Cabergoline

Brand Pfizer

In stock 1469 Items

Available since: 2019-09-19

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Clinical Pharmacology

Dostinex - hypoprolactinemic.

Pharmacodynamics

Cabergoline is a dopaminergic derivative of ergoline and is characterized by a pronounced and prolonged prolactin-lowering effect caused by direct stimulation of D₂-dopamine receptors of lactotropic pituitary cells. In addition, when taking higher doses compared with doses to reduce serum prolactin levels, cabergoline has a central dopaminergic effect due to stimulation of D₂-receptors.

A decrease in the concentration of prolactin in the blood plasma occurs within 3 hours after taking the drug 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.

Cabergoline has a strictly selective effect, does not affect the basal secretion of other pituitary and cortisol hormones. Prolactin-lowering effect of the drug is dose-dependent, both in terms of severity and duration of action.

Pharmacodynamic effects of cabergoline, not related to the therapeutic effect, include only a decrease in blood pressure. With a single dose of the drug, the maximum hypotensive effect is observed during the first 6 hours and is dose-dependent.

Pharmacokinetics

Cabergoline is rapidly absorbed from the gastrointestinal tract, C_max in plasma it is reached in 0.5–4 h, binding to plasma proteins is 41–42%. T_1/2 cabergoline, measured by urine excretion rate, is 63–68 h in healthy volunteers and 79–115 h in patients with hyperprolactinemia. Due to the long T_1/2, C_SS achieved in 4 weeks. 10 days after taking the drug in the urine and feces are found, respectively, about 18 and 72% of the dose, and the proportion of unchanged drug in the urine is 2-3%. The main product of cabergoline metabolism identified in urine is 6-allyl-8β-carboxy-ergoline at a concentration of up to 4–6% of the dose taken. The content in the urine of 3 additional metabolites does not exceed 3% of the dose. It has been established that metabolic products have a significantly smaller effect on suppressing the secretion of prolactin compared with cabergoline.

Meal does not affect the absorption and distribution of cabergoline.

Indications

prevention of physiological postpartum lactation (only for medical reasons);
suppression of the already established lactation (only for medical reasons);
treatment of disorders associated with hyperprolactinemia, including functional disorders such as amenorrhea, oligomenorrhea, anovulation and galactorrhea;
prolactin-secreting pituitary adenomas (micro- and macroprolactinomas, idiopathic hyperprolactinemia, or empty empty saddle syndrome in combination with hyperprolactinemia.

Composition

1 tablet contains:

Active substance: cabergoline 500 mcg;

Excipients: leucine; anhydrous lactose.

Cabergoline is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Dostinex	Pfizer	USA	pills
Bergolak	Veropharm	Russia	pills
Agalates	Teva	Israel	pills

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Dosage and Administration

Dostinex should be taken orally, preferably with a meal.

Forprevent lactation prescribe the drug in a dose of 1 mg (2 pills) once on the first day after birth.

Forsuppression of steady lactation appoint 0.25 mg (1/2 tablet) 2 times a day for 2 days (total dose is 1 mg).

Fortreatment of disorders associated with hyperprolactinemia, the drug is prescribed in a dose of 0.5 mg per week in 1 or 2 doses (1/2 tablet, for example, on Monday and Thursday). Increasing the weekly dose should be carried out gradually - at 0.5 mg with an interval of 1 month to achieve the optimal therapeutic effect. 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 up to 4.5 mg per week are used.
When prescribing the drug in a dose of 1 mg per week and above, the drug should be divided into 2 or more doses per week depending on tolerance.

Adverse reactions

From the CCC: heartbeat; rarely, orthostatic hypotension (with long-term use of Dostinex^® usually has a hypotensive effect); possibly asymptomatic reduction in blood pressure during the first 3-4 days after delivery (SBP - more than 20 mm Hg, DAD - more than 10 mm Hg).

From the nervous system: dizziness / vertigo, headache, fatigue, drowsiness, depression, asthenia, paresthesias, syncope.

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

Other: mastodynia, nasal bleeding, flushing to the skin of the face, transient hemianopia, vascular spasms of the fingers and muscle cramps of the lower limbs (like other ergot derivatives, Dostinex^® may have a vasoconstrictor effect).

Contraindications

postpartum arterial hypertension;
preeclampsia;
pregnancy;
Hypersensitivity to cabergoline or other components of the drug, as well as to any ergot alkaloids.

Drug interactions

There is no information on the interaction of cabergoline and ergot alkaloids; however, the simultaneous use of these medicines during long-term therapy with Dostinex is not recommended.
With simultaneous use with phenothiazine derivatives, butyrophenone, thioxanthene, metoclopramide, a weakening of the Dostinex effect is observed.
The simultaneous 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.

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 Dostinex's use of 0.5-2 mg per week for diseases associated with hyperprolactinemia, is not accompanied by an increased risk of miscarriage, premature birth, various pregnancy abnormalities and congenital malformations of the fetus.

Special instructions

After the selection of an effective dosing regimen, it is recommended to regularly (once per month) determine the level of prolactin in 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 ulcer or gastrointestinal bleeding, as well as patients with indications of a history of severe mental illness, especially psychosis.
Dostinex is prescribed with caution during therapy with drugs that have a hypotensive effect.
With long-term therapy, Dostinex should be administered in lower doses to patients with severe liver failure.
After discontinuation of Dostinex, a relapse of hyperprolactinemia is usually observed. However, a number of patients have persistent suppression of prolactin levels over several months. Most women register ovulatory cycles for at least 6 months after Dostinex is canceled.
It is impossible to 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 treatment with Dostinex, a complete study of the function of the pituitary is shown.
Dostinex restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Since pregnancy can occur even before menstruation is restored, it is recommended that pregnancy tests be performed at least once every 4 weeks during the amenorrhea period, and after menstruation is restored - every time there is a delay in menstruation for more than 3 days. Women who want to avoid pregnancy during the period of treatment with Dostinex, as well as after the cancellation of Dostinex and before the return of anovulation, should use non-hormonal methods of contraception.
Women who have become pregnant should be supervised by a physician in order to identify the symptoms of an increase in the pituitary gland in a timely manner, since an increase in the size of existing pituitary tumors is possible during pregnancy.
Side effects associated with taking the drug are dose-dependent. The likelihood of side effects can be reduced if you start Dostinex therapy at lower doses (for example, 0.25 mg 1 time per week), followed by a gradual increase in dose until the therapeutic dose level is reached. If persistent or severe side effects occur, a temporary dose reduction and then a more gradual increase (for example, an increase of 0.25 mg per week every 2 weeks) will contribute to a better tolerability of the drug.
With long-term therapy with Dostinex, no abnormal indicators of standard laboratory tests are typical; in women with amenorrhea, there was a decrease in hemoglobin levels during the first few months after the recovery of menstruation.

Overdosage

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

Treatment: It should be carried out activities aimed at removing non-absorbed drug (gastric lavage) and to maintain blood pressure. The use of dopamine antagonists is recommended.

Studies and clinical trials of Cabergoline (Click to expand)