Anastera (Tablets) Instructions for Use

Instructions
Dosage forms

ATC Code

L02BG03 (Anastrozole)

Active Substance

Anastrozole (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antitumor drug. Aromatase inhibitor

Pharmacotherapeutic Group

Antineoplastic agent, estrogen synthesis inhibitor

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 the conversion of androstenedione (with the participation of the aromatase enzyme).

The reduction in circulating estradiol levels has a therapeutic effect in women with breast cancer.

In postmenopausal women, Anastrozole at a daily dose of 1 mg causes an 80% reduction in estradiol levels.

Anastrozole has no progestogenic, androgenic, or estrogenic activity; at therapeutic doses, it does not affect the secretion of cortisol and aldosterone.

Pharmacokinetics

After oral administration, Anastrozole is rapidly absorbed from the gastrointestinal tract.

C_max in plasma is reached within 2 hours (on an empty stomach).

Food slightly reduces the rate, but not the extent of absorption.

Plasma protein binding is 40%.

There is no information on accumulation.

Anastrozole metabolism occurs via N-dealkylation, hydroxylation, and glucuronidation.

Triazole, the main metabolite found in plasma and urine, does not inhibit aromatase.

Anastrozole and its metabolites are excreted mainly in the urine (less than 10% unchanged) within 72 hours after a single dose administration.

T_1/2 from plasma is 40-50 hours.

The clearance of anastrozole after oral administration in volunteers with stabilized liver cirrhosis or impaired renal function does not differ from the clearance determined in healthy volunteers.

The pharmacokinetics of anastrozole in postmenopausal women do not change.

Indications

Breast cancer in postmenopausal women.

ICD codes

Open the list of ICD codes

ICD-10 code	Indication
C50	Malignant neoplasm of breast

ICD-11 code	Indication
2C65	Hereditary breast and ovarian cancer syndrome
2C6Y	Other specified malignant neoplasms of the breast
2C6Z	Malignant neoplasms of breast, unspecified

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Take one 1 mg tablet orally once daily.

Swallow the tablet whole with a sufficient amount of water.

Administer at approximately the same time each day to maintain consistent plasma concentrations.

Dosing may be taken with or without food; food intake slightly reduces the absorption rate but does not affect the overall extent of absorption.

Continue treatment for the duration prescribed by the physician.

In patients with severe renal impairment (creatinine clearance less than 20 mL/min) or moderate to severe hepatic impairment, the use of anastrozole is contraindicated.

Do not adjust the dose for elderly patients or for patients with mild to moderate renal impairment.

Confirm the patient’s postmenopausal status before initiating therapy; biochemical confirmation of hormonal status is required if uncertainty exists.

Do not use concomitantly with estrogen-containing therapies as anastrozole reduces their effectiveness.

Adverse Reactions

From the endocrine systemhot flashes, vaginal dryness, and hair thinning.

From the digestive system anorexia, nausea, vomiting, diarrhea.

In patients with advanced breast cancer, most of whom had liver metastases, an increase in GGT levels was observed, less frequently – ALP.

From the central nervous system asthenia, drowsiness, headache.

From metabolism a slight increase in total cholesterol levels.

Allergic reactions skin rash.

Contraindications

Premenopausal period, severe renal failure (creatinine clearance less than 20 ml/min), moderate and severe hepatic impairment, pregnancy, lactation, childhood, hypersensitivity to anastrozole.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation.

Use in Hepatic Impairment

Contraindication: moderate and severe hepatic impairment.

Use in Renal Impairment

Contraindication: severe renal failure (creatinine clearance less than 20 ml/min).

Pediatric Use

Contraindication: childhood.

Special Precautions

In case of uncertainty about the patient’s hormonal status, the menopausal state must be confirmed by additional biochemical tests.

The safety of anastrozole use in patients with moderate hepatic impairment has not been established.

Anastrozole should not be used concomitantly with estrogens.

Effect on ability to drive vehicles and operate machinery

During the treatment period, work requiring high concentration and rapid psychomotor reactions should be avoided.

Drug Interactions

Anastrozole reduces the effectiveness of estrogens.

Clinical studies have shown that when anastrozole is used concomitantly with antipyrine and cimetidine, drug interaction due to induction of liver microsomal enzymes is unlikely.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.

Medical Disclaimer