Metabolism of Trimethoprim in Man and Measurement of a New Metabolite: A New Fluorescence Assay

Abstract
Urinary concentrations of trimethoprim (TMP) and its metabolites were measured in eight healthy subjects after oral administration of 160 mg of TMP in two tablets of Septra® (trimethoprim-sulfamethoxazole). Improved procedures for extraction of polar metabolites and for enzymic cleavage of conjugated products were applied. The 1-oxide and conjugates of demethylated metabolites were found in substantially higher concentrations than those previously reported. A new metabolite, the 3-oxide of TMP, was identified, and urinary levels of this product were also measured.

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