Čes. slov. farm. 2002, 51(3):121-128

R-Adrenergic Receptor Blockers - the Group of Chiral Drugs: Different Effects of Individual Enantiomers

R. Čižmáriková

Katedra chemickej teórie liečiv Farmaceutickej fakulty Univerzity Komenského, Bratislava

The present review of (3-adrenergic receptor blockers deals with different pharmacodynamic, pharmacokinetic and toxicological effects of individual enantiomers in the group of arylaminoethanols and aryloxyaminopropanols. From the viewpoint of (3-adrenolytic aktivity, (-)-enantiomers in both groups are several times more effective and in many (3-blockers both enantiomers show different therapeutic indications. The absolute configuration in the sense of Cahn-Ingold-Prelog system exists in (-)-enantiomers in the group of arylaminoethanols (R) and in the group of aryloxyaminopropanols (S). Of the R-blockers hitherto used in therapeutic practice, pure enantiomers are (S)-(-)-penbutolol, (S)-(-)-timolol, and (S)-(-)-levobunolol. The hitherto research in this field, however, does not unambiguously answer, as the experience with labetalol, sotalol, and timolol shows, the question of the advantages of therapeutic use of pure enantiomeric forms.

Keywords: R-blockers; chirality; enantiomers; arylaminoethanols; phenoxyaminopropanols

Published: March 1, 2002  Show citation