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Active ingredients
Cabergolin
Release form
Pills
Composition
Cabergoline 500 mcg. Excipients: leucine, anhydrous lactose (lactopress), magnesium stearate.
Pharmacological effect
The dopamine receptor agonist, ergolin derivative, inhibits prolactin secretion. Stimulates dopamine D2 receptors of lactotropic 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 in women, the pulsating secretion of gonadotropins and the release of luteinizing hormone in the middle of the cycle are restored, anovulatory cycles are eliminated and the body's estrogen concentration increases, the severity of hypoestrogenic (weight gain, fluid retention, osteoporosis) and hyperadrogenic factors decrease. a) symptoms. In men, it reduces the decrease in libido caused by hyperprolactinemia, impotence (with a decrease in the concentration of prolactin, the concentration of testosterone increases), gynecomastia, and lactorrhea. Subject to the reverse development of the pituitary macroadenoma and associated symptoms (headache, disruption of the fields and visual acuity, functions of the cranial nerves and the anterior pituitary gland). Reduces the concentration of prolactin in patients with prolactinoma and pseudoprolactinoma (in the latter - without reducing the size of the pituitary adenoma). A decrease in the concentration of prolactin occurs 3 hours after administration and persists for 7–28 days in patients with hyperprolactinemia and 14–21 days when suppression of postpartum lactation. A decrease in prolactin concentration occurs within 2–4 weeks of treatment.
Pharmacokinetics
Absorption and distribution Absorption is high, does not depend on food intake. The time to reach Cmax in the blood plasma is 0.5-4 hours. Binding to plasma proteins is 41-42%. T1 / 2 is 63-68 h in healthy volunteers and 79-115 h in patients with hyperprolactinemia. Due to prolonged T1 / 2, the state of equilibrium concentration is achieved after 4 weeks of therapy. Metabolism and excretion Actively metabolized. Metabolites have a significantly lower effect in suppressing the secretion of prolactin compared with cabergoline.About 18% and 72% of the taken dose of cabergoline are excreted by the kidneys and through the intestines, respectively, while 2-3% are excreted as unchanged cabergoline by the kidneys.
Indications
- prevention of postpartum lactation; - suppression of the already established postpartum lactation; - treatment of disorders associated with hyperprolactinemia, including amenorrhea, oligomenorrhea, anovulation, galactorrhea; - prolactin-secreting pituitary adenomas (micro- and macroprolactinomas); idiopathic hyperprolactinemia; empty turkish saddle syndrome combined with hyperprolactinemia.
Contraindications
- age up to 16 years (safety and efficacy in this category of patients has not been established); - rare hereditary forms of galactose intolerance, congenital lactase lapp deficiency or impaired glucose-galactose absorption (since the preparation contains lactose); - Hypersensitivity to cabergoline or other components of the drug, as well as to any ergot alkaloids. The drug should be prescribed with caution in the following conditions and / or diseases: - arterial hypertension that developed during pregnancy (for example, pre-eclampsia) and / or postpartum arterial hypertension; - Severe diseases of the cardiovascular system, Raynaud's syndrome; - peptic ulcer, gastrointestinal bleeding; - severe liver failure; - severe psychotic and cognitive impairment (including in history); - presence of fibrotic changes of the heart (valvulopathy) and respiratory system (pleurisy / pleural fibrosis), incl. in the anamnesis; - simultaneous use with drugs that have a hypotensive effect (due to the risk of orthostatic hypotension).
Use during pregnancy and lactation
Since controlled clinical trials with the use of cabergoline in pregnant women have not been conducted, the prescription of the drug during pregnancy is possible only in case of emergency, when the potential benefits of using the drug for a woman far exceed the potential risk to the fetus. The onset of pregnancy should be avoided for at least one month after stopping taking cabergoline, given the long T1 / 2 of the drug and the availability of limited data on its effects on the fetus (according to available data, use of cabergoline at a dose of 0.5-2 mg per week for disorders associated with hyperprolactinemia, was not accompanied by an increase in the frequency of miscarriages, premature births, multiple pregnancies and congenital malformations).If the pregnancy has occurred on the background of treatment with cabergoline, the feasibility of discontinuing the drug should be considered, also taking into account 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 breastfeed. During treatment with cabergoline, breastfeeding should be stopped.
