Correlation between gastric irritancy and anti-inflammatory activity of non-steroidal anti-inflammatory drugs
John C. Dearden, Robert M. Nicholson
Abstract
John C. Dearden, Robert M. Nicholson
Abstract
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.
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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.
Key concepts: Potency, Anti-inflammatory, Pharmacology, ED50, Chemistry, Medicine, In vitro, Biochemistry