Index of drugs

Supplementary treatment of postmenopausal women with early stage of breast cancer who have been diagnosed with hormone receptors. Prolonged follow-up treatment in postmenopausal patients with hormone-dependent early-stage breast cancer, following standard supplementary treatment with Tamoxifen for 5 years. First-line treatment of advanced hormone-dependent breast cancer in postmenopausal women. Treatment of advanced breast cancer in postmenopausal women who are physiologically or artificially induced, who have had a recurrence or progression of the cancer process and who have previously been treated with anti-estrogen drugs. Neoadjuvant treatment of HER-2-negative breast cancer with hormone receptors in postmenopausal women, in whom chemotherapy is not appropriate treatment, and immediate surgery is not indicated. No drug efficacy was found in patients with hormone-free breast cancer.

1 tabl powl. contains: 2.5 mg letrozole; Table. contain lactose.

Anti-cancer drug - a non-steroidal aromatase inhibitor (an inhibitor of estrogen biosynthesis). Inhibition of tumor growth stimulation by estrogens is of fundamental importance in cancer therapy, in the case where the growth of cancerous tissue depends on the presence of estrogens and endocrine therapy is used. The drug inhibits aromatase by competing for the binding site in the heme group of the aromatase-cytochrome P-450 complex. This leads to the reduction of estrogen biosynthesis in all tissues in which aromatase is present (also in tumor tissue). Letrozole is highly specific in inhibiting aromatase activity. In postmenopausal women, daily doses of letrozole 0.1-5 mg do not cause changes in cortisol, aldosterone, 11-deoxycortisol, 17-hydroxyprogesterone and ACTH in plasma, plasma renin activity, LH and FSH levels, or thyroid function. Letrozole is rapidly and completely absorbed from the gastrointestinal tract, reaching C_max within 1 h (food slightly reduces the rate of absorption). The average absolute bioavailability is 99.9%. The drug is associated with plasma proteins in approximately 60%, mainly with albumin. The concentration of letrozole in erythrocytes accounts for approximately 80% of the plasma concentration. The main route of elimination of letrozole is metabolism to a pharmacologically inactive carbinol metabolite; CYP3A4 and CYP2A6 participate in it. The drug is mainly excreted in the urine. T_0,5 in the final phase of elimination is 2 days. Steady state is achieved within 2-6 weeks.

Hypersensitivity to letrozole or any of the excipients. Pre-menopausal state. Pregnancy and breastfeeding.

In patients whose postmenopausal condition is not clear, the levels of LH, FSH and / or estradiol should be determined before letrozole treatment to clearly determine the hormonal status in which the patient is. Letrozole should be administered with particular caution and after careful consideration of the benefit-risk balance in patients with creatinine clearance <10 ml / min or with severe hepatic insufficiency (Child-Pugh C). Patients with a history of osteoporosis and / or a history of osteoporosis or an increased risk of osteoporosis should have a bone density test prior to initiation of adjuvant or prolonged adjuvant treatment and should be followed to assess the development of osteoporosis during and after treatment. If appropriate, prophylaxis or treatment of osteoporosis should be recommended and monitored regularly. The drug is not recommended for use in children and adolescents up to 17 years of age. Due to the lactose content, the drug should not be used in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

Patients who may become pregnant (ie women in the perimenopausal or early postmenopausal period) should use effective contraception until the post-menopausal state is fully established. The preparation is contraindicated for use during pregnancy and breast-feeding.

Very common: hypercholesterolemia, hot flushes, increased sweating, joint pain, tiredness (including asthenia, general malaise). Common: anorexia, increased appetite, depression, headache, dizziness, hypertension, nausea, indigestion (only for the treatment of metastatic tumors), constipation, abdominal pain, diarrhea, vomiting, alopecia, rash (including erythematous, maculopapular) , reminiscent of psoriatic, follicular), dry skin, muscle pain, bone pain (only for the treatment of metastatic tumors), osteoporosis, bone fractures, genital tract bleeding, peripheral edema, weight gain. Uncommon: urinary tract infections, cancer pain (only for the treatment of metastatic tumors), leukopenia, anxiety (including nervousness), irritability, drowsiness, insomnia, impaired memory, impaired sensation (including paraesthesia, hypoaesthesia), impaired taste, stroke, cataracts, eye irritation, blurred vision, palpitations (only for the treatment of metastatic cancers), tachycardia, cardiac ischemic events (including new cases or exacerbation of existing angina, angina requiring surgery, myocardial infarction and myocardial ischemia) ), thrombophlebitis (including superficial and deep vein thrombophlebitis), dyspnea, cough, dry mouth, stomatitis (only for the treatment of metastatic tumors), increased liver enzymes, pruritus, urticaria, arthritis, increased the frequency of urination, will go away line from the genital tract, vaginal dryness, breast pain, general swelling, dry mucous membranes, thirst, fever, weight loss. Rare: pulmonary embolism, arterial thrombosis, ischemic stroke. Not known: hepatitis, anaphylactic reaction, angioneurotic edema, toxic epidermal necrolysis, erythema multiforme.

Orally. Adult and elderly patients: 2.5 mg once a day. In patients with advanced breast cancer or metastatic breast cancer, treatment should be continued until there is evidence that the cancer process has progressed. In adjuvant therapy and prolonged adjuvant treatment, treatment should be continued for 5 years or until tumor recurrence, whichever occurs first. In adjuvant therapy, a sequential therapy regimen (letrozole for 2 years followed by tamoxifen for 3 years) may also be considered. In neoadjuvant therapy, letrozole treatment may be continued for 4 to 8 months to achieve optimal tumor reduction; if there is not enough response, stop taking the medicine and schedule the surgery and (or) discuss with the patient further treatment options.Special groups of patients. No dosage adjustment is necessary for patients with renal impairment with creatinine clearance (CCr) ≥10 ml / min; insufficient data on the use of letrozole in patients with CCr <10 ml / min. No dose adjustment is required in patients with mild to moderate hepatic impairment (Child-Pugh A or B); insufficient data on patients with severe hepatic impairment (AUC and T_0,5 letrozole in the final phase may be about two-fold higher, in comparison to patients with normal organ function).
The drug should be taken with or without food.