Aromeston (Aromeston)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceExemestanExemestan
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    • Dosage form: & nbspfilm coated tablets
    Composition:

    1 tablet, film-coated, contains:

    active substance: exestan - 25 mg;

    Excipients: mannitol - 57.175 mg, microcrystalline cellulose - 10,4 mg, primogel (sodium carboxymethylstarch) - 4.5 mg. polysorbate (tween 80) - 0,2 mg, hypromellose (hydroxypropylmethylcellulose) - 1.5 mg, copsandadditional (Plasdon ES-630) - 0,4 mg, silicon dioxide colloid (aerosil) - 0.2 mg, magnesium stearate - 0.625 mg;

    film coating composition: Opadrai II white 3 mg [hypromellose (hydroxypropylmethylcellulose) - 0.84 mg, lactose monohydrate - 1.08 mg, macrogol (polyethylene glycol 4000) - 0.3 mg. titanium dioxide 0.78 mg].

    Description:Round, biconvex tablets, covered with a film shell of white or almost white color
    Pharmacotherapeutic group:Antitumor agent - estrogen synthesis inhibitor
    ATX: & nbsp

    L.02.B.G.06   Exemestan

    Pharmacodynamics:

    Exemestane is an irreversible steroid aromatase inhibitor, similar in structure to the natural substance androstenedione.In postmenopausal women, estrogens are produced primarily by converting androgens to estrogens under the action of the aromatase enzyme in peripheral tissues. Blocking the formation of estrogen by inhibiting aromatase is an effective and selective method for treating hormone-dependent breast cancer in postmenopausal women. The mechanism of action of exemestane is due to the fact that it irreversibly binds to the active center of aromatase, causing its inactivation. In postmenopausal women exemastane significantly reduces the concentration of estrogens in the blood serum, starting at a dose of 5 mg, with a maximum reduction (> 90%) achieved with doses of 10-25 mg. Patients in postmenopausal women with breast cancer, exemastane, taken daily in a dose of 25 mg, reduces the total level of the aromatase enzyme in the body by 98%. Exemestan does not possess progestogen and estrogenic activity. Only minor androgenic activity is revealed, mainly with the use of high doses.

    Exemestane has no effect on the biosynthesis of cortisol and aldosterone in the adrenal glands, which confirms the selectivity of the drug.In this regard, there is no need for replacement therapy with glucocorticosteroids and mineralocorticosteroids.

    When the drug is used, even at low doses, a slight increase in the levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) in the blood serum is observed, which is characteristic of the drugs of this pharmacological group and probably develops on the basis of feedback at the pituitary level: a decrease in the concentration of estrogens stimulates the secretion of gonadotropins in the pituitary gland.
    Pharmacokinetics:

    After oral administration exemastane is rapidly absorbed, absolute bioavailability is not established. It is assumed that it is limited by the pronounced effect of "first passage" through the liver. With a single dose of 25 mg, the maximum concentration in the blood plasma (Cmax), equal to 17 ng / ml, is achieved after 2 hours. Simultaneous food intake increases the bioavailability of exemestan by 40%. Pharmacokinetic parameters are linear. Linkage to plasma proteins is approximately 90%. Exemestan and its metabolites do not bind to erythrocytes. At repeated reception of unpredictable cumulation eksemestana it is not observed.

    The process of biotransformation of exemestane is carried out by oxidation of the methylene group in the 6 position under the action of the isoenzyme CYP3A4 and / or reduction of the 17-keto group under the action of aldocode-reductase followed by conjugation. Exemestane metabolism products are either inactive or less active with respect to aromatase inhibition than the parent compound. The final half-life is approximately 24 hours. Approximately equal amounts of exemestane (about 40%) are excreted by the kidneys and through the intestine within a week. From 0.1 to 1% is excreted by the kidneys unchanged.

    A marked relationship between the systemic effects of the drug and age is not established.

    In patients with severe renal insufficiency (creatinine clearance (CK) <30 ml / min.), The systemic effect of exemestane at 2 times higher, however, dose adjustment is not required.

    In patients with moderate or severe hepatic insufficiency, the systemic effect of exemestan is 2 to 3 times higher, however, dose adjustment is not required.

    Indications:

    - Common breast cancer in women in natural or induced postmenopausal women with progression of the disease on the background of anti-estrogen therapy,as well as with the progression of the disease after repeated use of various types of hormonal therapy.

    - Adjuvant therapy for the initial stage of breast cancer with positive estrogen receptors or unspecified receptor status in postmenopausal women after the completion of 2-3 years of initial adjuvant tamoxifen therapy to reduce the risk of relapse (distant or regional) and contralateral breast cancer.

