Influence of inflammatory disease on the clinical pharmacokinetics of atenolol and metoprolol

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Abstract
The influence of inflammatory disease on the pharmacokinetics of atenolol and metoprolol was investigated after administering single oral 100mg doses of the drugs to six subjects. Each subject had a respiratory tract infection with an erythrocyte sedimentation rate (ESR) of over 20 mm in the first hour and a body temperature of at least 38·5°. Since the subjects subsequently received atenolol and metoprolol when they were healthy, each person acted as his own control. Inflammatory disease had no influence on the kinetics of metoprolol. In contrast, mean peak plasma levels and AUC for atenolol were significantly lower, both by about 40 per cent, during infectious disease compared to the healthy state (p−1 in the healthy state to 128·21·6mlmin−1, when the ESR's were elevated. The elimination half‐life of atenolol, about 10 h, was not affected by the health status of the subjects. Reduced absorption in the gastro‐intestinal tract and enhanced elimination of atenolol from plasma might account for the decreased AUC and peak plasma levels of the drug during inflammatory disease.