Index of drugs

Treatment of advanced breast cancer in postmenopausal women. Efficacy has not been demonstrated in patients with a negative estrogen receptor except in cases of previous positive clinical response to tamoxifen. Adjunctive therapy for early invasive breast cancer in post-menopausal women with a positive hormone receptor. Adjunctive treatment of early breast cancer in postmenopausal women with positive hormone receptor who have undergone treatment with Tamoxifen for 2-3 years.

1 tabl powl. contains 1 mg of anastrozole. The preparation contains lactose.

A strong and selective non-steroidal aromatase inhibitor involved in the conversion of androstenedione to oestrone in peripheral tissues (subsequently transformed into estradiol). It has been shown that in post-menopausal women, the use of 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 the stimulation of excretion by ACTH (therefore, during treatment, no corticosteroid supplementation is required). 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). The presence of food reduces the rate of absorption to a small extent, but does not affect the extent of absorption. In postmenopausal women the pharmacokinetics of anastrozole is not age dependent. The drug binds to 40% of plasma proteins. In post-menopausal women, anastrozole is extensively metabolised, less than 10% of the dose is excreted in the urine in unchanged form within 72 hours of admission. Anastrozole is metabolized by N-dealkylation, hydroxylation and glucuronidation. Metabolites are mainly excreted in the urine. T_0,5 is 40-50 h.

Hypersensitivity to anastrozole or other components of the drug. Pre-menopausal patients. Pregnancy and breastfeeding. Moderate or serious liver disease. Co-administration of estrogen-containing medicines. Simultaneous treatment with tamoxifen.

It should not be used in pre-menopausal women; diagnosis of menopause should be determined based on the results of hormonal tests - the concentration of LH, FSH and / or estradiol. There are no data on the concomitant use of anastrozole and LHRH analogues. The simultaneous use with tamoxifen or oestrogens should be avoided as it may reduce the pharmacological effect of anastrozole. Anastrozole reduces the concentration of estrogen in the blood, so it can cause a decrease in bone mineral density, and consequently increase the risk of fractures - women with or with the risk of osteoporosis should have a bone densitometry performed at the beginning of treatment and then at regular intervals during therapy. Treatment or prevention of osteoporosis should be properly implemented and closely monitored; the use of specialized treatment with, for example, bisphosphonates may stop further bone demineralization and should be considered. Exposure to anastrozole is not increased in subjects with severe renal impairment (GFR <30ml / min); no studies have been performed on patients with breast cancer and severe renal failure - use caution. Exposure to anastrozole may increase in people with hepatic impairment; there have been no studies on the use of anastrozole in patients with breast cancer and moderate or severe hepatic impairment - use caution. The safety and efficacy of anastrozole in children and adolescents has not been established - it is not recommended for use in children and adolescents. Anastrozole should not be used in boys and should not be used in girls with growth hormone deficiency in combination with therapy with this hormone. Due to the lactose content, the preparation should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of Glucose and galactose.

The drug is contraindicated for use during pregnancy and during breastfeeding.

Most of the side effects are mild or moderate. Very common: hot flushes, weakness, joint pain and stiffness, arthritis, osteoporosis, headache, nausea, rash. Common: hair thinning, allergic reactions, vomiting, diarrhea, drowsiness, carpal tunnel syndrome, increase in alkaline phosphatase, ALAT and AST, vaginal bleeding, vaginal dryness, anorexia, hypercholesterolemia. Uncommon: increase in γ-glutamyltransferase and bilirubin, hepatitis, urticaria, and tendinitis. Rare: erythema multiforme, anaphylactic reaction, inflammation of blood vessels in the skin (including cases of Henoch-Schönleina purpura). Frequency unknown: Stevens-Johnson syndrome, angioneurotic edema.

Orally. Adult patients, including the elderly: 1 mg once a day. In the early stage of the disease, the recommended duration of treatment is 5 years. No dosage adjustment is required for patients with mild to moderate renal and hepatic impairment.