Three pharmacological blocks of a drug based on a β-adrenergic blocker: a strategy for its creation and effective clinical use

The three defining blocks of a β-blocker drug are the pharmacodynamic properties of the active ingredient (PD), the pharmacokinetic features (PK), and the dosage form (DF). The drug of choice β-blocker with pronounced clinical efficacy and a favorable safety profile is distinguished by: 1) high selectivity for target β-adrenergic receptors (mainly PD, PK); 2) high bioavailability and permeability of histohematic barriers (PK, LF); 3) maintaining plasma concentrations in the therapeutic range (PK, LF); 4) frequency of administration once a day (PD, duration of complex formation with receptors; PK, LF); 5) minimization of pharmacokinetic drug interactions (PK); 6) no relationship with food intake (PK). The clinical and pharmacological advantages of metoprolol succinate (Betaloc® ZOK) include long-term action, improved tolerability, control of blood pressure during the day, less pronounced side effects and drug interactions, ease of administration.