Summary
The kinetics of pefloxacin has been studied after a single intravenous infusion of 8 mg·kg−1 in 15 male patients with various degrees of renal failure. No difference in distribution or elimination of the drug was observed between patients with mild or severe renal impairment. The mean volume of distribution (Vd area) and the mean plasma clearance were 2.03l·kg−1 and 121.3 ml·min−1, respectively. The mean apparent elimination half-life was 13.5 h. These values are close to those observed in healthy subjects. No accumulation of the active N-desmethylmetabolite was observed in cases of severe failure as compared to mild impairment; its apparent elimination half-life was about twice that of the parent drug. The efficacy of a 4 h haemodialysis in 6 additional anuric subjects done to remove pefloxacin from the body was poor.
Similar content being viewed by others
References
Thibault M, Koumare B, Soussy CJ, Duval J (1981) Relations structure-activité dans le groupe des quinolones. Etude de l'activité antibactérienne de deux nouveaux composés. Ann Microbiol (Paris) 132: 267–281
Thabaut A, Durosoir JL (1982) Activité antibactérienne comparée in vitro de la pefloxacine (1589 RB), de l'acide nalidixique, de l'acide pipémidique et de la fluméquine. Pathol Biol (Paris) 30: 394–397
Hoogkamp-Korstanje JAA (1984) Comparative in vitro activity of five quinoline derivatives and five other antimicrobial agents used in oral therapy. Eur J Clin Microbiol 3: 333–338
Van Caekenberghe DL, Pattyn SR (1984) In vitro activity of ciprofloxacin compared with those of other new fluorinated piperazinyl-substituted quinoline derivatives. Antimicrob Agents Chemother 25: 518–521
Gaillot J, Frydman A, Le Roux Y, Fourtillan JB, Lefebvre MA, Duchier J, Djebbar F (1983) Pharmacokinetics of pefloxacin in man during a repeated treatment (400 mg b.i.d.) with i.v. infusion. In: Spitzy KH, Karrer K (éds.) Thirteenth International Congress of Chemotherapy, Vienna, part 110, pp 18–22
Wolff M, Regnier B, Daldoss C, Nkam M, Vachon F (1984) Penetration of pefloxacin into cerebrospinal fluid of patients with meningitis. Antimicrob Agents Chemother 26: 289–291
Montay G, Goueffon Y, Roquet F (1984) Absorption, distribution, metabolic fate and elimination of pefloxacin mesylate in mice, rats, dogs, monkeys and humans. Antimicrob Agents Chemother 25: 463–472
Montay G, Blain Y, Roquet F, Le Hir A (1983) High-performance liquid chromatography of pefloxacin and its main active metabolites in biological fluids. J Chromatogr 272: 359–365
Montay G, Tassel JP (1985) Improved high-performance liquid chromatographic determination of pefloxacin and its main active metabolite in human plasma or tissue. J Chromatogr 339: 214–218
D'Argenio DZ, Schumitzy A (1979) A program package for simulation and parameter estimation in pharmacokinetic systems. Comput Programs Biomed 9: 115–134
Gibaldi M, Perrier D (1975) Pharmacokinetics. Marcel Dekker, New-York
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Montay, G., Jacquot, C., Bariety, J. et al. Pharmacokinetics of pefloxacin in renal insufficiency. Eur J Clin Pharmacol 29, 345–349 (1985). https://doi.org/10.1007/BF00544092
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00544092