Selana coated pills 1 mg N28
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Active ingredients
Anastrozole
Release form
Pills
Composition
1 tab. anastrozole 1 mg.
Pharmacological effect
Antitumor agent. It is a selective non-steroidal aromatase inhibitor. In postmenopausal estradiol is mainly formed from estrone, which is produced in peripheral tissues by transformation from androstenedione (with the participation of the enzyme aromatase). Reducing circulating estradiol has a therapeutic effect in women with breast cancer. In postmenopausal anastrozole in a daily dose of 1 mg causes a decrease in estradiol levels by 80%. Anastrozole does not possess progestogenic, androgenic and estrogenic activity; in therapeutic doses does not affect the secretion of cortisol and aldosterone.
Pharmacokinetics
After oral administration, anastrozole is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached within 2 hours (on an empty stomach). Food somewhat reduces the rate, but not the degree of absorption. Plasma protein binding is 40%. There is no information about cumulation. Anastrozole is metabolized by N-dealkylation, hydroxylation and glucuronization. Triazole, the major metabolite that is detected in plasma and urine, does not inhibit aromatase. Anastrozole and its metabolites are mainly excreted in the urine (less than 10% - unchanged), within 72 hours after a single dose. T1 / 2 of plasma - 40-50 hours. The clearance of anastrozole after ingestion in volunteers with stabilized liver cirrhosis or renal dysfunction does not differ from clearance determined in healthy volunteers. The pharmacokinetics of anastrozole in postmenopausal women does not change.
Contraindications
The period of premenopause, severe renal failure (CC less than 20 ml / min), moderate and severe liver failure, pregnancy, lactation, childhood, hypersensitivity to anastrozole.
Use during pregnancy and lactation
Contraindicated in pregnancy and lactation.
Dosage and administration
Inside - 1 mg 1 time / day.
Side effects
On the part of the endocrine system: "hot flashes", vaginal dryness and thinning hair. On the part of 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 the level of GGT, more rarely ALP. From the side of the central nervous system: asthenia, drowsiness, headache. On the part of the metabolism: a slight increase in total cholesterol. Allergic reactions: skin rash.
special instructions
In case of uncertainty of the patient's hormonal status, the condition of the menopause must be confirmed by additional biochemical studies. The safety of using anastrozole in patients with moderately impaired liver function has not been established. Anastrozole should not be used simultaneously with estrogen. Influence on the ability to drive vehicles and control mechanisms During the period of treatment should not perform work that requires a high concentration of attention and quick psychomotor reactions.