Metabolites of pipemidic acid in human urine

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Abstract
The urine of men dosed orally with pipemidic acid [an antibacterial agent], contained the metabolites acetylpipemidic, formylpipemidic and oxopipemidic acids together with unchanged pipemidic acid. Each metabolite was equivalent to < 2% of the unchanged pipemidic acid present in human urine. All metabolites showed a similar antibacterial spectrum [Staphylococcus aureus, Bacillus subtilis, Listeria monocytogenes, Streptococcus pneumoniae, Escherichia coli, Shigella flexneri, S. sonnei, Salmonella typhimurium, Klebsiella pneumoniae, Proteus vulgaris, P. morganii, Brucella abortus and Pseudomonas aeruginosa] to pipemidic acid, but their potency was about 10 times lower than that of pipemidic acid. The acute toxicity of the metabolites in mice was as low as the parent compound. The role of the metabolites in the clinical efficacy and toxicity of the drug is likely to be small.