Treatment of advanced breast cancer in postmenopausal women (the efficacy of anastrozole has not been confirmed in patients with non-estrogen receptor tumors unless there has been a clinical response to prior Tamoxifen therapy). Supplementary treatment of early breast cancer in postmenopausal women who have been found to have an estrogen receptor in the tumor. Supplementary treatment of early breast cancer in postmenopausal women who have been found to have an estrogen receptor in the tumor, who received supplemental treatment with tamoxifen for 2-3 years.
Composition:
1 tabl powl. contains 1 mg of anastrozole. The preparation contains lactose.
Action:
A strong and highly selective non-steroidal aromatase inhibitor involved in the conversion of Androstenedione to estrone (then converted to estradiol) in peripheral tissues. In postmenopausal women, anastrozole 1 mg daily causes suppression of oestradiol production by over 80%. Anastrozole has no progestagen, androgenic and estrogenic activity. Anastrozole administered at a dose of up to 10 mg daily does not affect the secretion of cortisol and aldosterone both without and after stimulation of secretion by ACTH (no corticosteroid supplementation is required during treatment). Following oral administration, anastrozole is rapidly absorbed from the gastrointestinal tract. The maximum concentration in the blood usually occurs within 2 hours of admission (fasting). Food reduces the rate of absorption to a small extent, but does not affect its degree. In postmenopausal women the pharmacokinetics of anastrozole is not age dependent. The drug binds to 40% of plasma proteins. In postmenopausal women, anastrozole is extensively metabolised, less than 10% of the dose is excreted in urine unchanged within 72 hours of admission. It is metabolized by N-dealkylation, hydroxylation and glucuronidation. Metabolites are mainly excreted in the urine. T0,5 is 40-50 h.
Contraindications:
Hypersensitivity to anastrozole or other ingredients. Pre-menopausal patients. Pregnancy and breastfeeding. Severe renal failure (creatinine clearance <20 ml / min). Moderate or severe liver failure. Simultaneous treatment with tamoxifen. During treatment with anastrozole, estrogen-containing medicines should not be given.
Precautions:
Anastrozole reduces the concentration of estrogens in the blood and may cause a decrease in bone mineral density. Women with diagnosed osteoporosis or with the risk of osteoporosis should have a bone densitometry performed before starting treatment and then at regular intervals during therapy. If necessary, start treatment or prevention of osteoporosis and regularly check the effectiveness of these activities. There are no data on the effects of bisphosphonates used prophylactically or in the event of a reduction in the bone mineral density caused by the use of anastrozole. The drug should not be used in pre-menopausal women; in case of doubt, diagnosis of menopause should be based on the results of hormonal tests. There are no data on the concomitant use of anastrozole and LHRH analogues - these drugs should not be used at the same time, except in clinical trials. It is not indicated in children because the safety and efficacy of this medicine has not been established in this age group. Anastrozole should not be used in both boys and girls with growth hormone deficiency as a supplement to growth hormone therapy. There are no data on the possible long-term effects of anastrozole treatment in children. Due to the lactose content, the preparation should not be used in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
The use of the drug during pregnancy and breastfeeding is contraindicated.
Side effects:
Side effects are usually mild or moderate. Very common: headache, hot flushes, nausea, rash, joint pain and stiffness, weakness. Common: lack of appetite, hypercholesterolemia, drowsiness, carpal tunnel syndrome, diarrhea, vomiting, increased alkaline phosphatase, ALAT and AST, thinning and thinning of the hair, allergic reactions, vaginal dryness, vaginal bleeding (vaginal bleeding was observed mainly in the first weeks of treatment of patients with advanced breast cancer whose previous hormonal therapy has been changed to treatment with anastrozole). Uncommon: increased gamma-GT activity and bilirubin in the blood, hepatitis, a snapping finger. Rare: erythema multiforme, anaphylactic reactions.In addition, Stevens-Johnson syndrome and angioneurotic edema were observed. It reduces the level of estrogen in the blood and may reduce the bone mineral density, which may increase the risk of bone fractures in some patients.
Dosage:
Orally. Adult patients, including the elderly: 1 mg once a day. In patients with early breast cancer, treatment is recommended for 5 years. No dose adjustment is required in patients with mild to moderate renal impairment and mild hepatic insufficiency.
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