The significance of inhibition of prostaglandin synthesis in the selection of non-steroidal anti-inflammatory agents.
A statistically significant correlation can be shown to exist between the concentrations in which established non-steroidal anti-inflammatory agents inhibit prostaglandin synthesis in vitro and the doses in which they exert anti-inflammatory and antipyretic effects in animals. With regard to their antinociceptive activity, this relation is less distinct. Derivatives of clinically effective non-steroidal anti-inflammatory agents can interfere with prostaglandin synthesis in vitro without displaying any activity in vivo. Moreover, the capacity to inhibit this enzyme system is not a property exclusive to non-steroidal anti-inflammatory agents; tricyclic psychotropic drugs exert a similar action. The fact that a substance affects prostaglandin synthetase in vitro is consequently not a reliable indication that it possesses anti-inflammatory properties. On the other hand, the demonstration of effects of this type is important in elucidating the mechanism of action of a drug.
D000698:Analgesia; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D001241:Aspirin / Q000494:pharmacology; D001831:Body Temperature / Q000187:drug effects; D016861:Cyclooxygenase Inhibitors; D004487:Edema; D005439:Flufenamic Acid / Q000494:pharmacology; D007213:Indomethacin / Q000494:pharmacology; D008297:Male; D008528:Mefenamic Acid / Q000494:pharmacology; D010113:Oxyphenbutazone / Q000494:pharmacology; D010648:Phenylacetates / Q000494:pharmacology; D010653:Phenylbutazone / Q000494:pharmacology; D011448:Prostaglandin Antagonists; D011453:Prostaglandins / Q000096:biosynthesis*; D051381:Rats; D013329:Structure-Activity Relationship
D000893:Anti-Inflammatory Agents; D016861:Cyclooxygenase Inhibitors; D010648:Phenylacetates; D011448:Prostaglandin Antagonists; D011453:Prostaglandins; D008528:Mefenamic Acid; D005439:Flufenamic Acid; D010653:Phenylbutazone; D010113:Oxyphenbutazone; D001241:Aspirin; D007213:Indomethacin