European Journal of Clinical Pharmacology

, Volume 15, Issue 1, pp 63–68 | Cite as

Significance of the acetylation phenotype and the therapeutic effect of procainamide

  • P. Schröder
  • N. A. Klitgaard
  • E. Simonsen


In order to estimate the relative antiarrhythmic effect of procainamide and N-acetylprocainamide, 18 randomly selected, patients with arrhythmia were divided into two groups; the first was treated with Pronestyl® in the first half of the investigation period, followed by Duretter® in the second half, and the second group began with Duretter® and terminated with Pronestyl®. The concentrations of procainamide and N-acetylprocainamide were measured twice a day during the steady state part of each treatment period. The acetylation phenotype of the patients was determined with sulfadimidine, and was compared with the relative serum concentrations of procainamide and N-acetylprocainamide. N-acetylprocainamide was found to antagonize the action of procainamide.

Key words

procainamide N-acetylprocainamide arrhythmia acetylator phenotype antagonism 


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. 1.
    Koch-Weser, I., Klein, S. W.: Procainamide dosage schedules, plasma concentrations and clinical effects. J. Am. Med. Ass.215, 1454–1460 (1971)Google Scholar
  2. 2.
    Dreyfuss, I., Ross, I. I., Schreiber, E. C.: Absorption, excretion, and biotransformation of procainamide −C14 in the dog and Rhesus monkey. Arzneim.-Forsch.21, 948–951 (1971)Google Scholar
  3. 3.
    Dreyfuss, I., Bigger, I. T., Cohen, A. I., Schreiber, E. C.: Metabolism of procainamide in rhesus monkey and man. Clin. Pharmacol. Ther.13, 366–371 (1972)Google Scholar
  4. 4.
    Karlsson, E., Molin, L.: Polymorphic acetylation of procainamide in healthy subjects. Acta med. scand.197, 299–302 (1975)Google Scholar
  5. 5.
    Karlsson, E.: Plasma levels of procainamide after administration of conventional and sustained-release tablets. Europ. J. clin. Pharmacol.6, 245–250 (1973)Google Scholar
  6. 6.
    Frislid, K., Berg, M., Hansteen, V., Lunde, P. K. M.: Comparison of the acetylation of procainamide and sulfadimidine in man. Europ. J. clin. Pharmacol.9, 433–438 (1976)Google Scholar
  7. 7.
    Elson, I., Strong, J. M., Lee, W. K., Atkinson, A. J.: Anti-arrhythmic potency of N-acetylprocainamide. Clin. Pharmacol. Ther.17, 134–140 (1975)Google Scholar
  8. 8.
    Atkinson, A. J., Lee, W. K., Quinn, M. L., Kushner, W., Nevin, M. J., Strong, I. M.: Dose-ranging trial of N-acetylprocainamide in patients with premature ventricular contractions. Clin. Pharmacol. Ther.21, 575–587 (1977)Google Scholar
  9. 9.
    Lee, W. K., Strong, I. M., Kehoe, R. F., Dutcher, I. S., Atkinson, A. J.: Anti-arrhythmic efficacy of N-acetylprocainamide in patients with premature ventricular contractions. Clin. Pharmacol. Ther.19, 508–514 (1976)Google Scholar
  10. 10.
    Evans, D. A. P.: An improved and simplified method of detecting the acetylator phenotype. J. med. Genet.6, 405–407 (1969)Google Scholar
  11. 11.
    Klitgaard, N. A.: A routine method for the determination of procainamide and its main metabolite N-acetylprocainamide. Arch. Pharm. Chem. Sci. Ed.4, 61–64 (1976)Google Scholar
  12. 12.
    Karlsson, E., Molin, L., Norlander, B., Sjövist, F.: Acetylation of procainamide in man studied with a new gaschromatographic method. Br. J. clin. Pharmacol.1, 467–475 (1974)Google Scholar
  13. 13.
    Fremstad, D., Dahl, S., Jacobsen, S., Lunde, P. K. M., Nodland, K. J., Marthinsen, A. A., Waaler, T., Landmark, K. H.: A new sustained-release tablet formulation of procainamide. Europ. J. clin. Pharmacol.6, 251–255 (1973)Google Scholar
  14. 14.
    Refsum, H., Frislid, K., Lunde, P. K. M., Handmark, K. H.: Effects of N-acetylprocainamide as compared with procainamide in isolated rat atria. Europ. J. Pharmacol.33, 47–52 (1975)Google Scholar

Copyright information

© Springer-Verlag 1979

Authors and Affiliations

  • P. Schröder
    • 1
    • 2
  • N. A. Klitgaard
    • 1
    • 2
  • E. Simonsen
    • 1
    • 2
  1. 1.Medical DepartmentHaderslev HospitalDenmark
  2. 2.the Clinical Chemical DepartmentOdense University HospitalDenmark

Personalised recommendations