[Non-steroidal anti-inflammatory drugs and cyclooxygenase-2-specific inhibitors]

Abstract

The discovery of two isoenzymes of cyclooxygenase--COX-1 and COX-2--in the late eighties was followed by an intensive looking for drugs, which inhibit specifically COX-2 and have no influence on COX-1. After some years of trial and error it is now possible to measure the inhibition-capacity--e.g. of Rofecoxib, Celecoxib and all the conventional NSAIDs--in a human blood assay. New insights into localisation, expression and physiological function of COX-2 followed. We now are able to differentiate between "conventional" NSAIDs and COX-2 specific inhibitors (CSI, COXIBS), as a new class of substances. CSI firstly inhibit COX-1/COX-2 to a different extent and in a different manner. Secondly they have a different profile concerning unwanted--especially gastrointestinal--side effects. Further experiences and investigations have to confirm and establish this positive risk/benefit ratio.