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====== First-generation (flutamide, bicalutamide, nilutamide) ====== * '''MOA: acts by binding to the AR in a competitive fashion''' * '''Flutamide''' ** '''Short half-life,''' '''three times per day dosing''' * '''Bicalutamide''' ** '''Long half-life''', once per day dosing ** '''Pharmacokinetics are not affected by age, renal insufficiency, or moderate hepatic impairment''' ** '''Associated with maintenance of serum testosterone levels in the majority of patients''' ** '''150 mg/day bicalutamide monotherapy appears to have equivalent efficacy to medical or surgical castration in men with metastatic or locally advanced disease.''' *** Bicalutamide monotherapy (150 mg/day) is also associated with significantly better quality of life in the domains of sexual interest and physical capacity compared to surgical castration. There are, however''', higher rates of gynecomastia (66.2%) and breast pain (72.8%)''' * '''Nilutamide''' ** About 1/4 men on nilutamide therapy will note a '''delayed adaptation to darkness after exposure to bright illumination'''
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