Interaction of steady-state procainamide with H2-receptor antagonists cimetidine and ranitidine

Ther Drug Monit. 1987 Dec;9(4):378-83. doi: 10.1097/00007691-198712000-00003.


This study was designed to compare the effects of equivalent therapeutic doses of two H2 antagonists, cimetidine and ranitidine, on steady-state procainamide pharmacokinetics. Six healthy men were given 500 mg sustained-release procainamide every 6 h, for a total of 13 doses, on three occasions. Subjects were randomly assigned to three treatments by a Latin-square design: cimetidine 1,200 mg/day, ranitidine 300 mg/day, and no H2-receptor antagonist (control) for 4 days. Cimetidine significantly increased the procainamide area under the serum concentration-time curve by 43%, decreased renal clearance by 36%, and decreased the ratio of systemic clearance of procainamide to bioavailability by 28%. Ranitidine did not significantly alter procainamide steady-state pharmacokinetics.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Acecainide / pharmacokinetics
  • Adult
  • Cimetidine / pharmacology*
  • Drug Interactions
  • Humans
  • Intestinal Absorption / drug effects
  • Male
  • Procainamide / pharmacokinetics*
  • Ranitidine / pharmacology*


  • Cimetidine
  • Ranitidine
  • Acecainide
  • Procainamide