline, like other ergot drugs, is strictly not allowed to be used to prevent lactation in women who have undergone preeclampsia or have postpartum hypertension.

It was found that when using the drug Cabergoline to suppress physiological lactation at a dose of 0.5 mg, there is a 2-fold increase in the risk of side effects. Therefore, it is not recommended to use a dosage of more than 0.25 mg for this purpose.

Before taking the drug for the treatment of hyperprolactinemia, it is necessary to diagnose the condition of the pituitary gland to establish the possible development of a tumor of pituitary genesis. Pituitary swelling is most commonly associated with infertility, galactorrhea, and ameorrhea.

In women with hypogonadism of hyperprolactinemic origin, Cabergoline restores fertility and ovulation. Therefore, it is necessary to regularly, every month of taking the drug, conduct a pregnancy test (if the drug is used in the presence of amenorrhea). After fertility and menstruation have been restored, mechanical contraception should be used to prevent pregnancy. If pregnancy occurs during treatment with Dostinex, the drug is canceled and the state of the pituitary gland is monitored, since the clinical symptoms of the pituitary tumor may resume.

The drug Сabergoline 0.5 mg has a long half-life, therefore, after the resumption of the regularity of the menstrual cycle, Dostinex must be canceled 1 month before the expected conception. This is to prevent cabergoline from affecting the developing fetus.

If, while taking the drug, conception still occurs, Dostinex is canceled. In experiments on rats, it was found that cabergoline is excreted in breast milk. Despite the fact that research on humans has not been carried out, it is recommended to stop lactation if it is necessary to take the drug during breastfeeding.

Scientists have not studied the efficacy and safety of taking the drug in pediatric patients (up to 16 years old). In the first days of taking the drug, you must carefully drive vehicles and work in production with installations that require close attention.

Attention!

Description of the drug "Сabergoline (Dostinex)" on this page is a simplified and supplemented version of the official instructions for use. Before purchasing or using the drug, you should consult your doctor and familiarize yourself with the annotation approved by the manufacturer.

Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide on the appointment of the drug, as well as determine the doses and methods of its use.