Selective inhibitors of COX-2--are they safe for the stomach?
NSAIDs are widely used and beneficial for patients with inflammatory pain. However, NSAIDs cause significant adverse upper gastrointestinal effects, including increased mortality from serious ulcer complications. NSAIDs exert their anti-inflammatory effects by inhibiting the activity of the COX enzyme, which was recently shown to exist in two isoforms, a constitutive COX-1 and an inducible COX-2. The latter isoform is induced in inflammation, while the former is responsible for prostaglandin effects on platelet function and gastric mucosal defense. Two specific COX-2 inhibitors have recently been introduced into the market. The available data from clinical trials indicate that these new drugs have anti-inflammatory and analgesic effects similar to those of conventional NSAIDs, but reduced rates of adverse upper gastroduodenal effects, which are similar to those observed with placebo. This difference in rates of adverse effects might imply improved safety for patients requiring anti-inflammatory treatment. It has, however, to be kept in mind that specific COX-2 inhibitors lack cardiovascular protective effects. Considering the high consumption rate of NSAIDs to achieve pain relief in arthritis and other musculo-sceletal diseases, the reduced risk of gastrointestinal ulcers and ulcer complications may have a positive impact on population health and health economy.
Giercksky
K E
KE
Dept. of Surgery, University of Oslo, The Norwegian Radium Hospital, Montebello.
Haglund
U
U
Rask-Madsen
J
J
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000009:adverse effects*; D001172:Arthritis, Rheumatoid / Q000188:drug therapy; D000068579:Celecoxib; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000009:adverse effects* / Q000627:therapeutic use; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors*; D007783:Lactones / Q000009:adverse effects / Q000627:therapeutic use; D008565:Membrane Proteins; D010003:Osteoarthritis / Q000188:drug therapy; D010146:Pain / Q000188:drug therapy; D011451:Prostaglandin-Endoperoxide Synthases; D011720:Pyrazoles; D013270:Stomach / Q000187:drug effects*; D013276:Stomach Ulcer / Q000139:chemically induced; D013449:Sulfonamides / Q000009:adverse effects / Q000627:therapeutic use; D013450:Sulfones
D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D007783:Lactones; D008565:Membrane Proteins; D011720:Pyrazoles; D013449:Sulfonamides; D013450:Sulfones; C116926:rofecoxib; D051546:Cyclooxygenase 2; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases; D000068579:Celecoxib