Summary
The serum concentrations of α1-acid glycoprotein (AAG), albumin (HSA) and non-esterified fatty acids, and the serum binding of tertatolol were measured in four groups of individuals: healthy control subjects (n=24), and patients with inflammation (n=28), and hepatic (n=20) and renal (n=27) insufficiency.
Serum binding of tertatolol was increased in patients with inflammation (94.6%), decreased in patients with hepatic insufficiency (88.8%) and it was unchanged in patients with renal insufficiency (92.8%) as compared to controls (92.7%).
Multivariate analysis indicated that the changes were mainly related to concomitant changes in AAG concentration, which could account for 57% of intersubject variability in the bound/free ratio, and to a lesser extent in HSA, which accounted for only 4% of the variability in the binding.
The data show that the free fraction of the basic drug tertatolol in serum is affected by pathological conditions that cause changes in AAG concentration.
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Urien, S., Morin, D., Renouard, A. et al. Variation in serum binding of tertatolol mediated by disease-induced modification of alpha-acid glycoprotein concentration. Eur J Clin Pharmacol 34, 381–385 (1988). https://doi.org/10.1007/BF00542440
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DOI: https://doi.org/10.1007/BF00542440