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COX-2-specific inhibitors. The emergence of a new class of analgesic and anti-inflammatory drugs
EVERTS B; WAHRBORG P; HEDNER T
CLIN RHEUMATOL , 2000, vol. 19, n° 5, p. 331-343 Doc n°: 97546 Localisation : Bibliothèque Universitaire de Médecine de Nancy Descripteurs : DA6 - TRAITEMENTS - APPAREIL LOCOMOTEUR The prostaglandin series of bioactive compounds is formed by the interaction of two distinct but related enzymes, cyclo-oxygenase-1 (COX-1) and cyclo-oxygenase-2 (COX-2). COX-1 is a constitutive form which is present mainly in the gastric mucosa, kidney and platelets. COX-2 is mainly an inducible form, although also to some extent present constitutively in the CNS, the juxtaglomerular apparatus of the kidney and in the placenta during late gestation. Both isoforms contribute to the inflammatory process, but COX-2 is of considerable therapeutic interest as it is induced, resulting in an enhanced formation of prostaglandins, during acute as well as chronic inflammation. Conventional NSAIDs inhibit both isoforms to a similar extent and in an approximately equal dose and concentration range. The two recently developed and clinically available selective COX-2 inhibitors, celecoxib and rofecoxib, are about 100-1000 times more selective on the Langue : ANGLAIS Identifiant basis : 2000213472 |
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