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Xenobiotica
the fate of foreign compounds in biological systems
Volume 19, 1989 - Issue 11
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Research Article

Biological fate of sirdalud in animals and man

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Pages 1255-1265 | Received 24 Nov 1988, Accepted 15 Jun 1989, Published online: 22 Sep 2008
 

Abstract

1. 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.

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