Pharmacokinetics and pharmacodynamics of β-blockers: in search of the optimal drug

June 28, 2023
1541
Resume

β-blockers are a heterogeneous group of drugs in terms of their pharmacokinetic/pharmacodynamic parameters, which leads to clinically significant effects that must be taken into account in clinical practice. Analysis of the pharmacological characteristics of different representatives of this group allows us to consider bisoprolol as the optimal β-blockers due to a combination of promising pharmacokinetic properties. Clear linear pharmacokinetics, high cardio-selectivity and bioavailability, amphiphilicity and dual route of excretion, absence of presystemic metabolism, and independence of pharmacokinetics from genetic polymorphism of CYP2D6, CYP3A5, ADRB1 ensure minimal pharmacological variability of bisoprolol, which is the key to stability and reproducibility of clinical effects, high safety profile and minimal number of side effects.

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