Axastrol^® (Tablets) Instructions for Use

Marketing Authorization Holder

Grindeks, JSC (Latvia)

Manufactured By

Remedica, Ltd. (Cyprus)

ATC Code

L02BG03 (Anastrozole)

Active Substance

Anastrozole (Rec.INN registered by WHO)

Dosage Form

Axastrol®

Film-coated tablets, 1 mg: 28 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white, round, with a diameter of approximately 6.6 mm.

Excipients : lactose monohydrate – 65 mg, corn starch – 13 mg, povidone K30 – 2 mg, microcrystalline cellulose pH102 – 12 mg, sodium carboxymethyl starch type A – 4 mg, colloidal anhydrous silicon dioxide – 0.3 mg, magnesium stearate – 0.7 mg, talc – 2 mg.

Shell composition hypromellose 15 cps – 1.875 mg, macrogol 400 – 0.197 mg, titanium dioxide – 0.711 mg, talc – 0.217 mg.

14 pcs. – blister packs (2) – cardboard packs.

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 conversion from 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 evidence of accumulation.

Anastrozole metabolism occurs by 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 does not change.

Indications

Breast cancer in postmenopausal women.

ICD codes

Dosage Regimen

Take one 1 mg tablet orally once daily.

Swallow the tablet whole with water; do not crush or chew.

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

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

Continue treatment for the duration prescribed by the physician.

In the event of a missed dose, take it as soon as remembered unless it is nearly time for the next scheduled dose. Do not double the dose to make up for a forgotten tablet.

This regimen is indicated exclusively for the adjuvant treatment of postmenopausal women with hormone receptor-positive early breast cancer and the first-line treatment of postmenopausal women with hormone receptor-positive or hormone receptor unknown advanced breast cancer.

Confirm menopausal status before initiating therapy.

No dosage adjustment is required for patients with mild to moderate renal impairment or mild hepatic impairment.

The use of Axastrol is contraindicated in premenopausal women, patients with severe renal impairment (creatinine clearance less than 20 ml/min), and patients with moderate or severe hepatic impairment.

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 frequently – 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 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 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.