New NSAIDs and gastroduodenal damage.
Two isoforms of cyclooxygenase (COX) are described: COX-1 is a constitutive enzyme and is widely expressed in most tissues, COX-2 is an inducible enzyme and is abundant throughout the gastrointestinal tract. Expression of COX-2 can be induced locally by inflammatory stimuli and appears coincident with local prostaglandin (PG) production. Currently available non-steroidal antiinflammatory drugs (NSAIDs) are widely used for the treatment of inflammatory diseases; however, significant side-effects due to inhibition of COX-1 limit their use. Inhibitors of COX-2 are as active as non-selective NSAIDs and inhibit PG synthesis in inflammatory cells. In contrast to other NSAIDs, selective COX-2 inhibitors do not cause ulcers in the stomach or intestine.
Folco
G C
GC
Istituto di Scienze Farmacologiche, Università di Milano, Italy.
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000009:adverse effects*; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000009:adverse effects*; D006801:Humans; D007527:Isoenzymes / Q000502:physiology; D008565:Membrane Proteins; D009578:Nitrobenzenes / Q000009:adverse effects; D010437:Peptic Ulcer / Q000139:chemically induced*; D010544:Peroxidases / Q000502:physiology; D011451:Prostaglandin-Endoperoxide Synthases / Q000502:physiology; D011720:Pyrazoles / Q000009:adverse effects; D013449:Sulfonamides / Q000009:adverse effects; D013876:Thiophenes / Q000009:adverse effects
D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D008565:Membrane Proteins; D009578:Nitrobenzenes; D011720:Pyrazoles; D013449:Sulfonamides; D013876:Thiophenes; C080955:N-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide; C090859:1-((4-methylsulfonyl)phenyl)-3-trifluoromethyl-5-(4-fluorophenyl)pyrazole; C064874:DuP 697; D010544:Peroxidases; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; C496511:PTGS1 protein, human; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases