The influence of endotoxin-induced inflammation on the enantioselective phannacokinetics of propranolol, oxprenolol, and verapamil, which bind to a,-acid glycoprotein, was studied in the rat. The racemic mixtures were given orally. In the control animals, for propranolol and oxprenolol, the plasma c
Stereoselective pharmacokinetics of oxprenolol, propranolol, and verapamil: Species differences and influence of endotoxin
β Scribed by Martine E. Laethem; Frans M. Belpaire; Pascal Wijnant; Marc G. Bogaert
- Publisher
- John Wiley and Sons
- Year
- 1995
- Tongue
- English
- Weight
- 625 KB
- Volume
- 7
- Category
- Article
- ISSN
- 0899-0042
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β¦ Synopsis
The influence of endotoxin-induced inflammation was studied on the pharmacokinetics of the enantiomers of the racemic drugs oxprenolol, propranolol, and verapamil in rabbits and dogs. Enantioselective pharmacokinetics were seen for oxprenolol and propranolol in the rabbit and for propranolol and verapamil in the dog. In the dog, the enantioselective differences in plasma concentrations are due to differences in both protein binding and metabolism, whereas in the rabbit the ddferences are due solely to ddferences in metabolism. In both species endotoxin treatment increases the plasma concentrations of the enantiomers of the three drugs; both protein binding and metabolism are influenced. In rabbits and in dogs, the influence of endotoxin on the disposition of the three drugs is less enantioselective than was previously observed in the rat.
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