Active substanceCabergolineCabergoline
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  • Dostinex®
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  • Cabergoline
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  • Dosage form: & nbspPills.
    Composition:
    Each tablet contains:
    active substance: cabergoline 0.5 mg;
    excipients: lactose 75.9 mg, leucine 3.6 mg.
    Description:White flat oblong tablets marked "P" and "U", separated by a notch on one side and "700" with short notches on the top and bottom of the number - on the other hand.
    Pharmacotherapeutic group:Dopamine receptor agonist
    ATX: & nbsp

    G.02.C.B.03   Cabergoline

    Pharmacodynamics:

    Cabergoline is a dopaminergic derivative of ergoline and is characterized by a pronounced and prolonged prolactin-lowering effect due to direct stimulation D2dopamine receptors of lactotrophic cells of the pituitary gland. In addition, when taking higher doses compared with those for lowering the concentration of prolactin in the blood plasma, cabergoline has a central dopaminergic effect due to stimulation D2receptors.

    Reduction in the concentration of prolactin in the blood plasma is notedwithin 3 hours after taking the drug and persists for 7-28 days in healthy volunteers and patients with hyperprolactinaemia, 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 hormones of the pituitary and cortisol. The prolactin-lowering effect of cabergoline is dose-dependent, both in terms of severity and duration of action.

    The pharmacodynamic effects of cabergoline, not related to the therapeutic effect, are only a reduction in blood pressure (BP). With a single dose of the drug, the maximum hypotensive effect is noted within the first 6 hours and is dose-dependent.

    Pharmacokinetics:Cabergoline quickly absorbed from the gastrointestinal tract, the maximum concentration in the blood plasma is reached after 0.5-4 hours, the connection with the proteins of the blood plasma is 41-42%. The half-life of cabergoline, estimated by the rate of excretion by the kidneys, is 63-68 hours in healthy volunteers and 79-115 hours in patients with hyperprolactinaemia. Due to the long half-life, the equilibrium concentration is reached after 4 weeks.Ten days after the administration of cabergoline, approximately 18% and 72% of the dose are detected in urine and feces, respectively, and the proportion of unchanged cabergoline in 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. The content in the urine of 3 additional metabolites does not exceed 3% of the accepted dose. It has been established that metabolic products have a significantly lower effect on the inhibition of prolactin secretion compared to cabergoline. The intake of food does not affect the absorption and distribution of cabergoline.
    Indications:
    - Prevention of physiological lactation after childbirth.
    - Suppression of already established postpartum lactation.
    - Treatment of disorders associated with hyperprolactinemia, including amenorrhea, oligomenorrhoea, anovulation, galactorrhea.
    - Prolactin-secreting adenomas of the pituitary gland (micro- and macro-prolactinomas); idiopathic hyperprolactinaemia; syndrome of the "empty" Turkish saddle in combination with hyperprolactinemia.
    Contraindications:
    - increased sensitivity to cabergoline or other components of the drug, as well as to any ergot alkaloids.
    - disturbance of the function of the heart and respiration due to fibrotic changes or the presence of such conditions in the anamnesis.
    - with prolonged therapy: anatomical signs of the pathology of the valvular heart apparatus (such as, valve flap thickening, constriction of the valve lumen, mixed pathology narrowing and stenosis of the valve), confirmed by echocardiography (EchoCG) performed prior to initiation of therapy.
    - use in children and adolescents under the age of 16 (safety and efficacy of the drug are not established).
    - lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
    Carefully:
    Like other ergot derivatives, Dostinex® should be administered with caution under the following conditions and / or diseases:
    - arterial hypertension that has developed during the pregnancy, for example, pre-eclampsia or postpartum arterial hypertension (Dostinex® is prescribed only in cases where the potential benefit from the use of the drug significantly exceeds the possible risk);
    - severe cardiovascular diseases, Raynaud's syndrome;
    - peptic ulcer, gastrointestinal bleeding;
    - severe hepatic insufficiency (use of lower doses is recommended);
    - severe psychotic or cognitive impairment (including anamnesis);
    - simultaneous use with drugs that have hypotensive effect (due to the risk of developing orthostatic arterial hypotension).
    Pregnancy and lactation:Since controlled clinical studies using the drug Dostinex ® in pregnant women have not been conducted, the appointment of the drug during pregnancy is possible only in cases of extreme necessity, taking into account the benefit / risk ratio for the woman and the fetus.
    If the pregnancy occurred against the background of treatment with the drug Dostinex ®, should consider the desirability of drug withdrawal, also considering the benefit / risk ratio.
    According to available data, the use of the drug Dostinex® at a dose of 0.5-2 mg per week for violations associated with hyperprolactinaemia was not accompanied by an increase in the frequency of miscarriages, premature births, multiple pregnancies and congenital malformations.
    There is no information on excretion of the drug with breast milk, however, in the absence of the effect of using Dostinex ® to prevent or suppress lactation, mothers should refuse breastfeeding.For violations related to hyperprolactinemia, Dostinex® is contraindicated in patients planning breastfeeding.
    Dosing and Administration:

    Inside, with food.

