Universal reference book for medicines

Active ingredient: cabergoline

Type: Dopamine receptor agonist.
Prolactin secretion inhibitor
Manufacturer: VEROPHARM (Russia)
Composition, form of production and packaging
Tablets of
white color, oblong, biconcave, with a risk on one side.

1 tab.

cabergoline 500 mcg

Excipients: leucine, lactose anhydrous (lactopress), magnesium stearate.

2 pcs.
- vials polymeric (1) - packs cardboard.
8 pcs.
- vials polymeric (1) - packs cardboard.

Description of the drug approved by the manufacturer for the printed edition of 2013.


The dopamine receptor agonist, the ergoline derivative, inhibits the secretion of prolactin.
Stimulates dopamine D 2 receptors of lactotrophic pituitary cells; in high doses has a central dopaminergic effect. Reduces the concentration of prolactin in the blood, restores the menstrual cycle and fertility. By reducing the concentration of prolactin in the blood, the women recover the pulsating secretion of the gonadotropins and release the luteinizing hormone in the middle of the cycle, eliminate the anovulatory cycles and increase the concentration of estrogens in the body, reduce the severity of hypoestrogenic (weight gain, fluid retention, osteoporosis) and hyperandrogenic (acne, hirsutism ) of symptoms.
In men, reduces the hyperprolactinemia-related decrease in libido, impotence (with a decrease in the concentration of prolactin increases the concentration of testosterone), gynecomastia, lactorrhea.
The macroadenoma of the pituitary gland and the associated symptoms (headache, disturbance of the fields and visual acuity, functions of the cranial nerves and the anterior lobe of the pituitary gland) are reversed. Reduces the concentration of prolactin in patients with prolactinoma and pseudoprolactinoma (in the latter - without reducing the size of the pituitary adenoma). Reduction in the concentration of prolactin is observed 3 hours after administration and persists for 7-28 days in patients with hyperprolactinemia and 14-21 days - with suppression of postpartum lactation. Reduction in the concentration of prolactin occurs within 2-4 weeks of treatment.

Suction and distribution

Absorption is high, it does not depend on food intake.
The time to reach C max in blood plasma is 0.5-4 h. Binding to plasma proteins is 41-42%.
T 1/2 is 63-68 hours in healthy volunteers and 79-115 hours in patients with hyperprolactinaemia.
Due to prolonged T 1/2, the state of equilibrium concentration is achieved after 4 weeks of therapy.
Metabolism and excretion

It is actively metabolized.
Metabolites have a significantly lower effect on the inhibition of prolactin secretion compared to cabergoline.
It is excreted by the kidneys and through the intestine about 18% and 72% of the dose of cabergoline, respectively, while in the form of unchanged cabergoline, 2-3% are excreted by the kidneys.


- Prevention of postpartum lactation;

suppression of already established postpartum lactation;

- treatment of disorders associated with hyperprolactinemia, including amenorrhea, oligomenorrhoea, anovulation, galactorrhea;

- Prolactin secretion adenomas of the pituitary gland (micro- and macro-prolactinomas);
idiopathic hyperprolactinaemia; Syndrome of empty Turkish saddle in combination with hyperprolactinemia.

The drug is taken orally, with food.

To prevent lactation after childbirth - 1 mg once (2 tab.) On the first day after birth.

To suppress the steady lactation - 0.25 mg (1/2 tab.) 2 times / day every 12 hours for 2 days (total dose - 1 mg).

In order to reduce the risk of orthostatic hypotension in breast-feeding mothers, a single dose of Bergolak should not exceed 0.25 mg.

For the treatment of violations associated with hyperprolactinemia : the recommended initial dose is 0.5 mg per week in a single dose (1 tablet) or in 2 divided doses (for example, 1/2 tablets, for example, on Monday and Thursday).
The increase in the weekly dose should be carried out gradually - by 0.5 mg with a monthly interval 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 tolerability, a weekly dose of Bergolak can be taken once or divided into 2 or more receptions per week.
The division of the weekly dose into several doses is recommended when the drug is administered at a dose of more than 1 mg per week.
The likelihood of developing side effects can be reduced by starting therapy with a low-dose Bergolak (eg, 0.25 mg once a week), followed by a gradual increase 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 more gradual increase (for example, an increase of 0.25 mg per week every 2 weeks).

Adverse events are usually transient, but the severity is weak or moderately expressed and is dose-dependent.
Occur, mainly during the first 2 weeks of therapy and in most cases disappear on their own as the therapy continues or a few days after the abolition of cabergoline.
From the cardiovascular system: palpitations, flushes of blood to the skin of the face, spasms of the vessels of the fingers (like other ergot derivatives, cabergoline may have a vasoconstrictive effect), valvulopathy;
rarely - orthostatic hypotension (with prolonged treatment with cabergoline - hypotensive effect), there was an asymptomatic decrease in blood pressure during the first 3-4 days after delivery (systolic - more than 20 mm Hg, diastolic - more than 10 mm Hg .).
From the nervous system: dizziness / vertigo, headache, fatigue, drowsiness, depression, mania, asthenia, paresthesia, fainting.

On the part of the digestive system: nausea, vomiting, pain in the epigastric region, abdominal pain, constipation, gastritis, dyspepsia, impaired liver function.

Allergic reactions: hypersensitivity reactions, skin rashes.

