Aminopyrine: metabolism and effects in the rat after administration of inhibitors of hepatic monooxygenases

A. Di Nucci, P. L. Rugarli, B. Ferrini, A. Tarozzi, C. Gregotti, L. Manzo

Research output: Contribution to journalArticle

Abstract

The administration to the rat of the inhibitors of microsomal mixed function oxidases, SKF 52S-A 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 S2S-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.

Original languageEnglish
Pages (from-to)179-183
Number of pages5
JournalEuropean Journal of Drug Metabolism and Pharmacokinetics
Volume4
Issue number3
DOIs
Publication statusPublished - Jul 1979

Keywords

  • Aminopyrine
  • Drug metabolism
  • Inhibitors of monooxygenases
  • Oxine-5-sulphonic acid
  • SKF 525-A

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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