COX-2-selective inhibitors (COXIBs): gastrointestinal safety.
COX-2 selective inhibitors (coxibs) have been developed with the primary aim to reduce/avoid gastrointestinal (GI) toxicity observed during conventional (non-selective) non-steroidal anti-inflammatory (NSAID) therapy. Coxibs have clearly and convincingly been shown to be superior to conventional NSAIDs with significantly less GI side effects. When hard endpoints such as perforation, obstruction, and serious bleeding considered, coxibs reduce the risk by approximately 50 percent. Although selective COX-2 inhibition seems not to be enough for complete elimination of GI toxicity, coxibs posses no more GI toxicity than placebo in prospective clinical studies and further increase in COX-2 selectivity does not reduce GI toxicity. For the initial aim developed, thus coxibs fulfilled their promise and will soon replace conventional NSAIDs.
Pronai
L
L
2nd Department of Medicine, Faculty of Medicine, Semmelweiss University, Hungarian Academy of Science, Joint Research Unit, Budapest, Hungary. pronai@bel2.sote.hu
Hritz
I
I
Molnar
B
B
Herszenyi
L
L
Tulassay
Z
Z
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000009:adverse effects / Q000494:pharmacology; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000009:adverse effects* / Q000494:pharmacology*; D041981:Gastrointestinal Tract / Q000187:drug effects* / Q000201:enzymology*; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008565:Membrane Proteins; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism
D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D008565:Membrane Proteins; D051546:Cyclooxygenase 2; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases