Letrozol Winthrop® 2,5 mg

Description

Composition

One tablet contains

the active substance letrozole 2.5 mg,

excipients: lactose monohydrate (Flowlac 100), croscarmellose sodium (AC-Di-sol), povidone (Plasdone K-29/32), colloidal silicon dioxide (Aerosil 200), magnesium stearate,

Composition of the envelope: opadray yellow 03B82401 (composition: hypromellose, titanium dioxide (E 171), iron (III) yellow oxide (E172), macrogol 400, talc).

Description

Round tablets, slightly convex on both sides, with a truncated edge, coated with a dark yellow film coating, engraved ‘H’ on one side and ‘5’ on the other side.

Pharmacological properties

Absorption – high (food slows absorption); bioavailability – 99.9%. Binding to plasma proteins – 60% (55% – to albumin). Concentration in erythrocytes – 80% of its plasma content. The apparent volume of distribution at equilibrium at steady state is 1.87 l/kg. After daily administration at a dose of 2.5 mg/day, blood concentrations corresponding to the steady-state equilibrium state are reached within 2-6 weeks. No accumulation occurs during long-term treatment.

Metabolism – mainly in the liver with cytochrome P450 isoenzymes with the formation of a pharmacologically inactive carbinol derivative.

Excretion – mainly via the kidneys as metabolites and also via the intestines. T1/2 – 48 h. In renal and hepatic failure, pharmacokinetic parameters do not change. Excreted from plasma by haemodialysis.