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Influence of β-Receptor Antagonists on Pharmacokinetics of Cimetidine

  • Section 2B: Pharmacodynamics, Pharmacokinetics and Drug Interactions
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Summary

The pharmacokinetics of metoprolol, propranolol and atenolol were investigated in 6 healthy volunteers following 7 days of oral monotherapy with these drugs and after 7 days’ concurrent administration of each of these β- blockers with cimetidine. β- Blockers did not alter cimetidine kinetics to a significant extent. Administration of cimetidine did not lead to any interaction with atenolol, whereas mean peak plasma levels and AUC of metoprolol were increased by 70%, and those of propranolol by 95% (p < 0.05). Other pharmacokinetic properties of metoprolol and propranolol were not influenced to a statistically significant extent by cimetidine despite a tendency for the elimination half- life of metoprolol and propranolol to be prolonged. Measurement of exercise- induced tachycardia on the sixth day of administration showed no differences between monotherapy with the β- blockers and combined treatment with cimetidine. Except for 1 volunteer who complained of anxiety, weakness and sweating on the sixth day of cimetidine/metoprolol administration, no adverse effects were observed.

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Kirch, W., Spahn, H., Köhler, H. et al. Influence of β-Receptor Antagonists on Pharmacokinetics of Cimetidine. Drugs 25 (Suppl 2), 127–130 (1983). https://doi.org/10.2165/00003495-198300252-00037

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  • DOI: https://doi.org/10.2165/00003495-198300252-00037

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