Metabolites of pipemidic acid in human urine.

1. The urine of men dosed orally with pipemidic acid, contained the metabolites acetylpipemidic, formylpipemidic and oxopipemidic acids together with unchanged pipemidic acid. 2. Each metabolite was equivalent to less than 2% of the unchanged pipemidic acid present in human urine. 3. All metabolites showed a similar antibacterial spectrum 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. 4. These results indicate that the role of the metabolites in the clinical efficacy and toxicity of the drug is likely to be small.