the product in the database has an inactive status
indications:
Supplementary treatment in postmenopausal women at an early stage of breast cancer 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 postmenopausal breast cancer, occurring physiologically or artificially induced, in whom the recurrence or progression of the neoplastic process has occurred, which have previously been treated with anti-estrogen drugs. No drug efficacy was found in patients with breast cancer without estrogen receptors.
Composition:
1 tabl powl. contains 2.5 mg letrozole.
Action:
Anti-cancer drug - a non-steroidal aromatase inhibitor (an inhibitor of estrogen biosynthesis). Letrozole inactivates aromatase by competitively binding to the aromatase-cytochrome P-450 complex, which leads to the inhibition of estrogen biosynthesis in all tissues. Inhibition of tumor growth stimulation by estrogens is essential in the treatment of cancer in cases where the growth of cancerous tissue depends on the presence of estrogen and endocrine treatment is used. LetrozoI is rapidly and completely absorbed from the gastrointestinal tract (bioavailability - 99.9%). Food slightly reduces the rate of absorption of the drug, but has no effect on bioavailability. About 60% is bound to plasma proteins. The main route of elimination of letrozole is metabolism to a pharmacologically inactive metabolite - carbinol - which is mediated by the CYP3A4 and CYP2A6 isoenzymes. The drug is mainly excreted in the urine. T0,5 in the final phase of elimination is 2 days. Steady state is achieved within 2-6 weeks. Steady state concentrations are approximately 7-fold higher than concentrations measured after a single 2.5 mg dose. Renal impairment (daily creatinine clearance 9-116 ml / min) and mild to moderate hepatic impairment do not affect the pharmacokinetics of Ietrozole. In the case of severe hepatic insufficiency, the availability of the drug and the half-life in the final phase of elimination increase 2-3-fold.
Contraindications:
Hypersensitivity to letrozole or other components of the preparation. Pregnancy, breast-feeding. Do not use in pre-menopausal women.
Precautions:
The preparation is not indicated for use in children. For patients with creatinine clearance <10 ml / min and severe hepatic impairment, the benefit and risk of treatment should be carefully considered. Letrozole strongly reduces estrogen concentration. Patients who have a history of osteoporosis and / or fracture or who are at increased risk of osteoporosis should have, prior to initiating adjuvant or extended adjuvant treatment, densitometric bone density tests and should be monitored for the development of osteoporosis during treatment and after treatment. Treatment and prevention of osteoporosis should be introduced as justified and carefully monitored.
Pregnancy and lactation:
The preparation is contraindicated for use during pregnancy and during breastfeeding. In perimenopausal women who may become pregnant prior to starting treatment, a pregnancy test should be performed and an appropriate method of contraception should be used until the postmenopausal state has been confirmed.
Side effects:
Very common: joint pain; increased sweating; hot flashes, fatigue, including weakness. Common: lack of appetite, increased appetite, hypercholesterolemia; depression; headache, dizziness; nausea, vomiting, indigestion, constipation, diarrhea; alopecia, rash (including erythematous rash and maculopapular rash reminiscent of psoriatic, follicular); muscle pain, bone pain, osteoporosis, bone fractures; malaise, peripheral edema; weight gain.Uncommon: urinary tract infections; cancer pain (not applicable to adjuvant treatment and prolongation of adjuvant therapy); leucopenia; general edema; anxiety including irritability and irritability; drowsiness, insomnia, impaired memory, abnormal sensation including paraesthesia, hypoaesthesia, impaired taste, cerebral stroke; cataracts, eye irritation, blurred vision; palpitations, tachycardia; thrombophlebitis, including superficial and deep vein thrombophlebitis, hypertension, ischemic heart disease; shortness of breath, cough; abdominal pain, stomatitis, dry mouth; increase in liver enzymes; pruritus, dry skin, urticaria; arthritis; increasing the frequency of urination; bleeding from the genital tract, abundant white vaginal discharge, dry vagina, breast pain; fever, dry mucous membranes, thirst; weight loss. Rare: pulmonary embolism, arterial thrombosis, ischemic stroke.
Dosage:
Orally. Adult and elderly patients: The recommended dose is 2.5 mg once a day. Follow-up treatment should be continued for 5 years or until tumor disease returns. In adjuvant treatment, clinical experience is 2 years, and in extended adjuvant treatment - 4 years. In patients with advanced breast cancer or metastatic breast cancer, treatment should be continued until evidence indicates the progression of the cancer process. Patients with a creatinine clearance> 30 ml / min do not require dose adjustment. There are insufficient data on patients with creatinine clearance <30 ml / min and in patients with severe hepatic impairment.
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