Braser^® (Tablets) Instructions for Use

Marketing Authorization Holder

Hetero Labs, Limited (India)

Manufactured By

Hetero Labs, Limited (India)

Packaging and Quality Control Release

HETERO LABS, Limited (India)

Or

MAKIZ-PHARMA, LLC (Russia)

ATC Code

L02BG03 (Anastrozole)

Active Substance

Anastrozole (Rec.INN WHO registered)

Dosage Form

Braser®

Film-coated tablets, 1 mg: 30 or 60 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, round, biconvex, with an engraving “H” on one side of the tablet and “1” on the other; the core is white on the cross-section.

Excipients: lactose monohydrate (Pharmatose 200M) – 79.5 mg, povidone (Plasdone K29/32) – 4 mg, sodium carboxymethyl starch – 14 mg, magnesium stearate – 1.5 mg.

Shell composition Opadry white (Y-1-7000) – 2 mg: hypromellose HPMC 2910 (E464) – 62.5%, titanium dioxide (E171) – 31.25%, macrogol 400 (E1521) – 6.25%.

10 pcs. – blisters (3) – cardboard packs.
10 pcs. – blisters (6) – cardboard packs.

Clinical-Pharmacological Group

Antitumor drug. Aromatase inhibitor

Pharmacotherapeutic Group

Antineoplastic hormonal agents and hormone antagonists; hormone antagonists and related compounds; aromatase inhibitors

Pharmacological Action

Antitumor agent. It is a selective non-steroidal 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). The decrease 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 by N-dealkylation, hydroxylation, and glucuronidation. 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% 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 does not change.

Indications

Breast cancer in postmenopausal women.

ICD codes

Dosage Regimen

Take orally at a dose of 1 mg once daily.

Swallow the tablet whole with water. It can be taken with or without food.

Continue therapy for the duration prescribed by your physician.

For adjuvant treatment of early breast cancer, the recommended treatment duration is 5 years.

For advanced breast cancer, continue treatment until tumor progression is observed.

Do not adjust the dose without consulting your doctor.

In case of a missed dose, take it as soon as you remember. If it is almost time for the next dose, skip the missed dose and continue the regular schedule. Do not take a double dose to make up for a forgotten one.

Adverse Reactions

From the endocrine system hot flashes, vaginal dryness, and hair thinning.

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

In patients with advanced breast cancer, most cases with liver metastases showed an increase in GGT levels, less often – ALP.

From the CNS 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 studies.

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 not be performed.

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 25°C (77°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.