    Contraindications:

    Hypersensitivity to exemestane or any other component of the drug. Premenopausal endocrine status.

    Simultaneous use with preparations containing estrogens.

    Pregnancy and lactation.

    Child age (data on effectiveness and safety are absent).

    Carefully:

    Impaired liver or kidney function. Insufficiency of lactase, lactose intolerance, glucose-galactose malabsorption (in the drug form of the drug contains lactose).

    Dosing and Administration:

    Inside.

    Adults, including elderly patients

    The recommended dose is 25 mg once a day, after a meal.

    In patients with the initial stage of breast cancer, treatment with the drug is recommended to continue until the total duration of successive adjuvant hormone therapy reaches 5 years.

    Treatment of patients with advanced breast cancer is long. If signs of progression of the tumor develop, treatment with exemestane should be discontinued.

    Hepatic or renal insufficiency Correction of the dose is not required.

    Side effects:

    Side effects are usually minor or moderately severe.

    The undesirable reactions distributed over the body systems and frequency are listed below: very often (> 10%), often (> 1%, ≤10%), infrequently (> 0.1%, ≤ 1%), rarely (> 0.01 %, ≤ 0,1%).

    From the side of the digestive system: very often - nausea; often - anorexia, abdominal pain, vomiting, constipation, dyspepsia, diarrhea;

    From the nervous system: very often - insomnia, headache; often - depression, dizziness, carpal tunnel syndrome;

    From the side of the cardiovascular system: very often - "tides" of blood to the face;

    From the skin and skin appendages: very often sweating; often - skin rash, alopecia;

    From the musculoskeletal system: very often joint and musculoskeletal pain;

    Other: very often - increased fatigue; often - pain is not specified localization, peripheral edema or swelling of the legs.

    Approximately 20% of patients (especially in patients with initial lymphopenia) experienced a periodic decrease in the number of lymphocytes. However, the average number of lymphocytes in these patients did not change significantly with time and there was no concomitant increase in the incidence of viral infections.

    Sometimes there was an increase in the activity of "liver" transaminases and alkaline phosphatase, mainly in patients with metastases to the liver and bones, as well as in the presence of other liver damage (the connection with the drug is not established).

    Overdose:

    A single dose of the drug, which could cause the appearance of life-threatening symptoms, is not established. The use of exemestane in a single dose up to 800 mg in healthy women and in a daily dose of up to 600 mg in postmenopausal women with advanced breast cancer was well tolerated. Treatment is symptomatic under regular monitoring of vital functions and careful monitoring. There are no specific antidotes.

    Interaction:

    Preparations containing estrogens completely neutralize the pharmacological action of exemestane.

    The drug is metabolized by isoenzyme CYP3A4 cytochrome P450 and aldoketoreductases, and does not inhibit any of the major cytochrome P450 isoenzymes.

    The specific inhibition of the CYP3A4 isoenzyme by ketoconazole does not significantly affect the pharmacokinetics of exemestane.

    Powerful inducers of the isoenzyme CYP3A4 (incl. rifampicin, phenytoin, carbamazepine, phenobarbital, preparations of St. John's wort perfumed) can significantly reduce the concentration of exemestane in the blood. Despite the established pharmacokinetic interaction of exemestane with rifampicin, a strong inducer of CYP3A4, the pharmacological activity of exemestane (suppression of estrogens) remains unchanged, so dose adjustment is not required.

    Special instructions:

    Exemestane should not be given to women in pre-menopause, therefore, in those cases where it is clinically justified, postmenopausal status should be confirmed by determining the concentration of LH, FSH and estradiol.

    Exemestane should not be prescribed concomitantly with preparations containing estrogens.

    Effect on the ability to drive transp. cf. and fur:Patients should be warned about the possibility of appearance during treatment with exemestan drowsiness, asthenia and dizziness. If these symptoms occur, patients are advised to refrain from driving and practicing other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
    Form release / dosage:

    Tablets, film-coated 25 mg.

    Packaging:

    10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    30 tablets in a bike made of polymer materials.

    1 jar or 3 contour packs of 10 tablets together with instructions for use in a pack of cardboard.

    Storage conditions:

    At a temperature of no higher than 30 ° C. Keep out of the reach of children.

    Shelf life:

    2 of the year. Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-006090/10
    Date of registration:29.06.2010 / 02.10.2015
    Expiration Date:Unlimited
    The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia
    Manufacturer: & nbsp
    Information update date: & nbsp25.09.2017
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