Correlation between gastric irritancy and anti-inflammatory activity of non-steroidal anti-inflammatory drugs.
Gastric irritancies and anti-inflammatory potencies of 25 commercially available non-steroidal anti-inflammatory drugs (NSAIDs) have been measured in the rat. When irritancy is measured as the dose required to produce a specified level of gastric mucosal damage, it is found that irritancy increases with anti-inflammatory potency. However, when irritancy is measured as the level of gastric mucosal damage at the anti-inflammatory ED50 (which is a clinically realistic measure) then irritancy decreases as anti-inflammatory potency increases. Hence it should be possible to design high-potency, low-irritancy NSAIDs.
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000633:toxicity*; D002351:Carrageenan / Q000494:pharmacology; D005753:Gastric Mucosa / Q000187:drug effects*; D007509:Irritants; D007928:Lethal Dose 50; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D000893:Anti-Inflammatory Agents; D007509:Irritants; D002351:Carrageenan