Anastrozole

An antitumor agent. Is a selective nonsteroidal inhibitor of aromatase. In postmenopausal women, estradiol is mainly produced from estrone, which is produced in peripheral tissues by conversion from Androstenedione (with the participation of the enzyme aromatase). The reduction of circulating levels of estradiol exerts a therapeutic effect in women with breast cancer. In postmenopausal women anastrozole at a daily dose of 1 mg causes a decrease in estradiol by 80%. Anastrozole does not possess progestogenic, androgenic and estrogenic activity; in therapeutic doses does not affect the secretion of cortisol and aldosterone.

After intake of anastrozole is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached within 2 h (fasting). Food slightly reduces the rate but not extent of absorption. The plasma protein binding is 40%. Information on the cumulation no.
Metabolism of anastrozole is an N-dealkilirovanie, by hydroxylation and glukuronizatia. Triazole, the major metabolite of, determined in plasma and urine, does not inhibit aromatase.
Anastrozole and its metabolites are excreted mainly with urine (less than 10% in an unmodified form) within 72 h after a single dose. T1/2 of plasma – 40-50 hours
Clearance of anastrozole after ingestion in volunteers with stable hepatic cirrhosis or impaired renal function are not different from the clearance determined in healthy volunteers.

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