Disposition of 14C-oltipraz in animals. Pharmacokinetics in mice, rats and monkeys. Comparison of the biotransformation in the infected mouse and in the schistosomes
Heusse, D.; Marlard, M.; Bredenbac, J.; Decouvelaere, B.; Leroy, J.P.; Bieder, A.; Jumeau, H.
Arzneimittel-Forschung 35(9): 1431-1436
1985
ISSN/ISBN: 0004-4172 PMID: 3936507 Document Number: 242929
14C-oltipraz was given orally to female mice (at 100 and 250 mg/kg) infected with Schistosoma mansoni, and to Rhesus monkeys (20 mg/kg) and rats (50 mg/kg). In each host the pharmacokinetics in the plasma and RBCs were generally similar. In 3 or 4 days the mean urinary elimination of radioactivity was 57, 52 and 40% in monkeys, rats and mice, respectively. Corresponding figures for faecal elimination were 32, 39 and 60%. Most radioactivity was excreted over the first 48 h. There was a low percentage (< 1%) of unchanged oltipraz in the 0 to 24 h urine of mice treated with 100 mg/kg. During the first 24 h in mice, radioactivity was present mainly in the gastro-intestinal tract, bile urine, liver and kidneys. The maximum levels of total radioactivity in both male and female schistosomes occurred at 18 h after drug administration (100 and 375 micro g equivalents oltipraz/g males and females, respectively). Levels in the worms fell much more slowly than those in mouse blood.