| Item |
Information |
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Drug Groups
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approved |
|
Description
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An antiandrogen with about the same potency as cyproterone in rodent and canine species. |
| Indication |
For the management of locally confined Stage B2-C and Stage D2 metastatic carcinoma of the prostate |
| Pharmacology |
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. |
| Toxicity |
In animal studies with flutamide alone, signs of overdose included hypoactivity, piloerection, slow respiration, ataxia, and/or lacrimation, anorexia, tranquilization, emesis, and methemoglobinemia. |
| Affected Organisms |
| • |
Humans and other mammals |
|
| Biotransformation |
Flutamide is rapidly and extensively metabolized, with flutamide comprising only 2.5% of plasma radioactivity 1 hour after administration. |
| Absorption |
Rapidly and completely absorbed. |
| Half Life |
The plasma half-life for the alpha-hydroxylated metabolite of flutamide (an active metabolite) is approximately 6 hours. |
| Protein Binding |
94-96% |
| 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. |
| References |
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| External Links |
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