Oral pharmacokinetics and ascitic fluid penetration of pefloxacin in cirrhosis.
Plasma and ascitic fluid concentrations of pefloxacin in 10 cirrhotic patients and 8 healthy volunteers were determined following administration of a single oral dose of 400 mg. The mean elimination half-life was significantly increased in the patients (29.0 h) compared to in 8 healthy volunteers (12.3 h). In patients, the total plasma clearance (2.71 vs 6.85 l/h) and volume of distribution (1.12 vs 1.67 l/kg) were decreased. Estimated by the ratio of the AUC in peritoneal fluid and plasma, ascitic fluid penetration was 68% after one oral dose, and pronounced accumulation of pefloxacin in ascites was found after repeated doses. Oral pefloxacin would seem to be a convenient and useful treatment of spontaneous, gram-negative, bacterial peritonitis in cirrhosis. However, the decreased hepatic metabolism of the drug leads to a marked accumulation in plasma and ascites after repeated doses, and a reduced dose is required in these patients.
D000328:Adult; D000368:Aged; D000890:Anti-Infective Agents / Q000097:blood / Q000493:pharmacokinetics*; D001202:Ascitic Fluid / Q000378:metabolism*; D004058:Diffusion; D005260:Female; D006801:Humans; D008104:Liver Cirrhosis, Alcoholic / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D009643:Norfloxacin / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics; D015366:Pefloxacin
D000890:Anti-Infective Agents; D015366:Pefloxacin; D009643:Norfloxacin