Pharmacokinetics of selective β1-adrenergic blocking agents: prescribing implications

Pharmacokinetic properties of β1 selective adrenergic blocking agents pre-determine their clinical use in individual patients dependent on age, genetic polymorphisms, comorbidities, concomitant therapies, and kidney or liver dysfunction.

This paper reviews multiple searches of studies considering the pharmacokinetics of β1 selective blockers published in scientific journals from 1966 to June 2014. The pharmacokinetic parameters of these drugs in healthy populations, as well as changes of their values in the settings of advanced age, liver or renal failure, other comorbidities and enzyme or transporter polymorphisms are reviewed.

There is significant imbalance in the number and quality of studies on the pharmacokinetics of β1 selective blockers. Some members of the drug class, such as celiprolol and betaxolol were clearly under-investigated. Additionally, many questions about the extent and cause of pharmacokinetic variability of even the most widely studied β1 blockers, such metoprolol and bisoprolol, remain unanswered. In order to acquire complete and detailed knowledge of all factors that could influence pharmacokinetics of β1 selective blockers, population pharmacokinetic approaches linked with studies of genetic polymorphisms should be increasingly used in the future. This strategy provides methodological rigor and an ability to test effects of numerous factors at the same time.