Urinary concentrations and antibacterial activities of nitroxoline at 250 milligrams versus trimethoprim at 200 milligrams against uropathogens in healthy volunteers

Antimicrobial Agents and Chemotherapy
Florian M E WagenlehnerKurt G Naber

Abstract

Because of the increasing bacterial resistance of uropathogens against standard antibiotics, such as trimethoprim (TMP), older antimicrobial drugs, such as nitroxoline (NTX), should be reevaluated. This randomized crossover study investigated the urinary concentrations of parent drugs and their metabolites and their antibacterial activities (urinary inhibitory titers [UITs] and urinary bactericidal titers [UBTs]) against uropathogens at three different urinary pH values within 24 h in six healthy volunteers after a single oral dose of NTX at 250 mg versus TMP at 200 mg. In three additional volunteers, urinary bactericidal kinetics (UBK) were studied after oral administration of NTX at 250 mg three times a day. The mean urinary concentrations of NTX and NTX sulfate in 24 h were 0.012 to 0.507 mg/liter and 0.28 to 27.83 mg/liter, respectively. The mean urinary concentrations of TMP were 18.79 to 41.59 mg/liter. The antibacterial activity of NTX was higher in acidic urine than in alkaline urine, and that of TMP was higher in alkaline urine than in acidic urine. The UITs and UBTs of NTX were generally lower than those of TMP except for a TMP-resistant Escherichia coli strain, for which NTX showed higher UITs/UBTs than did TMP. UBK ...Continue Reading

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Citations

May 14, 2016·Expert Review of Clinical Pharmacology·Noha El Sakka, Ian M Gould
Sep 4, 2014·Antimicrobial Agents and Chemotherapy·M Kresken, B Körber-Irrgang
Oct 22, 2019·The Journal of Antimicrobial Chemotherapy·Fabiola Puértolas-BalintDan I Andersson
Sep 6, 2018·The Journal of Antimicrobial Chemotherapy·Rixt A WijmaAnouk E Muller

Related Concepts

Nitroxoline, potassium salt
Antibiotics
Bacterial Infections
Drug Administration Schedule
Alkalescens-Dispar Group
Hydrogen-Ion Concentration
Klebsiella rhinoscleromatis
Fungus Drug Sensitivity Tests
Nitroquinolines
Proteus mirabilis

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