Pharmacogenetic factors affecting β-blocker metabolism and response

Introduction beta-blockers are among the most widely prescribed of all drugs, used for treatment of a large number of cardiovascular diseases. Herein we evaluate literature pertaining to pharmacogenetics of beta-blocker therapy, provide insight into the robustness of the genetic associations, and determine the appropriateness for translating these genetic associations into clinical practice. Areas covered A literature search was conducted using PubMed to collate evidence on associations betweenCYP2D6, ADRB1, ADRB2, andGRK5genetic variation and drug-response outcomes in the presence of beta-blocker exposure. Pharmacokinetic, pharmacodynamic, and clinical outcomes studies were included if genotype data and beta-blocker exposure were documented. Expert opinion Substantial data suggest that specificADRB1andGRK5genotypes are associated with improved beta-blocker efficacy and have potential for use to guide therapy decisions in the clinical setting. While the data do not justify ordering aCYP2D6pharmacogenetic test, ifCYP2D6genotype is available in the electronic health record, there may be clinical utility for understanding dosing of beta-blockers.