Revista Egitania Sciencia - Volume 21 | ARTICLE

Title: STEREOISOMERS IN BETA-ADRENERGIC BLOCKERS THERAPY

Author: Carla Moutinho (carlamo@ufp.edu.pt), Carla Matos (cmatos@ufp.edu.pt), Joana Magalhães (25948@ufp.edu.pt), João Castro (19891@ufp.edu.pt), Carla Sousa (sousasil@ufp.edu.pt)

Publication: Revista Egitania Sciencia - Volume 21

Abstract:
The majority of currently marketed drugs are stereoisomers, which can be enantiomers or diastereomers. Since thalidomide’s disaster occurred, the chemical and pharmaceutical industry realized the importance of studying the chirality of drugs and their stereo-chemical properties. The analysis of the correlation between chirality and the toxicological and pharmacological properties has let not only to the elimination of adverse effects, but also to therapeutic benefits. There has been a tendency towards the marketing of new drugs in the form of enantiomers, supplanting the drugs which were marketed as racemic mixtures. The choice between an enantiomer and a racemic mixture depends on the therapeutic advantages, the adverse effects and the development costs. This work evidences the differences at biological activity levels and pharmacokinetic properties between the racemates and the stereoisomers of the β-adrenergics blockers. Similar to what happens with other drugs, in its majority, β-adrenergics blockers are prescribed as racemates. However, in human, its S-enantiomers are much more efficient than its antipodes, for example, in the treatment of cardiac pathologies, being the purification and administration of eutomer able to bring clinical benefit for the patient.

Keywords: Stereochemistry; Stereoisomers; Stereoselectivity; Racemic Mixture; Chirality;  -adrenergics blockers




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