Activity of metronidazole and its hydroxy and acid metabolites against clinical isolates of anaerobic bacteria.
Susceptibility of clinical isolates of anaerobic bacteria to metronidazole and its two oxidation products, 1-(2-hydroxyethyl)-2-hydroxymethyl-5-nitroimidazole (the "alcohol" metabolite) and 2-methyl-5-nitroimidazole-1-acetic acid (the "acid" metabolite), were determined by the agar dilution technique. Results disclosed that the alcohol metabolite, although less active than metronidazole, inhibited the organisms tested at levels considered susceptible for metronidazole. The acid metabolite was less active, not inhibiting the organisms at levels within the susceptible range. In other studies, mixtures of known concentrations of metronidazole and the metabolites were assayed in a bioassay system used to measure metronidazole levels. These studies showed that the bioassay will measure metronidazole or the alcohol metabolite; the acid metabolite is not measured at levels achieved in clinical specimens. Since the activity of the alcohol metabolite is comparable to that of metronidazole, we feel that microbiological assays can be used for therapeutic monitoring of metronidazole levels in clinical situations.
D000693:Anaerobiosis; D001419:Bacteria / Q000187:drug effects*; D001681:Biological Assay; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D008795:Metronidazole / Q000378:metabolism / Q000494:pharmacology*
D008795:Metronidazole