Abstract
Penetration of pefloxacin into the uroepithelium was studied in 20 patients (10 men and 10 women) receiving a single oral dose of 800 mg. Samples of serum, urine, and uroepithelium were taken 1.8 h (mean) after the dose. Pefloxacin and its active metabolite, norfloxacin, were assayed by liquid chromatography, and the microbiologically active compounds were quantified by a microbiological assay. Both procedures were correlated (r>0.7); nevertheless, slight differences detected in concentrations depended on the levels of norfloxacin achieved in the biological samples. The serum and tissue concentrations were higher than the concentration of bactericide (4 μg·ml−1), except in one case. The uroepithelium concentration of pefloxacin was proportional to the serum concentration (r=0.79). The urinary concentrations ranged from 1.2 μg·ml−1 to 82.4 μg·ml−1. The mean norfloxacin/pefloxacin ratios were 3% in serum, 8% in uroepithelium, and 44% in urine. The mean uroepithelium/serum concentration ratios were 1 for pefloxacin and 2.3 for norfloxacin. This result shows that, at a time close to that of the maximum concentration, there is good penetration of pefloxacin and norfloxacin into the uroepithelium.
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References
Gonzales JP, Henwood JM (1989) Pefloxacin. A review of its antibacterial activity, pharmacokinetic properties and thepapeutic use. Drugs 37:628–668
Wolfson JS, Hooper DC, Swartz MN (1989) Mechanisms of action and resistance to quinolone antimicrobial agents. In: Wolfson JS, Hooper DC, (eds) Quinolone antimicrobial agents. AFM Washington DC, pp 5–34
Brykier A, Veyssier, Kazmierzcak A (1994) Fluoroquinolones: propriétés physicochimiques et microbiologiques. In: Encycl Méd Chir (Maladies Infectieuses) Ed. Techniques, Paris, 8–004-B-10, pp 1–12
Montay G, Jacquot C, Bariety J, Cunci R (1985) Pharmacokinetics of pefloxacin in renal insufficiency. Eur J Clin Pharmacol 29:345–349
Barré J, Houin G, Tillement JP (1984) Dose-dependent pharmacokinetic study of pefloxacin, a new antibacterial agent, in humans. J Pharm Sci 73:1379–1382
Griggs DJ, Wise R (1989) A simple isocratic high-pressure liquid chromatographic assay of quinolones in serum. J Antimicrob Chemother 24:437–445
Montay G, Tassel JP (1985) Improved high-performance liquid chromatographic determination of pefloxacin and its metabolite norfloxacin in human plasma and tissue. J Chromatogr 339:214–218
Costa P, Galtier M, Laurelli JM, Nivard G, Louis JF, Favier M, Hansel S, Navratil H, Grasset D (1989) Epididymites aiguës et antibiothérapie. Mesure de la diffusion epididymaire de la péfloxacine. J Urol (Paris) 95:41–44
Johnson RA, Wicher DW (1982) In: Prentice-Hall (ed) Applied multivariate statistical analysis, part III, Chap. 8. Englewood Cliffs, New Jersey, pp. 359–400
Webberley JM, Andrews JM, Ashby JP, McLeod A, Wise R (1987) Pharmacokinetics and tissue penetration of orally administered pefloxacin. Eur J Clin Microbiol 6:521–524
Cardey J, Silvain C, Bouquet S, Breux JP, Becq-Giraudon B, Fourtillan JB, Beauchant M (1987) Oral pharmacokinetics and ascitic fluid penetration of pefloxacin in cirrhosis. Eur J Clin Pharmacol 33:469–472
Brion N, Lassana A, Mosset F, Lefevre JJ, Montay G (1986) Penetration of pefloxacin in human heart valves. J Antimicrob Chemother 17 [Suppl B]:89–92
Menozzi MG, Larini S, Chezzi C, Santini R, Simonazzi M, Bezzi E (1987) Blood, urine and urogenital tract tissue concentrations of norfloxacin (Sebercim*) after single oral dose in human patients. Clin Trials J 24:275–283
Jack DB, Fuentes Gonzales J, Laugher SJ (1986) The rapid measurement of distribution coefficient of 4-quinolones by reversed-phase thin-layer chromatography. International Symposium on new quinolones, Geneva, Switzerland. Abstract
Pangon B, Gehanno P, Daldoss C, Legrand P (1983) Tissue diffusion of pefloxacin: study in man. In: Spitzy KM, Karrer K (eds) Thirteenth International Congress of Chemotherapy. Vienna, part 110, pp 29–31
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Moreau, J.L., Royer-Morrot, M.J., Royer, R.J. et al. Penetration of pefloxacin and its desmethyl metabolite into the uroepithelium after a 800-MG single oral dose in human patients. Eur J Clin Pharmacol 49, 401–405 (1996). https://doi.org/10.1007/BF00203786
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DOI: https://doi.org/10.1007/BF00203786