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Biological fate of sirdalud in animals and man

1989; Taylor & Francis; Volume: 19; Issue: 11 Linguagem: Inglês

10.3109/00498258909043177

1366-5928

P. Koch, David R. Hirst, B. R. Von Wartburg,

Ion channel regulation and function

Abstract1. Biotransformation and excretion of the muscle relaxant drug, sirdalud, were studied after oral doses of 14C- and 3H-sirdalud in rats, dogs, rabbits, mice and humans. Sirdalud was well absorbed and almost completely metabolized in the five species.2. Excretion of metabolites was rapid and complete within a few days; the urine/faeces excretion ratio of the 14C label was about 70/30 in all species. Major metabolic pathways of sirdalud were oxidative degradation of the imidazoline ring and oxidation of the aromatic system.3. A novel oxidative biotransformation pathway of the benzothiadiazole ring system of sirdalud gave a sulphone analogue of the parent drug.