Effect of rifampicin on metoprolol and antipyrine kinetics.

Abstract

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. 1982 The British Pharmacological Society