Products
Flutamide was approved in many countries in 1984 in tablet form (Flucinom, 250 mg) and is no longer registered. It can be replaced by modern antiandrogens if needed or imported from abroad.
Structure and properties
Flutamide (C11H11F3N2O3, Mr = 276.2 g/mol) exists as a pale yellow crystalline powder that is practically insoluble in water. It is an aniline with a non-steroidal structure. Flutamide is a prodrug. Its effects are mainly due to the formation of the active metabolite 2-hydroxyflutamide.
Effects
Flutamide (ATC L02BB01) is antiandrogenic and suppresses testicular and adrenal androgen activity.
Indications
For the treatment of patients with advanced prostate cancer.
Dosage
According to the SmPC. The tablets are taken with liquid after meals. Three times daily dosing is required. This is in contrast to newer antiandrogens such as bicalutamide, for which one dose per day is sufficient.
Contraindications
Flutamide is contraindicated in hypersensitivity. Use must be carefully considered in the presence of impaired hepatic or renal function. For complete precautions, see the drug label.
Interactions
Drug-drug interactions have been described with oral anticoagulants.
Adverse effects
The most common possible adverse effects include gynecomastia, breast pain, galactorrhea, and small-nodule changes in the mammary gland. Flutamide is hepatotoxic and may cause hepatitis. Liver injury with lethal outcome has been reported in isolated cases. Other side effects occur.
