PMID: 18432131Apr 25, 2008Paper

What is new about nonsteroidal antiinflamatory drugs?

Polski merkuriusz lekarski : organ Polskiego Towarzystwa Lekarskiego
Małgorzata Dzielska-Olczak

Abstract

NSAIDs contain nonselective cyclooksygenase inhibitors (for COX-1 and COX-2), inhibitors to the preferential COX-2, the coxibs (sulphonamides, methylsulphones, phenylacethic acid derivatives) with 1000 fold selectivities for COX-2. COX-2 enzyme isoform are constitutively expressed in normal gastric tissue in animals and humans, in the cardiovascular system, renal, central nervous system and other. COX-2 is involved in the ischemic preconditioning mechanism and sulphones have a prooxidant activity. COX-2 inhibitors increased risk for thrombotic cardiovascular events. Long-term study VIGOR, CLASS, TARGET MEDAL revealed that celecoxib, rofecoxib, lumiracoxib, etoricoxib significantly reduced the risk of major gastrointestinal effects (ulcers, perforations, bleeding) than nonselective NSAIDs, but the rates of complicated upper gastrointestinal events were similar for etoricoxib and diclofenac. Only in VIGOR trial incidence of cardiovascular events was greater. No evidence that concomitant ASA reduced risk for cardivascular events. Potential differences in cardiovascular outcomes with the selective COX-2 inhibitors may be due to differences in the drugs molecular structures, pharmacokinetics and pharmacodynamics. In the "prothrombot...Continue Reading

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