Models for evaluating the pharmacokinetics and pharmacodynamics for β-blockers
Introduction: 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 the...
| Authors: | , , , |
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| Format: | article |
| Status: | Published version |
| Publication Date: | 2014 |
| Country: | Argentina |
| Institution: | Consejo Nacional de Investigaciones Científicas y Técnicas |
| Repository: | CONICET Digital (CONICET) |
| Language: | English |
| OAI Identifier: | oai:ri.conicet.gov.ar:11336/39296 |
| Online Access: | http://hdl.handle.net/11336/39296 |
| Access Level: | Open access |
| Keyword: | Blood Pressure Heart Rate Pharmacokinetic-Pharmacodynamic Modeling Population Pharmacokinetics Β Blockers https://purl.org/becyt/ford/3.1 https://purl.org/becyt/ford/3 |
| Summary: | Introduction: 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. Areas covered: 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. Expert opinion: 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. © 2014 Informa UK, Ltd. |
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