Flutamide: a review of its pharmacological and physico-chemical properties. Methods for analysis of pharmaceutical formulas

Abstract

Flutamide, 2-metil-N-[4-nitro-3-(trifluorometyl)phenyl]propanamide, á,á,á-trifluoro-2-methil-4'-nitro-mpropionotoluidide or 4'-nitro-3'-trifluoromethylisobutyranilide, is a nonsteroidal antiandrogenic drug devoid of hormonal agonist activity, used in treatment of advanced prostate cancer. It inihibits the binding of testosterone or the dihydrotestosterone to nuclear and cytoplasmic receptors in target cells. Flutamide is completely absorbed from the gastrointestinal tract and rapidly converted to a variety of metabolites. Is 94% to 96% bound to plasma proteins. The parent drug and metabolites are primarily eliminated by the urine. The principal side effects are gynecomastia and diarrhea. In bulk or pharmaceutical dosage forms, flutamide can be estimated by polarography, spectrophotometry, gas chromatography and high performance liquid chromatography. The present communication reports pharmacological and physico-chemical properties of flutamide and analytical methods for its estimation.