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Background: The successful treatment of bacterial prostatitis depends on an effective antimicrobial concentration in prostatic tissue against the infecting organism. In this study we compared the diffusion of 5 types of antimicrobials into the prostate., Methods: The concentrations of piperacillin, cefotiam, minocycline, amikacin, and ofloxacin were determined in prostatic fluid, prostatic tissue, and serum 2.5 to 3 hours after a single administration from 55 patients with benign prostatic hypertrophy., Results: Although amikacin showed the highest mean concentration both in prostatic tissue and prostatic fluid, the prostatic tissue/serum ratio was significantly higher (P < 0.01) for ofloxacin (1.49 +/- 0.80) and minocycline (0.94 +/- 0.39) compared with those for amikacin (0.49 +/- 0.21) and piperacillin (0.21 +/- 0.15). Also, the prostatic fluid/serum ratio was lower than the prostatic tissue/serum ratio for each drug, however, the prostatic fluid/serum ratio of ofloxacin was significantly higher than that of other antimicrobials tested (P < 0.01)., Conclusion: These results support earlier studies demonstrating that fluoroquinolones are a useful class of antimicrobials for the treatment of chronic bacterial prostatitis. They also suggest that in view of the pharmacokinetic properties and antimicrobial activities, amikacin and minocycline may be alternate antimicrobial options for selected patients with bacterial infections of the prostate.