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Arimidex - Highly selective nonsteroidal aromatase inhibitor. Aromatase is an enzyme through which in postmenopausal women, androstenedione in peripheral tissues is converted into estrone and then into estradiol. Reducing circulating estradiol has a therapeutic effect in patients with breast cancer. In postmenopausal medication in a daily dose of 1 mg causes a decrease in estradiol levels by 80%.
Arimidex does not possess progestogenic, androgenic and estrogenic activity.
Arimidex in a daily dose of up to 10 mg has no effect on the secretion of cortisol and aldosterone (therefore, the use of the drug does not require the replacement of corticosteroids).
After oral administration, anastrozole is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached within 2 hours (on an empty stomach). Food somewhat reduces the rate, but not the degree of absorption. Small changes in the rate of absorption do not lead to a clinically significant effect on the Css of the drug in plasma with a daily intake of 1 Arimidex tablet.
Anastrozole is associated with plasma proteins by 40%. Approximately 90-95% of Ńss is achieved after 7 days of taking the drug. There is no information about the cumulation of the drug and the dependence of the pharmacokinetic parameters of anastrozole on time and dose.
Anastrozole is metabolized by N-dealkylation, hydroxylation and glucuronization. Triazole, the major metabolite detected in plasma, does not inhibit aromatase.
Anastrozole is displayed slowly, T1 / 2 - 40-50 h.
Anastrozole and its metabolites are excreted mainly with urine (less than 10% of the excreted dose - unchanged), within 72 hours after taking the drug.
Pharmacokinetics in special clinical situations
The determined clearance of anastrozole after oral administration in volunteers with stabilized liver cirrhosis or renal dysfunction does not differ from clearance determined in healthy volunteers.
Anastrozole pharmacokinetics does not depend on age in postmenopausal women.
The drug is not prescribed to women in premenopausal women.
Adults, including elderly patients, the drug is prescribed 1 mg orally 1 time / day, long-term. If there is evidence of disease progression, the drug should be discontinued. As adjuvant therapy, the recommended duration of treatment is 5 years.
Patients with mild and moderately severe renal impairment do not require dose adjustment.
Patients with mild hepatic impairment do not require dose adjustment.
The tablet should be swallowed whole and washed down with water. It is recommended to take the drug at the same time of day.
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Tobradex eye drops 5ml