| Autor: |
Hardikar MS; Hardikar Hospital, Pune 411005. |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of the Indian Medical Association [J Indian Med Assoc] 2008 Sep; Vol. 106 (9), pp. 615-8, 622, 624. |
| Abstrakt: |
A chiral centre is noted in majority of the NSAIDs. For NSAIDs the enantiomer with S configuration almost exclusively possesses the ability to inhibit prostaglandin activity. R-enantiomers of NSAIDs have poor COX inhibitory activity. Some R-enantiomers are not inert, and many have different actions. The R- to S- chiral inversion varies with biological factors and property of NSAID. The S- to R- chiral inversion is rare for all the NSAIDs. Various preclinical and clinical studies have demonstrated that chirally pure NSAIDs like dexketoprofen, dexibuprofen and S-etodolac are more potent than their respective R enantiomers. Favourable pharmacokinetic and pharmacodynamic profile of dexketoprofen, dexibuprofen and S-etodolac make them effective and well tolerated drug for the treatment of painful inflammatory conditions at half doses of recemate. Thus chiral switch of NSAIDs is a rational approach for the treatment of painful inflammatory conditions. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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