Biliary excretion of conjugated hydroxyl benzodiazepines after administration of several benzodiazepines to rats, guinea pigs, and mice
✍ Scribed by Paolo Bertagni; Franca Marcucci; Emilio Mussini; Silvio Garattini
- Publisher
- John Wiley and Sons
- Year
- 1972
- Tongue
- English
- Weight
- 218 KB
- Volume
- 61
- Category
- Article
- ISSN
- 0022-3549
No coin nor oath required. For personal study only.
✦ Synopsis
The extent of biliary excretion of diazepam, N-demethyldiazepam, N-methyloxazepam, and oxazepam was studied in rats, guinea pigs, and mice. The intravenous administration of diazepam and N-demethyldiazepam was not followed by the excretion of these compounds or the corresponding hydroxylated free metabolites Nmethyloxazepam and oxazepam. respectively, in the bile of the three animal species. In rats, no conjugated derivatives were detected in the bile; in guinea pigs and mice, 3 and 4 % and 13 and 33 of diazepam and N-demtthyldiazepam, respectively, were recovered as conjugated oxazepam. The injection of N-methyloxazepam resulted in a lower excretion of conjugated N-methyloxazepam and oxazepam in rats than in guinea pigs or in mice. When oxazepam was injected intravenously, conjugated oxazepam was 6.5 and about 10 times higher in the bile of guinea pigs and mice, respectively, than of rats. The fact that hydroxylated metabolites are excreted as conjugated derivatives more by mice and guinea pigs than by rats may suggest the hypothesis of a more extensive enterohepatic circulation of these compounds in mice and guinea pigs than in rats.
Kepphrases 0 Benzodiazepines, conjugated hydroxyl-biliary excretion in rats, guinea pigs, mice 0 Biliary excretion+onjugated hydroxyl benzodiazepines in rats, guinea pigs, mice 0 Diazepam and N-demethyldiazepam-biliary excretion in rats, guinea pigs, mice 0 Oxazepam and N-methyloxazepam-biliary excretion in rats, guinea pigs, mice * Predoctoral fellow supported by U. Ravizza,