    Prevention of lactation: 1 mg once (2 tablets of 0.5 mg), on the first day after childbirth.

    Suppression of steady lactation: 0.25 mg (1/2 tablet) twice a day every 12 hours for two days (the total dose is 1 mg). In order to reduce the risk of orthostatic arterial hypotension in breast-feeding mothers, a single dose of the drug Dostinex® should not exceed 0.25 mg.

    Treatment of disorders associated with hyperprolactinemia: the recommended initial dose is 0.5 mg per week in a single dose (1 tablet 0.5 mg) or in two divided doses (1/2 tablet 0.5 mg, 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 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 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. In patients with hypersensitivity to dopaminergic drugs, the likelihood of developing side effects can be reduced by starting therapy with Dostinex® at a lower dose (for example, 0.25 mg once a week), then gradually increasing it to achieve a therapeutic dose. For improvement tolerability of the drug in the emergence of severe side effects may be a temporary dose reduction followed by a more gradual increase (for example, an increase of 0.25 mg per week every two weeks).

    Side effects:

    In clinical trials using the Dostinex® drug for prevention of physiological lactation (1 mg once) and for suppression of lactation (0.25 mg every 12 hours for 2 days), side effects were reported in approximately 14% of women. When using Dostinex ® for 6 months at a dose of 1-2 mg per week, divided into 2 doses, for the treatment of disorders associated with hyperprolactinemia, The incidence of adverse events was 68%.Adverse events occurred mainly during the first 2 weeks of therapy and in most cases disappeared with the continuation of therapy or a few days after the abolition of the drug Dostinex ®. Adverse events were usually transient, in severity - poorly or moderately expressed and were dose-dependent. At least once during therapy severe adverse events were noted in 14% of patients; Due to side effects, treatment was discontinued in approximately 3% of patients.

    The most common side effects are presented below:

    From the cardiovascular system: a feeling of palpitations; with prolonged use of Dostinex ® usually has an antihypertensive effect, in some cases, orthostatic arterial hypotension may occur; possibly asymptomatic decrease in blood pressure during the first 3-4 days after delivery (systolic - no less than 20 mm Hg, diastolic - no less than 10 mm Hg).

    From the nervous system: dizziness / vertigo, headache, fatigue, drowsiness, depression, asthenia, paresthesia, fainting, nervousness, anxiety, insomnia, impaired concentration.

    From the digestive systemNausea, vomiting, epigastric pain, abdominal pain, constipation, gastritis, dyspepsia, dryness of the oral mucosa, diarrhea, flatulence, toothache, feeling pharyngeal mucosa irritation.

    Other: mammalgia, dysmenorrhea, epistaxis, rhinitis, "tides" of blood to the skin, transient hemianopsia, spasms of blood vessels of the fingers and lower limbs muscle cramps (like other ergot derivatives, Dostineks® may have vasoconstrictor effect), blurred vision, flu-like symptoms, malaise , periorbital and peripheral edema, anorexia, acne, skin itching, joint pain.

    With prolonged therapy with the use of the drug Dostinex ® deviation from the standard of laboratory indicators was noted rarely; in women with amenorrhea, there was a decrease in hemoglobin levels during the first few months after the recovery of menstruation.

    The post-marketing study account also the following side effects associated with taking cabergoline: alopecia, increased creatinine phosphokinase activity in blood, mania, dyspnea, edema, fibrosis,liver function abnormalities, liver function abnormalities, hypersensitivity reactions, rash, respiratory disorders, respiratory failure, valvulopathy, pathological gambling addiction, hypersexuality, increased libido, aggressiveness, psychotic disorders, pericarditis, sudden falling asleep, weight gain or decrease , nasal congestion.

