Levosalbutamol as alternative to drugs on the basis of racemic salbutamol: Review of the results of pre-clinical research

Abstract

The aim of the work is to conduct an analytical review of the results of preclinical studies of levosalbutamol. The review discusses the pharmacodynamic features of the R-stereoisomer of salbutamol in vitro. The chemical bases of interaction of levosalbutamol with β2-adrenoreceptors, intracellular signaling cascades associated with β2-adrenoreceptors, and structural features of clinically significant ligands of β2-adrenoreceptors are presented. Broncholytic activity, influence on the contractility of the diaphragmatic muscles, mucociliary clearance of R-salbutamol in comparison with racemic salbutamol are described. The data presented indicate that all known β2-adrenergic receptor-dependent effects of racemic salbutamol, including bronchodilation, are realized by its R-enantiomer. There is evidence that the regular inhalation administration of racemic salbutamol is accompanied by a partial decrease in the bronchoprotective effect and an increase in airway hyperreactivity in response to the action of provocative factors. It was found that the development of hyperreactivity of the respiratory tract is excluded in the case of regular inhalation of levosalbutamol. Possible mechanisms of the paradoxical bronchoconstrictor effect of the salbutamol dystomer are described. This article shows the beneficial effect of levosalbutamol on mucociliary clearance, its anti-inflammatory activity and antiallergic effect. The image data are compared between the enantiomers and the racemate of salbutamol. Special attention is paid to the pharmacokinetics of enantiomers of salbutamol. The data presented from the preclinical studies provide evidence of chiral inversion of stereoisomers of salbutamol.