Introduction
An antiandrogen with about the same potency as cyproterone in rodent and canine species.
Uses
Flutamide is an antiandrogen used for locally confined stage B2-C and D-2 metastatic prostate carcinoma.
For the management of locally confined Stage B2-C and Stage D2 metastatic carcinoma of the prostate
Associated Conditions
Pharmacodynamics
Flutamide is a nonsteroidal antiandrogen. In animal studies, flutamide demonstrates potent antiandrogenic effects. It exerts its antiandrogenic action by inhibiting androgen uptake and/or by inhibiting nuclear binding of androgen in target tissues or both. Prostatic carcinoma is known to be androgen-sensitive and responds to treatment that counteracts the effect of androgen and/or removes the source of androgen, e.g. castration. Elevations of plasma testosterone and estradiol levels have been noted following flutamide administration.
Mechanism of Action
Flutamide is a nonsteroidal antiandrogen that blocks the action of both endogenous and exogenous testosterone by binding to the androgen receptor. In addition Flutamide is a potent inhibitor of testosterone-stimulated prostatic DNA synthesis. Moreover, it is capable of inhibiting prostatic nuclear uptake of androgen.
Absorption
Rapidly and completely absorbed.
Protein Binding
94-96%
Route of Elimination
Flutamide and its metabolites are excreted mainly in the urine with only 4.2% of a single dose excreted in the feces over 72 hours.
Half Life
The plasma half-life for the alpha-hydroxylated metabolite of flutamide (an active metabolite) is approximately 6 hours.
Toxicity
In animal studies with flutamide alone, signs of overdose included hypoactivity, piloerection, slow respiration, ataxia, and/or lacrimation, anorexia, tranquilization, emesis, and methemoglobinemia.
Food Interactions
- Take with or without food. The absorption is unaffected by food.