Dosage and administration
The drug is taken orally during meals. To prevent lactation after birth, 1 mg once (2 tab.) On the first day after birth. To suppress established 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 lactating mothers, a single dose of Bergolac should not exceed 0.25 mg. For the treatment of disorders associated with hyperprolactinemia: the recommended initial dose is 0.5 mg per week in 1 dose (1 tab.) Or in 2 doses (1/2 tab., For example, on Monday and Thursday). An increase in the weekly dose should be carried out gradually - by 0.5 mg with a monthly interval until the optimum therapeutic effect is achieved. The therapeutic dose is usually 1 mg per week, but can vary 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 tolerance, a weekly dose of Bergolac can be taken once or divided into 2 or more doses per week. The division of the weekly dose into several doses is recommended when prescribing the drug in a dose of more than 1 mg per week. The likelihood of side effects can be reduced by starting therapy with Bergolac from a low dose (for example, 0.25 mg 1 time per week), followed by a gradual increase until a therapeutic dose is reached. To improve the tolerability of the drug in the event of severe side effects, a temporary dose reduction is possible, followed by a more gradual increase (for example, an increase of 0.25 mg per week every 2 weeks).
Side effects
Side effects are usually transient, but the severity is mild or moderately pronounced and are dose-dependent. Occur mainly during the first 2 weeks of therapy and in most cases disappear on their own as the therapy continues or several days after discontinuation of cabergoline.On the part of the cardiovascular system: palpitations, flushing to the skin of the face, vascular spasms of the fingers (like other ergot derivatives, cabergoline may have a vasoconstrictor effect), valvulopathy; rarely - orthostatic hypotension (with long-term treatment with cabergoline - hypotensive effect), there was an asymptomatic decrease in blood pressure during the first 3-4 days after delivery (systolic - by more than 20 mm Hg, diastolic - by more than 10 mm Hg .). Nervous system disorders: dizziness / vertigo, headache, fatigue, drowsiness, depression, mania, asthenia, paresthesias, syncope. On the part of the digestive system: nausea, vomiting, pain in the epigastric region, abdominal pain, constipation, gastritis, dyspepsia, abnormal liver function. Allergic reactions: hypersensitivity reactions, skin rash. Others: mastodynia, nasal bleeding, transient hemianopsia, muscle cramps in the lower extremities, alopecia, increased serum CPK activity, edema, pleural fibrosis, respiratory disorders (including respiratory failure).
Overdose
Symptoms: nausea, vomiting, abdominal pain, constipation, lowering blood pressure, orthostatic hypotension, headache, calf muscle cramps, severe asthenia, sweating, drowsiness, psychomotor agitation, psychosis, hallucinations. Treatment: gastric lavage, blood pressure control, the appointment of dopamine receptor antagonists (phenothiazine derivatives, butyrophenone, thioxanthene, metoclopramide).
Interaction with other drugs
Not recommended simultaneous use with ergot alkaloids and their derivatives (with long-term therapy with cabergoline). With simultaneous use, dopamine receptor antagonists (phenothiazine derivatives, butyrophenone, thioxanthene; metoclopramide) can weaken the effect of cabergoline. Simultaneous use of cabergoline with macrolides is not recommended due to the possible increase in plasma concentration of cabergoline. The mechanism of interaction of macrolides with cabergoline has not been sufficiently studied, but, apparently, due to the ability of macrolides and cabergoline to competitively inhibit the cytochrome P450 system.
special instructions
Before the appointment of cabergoline, it is necessary to conduct a full study of the function of the pituitary gland.With increasing doses of the drug, patients should be under the supervision of a physician in order to establish the smallest dose that provides a therapeutic effect. During the period of treatment it is recommended to regularly (once a month) determine the concentration of prolactin in the serum. Normalization of prolactin concentration is usually observed within 2-4 weeks of treatment with cabergoline. After withdrawal of cabergoline, hyperprolactinemia recurs usually, however, in some patients, a persistent decrease in prolactin concentration persists for several months. 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 menstruation is restored, it is recommended to carry out pregnancy tests at least once every 4 weeks during the amenorrhea period, and after menstruation is restored - every time there is a delay of menstruation for more than 3 days. Barrier methods of contraception should be used during treatment with cabergoline, as well as after discontinuation of the drug before repeating anovulation. If pregnancy occurred during treatment, the expediency of discontinuation of the drug should be considered. Women who have become pregnant should be under the supervision of a physician for the timely detection of symptoms of an increase in the pituitary (during pregnancy, an increase in the size of already existing pituitary tumors is possible). After long-term 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, including in the anamnesis. Patients with arterial hypertension that developed during pregnancy (for example, preeclampsia) and / or postpartum arterial hypertension are prescribed cabergoline only when the potential benefit of using the drug significantly exceeds the possible risk. The use of cabergoline causes drowsiness. In patients with Parkinson's disease, the use of dopamine receptor agonists may cause sudden sleep.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 control mechanisms During the period of treatment it is recommended to refrain from driving and other activities that require increased concentration of attention and speed of psychomotor reactions.