rosoxacin and Prostatitis

The distribution in the prostate of norfloxacin and rosoxacin, both quinoline carboxylic acid derivatives, was investigated in an experimental dog model. The concentrations in prostatic interstitial fluid (PIF) and prostatic secretion (PS) of both antimicrobials were lower than the corresponding plasma (P) concentrations, as might be expected for acidic compounds. Norfloxacin achieved significantly higher PS/P and PIF/P ratios than rosoxacin following intravenous infusion; there were no differences between the two drugs in the various tissue/plasma ratios. The concentrations of both norfloxacin and rosoxacin in PIF, PS, and urine were in the minimal inhibitory range for most gram-negative pathogens causing bacterial prostatitis and urinary tract infections. Clinical trials may be warranted for both drugs.

Topics: 4-Quinolones; Administration, Oral; Animals; Anti-Infective Agents; Dogs; Drug Evaluation, Preclinical; Infusions, Parenteral; Male; Nalidixic Acid; Norfloxacin; Prostate; Prostatitis; Quinolines; Quinolones; Time Factors; Tissue Distribution; Urinary Tract Infections

A study of the new anti-bacterial agent, rosoxacin, a quinoline derivative was made in male subjects with uncomplicated acute gonorrhoea using a single oral dose of 200 mg and a single dose of 300 mg. Of the eight patients who received a single dose of 200 mg, post-treatment urethral smears and cultures for N. gonorrhoeae were positive in all and these subjects were considered as treatment failures. In contrast, a single dose of 300 mg was highly effective as all twenty-four who received this dose were cured as judged by negative urethral smears and cultures on the 7th post-treatment day. Of the thirty-eight isolates of M. gonorrhoeae obtained in the study, fifteen (39.5%) were penicillinase-producing, indicating that rosoxacin is effective in treating penicillin-resistant gonorrhoea. Mild to moderate dizziness and/or drowsiness was experienced by four of twenty-nine patients evaluated for safety on the 300 mg single dose, giving an incidence of side-effects of 14%. The symptoms were of brief duration and were self-limiting. A single oral dose of this drug appears to be an ideal treatment for the rapid cure of acute gonorrhoea.

Topics: 4-Quinolones; Acute Disease; Administration, Oral; Adult; Anti-Bacterial Agents; Dose-Response Relationship, Drug; Drug Resistance, Microbial; Gonorrhea; Humans; Male; Microbial Sensitivity Tests; Middle Aged; Neisseria gonorrhoeae; Prostatitis; Quinolines; Quinolones