Skip to main content
NCBI home page
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1982 Feb;13(2):203–208. doi: 10.1111/j.1365-2125.1982.tb01357.x

Ethanol-induced increase in procainamide acetylation in man.

H Olsen, J Mørland
PMCID: PMC1402013  PMID: 7059417

Abstract

1 The effect of ethanol on procainamide pharmacokinetics was studied in humans by two different experimental designs. In one, ethanol was given 1.5 h after taking the drug followed by hourly drinks, while in the other ethanol was given 2 h before and subsequently after taking the drug. 2 In both studies, ethanol caused a significant reduction of T1/2 and a significant increase in total clearance of procainamide, while the apparent volume of distribution of procainamide, as well as the renal clearance of both procainamide and N-acetylprocainamide were unaffected by ethanol treatment. 3 Ethanol treatment increased the percentage of N-acetylprocainamide measured in blood and urine and the ratio of AUCNAPA/AUCPA significantly. 4 The T1/2 and total clearance of procainamide was significantly different in slow and rapid acetylators.

Full text

PDF
203

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Drayer D. E., Reidenberg M. M., Sevy R. W. N-acetylprocainamide: an active metabolite of procainamide. Proc Soc Exp Biol Med. 1974 Jun;146(2):358–363. doi: 10.3181/00379727-146-38104. [DOI] [PubMed] [Google Scholar]
  2. EVANS D. A., MANLEY K. A., McKUSICK V. A. Genetic control of isoniazid metabolism in man. Br Med J. 1960 Aug 13;2(5197):485–491. doi: 10.1136/bmj.2.5197.485. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Estler C. J. Effect of ethanol on levels of isoniazid, sulfanilamide and sulfapyridin in mouse blood. Experientia. 1979 Mar 15;35(3):368–369. doi: 10.1007/BF01964357. [DOI] [PubMed] [Google Scholar]
  4. Evans D. A. An improved and simplified method of detecting the acetylator phenotype. J Med Genet. 1969 Dec;6(4):405–407. doi: 10.1136/jmg.6.4.405. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Frislid K., Berg M., Hansteen V., Lunde P. K. Comparison of the acetylation of procainamide and sulfadimidine in man. Eur J Clin Pharmacol. 1976 Mar 22;09(5-6):433–438. doi: 10.1007/BF00606561. [DOI] [PubMed] [Google Scholar]
  6. Frislid K., Bredesen J. E., Lunde P. K. Letter: Fluorometric or gas-liquid chromatographic determination of procainamide? Clin Chem. 1975 Jul;21(8):1180–1182. [PubMed] [Google Scholar]
  7. Giardina E. G., Dreyfuss J., Bigger J. T., Jr, Shaw J. M., Schreiber E. C. Metabolism of procainamide in normal and cardiac subjects. Clin Pharmacol Ther. 1976 Mar;19(3):339–351. doi: 10.1002/cpt1976193339. [DOI] [PubMed] [Google Scholar]
  8. Graffner C., Johnsson G., Sjögren J. Pharmacokinetics of procainamide intravenously and orally as conventional and slow-release tablets. Clin Pharmacol Ther. 1975 Apr;17(4):414–423. doi: 10.1002/cpt1975174414. [DOI] [PubMed] [Google Scholar]
  9. Karlsson E., Molin L. Polymorphic acetylation of procaine amide in healthy subjects. Acta Med Scand. 1975 Apr;197(4):299–302. doi: 10.1111/j.0954-6820.1975.tb04921.x. [DOI] [PubMed] [Google Scholar]
  10. LESTER D. THE ACETYLATION OF ISONIAZID IN ALCOHOLICS. Q J Stud Alcohol. 1964 Sep;25:541–543. [PubMed] [Google Scholar]
