Penetration of pefloxacin and its desmethyl metabolite into the uroepithelium after a 800-mg single oral dose in human patients.
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 micrograms.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 micrograms.ml-1 to 82.4 micrograms.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.
Moreau
J L
JL
Clinique Ambroise Paré, Nancy, France.
Royer-Morrot
M J
MJ
Lozniewski
A
A
Trackoen
G
G
Delavault
P
P
Royer
R J
RJ
D000284:Administration, Oral; D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000652:urine; D000892:Anti-Infective Agents, Urinary / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000652:urine; D002853:Chromatography, Liquid; D004848:Epithelium / Q000378:metabolism; D005260:Female; D006801:Humans; D008297:Male; D008826:Microbial Sensitivity Tests; D008875:Middle Aged; D009643:Norfloxacin / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D015366:Pefloxacin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D012044:Regression Analysis; D001743:Urinary Bladder / Q000378:metabolism
D000890:Anti-Infective Agents; D000892:Anti-Infective Agents, Urinary; D015366:Pefloxacin; D009643:Norfloxacin