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Acetylation of procaine amide in man. A preliminary communication

Summary

The metabolism of procaine amide was studied in 41 cardiac patients who had achieved steady state plasma concentrations of the drug. Acetylated procaine amide accounted for 31±12% (range 16 – 63%) of the overall urinary recovery of the drug and is therefore a main metabolite in man. Plasma levels of the metabolite were usually lower but sometimes exceeded those of the parent compound with variations between 1 and 15 µg/ml. The metabolite had a weaker effect than procaine amide on the maximal electrical driving velocity of isolated atrial strips from guinea pig.

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Discussed in preliminary form at the America-Swedish workshop on clinical pharmacology at N.I.H. Bethesda, Maryland, USA, January 1973.

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Karlsson, E., Åberg, G., Collste, P. et al. Acetylation of procaine amide in man. A preliminary communication. Eur J Clin Pharmacol 8, 79–81 (1975). https://doi.org/10.1007/BF00616419

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Key words

  • Procaine amide
  • N-acetylprocaine amide
  • plasma concentration
  • renal excretion
  • acetylator phenotype