Description
Celana Pharmacodynamics
Anastrozole is a highly selective nonsteroidal aromatase inhibitor. Aromatase is an enzyme by which, in postmenopausal women, androstenedione is converted in peripheral tissues to estrone and then to estradiol. Anastrozole has antitumor activity against estrogen-dependent breast tumors in postmenopausal women. In the postmenopausal period the drug in a daily dose of 1 mg causes decrease in concentration of estradiol by 80 %.
Anastrozole has no progestogenic, androgenic or estrogenic activity. Anastrozole in a daily dose up to 10 mg has no effect on cortisol and aldosterone secretion (therefore, no corticosteroid replacement therapy is required).
Indications
-Adjuvant therapy of early breast cancer, with positive hormone receptors in postmenopausal women, including, after adjuvant therapy with tamoxifen for 2-3 years.
-First-line therapy for locally advanced or metastatic breast cancer with positive or unknown hormone receptors in postmenopausal women.
-Second-line therapy for advanced advanced breast cancer after tamoxifen treatment in postmenopausal women.
Contraindications
-High sensitivity to anastrozole or other drug components;
-Pregnancy and the period of breast-feeding;
-Premenopause;
-Severe renal failure (creatinine clearance less than 20 ml/min);
-Moderate or severe hepatic impairment (safety and efficacy not established);
Concomitant therapy with tamoxifen or oestrogen-containing medications;
-Children (safety and effectiveness in children has not been established).
Caution
Osteoporosis, hypercholesterolemia, lactase deficiency, lactose intolerance, glucose-galactose malabsorption (the drug form contains lactose), coronary heart disease, liver function disorders.
Dosage and administration
- The tablet should be swallowed whole and drink water. It is recommended to take the drug at the same time of the day.
- Adults, including elderly patients, should take 1 mg orally once a day for a long time. If there are signs of disease progression, the drug should be discontinued. As adjuvant therapy, the recommended duration of treatment is 5 years.
- Patients with mild to moderate renal insufficiency do not require dose adjustment.
- Patients with mild hepatic impairment do not require dose adjustment.