Other: mastodinia, epistaxis, transient hemianopsia, muscle cramps of the lower limbs, alopecia, increased activity of CKK in the blood serum, edema, pleural fibrosis, respiratory disorders (including respiratory failure).


- age under 16 years (safety and efficacy in this category of patients not established);

- rare hereditary forms of intolerance to galactose, congenital deficiency of lactase lapp or impaired absorption of glucose-galactose (because the preparation contains lactose);

- Hypersensitivity to cabergoline or other components of the drug, as well as to any ergot alkaloids.

Caution should be given to the drug in the following conditions and / or diseases:

- arterial hypertension, developed against a background of pregnancy (for example, pre-eclampsia) and / or postpartum arterial hypertension;

- Severe diseases of the cardiovascular system, Raynaud's syndrome;

- Peptic ulcer, gastrointestinal bleeding;

severe hepatic impairment;

- severe psychotic and cognitive impairment (including in anamnesis);

- presence of fibrotic changes of the heart (valvulopathy) and respiratory system (pleurisy / pleural fibrosis), incl.
in the anamnesis;
- simultaneous reception with drugs that have hypotensive effect (due to the risk of developing orthostatic hypotension).


Since controlled clinical studies with the use of cabergoline in pregnant women have not been performed, the appointment of the drug in pregnancy is possible only in case of emergency, when the potential benefit of using the drug for a woman significantly exceeds the possible risk to the fetus.

Pregnancy should be avoided for at least one month after cessation of cabergoline, given the long T 1/2 of the drug and the availability of limited data on its effects on the fetus (according to available data, the use of cabergoline 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 pregnancies and congenital malformations).

If the pregnancy occurred against the background of treatment with cabergoline, should consider the feasibility of discontinuing the drug, also considering the ratio of the potential benefits of using the drug for a woman and the possible risk to the fetus.

Since cabergoline suppresses lactation, the drug should not be given to mothers who want to breast-feed.
During treatment with cabergoline, breastfeeding should be discontinued.

With caution should prescribe the drug in severe hepatic insufficiency.


Contraindicated in patients under the age of 16 years (safety and efficacy in this category of patients not established).


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


Before the appointment of cabergoline, a complete examination of the pituitary gland function is necessary.

With an increase in the dose of the drug, patients should be under the supervision of a physician in order to establish the lowest dose providing a therapeutic effect.During the period of treatment, it is recommended that the concentration of prolactin in the blood serum be determined regularly (once a month).
Normalization of prolactin concentration is usually observed within 2-4 weeks of therapy with cabergoline.
After the withdrawal of cabergoline, a relapse of hyperprolactinemia is usually observed, but in some patients persistent decreases in prolactin concentrations persist for several months.
In most women, ovulatory cycles persist for at least 6 months after the abolition of cabergoline.
Cabergoline restores ovulation and fertility in women with hyperprolactinemic hypogonadism.
Since pregnancy can occur before the recovery of menstruation, it is recommended to conduct pregnancy tests at least once every 4 weeks during the amenorrhea period, and after the recovery of menstruation - every time the menstruation is delayed by more than 3 days.
It is necessary to use barrier methods of contraception during treatment with cabergoline, as well as after discontinuation of the drug before the recurrence of anovulation.
If the pregnancy occurred during treatment should consider the feasibility of drug discontinuation. Women who have become pregnant should be under the supervision of a doctor to promptly detect symptoms of an increase in the pituitary gland (during pregnancy, an increase in the size of pre-existing pituitary tumors may be possible).
After prolonged administration of cabergoline, pleural effusion / pleural fibrosis and valvulopathy were observed in patients, therefore, cabergoline should be used with caution in patients with current manifestations and / or clinical symptoms of cardiac dysfunction, incl.
in the anamnesis.
Patients with hypertension that develops against the background of pregnancy (eg, pre-eclampsia) and / or postpartum arterial hypertension are prescribed cabergoline only when the potential benefit of using the drug is significantly greater than the possible risk.

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 cabergoline or discontinue therapy.
Studies on the use of cabergoline in elderly patients with disorders associated with hyperprolactinemia have not been conducted.

Impact on the ability to drive vehicles and manage mechanisms

During the period of treatment, it is recommended to refrain from driving vehicles and other activities that require an increased concentration of attention and speed of psychomotor reactions.


Symptoms: nausea, vomiting, abdominal pain, constipation, decreased blood pressure, orthostatic hypotension, headache, spasms of the calf muscles, severe asthenia, sweating, drowsiness, psychomotor agitation, psychosis, hallucinations.

Treatment: gastric lavage, control of blood pressure, administration of antagonists of dopamine receptors (derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide).


It is not recommended simultaneous use with ergot alkaloids and their derivatives (with prolonged therapy with cabergoline).

When used simultaneously, dopamine receptor antagonists (derivatives of phenothiazine, butyrophenone, thioxanthene, metoclopramide) can weaken the action of cabergoline.

It is not recommended simultaneous use of cabergoline with macrolides in connection with a possible increase in the concentration of cabergoline in the blood plasma.
The mechanism of interaction of macrolides with cabergoline is not sufficiently studied, but, apparently, due to the ability of macrolides and cabergoline to competitively inhibit the cytochrome P450 system.

The drug is released by prescription.


List B. The drug should be stored out of reach of children at a temperature of no higher than 25 ° C.
Shelf life - 2 years.
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