anazole

Description

Description

New generation anthropogenic medicine. The main component is the active ingredient Anastrozol.
The drug first appeared on the market in 1995. At first, the remedy was used only for medicinal purposes. Anastrozole has been used during the treatment of various tumors. Today in medicine the drug is practically not used. Basically, Anastrozolol is used by bodybuilders.

Pharmacodynamics

Anastrozole – highly selective nonsteroidal aromatase inhibitor of the enzyme that the body then converts androstenedione in peripheral tissues to estrone and estradiol in postmenopausal women. The therapeutic effect in patients with breast cancer is achieved by reducing the amount of circulating estradiol. In postmenopausal women, anastrozole causes an 80% decrease in a daily dose of 1 mg of estradiol.
It does not have gestagenic, androgenic and estrogenic activity. The daily dose of 10 mg does not affect the secretion of cortisol and aldosterone. It does not require corticosteroid substitution. Anastrozole may reduce bone mineral density in patients with early gormonpozitivnym breast cancer in postmenopausal women. Anastrazole separately and in combination with bisphosphonates does not change the level of lipids in plasma.

Pharmacokinetic properties

Rapidly absorbed, peak plasma concentration is reached within 2 hours of ingestion. Food slightly reduces the rate of absorption.The degree of reduction has no clinically significant effect on steady-state plasma drug concentration at a single daily dose equivalent. Approximately 90-95% of anastrozole equilibrium concentration reached after 7 days of treatment. Data on pharmacokinetic parameters as a function of time and dose are available. Postmenopausal elderly women did not affect the pharmacokinetics. Relationship to plasma proteins – 40%.
Anastrozole is slowly eliminated from the body. The plasma half-life is 40-50 hours. Extensively metabolized in postmenopausal women. In unchanged allocated 10% of the dose in the urine within 72 hours after administration. It is metabolized by N-dealkylation, hydroxylation and glucuronidation. The major metabolite of triazole has no activity. Metabolites are excreted in the urine. Cirrhosis of the liver or renal function does not affect the clearance of anastrozole after oral administration.

Indications

Adjuvant treatment of gormonopolozhitelnogo early postmenopausal breast cancer. Advanced breast cancer in postmenopausal women.
Adjuvant treatment gormonopolozhitelnogo early breast cancer in postmenopausal women after treatment with tamoxifen for 2-3 years.

anazole