Treatment of advanced breast cancer in postmenopausal women, with the exception of patients with estrogenegative cancer, unless they have previously had a positive clinical response to tamoxifen. Additive for treatment of invasive estrogenpositive breast cancer in the early stages with positive indicators of the hormone receptor in postmenopausal patients. Additive for the treatment of estrogenpositive breast cancer in the early stages in postmenopausal patients who have had adjuvant therapy with tamoxifen for 2-3 yEars and Nose.
active substance: anastrozole;
1 tablet containing 1 mg of anastrozole;
Egystrozol Excipients: lactose monohydrate, sodium starch glycolate (type A), povidone, magnesium stearate, macrogol 400, hypromellose, titanium dioxide (E l71).
Egystrozol Dosage form
Main physical and chemical properties: white round biconvex tablets, film-coated with the inscription “ANA” and “1” on one side.
Hormone antagonists and similar drugs.
Enzyme inhibitors. ATX code L02B G03.
Mechanism of action and pharmacodynamic effects
Anastrozole is a potent and highly selective nonsteroidal aromatase inhibitor. In postmenopausal women, estradiol is mainly produced by the conversion of androstenedione to estrone in peripheral tissues by the aromatase enzyme complex. Estrone is further converted to estradiol. Decreased levels of circulating estradiol have been shown to have a therapeutic effect in women with breast cancer. In postmenopausal women, taking anastrozole in a daily dose of 1 mg reduced estradiol levels by more than 80%, which was confirmed by a highly sensitive test.
Anastrozole has no progestogenic or androgenic activity.
Anastrozole in daily doses up to 10 mg does not affect cortisol and aldosterone secretion measured before and after the standard adrenocorticotropic hormone (ACTH) stimulation test. Therefore, corticosteroid replacement therapy is not required.
Absorption of anastrozole is rapid, the maximum concentration in blood plasma is usually reached within 2 hours (on an empty stomach). Food slows down a bit, but not the degree of absorption. Minor changes in the rate of absorption do not lead to a clinically significant effect on steady-state plasma concentrations with anastrozole tablets once daily. Approximately 90-95% of steady-state plasma concentrations of anastrozole are reached after 7 days of taking the drug, the accumulation is 3-4 times. There is no information on the dependence of pharmacokinetic parameters of anastrozole on time or dose.
The pharmacokinetics of anastrozole do not depend on the age of postmenopausal women.
Only 40% of anastrozole is bound to plasma proteins.
Anastrozole is excreted slowly, with a plasma half-life of 40-50 hours. Food slows down the rate of absorption a little, but not its degree. Anastrozole is extensively metabolized in postmenopausal women, with less than 10% of the dose excreted unchanged in the urine within 72 hours after dosing. Metabolism of anastrozole is carried out by N-dealkylation, hydroxylation and glucuronidation. Metabolites are excreted mainly in the urine. Triazole, the major metabolite in plasma, does not inhibit aromatase.
Renal or hepatic impairment
Compared to the corresponding control in volunteers with compensated liver cirrhosis, the apparent clearance (CL / F) of anastrozole after oral administration was approximately 30% lower (study 1033IL / 0014).
Plasma concentrations of anastrozole in volunteers with cirrhosis of the liver were within the range of concentrations observed in healthy subjects.
In studies 1033IL / 0018 in volunteers with severe renal impairment (glomerular filtration rate [GFR] <30 ml / min), the apparent clearance (CL / F) of anastrozole after oral administration was not altered, consistent with the fact that anastrozole is excreted primarily by metabolism. .
Plasma anastrozole concentrations observed in long-term efficacy studies in patients with renal impairment were within the range of plasma anastrozole concentrations observed in patients without renal impairment. The use of anastrozole in patients with severe renal impairment requires caution.
Treatment of advanced breast cancer with positive hormone receptors in postmenopausal women.
Adjuvant treatment of invasive early-stage breast cancer with positive hormone receptor levels in postmenopausal patients.
Adjuvant treatment of invasive breast cancer with positive hormone receptors in the early stages in postmenopausal patients who have been treated with tamoxifen for 2-3 years.
Egistrozole is contraindicated in patients:
during pregnancy or breastfeeding;
with known hypersensitivity to anastrozole or to any of the excipients.