Chiral NSAIDS: so what?
There are often both pharmacodynamic and pharmacokinetic differences between enantiomers. Intuitively then, the use of single enantiomers of chiral NSAIDs is preferable to administering the racemate and monitoring the "active" enantiomer in studies involving racemic drugs is preferred. However, limited clinical studies of (S)-2-arylpropionates, while demonstrating expected antiinflammatory activity, have not yet improved attempts to establish concentration-effect relationships for these drugs. This may be because actions of the "inactive" (R)-enantiomers are important or it may be a reflection of a greater variability in other factors such as the disease itself and methods to assess disease activity.
Department of Clinical Pharmacology, St. Vincent's Hospital, Sydney, Australia.
K M
KM
Williams
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006801:Humans; D050356:Lipid Metabolism; D013237:Stereoisomerism
D000894:Anti-Inflammatory Agents, Non-Steroidal