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Expert Opin Drug Metab Toxicol. 2014 Apr;10(4):525-41. doi: 10.1517/17425255.2014.885951. Epub 2014 Mar 5.

Models for evaluating the pharmacokinetics and pharmacodynamics for β-blockers.

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Universidad de Buenos Aires, School of Pharmacy and Biochemistry, Facultad de Farmacia y Bioquímica, Department of Pharmacology , Junín 956, (C1113AAD) Buenos Aires , Argentina +54 11 4964 8265 ; +54 11 4508 3645 ;



β-blocker therapy plays an important role in the treatment of various diseases, including hypertension, myocardial infarction and heart failure. Although all β-blockers shared their ability to competitively block β1-adrenoceptor, this therapeutic class showed great heterogeneity in their pharmacokinetic (PK) and pharmacodynamic (PD) properties.


The present review describes the models used for PK and PK/PD evaluation of β-blockers and their applicability in preclinical and clinical studies. PK behavior of different β-blockers has been studied by means of individual compartmental and population PKs, allowing the estimation of relevant PK parameters and factors involved in intersubject variability. Different PK/PD models have been developed for the in vivo estimation of PD parameters of different cardiovascular effects of β-blockers.


PK models and PK/PD modeling have clearly contributed to characterization of the PK and PD properties of β-blockers. Differences in cardiovascular actions between classical β-blockers and vasodilatory β-blockers need to be further studied in order to confirm the clinical benefits of the new-generation of β-blockers. PK/PD modeling may contribute to clarify the importance of heterogeneity of PK and PD properties of β-blockers potentially improving the selection of the adequate agent and dose regimen in the treatment of cardiovascular diseases.

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