Antitumor agent

Indications
Adjuvant treatment of hormone receptor-positive early breast cancer in postmenopausal women, even after 2 to 3 years of adjuvant tamoxifen therapy. First-line treatment of locally advanced or metastatic breast cancer with positive or unknown hormone receptors in postmenopausal women. Second-line treatment of advanced breast cancer that progresses after tamoxifen therapy in postmenopausal women.
Contraindications
- Hypersensitivity to the components of the drug.
- Pregnancy and lactation period
- Contraindicated in premenopausal women
- Severe renal impairment (creatinine clearance less than 20 ml/min)
- Moderate or severe hepatic impairment (safety and efficacy not established)
- Concomitant treatment with tamoxifen or estrogen-containing drugs.
- Children’s age (safety and effectiveness in children have not been established).
With caution:
Osteoporosis, hypercholesterolemia, coronary artery disease, hepatic dysfunction, lactase deficiency, glucose and galactose malabsorption.
Special instructions
If the patient’s hormonal status is uncertain, menopausal status should be confirmed by additional biochemical studies. The safety of anastrozole in patients with moderate hepatic impairment has not been established. The drug should not be used simultaneously with estrogens. Influence on the ability to drive vehicles and control mechanisms. During the treatment period, work requiring high concentration of attention and rapid psychomotor reactions should not be performed.
Pharmacological effect
It is a selective nonsteroidal aromatase inhibitor. In postmenopausal women, estradiol is mainly formed from estrone, which is produced in peripheral tissues by conversion of androstenedione (with the participation of the aromatase enzyme). Decreasing circulating estradiol levels has a therapeutic effect in women with breast cancer. In postmenopausal women, a daily dose of 1 mg results in an 80% decrease in estradiol levels. The drug does not have progestin, androgenic and estrogenic activity; in therapeutic doses, it does not affect the secretion of cortisol and aldosterone.
Method of application and dosage.
Inside, the tablet is swallowed whole with water. It is recommended to use at the same time.
Adults, including the elderly: 1 mg once daily, long term. If signs of disease progression appear, the drug should be discontinued. In adjuvant treatment, the recommended duration of treatment is 5 years.
In renal insufficiency, a mild to moderate dose adjustment is not necessary.
In case of mild hepatic insufficiency, no dosage adjustment is necessary.
Interaction with other drugs
Anastrozole reduces the effectiveness of estrogen. Clinical studies have shown that with the simultaneous use of anastrozole with antipyrine and cimetidine, drug interactions due to the induction of microsomal liver enzymes are unlikely.
Overdose
Cases of overdose are isolated and accidental.
A single dose of the drug, which could cause life-threatening symptoms, has not been established.
Treatment: There is no specific antidote.
Symptomatic treatment: induction of vomiting (if the patient is conscious), dialysis, general supportive care, monitoring of the patient and monitoring of the functioning of vital organs and systems.

Side effects
- From the endocrine system: hot flashes, vaginal dryness and hair loss.
- From the digestive system: anorexia, nausea, vomiting, diarrhea. In patients with advanced breast cancer, most often with liver metastases, there was an increase in the level of GGT, less often – ALP.
- From the side of the central nervous system: asthenia, drowsiness, headache.
- From the side of metabolism – a slight increase in total cholesterol.
- Allergic reactions: skin rash.
Composition
Active ingredients: anastrozole 1 mg.
Excipients: lactose monohydrate 72 mg, microcrystalline cellulose 15.6 mg, povidone 3 mg, magnesium stearate 0.9 mg, colloidal silicon dioxide 0.5 mg, sodium carboxymethyl starch 2 mg.
The composition of the film shell: hypromellose 1.65 mg, macrogol-4000 0.45 mg, titanium dioxide 0.9 mg.