COX-1 AND COX-2 INHIBITION - WISH AND REA LITY OF A SPECIFIC THERAPY WITH NONSTEROIDAL ANTIRHEUMATICS

Nonsteroidal anti-inflammatory drugs (NSAIDs) exert their anti-inflamm atory action as well as most of their unwanted side effects via inhibi tion of cyclooxygenase (COX), the key enzyme of prostaglandin biosynth esis. It has been recently shown that at least 2 isozymes of cyclooxyg enase exist which differ in regulation and in their physiological func tions. COX-1 is a constitutive enzyme with important physiological fun ctions i.e. in the kidney and the GI-tract. On the other hand the indu cible COX-2 is responsible for pathophysiological processes such as in flammation. These differences between both isozymes may lead to the de velopment of selective COX-2 inhibitors with less renal and gastrointe stinal side effects. Numerous in vitro studies have shown that there a re indeed selective COX-2 inhibitors which are, however, not yet on th e market. In animal experiments they proved to be effective anti-infla mmatory agents with a lower incidence of gastrointestinal side effects . However, further experimental and clinical studies will be necessary , mainly with regard to new untypical side effects to show whether or not selective COX-2 inhibitors are of clinical value in the treatment of rheumatic disorders.