Aminopyrine: metabolism and effects in the rat after administration of inhibitors of hepatic monooxygenases.
The administration to the rat of the inhibitors of microsomal mixed function oxidase, SKF 525A and Oxine-5-sulphonic acid (OSA) caused a significant decrease of the hepatic aminopyrine N-demethylase activity, as well as an increase in the plasma levels and antipyretic activity of orally administered aminopyrine. The plasma concentrations of the aminopyrine metabolite 4-aminoantipyrine were reduced in SKF 525-A treated animals while they were slightly increased in those pretreated with OSA. These findings suggest that the in vivo changes of aminopyrine disposition and activity brought about by SKF 525-A were the result of an inhibited hepatic drug metabolism, while the effects produced by OSA were due to a more rapid intestinal absorption of aminopyrine.
D000632:Aminopyrine / Q000097:blood / Q000378:metabolism* / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal; D004347:Drug Interactions; D005260:Female; D066298:In Vitro Techniques; D008862:Microsomes, Liver / Q000201:enzymology; D006899:Mixed Function Oxygenases / Q000037:antagonists & inhibitors*; D010088:Oxidoreductases / Q000037:antagonists & inhibitors*; D015125:Oxyquinoline / Q000494:pharmacology; D011335:Proadifen / Q000494:pharmacology; D051381:Rats; D013997:Time Factors
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000632:Aminopyrine; D015125:Oxyquinoline; D011335:Proadifen; D006899:Mixed Function Oxygenases; D010088:Oxidoreductases