The Beta-adrenoblockers (β-AB) were among the first drugs investigated for stereoisomeric spatial aspects withthe formation of (-) levorotatory and (+) dextrorotatory isomers. The drugs, depending on the chemical structure, are subdivided into arylaminoethanols (sotalol, labetalol) or aryloxaminopropanols (propranolol, metoprolol, atenolol, celiprolol, carvedilol, nebivolol). According to β-adrenoblocking activity more active are the (-) isomers, to which can be assigned the configuration (R) for the arylaminoethanol group and (S) for the aryloxaminopropanol group. Elucidation of the correlation between β-AB stereoisomerism and their pharmacodynamic properties. Most β-AB have been introduced into the clinic as racemates, and penbutolol, timolol, atenolol and levobunolol as pure enantiomers. The crucial role in binding to receptors is provided by amino- and hydroxy- groups and substituted aromatic rings of the active enantiomers. Labetalol is a fusion of four stereoisomers, of which the (SR) isomer exerts adrenoblocking activity and the (RR) – β-adrenoblocking. Metoprolol through the (S) (-) enantiomer has affinity for β1 receptors, and through the (R) (+) isomer it blocks equally both β1 and β2-receptors. Carvedilol, β-AB with a adrenoblocking activity and antioxidant effect, in racemate form is used as an antihypertensive and in congestive heart failure therapy. The (S) enantiomer blocks α- and β-receptors, and the (R) form is a pure α1-receptor antagonist. Th racemate practically does not reduce heart rate, while (R) -carvedilol causes a slight tachycardia. Nebivolol contains four stereogenic centers, which form 10 isomers. Nebivolol (+) with configuration (SRRR) has β1-adrenoblocking activity, and the () isomer (RSSS) has a vasodilating effect by activating NO endothelial synthase. Racemic Nebivolol (±) and (+) enantiomer have 200 times higher selective activity towards β1-receptors than (-) - nebivolol. The pharmacodynamic properties of β-AB are determined by the specific interactions of stereoisomers with receptors, as well as membrane transporters, plasma proteins, enzymes involved in metabolic processes, etc. The more active stereoisomers form three types of interactions complementary to the active site of the receptor, while the less active stereoisomers form only two types of interactions.