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

Pharm Weekbl Sci. 1984 Apr 27;6(2):80-7. doi: 10.1007/BF01953959.

Abstract

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.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Chromatography, High Pressure Liquid
  • Chromatography, Thin Layer
  • Dogs
  • Kidney / metabolism
  • Kinetics
  • Protein Binding
  • Sulfamerazine* / analogs & derivatives*
  • Sulfamerazine* / blood
  • Sulfamerazine* / isolation & purification
  • Sulfamerazine* / metabolism

Substances

  • N(4)-acetylsulfamerazine
  • 4-hydroxysulfamerazine
  • N-4-acetyl-4-hydroxysulfamerazine
  • Sulfamerazine