Isolation and identification of 4-hydroxysulfamerazine and preliminary studies on its pharmacokinetics in dogs.
For the following compounds: sulfamerazine, 4- hydroxysulfamerazine , N4- acetylsulfamerazine , N4-acetyl-4- 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.
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D004285:Dogs; D007668:Kidney / Q000378:metabolism; D007700:Kinetics; D011485:Protein Binding; D013416:Sulfamerazine / Q000031:analogs & derivatives* / Q000097:blood / Q000302:isolation & purification / Q000378:metabolism; D000096926:Benzenesulfonamides
D013416:Sulfamerazine; C037923:N(4)-acetylsulfamerazine; C041654:4-hydroxysulfamerazine; D000096926:Benzenesulfonamides; C041655:N-4-acetyl-4-hydroxysulfamerazine