Description of the active substance :.
This information is a reference and it is not enough that the drug was prescribed by a doctor. .
Antitumor agent. It is a selective non-steroid aromatase inhibitor. In postmenopause, estradiol is mainly formed from estrone, which is produced in peripheral tissues by conversion from androstenedione (with the participation of the aromatase enzyme). Reducing the level of circulating estradiol has a therapeutic effect in women with breast cancer. In post-menopause, anastrozole at a daily dose of 1 mg causes a decrease in the level of estradiol by 80%. Anastrozole does not possess progestagen, androgenic and estrogenic activity; in therapeutic doses does not affect the secretion of cortisol and aldosterone.
After oral administration anastrozole is quickly absorbed from the digestive tract. C max in plasma is achieved within 2 hours (on an empty stomach). Food decreases the speed somewhat, but not the degree of absorption. The binding with plasma proteins is 40%. There is no information on cumulation.
Anastrozole metabolism is carried out by N-dealkylation, hydroxylation and glucuronization. Triazole, the main metabolite, determined in plasma and urine, does not inhibit aromatase.
Anastrozole and its metabolites are excreted mainly in the urine (less than 10% in unchanged form), within 72 hours after the administration of a single dose. T 1/2from the plasma - 40-50 h.
The clearance of anastrozole after ingestion in volunteers with stabilized liver cirrhosis or renal dysfunction does not differ from the clearance determined in healthy volunteers.
The pharmacokinetics of anastrozole in postmenopausal women does not change.
Breast cancer in postmenopausal women.
Inside - 1 mg 1 time / day.
From the endocrine system: "hot flashes", dryness of the vagina and thinning of the hair.
From the digestive system: anorexia, nausea, vomiting, diarrhea. In patients with advanced breast cancer, in most cases with metastases to the liver there was an increase in GGT level, more rarely - AP.
From the side of the central nervous system: asthenia, drowsiness, headache.
From the side of metabolism: a slight rise in the level of total cholesterol.
Allergic reactions: skin rash.
Premenopausal period, expressed renal failure (CC less than 20 ml / min), moderate and severe hepatic insufficiency, pregnancy, lactation, children's age, hypersensitivity to anastrozole.
PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindication: marked renal failure (CC less than 20 ml / min).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindications: Moderate and severe hepatic impairment.
APPLICATION FOR CHILDREN
Contraindication: children's age.
In the case of uncertainty of the hormonal status of the patient, the state of menopause must be confirmed by additional biochemical studies.
The safety of the use of anastrozole in patients with moderate impairment of liver function has not been established.
Anastrozole should not be used concomitantly with estrogen.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, one should not perform work that requires high concentration of attention and rapid psychomotor reactions.
Anastrozole reduces the effectiveness of estrogens.
Clinical studies have shown that with the simultaneous use of anastrozole with antipyrine and cimetidine, the drug interaction caused by the induction of microsomal liver enzymes is unlikely.