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Background <p>Metoprolol is a cardioselective beta-1 adrenergic receptor blocker, for which about 70–80% of metabolism occurs via the cytochrome P450 2D6 enzyme. Amiodarone and its active metabolite desethylamiodarone are weak inhibitors of cytochrome P450 2D6.</p> Methods <p>In this study, the drug interaction between metoprolol and amiodarone was objectified by determining the serum concentrations of both drugs including their metabolites.</p> Results <p>Patients with concentrations of amiodarone and/or desethylamiodarone ≥ 0.5&#xa0;mg/L achieved a significantly higher concentration-to-dose ratio and lower weight-adjusted apparent clearance of metoprolol than patients who were not taking amiodarone. A significant correlation was found between the concentration of metoprolol and its dose and concentrations of both amiodarone and desethylamiodarone. The concentration-to-dose ratio and the apparent clearance index of metoprolol correlated with the concentrations of metoprolol, amiodarone, and desethylamiodarone. Lower heart rate was found at concentrations of metoprolol ≥ 12.0&#xa0;µg/L and/or amiodarone or desethylamiodarone ≥ 0.5&#xa0;mg/L compared to drug concentrations measured below these values.</p> Conclusion <p>Due to the variability of concentrations achieved after administration of the same daily dose of metoprolol and amiodarone, it is advisable to monitor amiodarone and desethylamiodarone concentrations and, if necessary, metoprolol concentrations in patients taking this combination.</p>

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Objectification of the Drug Interaction of Metoprolol and Amiodarone by Determining Their Serum Concentrations Including Metabolites: An Observational Study

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年7月20日

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  • Martin Kolek,
  • Ivana Kacirova,
  • Erika Hrudikova,
  • Jana Duricova,
  • Romana Urinovska,
  • Milan Grundmann

摘要

Background

Metoprolol is a cardioselective beta-1 adrenergic receptor blocker, for which about 70–80% of metabolism occurs via the cytochrome P450 2D6 enzyme. Amiodarone and its active metabolite desethylamiodarone are weak inhibitors of cytochrome P450 2D6.

Methods

In this study, the drug interaction between metoprolol and amiodarone was objectified by determining the serum concentrations of both drugs including their metabolites.

Results

Patients with concentrations of amiodarone and/or desethylamiodarone ≥ 0.5 mg/L achieved a significantly higher concentration-to-dose ratio and lower weight-adjusted apparent clearance of metoprolol than patients who were not taking amiodarone. A significant correlation was found between the concentration of metoprolol and its dose and concentrations of both amiodarone and desethylamiodarone. The concentration-to-dose ratio and the apparent clearance index of metoprolol correlated with the concentrations of metoprolol, amiodarone, and desethylamiodarone. Lower heart rate was found at concentrations of metoprolol ≥ 12.0 µg/L and/or amiodarone or desethylamiodarone ≥ 0.5 mg/L compared to drug concentrations measured below these values.

Conclusion

Due to the variability of concentrations achieved after administration of the same daily dose of metoprolol and amiodarone, it is advisable to monitor amiodarone and desethylamiodarone concentrations and, if necessary, metoprolol concentrations in patients taking this combination.