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Molecular Pharmacology, Vol 17, 239-244, Copyright © 1980 by the American Society for Pharmacology and Experimental Therapeutics

The Reductive Metabolism of Metronidazole and Ronidazole by Aerobic Liver Microsomes

EDWARD PEREZ-REYES 1, B. KALYANARAMAN 1, and RONALD P. MASON 1

1 Laboratory of Environmental Biophysics, National Institute of Environmental Health Sciences, Post Office Box 12233, Research Triangle Park, North Carolina 27709

Rat hepatic microsomal incubations supplemented with NADPH reduce metronidazole to its nitro anion radical. Under aerobic conditions, oxygen reacts with the anion radical to produce superoxide and to regenerate metronidazole. Superoxide production was followed by spin-trapping with DMPO, by the adrenochrome assay, and by the stimulation of oxygen consumption. Under anaerobic conditions, the anion radical is thought to be further reduced to a toxic intermediate. This metabolic cycle explains the reductive activation of metronidazole, and provides an explanation for the selective toxicity of metronidazole toward anaerobic infections and hypoxic tumor cells. Ronidazole follows the same metabolic pathway, so it is likely that all 5-nitroimidazoles will have an aerobic futile metabolism.

Submitted on September 7, 1979
Accepted on November 12, 1979




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