PROTEIN-BINDING AND STEREOSELECTIVITY OF NONSTEROIDAL ANTIINFLAMMATORY DRUGS

Stereoselective binding of nonsteroidal anti-inflammatory drugs (NSAID s) can be studied using various techniques. Thus the results obtained by different investigators may be poorly consistent and even contradic tory. NSAIDs are bound stereoselectively to serum albumin to different degrees depending on the drug investigated (ibuprofen, indoprofen, ca rprofen, etodolac, ketoprofen and flurbiprofen). For other drugs, both enantiomers are bound to a similar extent (pirprofen, fenoprofen). Th is stereoselectivity could vary with experimental conditions, in parti cular with protein concentration (ketoprofen, etodolac), leading to in dividual differences. Finally, the stereoselectivity of protein bindin g and of pharmacokinetics can be compared: differences in binding betw een enantiomers can explain their differences in pharmacokinetics, onc e metabolic properties such as inversion have been taken into account.