Metabolism and Techniques for Assay of Trimethoprim and Sulfamethoxazole
Abstract
mation products recognized until now are shown in figure 1. The first formula in the upper row describes the unaltered mother substance by the numbering of the different positions and the chemical name. The other formulas of the upper row represent three metabolites that are excreted exclusively without conjugation: metabolite II (formed by hydroxylation of TMP in the methylene bridge), metabolite III (the N'-oxide), and metabolite VI (the a-carbonyl derivative of TMP). The lower row shows (on the left) two transformation products, in which one of the three methoxy groups of the mother compound is demethylated, namely, that of position 3' in metabolite IV and that of position 4' of the benzyl ring in metabolite I. Both derivatives are excreted in
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The substances expected to be found in urine accounted for approximately 90% of the total signal intensities observed for all sulfamethoxazole-associated signals.
“the substances expected to be found in urine [31] accounted for approximately 90% of the total signal intensities observed for all the sulfamethoxazole-associated signals”
From Pharmacometabolomics Study of Sulfamethoxazole and Trimethoprim in Kidney Transplant Recipients: Real-World Metabolism and Urinary Excretion (2025) · cites this paper as [31]
Glucuronide conjugates of the two demethylated trimethoprim metabolites were found.
“However, glucuronide conjugates of these two metabolites were found, consistent with the previous report [31] stating that both are “excreted partly as such, but mainly conjugated with glucuronic acid.””
From Pharmacometabolomics Study of Sulfamethoxazole and Trimethoprim in Kidney Transplant Recipients: Real-World Metabolism and Urinary Excretion (2025) · cites this paper as [31]
All metabolites expected based on a previous report were detected in this study, except for two demethylated forms of trimethoprim.
“all the metabolites expected to be present based on a previous report [31] were detected in this study, except for two demethylated forms of trimethoprim.”
From Pharmacometabolomics Study of Sulfamethoxazole and Trimethoprim in Kidney Transplant Recipients: Real-World Metabolism and Urinary Excretion (2025) · cites this paper as [31]
The observed metabolite profiles broadly align with the existing mass balance data reported for trimethoprim and sulfamethoxazole.
“the observed metabolite profiles broadly align with the existing mass balance data reported for trimethoprim and sulfamethoxazole”
From Pharmacometabolomics Study of Sulfamethoxazole and Trimethoprim in Kidney Transplant Recipients: Real-World Metabolism and Urinary Excretion (2025) · cites this paper as [31]
Cites
A NEW COUPLING COMPONENT FOR SULFANILAMIDE DETERMINATION
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Self-citationSpectrofluorimetric Method for the Determination of Trimethoprim in Body Fluids
Schwartz, D. E., Koechlin, B. A., & Weinfeld, R. E. (2009) · Chemotherapy · doi:10.1159/000220652 · Cited by 113 · see citing works
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Vree, T. B., van der Ven, A. J. A. M., Koopmans, P. P., van Ewijk-Beneken Kolmer, E. W. J., & Verwey-van Wissen, C. P. W. G. M. (1995) · Clinical Drug Investigation · doi:10.2165/00044011-199509010-00008 · Cited by 18 · see citing works
Hof, M. A. J., de Haan, H., Stepanovic, S., Bakker, S. J. L., Hak, E., Hopfgartner, G., Klont, F., & Investigators, T. (2025) · Metabolites · doi:10.3390/metabo15070473 · Cited by 1 · see citing works
“However, glucuronide conjugates of these two metabolites were found, consistent with the previous report [31] stating that both are “excreted partly as such, but mainly conjugated with glucuronic acid.””
Influential
- Authors
- Rieder, J.
- Affiliations
- F. Hoffmann-La Roche AG (CH)
- Corresponding author
- Rieder, J.
- Venue
- Journal of Infectious Diseases
- Publisher
- Oxford University Press (OUP)
- Published
- 1973-11-01
- Volume
- 128
- Issue
- Supplement 3
- Pages
- S567-S573
- ISSN
- 0022-1899 (ISSN-L)
- 1537-6613
- OpenAlex
- W2023292937
- Cited by
- 43
- References
- 6
- Citations by year
- 2025: 1 · 2024: 1 · 2023: 1 · 2022: 2 · 2019: 1 · 2018: 2 · 2015: 2
- FWCI
- 0.86
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- The Journal of Infectious Diseases (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Physical Sciences › Chemistry › Analytical Chemistry › Analytical Methods in Pharmaceuticals
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Health Sciences › Medicine › Pharmacology › Antibiotics Pharmacokinetics and Efficacy
- Keywords
- trimethoprim, sulfamethoxazole, drug metabolism, metabolites, hydroxylation, N-oxides, demethylation, conjugation, excretion, assay technique
- MeSH terms
- Animals, Bacillus, Biological Assay, Chromatography, Gas, Fluorometry, Humans, Polarography, Protein Binding, Spectrophotometry, Sulfamethoxazole, Sulfur Radioisotopes, Trimethoprim
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