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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Mark, L.C., Kayden, H.J., Steele, J.M., Cooper, J.R., Berlin, I., Rowenstine, E.A., Brodie, B.B.: The physiological disposition and cardiac effect of procaine amide. J. Pharmacol. exp. Ther.102 5–15 (1951)
Koch-Weser, J., Klein, S.W.: Procaine amide dosage schedules, plasma concentrations and clinical effects. J. Amer.med.Ass.215 1454–1460 (1971)
Weily, H.S., Genton, E.: Pharmacokinetics of procainamide. Arch. intern. Med.130 366–369 (1972)
Collste, P., Karlsson, E.: Arrhythmia prophylaxis with procaine amide: plasma concentrations in relation to dose. Acta med.scand.194 405–411 (1973)
Karlsson, E.: Plasma levels of procaine amide after administration of conventional and sustained-release tablets. Europ. J. clin. Pharmacol.6 245–250 (1973)
Fremstad, D., Dahl, S., Jacobsen, S., Lunde, P.K.M., Nadland, K.J., Marthinsen, A.A., Waaler, T., Landmark, K.H.: A new sustained-release tablet formation of procainamide. Europ. J. clin. Pharmacol.6 251–255 (1973)
Dreyfuss, J., Bigger, J.T.H. Jr., Cohen, A.I., Schreiber, E.C.: Metabolism of procainamide in rhesus monkey and man. Clin. Pharmacol. Ther.13 366–371 (1972)
Evans, D.A.P.: Genetic variations in the acetylation of isoniazid and other drugs. Ann. N.Y. Acad. Sci.151 723–733 (1968)
Perry, H.M. Jr.: Late toxicity to hydralazine resembling systemic lupus erythematosus or rheumatoid arthritis. Am. J. Med.54 58–72 (1973)
Dubois, E.L.: Procainamide induction of a systemic lupus erythematosus-like syndrome. Medicine (Baltimore)48 217–228 (1969)
Hanngren, Å., Borgå, O., Sjöqvist, F.: Inactivation of isoniazid (INH) in Swedish tuberculous patients before and during treatment with paraaminosalicylic acid (PAS). Scand. J. resp. Dis.51 61–69 (1970)
Williams, E.M.V., Szekeres, L.: A comparison of tests for antifibrillatory action. Brit. J. Pharmacol.17 424–432 (1961)
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
- Procaine amide
- N-acetylprocaine amide
- plasma concentration
- renal excretion
- acetylator phenotype