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

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

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 conjugate...

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Bibliographic Details
Published in:The Journal of infectious diseases Vol. 128; no. Supplement-3; pp. S580 - S583
Main Authors: Sigel, Carl W., Kunin, Calvin M., Grace, Michael E., Nichol, Charles A.
Format: Journal Article
Language:English
Published: United States The University of Chicago Press 01-11-1973
University of Chicago Press
Subjects:
Chromatography, Thin Layer
Cyclic N-Oxides - urine
Dosage
Fluorescence
Humans
Male
Metabolic diseases
Metabolites
Methods
Radioactive decay
Research and development laboratories
Section II. Metabolism and Pharmacokinetics
Solvents
Trimethoprim - metabolism
Trimethoprim - urine
Urine
Writing tablets
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Summary: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.
Bibliography:istex:FBAB7F8593A6239209587E05F45FE5AB88112750
Please address requests for reprints to Dr. Carl W. Sigel, Wellcome Research Laboratories, Burroughs Wellcome Company, Research Triangle Park, N.C. 27709.
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ISSN:0022-1899
1537-6613
DOI:10.1093/infdis/128.Supplement_3.S580