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Pharmacodynamics and Pharmacokinetics of the Profens: Enantioselectivity, Clinical Implications, and Special Reference to S(+)-Ibuprofen

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dc.contributor.authorEvans, A.M.
dc.date.issued1996
dc.description.abstractThe 2-arylpropionic acid derivatives, or "profens," are an important class of nonsteroidal antiinflammatory drugs (NSAIDs) that have been in clinical use for almost 30 years. Widely used members of this drug class include naproxen, ibuprofen, ketoprofen, flurbiprofen, and tiaprofenic acid. With the exception of S-naproxen, the profens have until recently been used clinically as racemic agents, and a "single enantiomer versus racemate" debate has emerged. Several important issues should be considered in the debate: the antinociceptive activity of the R-enantiomer of at least one profen (flurbiprofen), the possible role of cyclooxygenase (COX)-independent properties of the R-enantiomers in the gastrointestinal toxicity of the racemates, the increase in the formation of potentially immunogenic drug-protein adducts when racemates are administered, and the likelihood that the use of racemates increases the propensity of the profens to alter the pharmacokinetics of other drugs. This review will demonstrate how the use of individual enantiomers can improve understanding of the mechanisms by which the profens elicit their biologic effects.
dc.identifier.citationJournal of Clinical Pharmacology, 1996; 36(S12):7-15
dc.identifier.doi10.1002/j.1552-4604.1996.tb00003.x
dc.identifier.issn0091-2700
dc.identifier.issn1552-4604
dc.identifier.urihttps://hdl.handle.net/1959.8/43359
dc.language.isoen
dc.publisherWiley Blackwell Publishing
dc.rightsCopyright 1996 American College of Clinical Pharmacology
dc.source.urihttps://doi.org/10.1002/j.1552-4604.1996.tb00003.x
dc.subjectpranoprofen
dc.subjectdrug absorption
dc.subjectdrug clearance
dc.subjectdrug distribution
dc.subjectdrug effect
dc.subjectalminoprofen
dc.subjectbenoxaprofen
dc.subjectbermoprofen
dc.subjectcarprofen
dc.subjectcicloprofen
dc.subjectfenoprofen
dc.subjectflunoxaprofen
dc.subjectibuprofen
dc.subjectindoprofen
dc.subjectrug mechanism
dc.subjectenantiomer
dc.subjectgastrointestinal toxicity
dc.titlePharmacodynamics and Pharmacokinetics of the Profens: Enantioselectivity, Clinical Implications, and Special Reference to S(+)-Ibuprofen
dc.typeJournal article
pubs.publication-statusPublished
ror.mmsid9915912125401831

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