Anastrozol Devatis 1 mg Filmtabletten

Description

Anastrozole is a highly selective non-steroidal inhibitor of aromatase enzyme, which in the body of postmenopausal women converts androstenedione in peripheral tissues into estrone and further into estradiol. The therapeutic effect in breast cancer patients is achieved by reducing circulating estradiol levels. In postmenopausal women, anastrozole in a daily dose of 1 mg causes a decrease in estradiol levels by 80%.
He has progestogenic, androgenic and estrogenic activity. Daily dose up to 10 mg has no effect on cortisol and aldosterone secretion. Substitution of corticosteroids is not required. Anastrozole may cause a decrease in bone mineral density in postmenopausal patients with hormone-positive early breast cancer. Anastrozole alone, as well as in combination with bisphosphonates does not change plasma lipid levels.

It is rapidly absorbed, the maximum concentration in plasma is reached within 2 hours after ingestion on an empty stomach. Food slightly reduces the rate of absorption. The rate of reduction has no clinically significant effect on the equilibrium plasma concentration of the drug at a single daily dose. Approximately 90-95% of the equilibrium concentration of anastrozole is reached after 7 days of drug administration. There is no information about time and dose dependence of pharmacokinetic parameters. Age of postmenopausal women does not affect pharmacokinetics. The binding to plasma proteins is 40%.
Anastrozole is eliminated from the body slowly. The plasma elimination half-life is 40-50 hours. Extensively metabolized in postmenopausal women. Unchanged 10% of the dose is excreted with urine within 72 hours after administration. Metabolized by N-dealkylation, hydroxylation and glucuronidation. The major metabolite triazole has no activity. Excretion of metabolites occurs with urine.