Biological fate of sirdalud in animals and man.
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.
Koch
P
P
Sandoz Ltd, Basle, Switzerland.
Hirst
D R
DR
von Wartburg
B R
BR
D000284:Administration, Oral; D000327:Adsorption; D000818:Animals; D001711:Biotransformation; D002250:Carbon Radioisotopes; D003000:Clonidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism / Q000493:pharmacokinetics; D004285:Dogs; D005243:Feces / Q000032:analysis; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D008657:Metabolic Clearance Rate; D051379:Mice; D009125:Muscle Relaxants, Central / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D051381:Rats; D011919:Rats, Inbred Strains
D002250:Carbon Radioisotopes; D009125:Muscle Relaxants, Central; C023754:tizanidine; D003000:Clonidine