The comparative pharmacokinetics of five quinolones

Abstract

The pharmacokinetics and tissue penetration of five quinolones were studied in volunteers. The compounds were norfloxacin (400 mg po), enoxacin (400 mg iv and 600 mg po), ciprofloxacin (100 mg iv and 500 mg po), ofloxacin (600 mg po) and pefloxacin (400 mg iv). Of the oral agents studied ofloxacin and ciprofloxacin were the most rapidly absorbed (Tmax = 1.2 h) and enoxacin the least (Tmax = 1.9 h). The serum levels attained were highest in the case of ofloxacin (after allowing for the higher dose administered). The serum half-lives were norfloxacin 3.75 h, ciprofloxacin 3.9 h (po), 4.0 h (iv), ofloxacin 7.0 h, enoxacin 6.2 h (po), 5.1 h (iv) and pefloxacin 10.5 h. All agents penetrated blister fluid readily. The 24 h urine recovery was 62% for oral enoxacin, 46.4% for iv enoxacin (plus 12.2% for oxo-enoxacin), 27% for norfloxacin, 30.6% for oral ciprofloxacin, 75.7% for iv ciprofloxacin, 73% for ofloxacin and 4.9% for pefloxacin (plus 9.2% for the norfloxacin metabolite and 17.8% for pefloxacin N-oxide).