Oral pharmacokinetics and ascitic fluid penetration of pefloxacin in cirrhosis

• Published in: European journal of clinical pharmacology 1987-01, Vol.33 (5), p.469-472
• Main Authors: CARDEY, J, SILVAIN, C, BOUQUET, S, BREUX, J. P, BECQ-GIRAUDON, B, FOURTILLAN, J. P, BEAUCHANT, M
• Format: Article
• Language: English
• Subjects: Adult; Aged; Anti-Infective Agents - blood; Anti-Infective Agents - pharmacokinetics; Antibacterial agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Ascitic Fluid - metabolism; Biological and medical sciences; Diffusion; Female; Humans; Liver Cirrhosis, Alcoholic - metabolism; Male; Medical sciences; Middle Aged; Norfloxacin - analogs & derivatives; Norfloxacin - blood; Norfloxacin - pharmacokinetics; Pefloxacin; Pharmacology. Drug treatments
• ISSN: 0031-6970; 1432-1041
• DOI: 10.1007/BF00544237

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.