Isolation and identification of 4-hydroxysulfamerazine and preliminary studies on its pharmacokinetics in dogs

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Abstract
For the following compounds: sulfamerazine, 4-hydroxysulfamerazine, N4acetylsulfamerazine, N4-acetyl4-hydroxysulfamerazine, the following data are reported: biosynthesis in the dog, isolation, identification by MS and NMR, TLC (Rf values) and HPLC (capacity factors and molar extinction), half-life of elimination, metabolism, renal excretion and protein binding in dog. Dogs are unable to acetylate sulfamerazine, but eliminate predominantly by hydroxylation of the N1-substituent. Administered N4-acetylsulfamerazine is predominantly eliminated by deacetylation to sulfamerazine which in turn is hydroxylated. The renal clearances of sulfamerazine and N4-acetylsulfamerazine in the dog are identical. The renal excretion of both compounds proceeds by the passive processes of glomerular filtration and tubular reabsorption.4-Hydroxysulfamerazine and its glucuronide have a higher renal clearance than sulfamerazine.