Index of drugs

Supplementary treatment in postmenopausal women with invasive early breast cancer with the presence of estrogen receptors after 2-3 years of initial adjuvant treatment with tamoxifen. Treatment of advanced breast cancer in women during natural or post-menopausal treatment in whom the disease has progressed after antioestrogen therapy. Exestin was not shown to be effective in patients who have not detected estrogen receptors in tumor cells.

1 tabl powl. contains 25 mg of exemestane. The tablets contain mannitol (90.40 mg).

Anti-cancer drug - an irreversible, steroidal aromatase inhibitor, structurally similar to the naturally occurring androstendione. Blocks the biosynthesis of estrogen by inhibiting aromatase. Decreased estrogen concentration is an effective and selective way to treat hormone-dependent breast cancer in postmenopausal women. It has no oestrogenic or progestagenic activity, while low androgenic activity has been observed as a result of high doses of the drug. It does not affect the synthesis of cortisol or aldosterone, both without and after ACTH stimulation; no substitution of glucocorticosteroids and mineralocorticosteroids is necessary. After oral administration, the drug is rapidly and extensively absorbed from the gastrointestinal tract. The absolute bioavailability of the drug is unknown in humans (most likely it is limited by a strong first-pass effect). Food increases the bioavailability of exemestane. The drug is 90% bound to plasma proteins. It is metabolized by oxidation with CYP3A4 and / or reduction by aldoketoreductase, followed by a coupling process. Metabolites are inactive or aromatase inhibition as a result of their action is less than the drug in unmetabolized form. T_0,5 drug is 24 hours.

Hypersensitivity to the active substance or to any of the excipients. Women before menopause. Pregnancy or breast-feeding.

Exemestane should not be given to pre-menopausal women. Therefore, if necessary, LH, FSH and estradiol should be determined before starting treatment to ensure that the patient is post-menopausal. Use with caution in patients with impaired liver or kidney function. Exemestane is a potent estrogen-lowering compound - at the time of use, patients have been shown to decrease bone mineral density and increase the frequency of fractures. When initiating complementary treatment with an evicted test, bone mineral density should be determined in patients with osteoporosis or a risk of developing osteoporosis based on current clinical guidelines and practice. In patients with advanced disease, bone mineral density (BMD) should be individually determined. Patients treated with exemestane should closely monitor and implement osteoporosis treatment or prophylaxis in patients at risk. Before starting treatment with an aromatase inhibitor, routine determination of 25-hydroxyvitamin D should be considered from the view of the high incidence of severe deficiency in women with early breast cancer (EBC). Women with vitamin D deficiency should receive supplementary treatment for this vitamin deficiency.

The drug is contraindicated during pregnancy and breastfeeding.

Very common: insomnia, headache, hot flushes, nausea, increased sweating, joint pain and musculoskeletal pain (including joint pain, less frequently limb pain, osteoarthritis, backache, arthritis, muscular pain and joint stiffness) ), feeling of excessive fatigue. Common: anorexia, depression, dizziness, carpal tunnel syndrome, paresthesia, abdominal pain, vomiting, constipation, dyspepsia, diarrhea, rash, alopecia, urticaria, pruritus, osteoporosis, bone fractures, pain, peripheral edema. Uncommon: leukopenia, hypersensitivity, drowsiness, hepatitis, cholestatic hepatitis, increased bilirubin, increased ALP, acute generalized pustular rash, weakness. Rare: thrombocytopenia. Frequency unknown: decreased number of lymphocytes.Severe thrombocytopenia and leukopenia have been reported rarely in patients with advanced breast cancer; in approximately 20% of patients, sporadic reductions in the number of lymphocytes in the blood have been observed, especially in those with pre-treatment lymphopenia (these have not been observed in early-stage patients). In the early breast cancer (IES) study, the incidence of ischemic events in the exemestane and Tamoxifen treated groups was 4.5% and 4.2%, respectively. There were no significant differences in the incidence of cardiac complications (arterial hypertension, myocardial infarction and heart failure) for exemestane compared to tamoxifen. In the IES study, exemestane was associated with a higher incidence of hypercholesterolemia compared with tamoxifen (3.7% vs. 2.1%). In the IES study, a higher incidence of gastric ulcer was observed in the exemestane group compared to the tamoxifen group (0.7% and <0.1% respectively); the majority of patients receiving exemestane who were diagnosed with a stomach ulcer took NSAIDs simultaneously and / or in the past.

Orally. Adults (also elderly patients): the recommended dose is 1 tablet. once a day. In patients with early breast cancer, treatment should be managed so that the total time of hormonal combination therapy (tamoxifen followed by exemestane) is 5 years, or it should be terminated earlier if tumor recurs. In patients with advanced breast cancer, treatment with exemestane should be continued until a definite tumor progression is observed.Special groups of patients. No dosage adjustment is required in patients with renal or hepatic impairment. The preparation is not indicated for use in children and adolescents.Way of giving. The drug should be taken preferably after a meal.