Anastrozole is a highly selective non-steroidal agent that inhibits the properties of the aromatase enzyme. When using the properties of this drug in the female half of the population who are in the menopausal period, the amount of estradiol in the blood decreases, since the metabolism of extradiol occurs with the help of aromatase (the enzyme converts androgens into estrogens).
The drug has the property of negatively affecting the development of oncological processes in the mammary glands. Anastrozole Tl does not have the property of increasing the activity of estrogens, androgens and progestogens, and also does not affect the production of cortisol and aldosterone.
When using the drug, there is no need to carry out replacement therapy with corticosteroids.Antitumor agent. It is a selective nonsteroidal aromatase inhibitor. In postmenopause, estradiol is mainly formed from estrone, which is produced in peripheral tissues by conversion from androstenedione (with the participation of the aromatase enzyme). Reducing the level of circulating estradiol has a therapeutic effect in women with breast cancer. In postmenopausal women, anastrozole at a daily dose of 1 mg causes an 80% decrease in estradiol levels. Anastrozole does not have progestogenic, androgenic and estrogenic activity, in therapeutic doses it does not affect the secretion of cortisol and aldosterone.
Androstenedione — the main source of circulating estrogens in postmenopausal women, is converted in the peripheral tissues to estrone, and then to estradiol, this process occurs with the participation of the aromatase enzyme. The mechanism of action of anastrozole is associated with the inhibition of aromatase (a selective nonsteroidal inhibitor) in peripheral tissues, including fat, which leads to a decrease in the amount of estradiol.
Method of application
When treated with anastrozole at the recommended dose — 1 mg per day — the level of estradiol decreases by 70% within 24 hours, by 80% - after 14 days. Suppression of the level of estradiol in the blood serum persists for 6 days after stopping the daily intake of 1 g of anastrozole. Reducing the level of circulating estradiol has a therapeutic effect on breast tumors in postmenopausal women. When taken daily at doses of 3, 5 and 10 mg, anastrozole had no effect on the secretion of cortisol and aldosterone. Anastrozole did not exhibit direct progestogenic, androgenic, or estrogenic activity in animals, but it did alter the levels of circulating progesterone, androgens, and estrogens.
After ingestion, 83-85% of the dose is absorbed, food intake affects the absorption (reduces the absorption). Cmax is reached after 2 hours (on an empty stomach). In the blood, up to 40% is bound to plasma proteins. The equilibrium concentration in the blood with a daily intake is reached after about 7 days, its value is 3-4 times higher than with a single dose. Anastrozole is intensively metabolized in postmenopausal women, less than 10% is excreted unchanged in the urine within 72 hours after administration, 60% is excreted as metabolites.Application of the substance Anastrozole
Adjuvant therapy for early hormone-positive breast cancer in postmenopausal women, treatment of advanced breast cancer in postmenopausal women, adjuvant therapy for early hormone-positive breast cancer in postmenopausal women after tamoxifen therapy
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