    Overdose:
    Symptoms of overdose (probably, symptoms of hyperstimulation of dopamine receptors): nausea, vomiting, dyspeptic disorders, orthostatic arterial hypotension, confusion, psychosis, hallucinations.
    In case of overdose, ancillary measures should be taken to remove the non-sucking drug (gastric lavage) and, if necessary, maintain blood pressure. Dopamine antagonists may be prescribed.
    Interaction:
    Information on the interaction of cabergoline and other ergot alkaloids is absent, so the simultaneous use of these drugs during long-term therapy with Dostinex® is not recommended.
    Because the cabergoline has a therapeutic effect by direct stimulation of dopamine receptors, it can not be administered simultaneously with drugs acting as dopamine antagonists (phenothiazines, butyrophenones, thioxanthenes, metoclopramide and others), t. they can weaken the action of cabergoline, aimed at reducing the concentration of prolactin. Like other ergot derivatives, cabergoline Do not use concomitantly with macrolide antibiotics (eg, erythromycin), because this can lead to an increase in the systemic bioavailability of cabergoline.
    Special instructions:
    Before the appointment of the drug Dostinex ® for the treatment of violations associated with hyperprolactinemia, it is necessary to conduct a full study of the pituitary gland function. In addition, an assessment should be made of the condition of the cardiovascular system, including EchoCG, in order to detect abnormalities in valve function that occur asymptomatically.
    As with other ergot derivatives, after prolonged administration of cabergoline, patients experienced pleural effusion / pleural fibrosis and valvulopathy. In some cases, patients received previous therapy with dopamine agonist agonists.Therefore, Dostinex ® should not be used in patients with existing signs and / or clinical symptoms of cardiac or respiratory function disorder associated with fibrotic changes or with such conditions in the anamnesis. It is necessary to cancel taking the drug in case of signs of appearance or deterioration of blood regurgitation, narrowing of the lumen of the valves or thickening of valve flaps (see section "Contraindications").
    It was found that the rate of erythrocyte sedimentation increases with the development of pleural effusion or fibrosis. In the case of an unexplained increase in the rate of erythrocyte sedimentation, radiographic examination of the chest is recommended. In the diagnosis can also help study the concentration of creatinine in the blood plasma, the evaluation of renal function. After discontinuation of the drug Dostinex ® in patients with pleural effusion / pleural fibrosis or valvulopathy, symptoms improved.
    It is not known whether cabergoline worsen the condition of patients with signs of regurgitation of blood. Cabergoline It should not be used in the detection of fibrous lesions of the valvular heart apparatus (see Fig.section "Contraindications"). Fibrotic disorders can develop asymptomatically. In this regard, the condition of patients receiving long-term therapy with cabergoline and paying particular attention to the following symptoms should be regularly monitored:
    - pleuro-pulmonary disorders: such as shortness of breath, difficulty breathing, an impassable cough or pain in the chest;
    - renal failure or obstruction of the vessels of the ureters or abdominal organs that may be accompanied by pain in the side or in the lumbar region and edema of the lower extremities, any swelling or tenderness when touching the abdomen, which may indicate the development of retroperitoneal fibrosis;
    - Pericardial fibrosis and fibrosis of the valves of the heart valves often manifest as heart failure. In this regard, it is necessary to exclude the fibrosis of the valves of the heart valves (and constrictive pericarditis) with the appearance of symptoms of heart failure.
    It is necessary to regularly monitor the patient's condition for the development of fibrotic disorders. The first time EchoCG should be performed 3-6 months after the start of therapy.This study should then be performed depending on the clinical evaluation of the patient's condition, paying special attention to the symptoms described above, at least every 6-12 months of therapy.
    The need for other monitoring methods (for example, physical examination, including auscultation of the heart, radiography, computed tomography) is assessed individually for each patient.
    With increasing doses, patients should be under the supervision of a physician to establish the lowest effective dose that provides a therapeutic effect. After the effective dosing regimen is selected, it is recommended to conduct a regular (once a month) determination of the concentration of prolactin in the serum. Normalization of prolactin concentration is usually observed within 2-4 weeks of treatment.
    After the abolition of the drug Dostinex®, a relapse of hyperprolactinemia is usually observed, however, in some patients persistent inhibition of prolactin concentration is observed for several months. In most women, ovulatory cycles persist for at least 6 months after discontinuation of the Dostinex® drug.
    Dostinex® restores ovulation and fertility in women with hyperprolactinemic hypogonadism. Since pregnancy can occur before the recovery of menstruation, it is recommended that pregnancy tests be performed at least once every 4 weeks during the amenorrhea period, and after the recovery of menstruation, every time the menstrual period is delayed by more than 3 days. Women who want to avoid pregnancy should use barrier methods of contraception during treatment with Dostinex®, and after the drug is discontinued before the anovulation recurs. Women who have become pregnant should be under the supervision of a doctor to detect symptoms of pituitary gland enlargement in time, since during pregnancy it is possible to increase the size of pre-existing pituitary tumors.
    Dostinex® should be administered at lower doses to patients with severe hepatic impairment (Child-Pugh class C), who show prolonged therapy with the drug. With a single dose of 1 mg to such patients, there was an increase in AUC (area under the concentration-time curve) compared with healthy volunteers and patients with lessmarked hepatic insufficiency.
    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 the drug Dostinex® or discontinue therapy.
    Studies on the use of the drug in elderly patients with impairments associated with hyperprolactinemia have not been conducted. The safety and efficacy of the drug in children younger than 16 years is not established.
    Effect on the ability to drive transp. cf. and fur:Patients taking the drug Dostinex ® should refrain from managing vehicles and mechanisms and other potentially dangerous activities requiring concentration of attention and speed of psychomotor reactions.
    Form release / dosage:
    Tablets 0.5 mg.
    Packaging:
    2 or 8 tablets in a bottle of dark glass type I, closed with a screwed aluminum cover with a plastic insert containing a drying agent and porous paper on the bottom. 1 bottle with instructions for use in a cardboard pack.
    Storage conditions:At a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:2 years.Do not use after expiry date.
    Terms of leave from pharmacies:On prescription
    Registration number:П N013905 / 01
    Date of registration:19.11.2007/14.10.2015
    The owner of the registration certificate:Pfizer Italy Sr.L.Pfizer Italy Sr.L. Italy
    Manufacturer: & nbsp
    Representation: & nbspPfizer H. Si. Pi. CorporationPfizer H. Si. Pi. Corporation
    Information update date: & nbsp26.04.2016
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