  11. Lertora J. J., Atkinson A. J., Jr, Kushner W., Nevin M. J., Lee W. K., Jones C., Schmid F. R. Long-term antiarrhythmic therapy with N-acetylprocainamide. Clin Pharmacol Ther. 1979 Mar;25(3):273–282. doi: 10.1002/cpt1979253273. [DOI] [PubMed] [Google Scholar]
  12. Lindros K. O. Interference of ethanol and sorbitol with hepatic ketone body metabolism in normal, hyper- and hypothyroid rats. Eur J Biochem. 1970 Mar 1;13(1):111–116. doi: 10.1111/j.1432-1033.1970.tb00905.x. [DOI] [PubMed] [Google Scholar]
  13. Mezey E. Ethanol metabolism and ethanol-drug interactions. Biochem Pharmacol. 1976 Apr 15;25(8):869–875. doi: 10.1016/0006-2952(76)90305-1. [DOI] [PubMed] [Google Scholar]
  14. Morland J., Olsen H. Metabolism of sulfadimidine, sulfanilamide, p-aminobenzoic acid, and isoniazid in suspensions of parenchymal and nonparenchymal rat liver cells. Drug Metab Dispos. 1977 Nov-Dec;5(6):511–517. [PubMed] [Google Scholar]
  15. Olsen H., Mørland J. Ethanol-induced increase in drug acetylation in man and isolated rat liver cells. Br Med J. 1978 Nov 4;2(6147):1260–1262. doi: 10.1136/bmj.2.6147.1260. [DOI] [PMC free article] [PubMed] [Google Scholar]
  16. Refsum H., Frislid K., Lunde P. K., Landmark K. H. Effects of N-acetylprocainamide as compared with procainamide in isolated rat atria. Eur J Pharmacol. 1975 Aug;33(1):47–52. doi: 10.1016/0014-2999(75)90136-3. [DOI] [PubMed] [Google Scholar]
  17. Reidenberg M. M., Drayer D. E., Levy M., Warner H. Polymorphic acetylation procainamide in man. Clin Pharmacol Ther. 1975 Jun;17(6):722–730. doi: 10.1002/cpt1975176722. [DOI] [PubMed] [Google Scholar]
  18. Rubin E., Hutterer F., Lieber C. S. Ethanol increases hepatic smooth endoplasmic reticulum and drug-metabolizing enzymes. Science. 1968 Mar 29;159(3822):1469–1470. doi: 10.1126/science.159.3822.1469. [DOI] [PubMed] [Google Scholar]
  19. Rubin E., Lieber C. S. Hepatic microsomal enzymes in man and rat: induction and inhibition by ethanol. Science. 1968 Nov 8;162(3854):690–691. doi: 10.1126/science.162.3854.690. [DOI] [PubMed] [Google Scholar]
  20. Schüppel R. Konjugationsreaktionen im Arzneistoffwechsel der Ratte bei akuter Athanolbelastung. Naunyn Schmiedebergs Arch Pharmakol. 1969;265(3):233–243. [PubMed] [Google Scholar]
  21. Sellers E. M., Holloway M. R. Drug kinetics and alcohol ingestion. Clin Pharmacokinet. 1978 Nov-Dec;3(6):440–452. doi: 10.2165/00003088-197803060-00002. [DOI] [PubMed] [Google Scholar]
  22. Siess E. A., Brocks D. G., Wieland O. H. Subcellular distribution of key metabolites in isolated liver cells from fasted rats. FEBS Lett. 1976 Oct 15;69(1):265–271. doi: 10.1016/0014-5793(76)80701-6. [DOI] [PubMed] [Google Scholar]
  23. Thomas B. H., Solomonraj G. Drug interactions with isoniazid metabolism in rats. J Pharm Sci. 1977 Sep;66(9):1322–1326. doi: 10.1002/jps.2600660930. [DOI] [PubMed] [Google Scholar]
  24. Weber W. W., Cohen S. N. N-acetylation of drugs: isolation and properties of an N-acetyltransferase from rabbit liver. Mol Pharmacol. 1967 May;3(3):266–273. [PubMed] [Google Scholar]

Articles from British Journal of Clinical Pharmacology are provided here courtesy of British Pharmacological Society

RESOURCES