Index of drugs

Treatment of advanced breast cancer in postmenopausal women who have been found to have an estrogen receptor in the tumor. Supplementary treatment of early breast cancer in postmenopausal women who have been found to have an estrogen receptor in the tumor. Supplementary treatment of early breast cancer in postmenopausal women who have been found to have an estrogen receptor in the tumor after 2-3 years of adjuvant tamoxifen.

1 tabl powl. contains 1 mg of anastrozole (and 87 mg of lactose).

A strong and highly selective non-steroidal aromatase inhibitor involved in the conversion of Androstenedione to estrone (then converted to estradiol) in peripheral tissues. In postmenopausal women, anastrozole 1 mg daily causes suppression of oestradiol production by over 80%. Anastrozole has no progestagen, androgenic and estrogenic activity. Anastrozole administered at a dose of up to 10 mg daily does not affect the secretion of cortisol and aldosterone both without and after stimulation of secretion by ACTH (no corticosteroid supplementation is required during treatment). Following oral administration, anastrozole is rapidly absorbed from the gastrointestinal tract. The maximum concentration in the blood usually occurs within 2 hours of admission (fasting). Food reduces the rate of absorption to a small extent, but does not affect its degree. In postmenopausal women the pharmacokinetics of anastrozole is not age dependent. The drug binds to 40% of plasma proteins. In postmenopausal women, anastrozole is extensively metabolised, less than 10% of the dose is excreted in urine unchanged within 72 hours of admission. It is metabolized by N-dealkylation, hydroxylation and glucuronidation. Metabolites are mainly excreted in the urine. T_0,5 is 40-50 h.

Hypersensitivity to the active substance or to any of the excipients. Pregnancy and breastfeeding.

It should not be used in pre-menopausal women; diagnosis of menopause should be determined based on the results of hormonal tests - the concentration of LH, FSH and / or estradiol. There are no data on the concomitant use of anastrozole and LHRH analogues. The simultaneous use with Tamoxifen or oestrogens should be avoided as it may reduce the pharmacological effect of anastrozole. Anastrozole reduces the concentration of estrogen in the blood, so it can cause a decrease in bone mineral density, and consequently increase the risk of fractures - women with or with the risk of osteoporosis should have a bone densitometry performed at the beginning of treatment and then at regular intervals during therapy. If there are indications, treatment or prevention of osteoporosis should be implemented and closely monitored; the use of specialized treatment with, for example, bisphosphonates may stop further bone demineralization and should be considered. Anastrozole has not been studied in patients with breast cancer and moderate or severe kidney problems. In patients with severe renal impairment, exposure to anastrozole (GRF <30 ml / min) is not increased; in patients with severely impaired renal function anastrozole should be used with caution. Patients with hepatic impairment may have increased exposure to anastrozole. Anastrozole has not been studied in patients with breast cancer and moderate or severe hepatic impairment - use caution; treatment should be based on an assessment of the benefits and risks in each patient. The preparation should not be used in boys with growth hormone deficiency in combination with growth hormone therapy (efficacy has not been demonstrated and safety has not been established). It must not be used in girls who are deficient in growth hormone as a supplement to growth hormone therapy. Due to the lactose content, the preparation should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of Glucose and galactose.

The drug is contraindicated during pregnancy and breastfeeding.

Very common: headache, hot flushes, nausea, rash, joint pain and stiffness, arthritis, osteoporosis, weakness. Common: anorexia, hypercholesterolemia, drowsiness, carpal tunnel syndrome, diarrhea, vomiting, ALP, ALT and AST elevation, thinning and thinning (alopecia), allergic reactions, bone pain, muscle pain, vaginal dryness, vaginal bleeding (usually patients with advanced breast cancer, during the first few weeks after switching from hormonal therapy to anastrozole therapy, if bleeding is prolonged, a change in treatment should be considered). Uncommon: hypercalcemia (with or without increase in parathyroid hormone), increase in GGTP activity, increase in serum bilirubin, hepatitis, urticaria, skipping fingers. Rare: erythema multiforme, anaphylactoid reaction, dermatitis (including cases of Henoch-Schonlein purpura). Very rare: Stevens-Johnson syndrome, angioneurotic edema.

Orally. Adult patients (including the elderly): 1 mg once a day. In postmenopausal patients with early breast cancer who have been found to have an estrogen receptor in the tumor, hormone replacement therapy is recommended for 5 years.Special groups of patients. No dose adjustment is required in patients with mild or moderate renal impairment or with mild hepatic insufficiency. Caution should be used when treating patients with severely impaired renal function or severe hepatic impairment. The drug is not recommended for use in children and adolescents (insufficient data on safety and efficacy).