Abstract:
:The influence of endotoxin-induced inflammation on the enantioselective pharmacokinetics of propranolol, oxprenolol, and verapamil, which bind to alpha 1-acid glycoprotein, was studied in the rat. The racemic mixtures were given orally. In the control animals, for propranolol and oxprenolol, the plasma concentrations of the (R)-enantiomer were higher than those of the (S)-enantiomer, while for verapamil the reverse was true. Protein binding and intrinsic clearance are the main factors responsible for this enantioselectivity. After endotoxin treatment, for the three drugs tested the plasma concentrations and the plasma binding of both enantiomers were significantly increased. This effect was more pronounced for (R)-propranolol, (R)-oxprenolol, and (S)-verapamil than for their respective antipodes. The enantioselective effect of endotoxin on the plasma concentrations of the drugs studied seems mainly due to the enantioselective increase in binding to alpha 1-acid glycoprotein.
journal_name
Chiralityjournal_title
Chiralityauthors
Laethem ME,Belpaire FM,Wijnant P,Rosseel MT,Bogaert MGdoi
10.1002/chir.530060508subject
Has Abstractpub_date
1994-01-01 00:00:00pages
405-10issue
5eissn
0899-0042issn
1520-636Xjournal_volume
6pub_type
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