Differential inhibition of cyclooxygenase-1 (COX-1) and-2 (COX-2) by NSAIDS: Consequences on anti-inflammatory activity versus gastric and renal safety |
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| Authors: | M Pairet L Churchill G Trummlitz G Engelhardt |
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| Institution: | (1) Department of Biological Research, Boehringer Ingelheim Research Laboratories, Birkendorfer Strasse 65, 88397 Biberach an der Riss, Germany;(2) Department of Inflammatory Disease, Boehringer Ingelheim Pharmaceuticals Inc., Ridgefield, CT, USA |
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| Abstract: | The discovery of an inducible isoform of cyclooxygenase (COX-2) requires a refinement of the theory that inhibition of cyclooxygenase
activity is responsible for both therapeutic and side-effects of nonsteroidal anti-inflammatory drugs (NSAIDs). Pharmacological
results with developmental compounds suggest that COX-2 is the relevant target for the therapeutic (i.e. anti-inflammatory)
effects of NSAIDs, whereas gastric and renal side-effects are related to inhibition of constitutive COX-1. However a role
of COX-1 in inflammation cannot be excluded. Furthermore, more research effort is needed to investigate the functional relevance
of COX-2 in normal tissue. |
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| Keywords: | COX-1 COX-2 NSAIDs |
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