COX-2 inhibitors compared and contrasted.
Non-steroidal anti-inflammatory drugs (NSAIDs) are the principal drug treatments for inflammation, pain and fever. They act primarily by inhibiting prostaglandin (PG) synthesis but this can cause adverse events (AEs). Since the discovery of two PG synthesising enzymes, COX-1 and COX-2, and the substantial evidence that sparing COX-1 is advantageous for gastric safety, great interest has focused on selective COX-2 inhibitors. Much of the impetus has come from the most recently developed compounds celecoxib and rofecoxib, which have shown spectacular sales growth. However, the older drugs etodolac, nimesulide and meloxicam, made before COX-2 was discovered, are also COX-1-sparing and have good GI safety and therapeutic activities. These five compounds show similarities and differences that are discussed in relation to aspects that include their uses, efficacy, actions and safety.
Bennett
A
A
Academic Department of Surgery, The Rayne Institute, Guy's, King's and St Thomas' Medical School, King's College, London, SE5 9NU, UK.
Tavares
I A
IA
D000818:Animals; D001172:Arthritis, Rheumatoid / Q000188:drug therapy; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000009:adverse effects / Q000737:chemistry / Q000191:economics / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors*; D008565:Membrane Proteins; D010146:Pain / Q000188:drug therapy; D011448:Prostaglandin Antagonists / Q000494:pharmacology; D011451:Prostaglandin-Endoperoxide Synthases; D009626:Terminology as Topic
D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D008565:Membrane Proteins; D011448:Prostaglandin Antagonists; D051546:Cyclooxygenase 2; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases