European Journal of Clinical Pharmacology

, Volume 14, Issue 4, pp 261–265 | Cite as

The pharmacokinetics of slow-release procainamide

  • W. J. Tilstone
  • D. H. Lawson
  • W. Campbell
  • I. Hutton
  • T. D. V. Lawrie
Originals

Summary

Procainamide was given to 20 patients with normal renal function as an i.v. bolus of 500 mg followed by 1.0 or 1.5 g eight-hourly by mouth in the form of a slow release preparation (Durules). 97.6±27.1 (SD)% of the oral procainamide was absorbed, the absorption half life being 1.54 h. The elimination half life following the oral formulation was 6.0±0.8 h, compared to a mean of 3.4±0.4 h following i.v. administration. Elimination half life following i.v. administration was slightly related to acetylator status, being 2.75±0.9 h in fast acetylators, and 4.4±2.4 h in slow acetylators. This dependence on acetylator status was not seen in half life following oral administration. Total body clearance, steady state plasma procainamide and N-acetylprocainamide were not significantly dependent on acetylator status, although a few patients who are slow acetylators had unexpectedly low clearance and high steady state procainamide concentrations when given the higher dose.

Key words

Procainamide slow release formulations bioavailability 

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References

  1. Campbell, W., Tilstone, W. J., Lawson, D. H., Hutton, I., Lawrie T. D. V.: Acetylator phenotype and the clinical pharmacology of slow release procainamide. Br. J. clin. Pharmacol.3, 1023–1026 (1976)Google Scholar
  2. Galeazzi, R. L., Benet, L. Z., Scheiner, L. B.: Relationship between the pharmacokinetics and pharmacodynamics of procainamide. Clin. Pharmacol. Ther.20, 278–289 (1976)Google Scholar
  3. Gibaldi, M., Perrier, D.: Pharmacokinetics. New York: Marcel Dekker 1975Google Scholar
  4. Giardina, E. G., Dreyfuss, J., Bigger, J. T., Shaw, J. M., Schreiber, E. C.: Metabolism of procainamide in normal and cardiac subjects. Clin. Pharmacol. Ther.19, 339–351 (1976)Google Scholar
  5. Graffner, C., Johnsson, G., Sjogren, J.: Pharmacokinetics of procainamide intravenously and orally as conventional and slow release tablets. Clin. Pharmacol. Ther.17, 414–423 (1975)Google Scholar
  6. Koch-Weser, J., Klein, S. W.: Procainamide dosage schedules, plasma concentrations and clinical effects. J. Am. med. Ass.215, 1454–1460 (1971)Google Scholar
  7. Lawson, D. H., Jick, H.: Adverse reactions to procainamide. Br. J. clin. Pharmacol.4, 507–511 (1977)Google Scholar
  8. Lima, J. J., Jusko, W. J.: Determination of procainamide acetylator status. Clin. Pharmacol. Ther.23, 25–29 (1978)Google Scholar
  9. Price Evans, D. A.: An improved and simplified method of detecting the acetylator phenotype. J. Med. Genet.6, 405–407 (1969)Google Scholar
  10. Simons, K. J., Levy, R. H., Cutler, R. E., Christopher, G. T., Lindner, A.: The pharmacokinetics of procainamide in normal subjects using a specific gas chromatographic assay. Res. Commun. chem. Pathol. Pharmacol.11, 173–185 (1975)Google Scholar
  11. Tilstone, W. J., Lawson, D. H.: Capacity-limited elimination of procainamide in man. Res. Commun. chem. Pathol. Pharmacol.21, 343–346 (1978)Google Scholar

Copyright information

© Springer-Verlag 1978

Authors and Affiliations

  • W. J. Tilstone
    • 1
    • 2
  • D. H. Lawson
    • 1
    • 2
  • W. Campbell
    • 1
    • 2
  • I. Hutton
    • 1
    • 2
  • T. D. V. Lawrie
    • 1
    • 2
  1. 1.Forensic Science Unit, School of Pharmaceutical SciencesUniversity of StrathclydeGlasgowScotland
  2. 2.Clinical Pharmacology Service and Department of Medical CardiologyRoyal InfirmaryGlasgowScotland

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