Index of drugs

Treatment of advanced breast cancer in postmenopausal women who have been found to have an estrogen receptor in the tumor.

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

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. T_0,5 is 40-50 h.

Hypersensitivity to anastrozole or other ingredients. Pregnancy and breastfeeding.

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 during pregnancy and breastfeeding.

Very common: headache, hot flushes, nausea, rash, joint pain and stiffness, arthritis, osteoporosis, asthenia. Common: anorexia, hypercholesterolemia, drowsiness, carpal tunnel syndrome, diarrhea, vomiting, increased alkaline phosphatase, ALT and AST, thinning and thinning of the hair, allergic reactions, bone pain, dry vagina, vaginal bleeding.Uncommon: increased GGT activity, increased bilirubin in the blood, urticaria, a crackling finger. Rare: erythema multiforme, anaphylactoid reactions, cutaneous vasculitis (including cases of Henoch-Schönlein purpura). Very rare: Stevens-Johnson syndrome, angioneurotic edema.

Orally. Adult patients, including the elderly: 1 mg once a day. No dose adjustment is required in patients with mild to moderate renal or hepatic impairment.