Anastrozole is a highly selective non-steroidal aromatase inhibitor that in the body of postmenopausal women turns androstenedione in peripheral tissues to estrone and then to estradiol. The therapeutic effect in patients with breast cancer is achieved by reducing the level of circulating estradiol. In postmenopausal women, anastrozole in a daily dose of 1 mg causes a decrease in the level of estradiol by 80%.
Does not possess progestogen, androgenic and estrogenic activity. The daily dose of up to 10 mg does not affect the secretion of cortisol and aldosterone. No replacement for corticosteroids is required. Anastrozole can cause a decrease in bone mineral density in patients with hormone-positive early breast cancer in postmenopausal women. Anastrazole alone, and also in combination with bisphosphonates does not change the level of lipids in the plasma.
Indications for use
Adjuvant therapy for early hormone-positive breast cancer in postmenopausal women. Common breast cancer in postmenopausal women.
Adjuvant therapy for early hormone-positive breast cancer in postmenopausal women after tamoxifen therapy for 2-3 years.
From the side of the vascular system: very often – tides.
From the musculoskeletal system: very often – arthralgia, joint stiffness, arthritis; Often – pain in the bones; Infrequently – a trigger finger.
On the part of the reproductive system: often – dryness of the mucous membrane of the vagina, vaginal bleeding (mainly during the first weeks after reversing or changing the previous hormone therapy for anastrozole).
From the side of the rut and the dermal appendages: very often a skin rash; Often – alopecia, allergic reactions; Infrequently – hives; Rarely – erythema multiforme, anaphylactoid reaction, skin vasculitis (including isolated cases of purpura (Shenlaine-Genoch syndrome)); Very rarely – Stevens-Johnson syndrome, angioedema.
From the side of digestion: very often – nausea; Often – diarrhea, vomiting.
From the hepatobiliary system: often – increased activity of alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase; Infrequently – increased activity of gamma-glutamyl transferase and bilirubin concentration, hepatitis.
From the nervous system: very often – headache; Often – drowsiness, carpal tunnel syndrome (mainly observed in patients with risk factors of the disease).
From the side of metabolism: often – anorexia, hypercholesterolemia. Admission of the drug can cause a decrease in bone mineral density due to a decrease in the concentration of circulating estradiol, thereby increasing the risk of osteoporosis and bone fractures.
Other: very often – asthenia of mild to moderate severity.
Hypersensitivity to anastrozole or other constituents of the drug; Premenopause in women; Marked renal failure (creatinine clearance less than 20 ml / min); Moderate or severe hepatic impairment (safety and efficacy not established); Concomitant therapy with tamoxifen or preparations containing estrogens. Pregnancy and lactation; Children’s age (safety and efficacy in children not established).
Cases of overdose are single and random. A single dose of a drug that could lead to life-threatening symptoms has not been established.
Treatment: there is no specific antidote. Treatment is symptomatic. Induction of vomiting (if the patient is conscious). Dialysis. General supportive therapy, monitoring the patient and monitoring the function of vital organs and systems.