Composition
Film-coated tablets are white, round, biconvex, with the inscription “ANA 1” on one side of the tablet; on the break – white or almost white in color.
1 tab. | |
Anastrozolee | 1 mg |
Auxiliary substances:
lactose monohydrate,
povidone,
sodium carboxymethyl starch,
magnesium stearate.
Film shell:
opadrai white (macrogol 400, hypromellose, titanium dioxide).
Pharmacological action
Antitumor agent. It is a selective nonsteroidal aromatase inhibitor. In postmenopausal women, 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 postmenopausal women, Anastrozolee in a daily dose of 1 mg causes a decrease in estradiol levels by 80%. Anastrozolee does not have progestogenic, androgenic and estrogenic activity; in therapeutic doses, it does not affect the secretion of cortisol and aldosterone. Pharmacokineticsafter oral use, Anastrozolee is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached within 2 hours (on an empty stomach). Food slightly reduces the rate, but not the degree of absorption. Binding to plasma proteins is 40%. There is no information about cumulation. Anastrozolee is metabolized by N-dealkylation, hydroxylation, and glucuronidation. Triazole, the main metabolite detected in plasma and urine, does not inhibit aromatase. Anastrozolee and its metabolites are mainly excreted in the urine (less than 10% unchanged) within 72 hours after a single dose. T1 / 2 from plasma – 40-50 hours. The clearance of Anastrozolee after oral use in volunteers with stable cirrhosis of the liver or impaired renal function does not differ from the clearance determined in healthy volunteers. The pharmacokinetics of Anastrozolee in postmenopausal women do not change.
Indications
Postmenopausal breast cancer.
Contraindications
Premenopausal period, severe renal insufficiency (creatinine clearance less than 20 ml / min), moderate to severe hepatic insufficiency, pregnancy, lactation, childhood, hypersensitivity to Anastrozolee.
Side effects
From the endocrine system: hot flashes, vaginal dryness, and thinning hair. From the digestive system: anorexia, nausea, vomiting, diarrhea. In patients with advanced breast cancer, in most cases with liver metastases, an increase in GGT levels was noted, less often – ALP. From the central nervous system: asthenia, drowsiness, headache. From the side of metabolism: a slight increase in the level of total cholesterol. Allergic reactions: skin rash.
Interaction
Anastrozolee reduces the effectiveness of estrogens. Clinical studies have shown that when Anastrozolee is co-administered with antipyrine and cimetidine, drug interaction due to the induction of microsomal liver enzymes is unlikely.
How to take, course of use and dosage
Inside – 1 mg 1 time/day.
Special instructions
In case of uncertainty of the hormonal status of the patient, the state of menopause should be confirmed by additional biochemical studies. The safety of using Anastrozolee in patients with moderate hepatic impairment has not been established. Anastrozolee should not be used simultaneously with estrogens. Influence on the ability to drive motor vehicles and control mechanisms During treatment, you should not perform work that requires high concentration of attention and rapid psychomotor reactions.
Active ingredient
Anastrozolee
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Description
For adults as directed by your doctor
Indications
Cancer
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