title: The pharmacokinetics and therapeutic efficacy of fleroxacin and pefloxacin in a rat abscess model.
abstract: The penetration, pharmacokinetics and therapeutic efficacy of fleroxacin and pefloxacin were investigated in a rat abscess model. Abscesses were induced by implanting a dialysis tube unit contaminated with Serratia marcescens in the subcutaneous tissue. Simultaneous serum, interstitial fluid (IF) and abscess fluid concentrations of the investigated antibiotics were measured 24 and 96 h after implantation. The concentrations were determined at various time intervals after the last intramuscular administration of each drug (20 mg/kg). Peak fleroxacin and pefloxacin concentrations in the serum of the infected animals were 14.6 +/- 4.7 mg/l and 13 +/- 2.9 mg/l respectively, peak fleroxacin and pefloxacin abscess fluid concentrations after 24 h were 12.3 +/- 2.5 mg/l and 8.9 +/- 2.2 mg/l, respectively (85% and 68% of peak serum concentrations). Abscess fluid concentrations at 96 h were: fleroxacin 4.7 +/- 2.6 mg/l and pefloxacin 4.5 +/- 1.7 mg/l. Both antimicrobials persisted significantly longer in the abscess fluid than in serum. Both drugs failed to sterilize the abscesses following a single administration; however after four consecutive administrations all abscesses became sterile. We conclude that fleroxacin and pefloxacin may be suitable for the therapy of closed space infections caused by susceptible micro-organisms.
authors.affiliation: Infectious Diseases Unit, Chaim Sheba Medical Center, Tel-Aviv University School of Medicine, Tel-Hashomer, Israel.
authors.forename: E
authors.initials: E
authors.lastname: Leibovitz
authors.forename: G
authors.initials: G
authors.lastname: Keren
authors.forename: M
authors.initials: M
authors.lastname: Shabtai
authors.forename: A
authors.initials: A
authors.lastname: Barzilai
authors.forename: E
authors.initials: E
authors.lastname: Rubinstein
mesh_terms: D000038:Abscess / Q000188:drug therapy* / Q000382:microbiology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000493:pharmacokinetics / Q000627:therapeutic use*; D002939:Ciprofloxacin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D015169:Colony Count, Microbial; D004195:Disease Models, Animal; D004756:Enterobacteriaceae Infections / Q000188:drug therapy* / Q000382:microbiology; D005260:Female; D016576:Fleroxacin; D006207:Half-Life; D015366:Pefloxacin / Q000493:pharmacokinetics / Q000627:therapeutic use*; D051381:Rats; D012706:Serratia marcescens
chemical_list: D000900:Anti-Bacterial Agents; D015366:Pefloxacin; D002939:Ciprofloxacin; D016576:Fleroxacin