ANASTROZOLE 1MGX50T

TECHPHARM (INDIA)

Anastrozole 1 mg

DOSAGE FORM

Film-coated tablets 1 mg

COMPOUND

One tablet contains:

active substance – anastrozole 1.0 mg,

excipients: lactose monohydrate (milk sugar), microcrystalline cellulose, povidone (polyvinylpyrrolidone), magnesium stearate, colloidal silicon dioxide, sodium carboxymethyl starch,

shell composition: hypromellose, macrogol-4000, titanium dioxide (E171).

ADVERTISING

DESCRIPTION

The tablets are round, biconvex, film-coated, white or almost white; two layers are visible at the break - a white or almost white core and a film shell.

PHARMACOTHERAPEUTIC GROUP

Antitumor hormonal drugs. Enzyme inhibitors. Anastrazole.

Pharmacological properties

Pharmacokinetics

Absorption of anastrozole is rapid, with maximum plasma concentrations achieved within two hours after oral administration (on an empty stomach). Food slightly reduces the rate of absorption, but not its extent, and does not lead to a clinically significant effect on the steady-state plasma concentration of anastrozole with a single daily dose of anastrozole. After seven days of taking the drug, approximately 90-95% of the equilibrium concentration of anastrozole in the blood plasma is achieved. There is no information on the dependence of the pharmacokinetic parameters of anastrozole on time or dose. The pharmacokinetics of anastrozole does not depend on the age of postmenopausal women. Communication with blood plasma proteins - 40%.

Anastrozole is eliminated slowly, with a plasma half-life of 40-50 hours. Extensively metabolized in postmenopausal women. Less than 10% of the dose taken is excreted unchanged by the kidneys within 72 hours after taking the drug. The metabolism of anastrozole occurs through the stages of N-dealkylation, hydroxylation and glucuronidation. Triazole, the major plasma metabolite of anastrozole, does not inhibit aromatase. Metabolites are excreted mainly by the kidneys.

The clearance of anastrozole after oral administration in patients with liver cirrhosis or impaired renal function does not change.

PHARMACODYNAMICS

Anastrozole is a highly selective non-steroidal inhibitor of aromatase, an enzyme that converts androstenedione in peripheral tissues into estrone and then into estradiol in postmenopausal women. Reducing circulating concentrations of estradiol has been shown to have a beneficial effect in women with breast cancer. In postmenopausal women, anastrozole at a daily dose of 1 mg causes a decrease in estradiol concentrations by 80%.

Anastrozole does not have progestogenic, androgenic or estrogenic activity. Regular intake of daily doses of anastrozole up to 10 mg does not affect the secretion of cortisol or aldosterone, therefore, when prescribing it, corticosteroid replacement is not required.

INDICATIONS FOR USE

- adjuvant therapy for early hormone-positive breast cancer in postmenopausal women

- treatment of advanced breast cancer in postmenopausal women

- adjuvant therapy for early hormone-positive breast cancer in postmenopausal women after tamoxifen therapy for 2-3 years

DIRECTIONS FOR USE AND DOSES

Inside. Swallow the tablet whole with water. It is recommended to take the drug at the same time, regardless of meals.

Adults, including the elderly: 1 mg orally per day for a long time. If signs of disease progression appear, the drug should be discontinued.

Mild to moderate renal impairment: No dosage adjustment is required in patients with mild to moderate renal impairment.

Mild hepatic impairment: No dose adjustment is required in patients with mild hepatic impairment.