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 (1...

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Bibliographic Details
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
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Summary: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.
ISSN:0031-6970
1432-1041
DOI:10.1007/BF00544237