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Related Experiment Videos

[Present status of nitroxoline].

E Bergogne-Berezin1, G Berthelot, C Muller-Serieys

  • 1Service de Microbiologie, CHU Xavier-Bichat, Paris.

Pathologie-Biologie
|June 1, 1987
PubMed
Summary
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Nitroxoline is rapidly absorbed and quickly eliminated in urine, with significant levels detected within an hour. This pharmacokinetic study provides key data for its use in treating urinary tract infections.

Area of Science:

  • Pharmacology
  • Microbiology

Background:

  • Nitroxoline (8-hydroxy-5-nitroquinoline) has a history of use since 1962 for urinary tract infections, primarily against gram-negative bacteria.
  • Recent findings highlight nitroxoline's expanded activity against fungi, Mycoplasma, Ureaplasma urealyticum, and Trichomonas, prompting renewed interest in the drug.

Purpose of the Study:

  • To update knowledge on nitroxoline's behavior in the body.
  • To conduct a pharmacokinetic study of nitroxoline in serum and urine after single and multiple oral doses.

Main Methods:

  • Eight healthy volunteers participated in the study.
  • Serum and urine samples were analyzed using both microbiological assays and High-Performance Liquid Chromatography (HPLC).
  • Comparative analysis was performed on the same samples to assess nitroxoline and its metabolites.

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Main Results:

  • Nitroxoline was rapidly absorbed, with measurable serum levels appearing 15-30 minutes post-administration.
  • Key pharmacokinetic parameters were determined: Tmax (1.75 ± 1.04 h), Cmax (5.59 ± 3.15 mg/l), and t 1/2 beta (2.63 ± 2.66 h).
  • Early hepatic metabolism to conjugated derivatives was observed, with variable kinetics and quantification among subjects.
  • Rapid urinary elimination was evident, with high levels of free and conjugated nitroxoline detected as early as 1 hour and persisting up to 24 hours.

Conclusions:

  • Nitroxoline demonstrates rapid absorption and early hepatic metabolism.
  • The drug is quickly eliminated via urine, maintaining high concentrations for an extended period.
  • These pharmacokinetic findings are crucial for understanding nitroxoline's efficacy and optimizing its use in treating various infections.