Effect of rifampicin on metoprolol and antipyrine kinetics

Br J Clin Pharmacol. 1982 Mar;13(3):387-91. doi: 10.1111/j.1365-2125.1982.tb01390.x.


1 Effects of rifampicin on the pharmacokinetics of single oral doses of metoprolol and antipyrine are reported. 2 Rifampicin, administered daily for 15 days, reduced the area under the plasma concentration-time curve (AUC) of metoprolol but the rate constant for elimination (beta) of metoprolol from plasma did not alter significantly. 3 Administration of rifampicin for 13 days reduced AUC and increased beta of antipyrine. Thirteen days after discontinuing rifampicin. AUC and beta of antipyrine remained significantly different from the initial values. 4 Some loss of beta-adrenoceptor blockade should be anticipated if rifampicin is administered to patients who are receiving metoprolol.

MeSH terms

  • Adult
  • Antipyrine / metabolism*
  • Drug Interactions
  • Humans
  • Kinetics
  • Male
  • Metoprolol / metabolism*
  • Propanolamines / metabolism*
  • Rifampin / pharmacology*


  • Propanolamines
  • Metoprolol
  • Antipyrine
  • Rifampin