The interaction between H2-receptor antagonists and beta-adrenoceptor blockers

Br J Clin Pharmacol. 1984;17 Suppl 1(Suppl 1):51S-57S. doi: 10.1111/j.1365-2125.1984.tb02428.x.


The degrees of interactions between the H2-receptor antagonists, cimetidine and ranitidine, and several beta-adrenoceptor blockers were investigated in healthy volunteers following 7 days of oral monotherapy with penbutolol, propranolol, metoprolol, pindolol and atenolol, and after co-administration with each of the H2-receptor antagonists. The kinetic parameters of unmetabolised penbutolol and penbutolol glucuronide were unaffected, whereas the levels of 4-hydroxypenbutolol and 4-hydroxypenbutolol glucuronide were significantly reduced. Furthermore, cimetidine led to a marked increase in propranolol and metoprolol plasma levels. During co-administration with cimetidine, pindolol plasma levels were only slightly raised, whereas the pharmacokinetics of atenolol were not affected. With regard to pharmacodynamics, the inhibition of exercise-induced tachycardia by each of the beta-adrenoceptor blockers was not affected by cimetidine. Ranitidine did not alter atenolol plasma levels, but did raise the peak plasma concentration of metoprolol by about 30%. It is concluded that cimetidine interactions do occur and can be predicted for substances metabolised by the cytochrome P-450 pathway.

MeSH terms

  • Adrenergic beta-Antagonists / metabolism
  • Adrenergic beta-Antagonists / pharmacology*
  • Atenolol / pharmacology
  • Cimetidine / pharmacology
  • Drug Interactions
  • Histamine H2 Antagonists / pharmacology*
  • Humans
  • Kinetics
  • Metoprolol / pharmacology
  • Penbutolol / pharmacology
  • Pindolol / pharmacology
  • Propranolol / pharmacology
  • Ranitidine / pharmacology


  • Adrenergic beta-Antagonists
  • Histamine H2 Antagonists
  • Atenolol
  • Penbutolol
  • Cimetidine
  • Ranitidine
  • Propranolol
  • Pindolol
  • Metoprolol