CABASER 2mg (20 tabs) (aka Cabergoline, Dostinex) is a powerful drug for reducing the levels of prolactin in patients with pituitary tumors. However, it gained popularity as a “pleasure drug”, since it can increase libido and greatly improve the quality of sex.
Besides, it found its place in sports pharmacology. Athletes who use steroids, which may cause progestogenic side effects, e.g. Nandrolone and Trenbolone, take Cabergoline in order to prevent them.
Indications for use
Hyperprolactinemia (macro- and microadenomas of the pituitary gland, idiopathic hyperprolactinemia).
Prevention or suppression of physiological lactation in the postpartum period.
It is an agonist of dopamine receptors of prolonged action. It has high affinity for D2-dopamine receptors, low – for D1-dopamine, alpha1- and alpha2-adrenergic, 5-HT1- and 5-HT2-serotonin receptors.
Eating does not affect pharmacokinetics. According to studies in 12 healthy volunteers, Cmax is achieved after 2-3 hours and amounts to 30–70 pg / ml with a single dose of 0.5–1.5 mg. Plasma concentration in the dose range of 0.5–7 mg increased in proportion to the dose in 12 healthy volunteers and 9 patients with parkinsonism. It was noted (a study on 12 healthy volunteers) that the equilibrium concentration of cabergoline with multiple doses during the week exceeds that after a single dose by 2–3 times.
The absolute bioavailability of cabergoline is unknown; a significant portion of the dose is exposed to the effect of “first passage” through the liver. Binding to plasma proteins does not depend on plasma concentration and is 40–42%.
Cabergoline and / or its metabolites are well distributed in tissues: in animal studies with a measurement of total radioactivity, more than 100-fold excess of the concentration of cabergoline and / or its metabolites in the pituitary gland was revealed in comparison with their content in blood plasma.
It undergoes extensive metabolism mainly by hydrolysis by an acylurea bond or urea residues (in this case, the hypoprolactinemic effect is reduced, since the main metabolites of cabergoline do not have a similar effect).
Biotransformation in the liver with the participation of cytochrome P450 is minimal; in rat studies, cabergoline did not induce or inhibit cytochrome P450. T1 / 2 is 63–69 hours; slow elimination provides a prolonged hypoprolactinemic effect.
Extrarenal and renal clearance of cabergoline is about 3.2 l / min and 0.08 l / min, respectively.
Studies in 5 healthy volunteers revealed that cabergoline is excreted by the kidneys and intestines (22% and 60%, respectively) within 20 days; less than 4% is found in urine unchanged. Renal excretion in patients with hyperprolactinemia is similar to that in healthy volunteers.
Use during pregnancy
Contraindicated during pregnancy, during lactation.
Severe impaired liver function, pregnancy, a history of postpartum psychosis, lactation, hypersensitivity to cabergoline and ergot alkaloids.
Side effects of CABASER 2mg (20 tabs)
When used to prevent or suppress lactation, moderate dizziness, headache, nausea, abdominal pain, drowsiness, and a slight decrease in blood pressure are possible.
With systematic use (hyperprolactinemia), nausea, headache, dizziness, asthenia, dyspepsia, abdominal pain, gastritis, constipation, vomiting, hot flashes, tenderness of the mammary glands, paresthesia, decreased blood pressure, and depression are possible.
Dosage and administration
Intended for oral administration. To prevent lactation – once on the first day after birth at a dose of 1 mg.
To suppress the already existing lactation – within two days, 250 μg every 12 hours. In the treatment of hyperprolactinemia, doses are selected individually. The initial dose is usually 500 mcg per week, usually in one go (sometimes in two divided doses). In the future, if necessary, the dose is gradually increased – by 500 mcg per week with an interval of 1 month. Typically, the therapeutic dose is 1-2 mg per week, in some cases it can be increased to 4.5 mg per week. If the weekly dose exceeds 1 mg, then it is recommended to divide it into 2 doses. In some cases, a dose of 250-500 mcg per week is effective.
Symptoms: nasal congestion, fainting, hallucinations.
Treatment: symptomatic, maintaining blood pressure.
Special instructions for admission
It is used with caution in patients with cardiovascular diseases, Raynaud’s syndrome, impaired renal function, peptic ulcer of the stomach and duodenum, gastrointestinal bleeding, a history of serious mental illness, as well as during treatment with antihypertensive drugs.
In order to prevent (suppress) lactation, it is not recommended for patients with preeclampsia, as well as for postpartum hypertension.
It is not recommended to be used simultaneously with macrolide antibiotics (including with erythromycin), because increased bioavailability of cabergoline and the severity of its side effects.
The simultaneous use with antipsychotics, metoclopramide is not recommended, because, by blocking dopamine receptors, they reduce the effect of cabergoline.
Combination with ergot alkaloids and their derivatives is not recommended.
At a temperature not exceeding 25 ° C.