title: Effect of amiodarone and desethylamiodarone on the pharmacokinetics of antipyrine in the rat.
abstract: The effect of amiodarone on hepatic drug metabolism in vivo was examined in the rat using antipyrine as a model substrate. Pretreatment with oral amiodarone hydrochloride, 100 mg/kg/day, for 5 days resulted in a 19% reduction in antipyrine clearance and a 22% increase in half-life. The administration of single oral doses of amiodarone hydrochloride, 100 mg/kg, 1 or 5 hr prior to antipyrine administration had no significant effect on antipyrine pharmacokinetics. The administration of a single intravenous dose of amiodarone hydrochloride, 50 mg/kg, reduced antipyrine clearance by 32% and increased the half-life by 46%. The desethyl metabolite of amiodarone was also found to reduce antipyrine clearance (21%) after a single oral dose of 100 mg/kg.
mesh_terms: D000284:Administration, Oral; D000638:Amiodarone / Q000031:analogs & derivatives* / Q000494:pharmacology*; D000818:Animals; D000983:Antipyrine / Q000097:blood / Q000493:pharmacokinetics*; D004305:Dose-Response Relationship, Drug; D007275:Injections, Intravenous; D008099:Liver / Q000187:drug effects / Q000378:metabolism*; D008297:Male; D008657:Metabolic Clearance Rate / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains
chemical_list: C036116:desethylamiodarone; D000638:Amiodarone; D000983:Antipyrine