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Title: Pharmacokinetics, metabolism, and renal excretion of sulfadimidine and its N4-acetyl and hydroxy metabolites in humans. Author: Vree TB, Hekster YA, Nouws JF, Baakman M. Journal: Ther Drug Monit; 1986; 8(4):434-9. PubMed ID: 3824429. 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.[Abstract] [Full Text] [Related] [New Search]