Features Anastrozole in the UK
Anastrozole - a highly selective inhibitor of non-steroidal aromatase enzyme in an organism that postmenopausal women converts androstenedione in peripheral tissues, estrone and then to estradiol. The therapeutic effect in patients with breast cancer is achieved by reducing levels of circulating estradiol. In postmenopausal women, anastrozole at a daily dose of 1 mg estradiol levels causes a decrease of 80%.
It has no progestogenic, androgenic and estrogenic activity. The daily dose of 10 mg did not affect the secretion of aldosterone and cortisol. Not required substitution corticosteroids. Anastrozole may cause a reduction in bone mineral density in patients with gormonpozitivnym early breast cancer in postmenopausal women. Anastrazole separately and also in combination with bisphosphonates not alter lipid levels in plasma.
Rapidly absorbed, the maximum plasma concentration is reached within 2 hours after ingestion fasting. Food slightly decreases the rate of absorption. The degree of reduction has no clinically significant effect on the equilibrium concentration of drug in the plasma at a single dose daily dose. Approximately 90-95% of the equilibrium concentration of anastrozole is achieved after 7 days of dosing. Data on the pharmacokinetic parameters depending on the time and dose of no. Age postmenopausal women does not affect the pharmacokinetics. Relationship to plasma proteins - 40%.
Anastrozole is eliminated from the body slowly. plasma half-life period is 40-50 hours. Extensively metabolized in postmenopausal women. The unchanged allocated 10% of the dose in the urine within 72 hours after ingestion. It is metabolized by N-dealkylation, hydroxylation and glucuronidation. The main triazol metabolite has no activity. Excretion of urine metabolites occurs. Cirrhosis of the liver or renal function does not alter the clearance of anastrozole after oral administration.
Adjuvant treatment of postmenopausal breast cancer early gormonopolozhitelnogo. Advanced breast cancer in postmenopausal women.
Adjuvant therapy gormonopolozhitelnogo early breast cancer in postmenopausal women after tamoxifen therapy for 2-3 years.
Dosing and Administration
Inside, the tablet is swallowed whole with water. It is recommended to use one and the same time.
The daily dose in the UK for adults including the elderly is one 1 mg once a day. If signs of progression of the disease taking the drug should be discontinued. In the adjuvant treatment of the recommended duration of treatment is 5 years.
In violation of renal function, mild to moderate dose adjustment is required.
If any of the functions of the liver mild dose adjustment is required.