Imipenem (thienamycin formamidine) is an antibiotic active against a broad spectrum of bacteria. Its primary metabolite arises from cleavage of the lactam ring. The metabolite can be formed in-vitro by acid-catalyzed or enzymatic hydrolysis. In animals and man, this metabolite can be generated systemically as well as in the kidneys following the excretion of imipenem into the urine. In man, this dehydropeptidase-catalyzed renal metabolism is minimized by the coadministration of cilastatin, a competitive inhibitor. A specific HPLC assay has been developed to evaluate the disposition of this metabolite in humans having normal or end-stage renal function. The assay employs ion-pair, reversed-phase chromatography, and post-column acid treatment of the analyte for ultraviolet detection.
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