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Pharmacokinetics, Metabolism, and Renal Excretion of Sulfadimidine and Its N4-Acetyl and Hydroxy Metabolites in Humans
Abstract
Sulfadimidine is acetylated and hydroxylated in humans. The hydroxylation pathways account for 10-20% of the dose, leaving the acetylation as the major metabolic pathway. The hydroxylation pathways are independent of the acetylator phenotype. The plasma concentration-time curve of sulfadimidine in fast acetylators is biphasic, with half-lives of 1.7 and 5.4 h, whereas that in slow acetylators is monophasic, with a half-life of 7.6 h. Hydroxylation of a methyl group in sulfadimidine lowers the protein binding from 90 to 60%, while acetylation does not affect the protein binding. Methyl hydroxylation markedly increases the renal clearance.
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“SMX is metabolized by N-acetyltransferases (NAT1/NAT2) to form N4-acetyl sulfamethoxazole (NA-SMX), and by cytochrome P450-mediated oxidation to form SMX-hydroxylamine (SMX-HA).”
From N-Acetyltransferase (NAT) 1 and NAT2 Enzyme Activities Drive Interindividual Variability in Sulfamethoxazole N-Acetylation (2025) · cites this paper as [20]
In the citing paper
“A previous study in 10 male and two female healthy volunteers given an oral dose of sulfamethazine (12–17 mg/kg by bodyweight) showed that 61–81% of the dose was excreted as NA-SMZ, showing that hydroxylation pathways account for 10–20% of the metabolism, which may affect the overall determination of NAT2 activity.20”
From N-Acetyltransferase (NAT) 1 and NAT2 Enzyme Activities Drive Interindividual Variability in Sulfamethoxazole N-Acetylation (2025) · cites this paper as [20]
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Metadata
- Authors
- Vree, T. B., Hekster, Y. A., Nouws, J. F. M., & Baakman, M.
- Affiliations
- Radboud University Nijmegen (NL)
- Corresponding author
- Vree, T. B.
- Hekster, Y. A.
- Venue
- Therapeutic Drug Monitoring
- Published
- 1986-12
- Volume
- 8
- Issue
- 4
- Pages
- 434-439
- ISSN
- 0163-4356 (ISSN-L)
- OpenAlex
- W2003333461
- Cited by
- 21
- References
- 0
- Citations by year
- 2025: 1 · 2024: 2 · 2020: 1 · 2015: 2 · 2012: 1
- FWCI
- 2.25
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Therapeutic Drug Monitoring (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Health Sciences › Medicine › Pharmacology (medical) › Antibiotics Pharmacokinetics and Efficacy
- Health Sciences › Medicine › Pharmacology (medical) › Drug-Induced Adverse Reactions
- Keywords
- sulfamethazine, pharmacokinetics, drug metabolism, hydroxylation, acetylator phenotype, renal excretion, renal clearance, plasma protein binding, half-life, sulfonamide metabolites
- MeSH terms
- Acetylation, Adult, Female, Half-Life, Humans, Kinetics, Male, Phenotype, Protein Binding, Sulfamethazine
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