[Non-steroidal anti-inflammatory agents (NSAID's) with lesser side effects by selective inhibition of cyclo-oxygenase-2].
The efficacy and the adverse effects of non-steroid anti-inflammatory drugs (NSAIDs) are related mostly to inhibition of cyclo-oxygenase (COX), the main enzyme in prostaglandin synthesis. There are two isoenzymes: COX-1, mostly involved in the production of prostaglandins that are important for the normal function of the organism, such as protection of the stomach, vascular homeostasis and kidney function, and COX-2 which is induced by proinflammatory stimuli and is mostly present in inflammatory cells. Conceivably, the COX-1 and COX-2 functions are not separated very strictly. For instance, COX-2 may also come to expression as a reaction to physiological stimuli not connected with an inflammation. It is not yet clear how COX-2 selectivity can best be assessed. The degree of selectivity depends among other things on the test used and the time interval after which the activity is read. Because of the variable findings it is important to rank different NSAIDs on the basis of one and the same test. Use of NSAIDs that mostly inhibit COX-2 appears to result in reduction of the risk of gastric ulcer development. It is to be expected that the selective COX-2 inhibitors now being developed will make the use of NSAIDs even safer.
Bijlsma
J W
JW
Academisch Ziekenhuis, afd. Reumatologie en Klinische Immunologie, Utrecht.
Van de Putte
L B
LB
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000145:classification / Q000494:pharmacology*; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D015195:Drug Design; D005260:Female; D006471:Gastrointestinal Hemorrhage / Q000139:chemically induced / Q000517:prevention & control; D006801:Humans; D007527:Isoenzymes / Q000378:metabolism*; D007535:Isomerases / Q000096:biosynthesis; D008297:Male; D008565:Membrane Proteins; D011247:Pregnancy; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism*; D011453:Prostaglandins / Q000096:biosynthesis; D013276:Stomach Ulcer / Q000517:prevention & control*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D007527:Isoenzymes; D008565:Membrane Proteins; D011453:Prostaglandins; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; C496511:PTGS1 protein, human; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases; D007535:Isomerases
Niet-steroïde anti-inflammatoire medicijnen (NSAID's) met minder bijwerkingen door selectieve remming van cyclo-oxygenase-2.