Stereoselective effects of (R)- and (S)-carvedilol in humans.

Author: KleinW, KoshucharovaG, LercherP, LiebmannP M, LindnerW, MaierR, SakotnikA, StoschitzkyK

Paper Details 
Original Abstract of the Article :
Carvedilol is currently used as the racemic mixture, (R,S)-carvedilol, consisting of equal amounts of (R)-carvedilol, an alpha-blocker, and (S)-carvedilol, an alpha- and beta-blocker, which have never been tested in their optically pure forms in human subjects. We performed a randomized, double-blin...See full text at original site
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引用元:
https://doi.org/10.1002/chir.1042

データ提供:米国国立医学図書館(NLM)

Stereoselective Effects of (R)- and (S)-Carvedilol in Humans

This study investigates the distinct effects of the two enantiomers of carvedilol, a medication used for treating cardiovascular conditions. The researchers conducted a randomized, double-blind, placebo-controlled, crossover study in healthy volunteers, comparing the effects of (R)-carvedilol, (S)-carvedilol, and the racemic mixture (R,S)-carvedilol. The primary objective was to determine the specific pharmacological actions of each enantiomer and their impact on cardiovascular function.

Distinct Pharmacological Actions of Carvedilol Enantiomers

The study revealed that (S)-carvedilol exhibited beta-blocking properties, leading to a decrease in heart rate during exercise. In contrast, (R)-carvedilol appeared to increase sympathetic tone, potentially as a physiological response to the alpha-blocking effect. This research highlights the importance of considering the stereoselective effects of drugs, as different enantiomers can exert distinct actions in the body.

Implications for Drug Development and Treatment

This study's findings have important implications for drug development and treatment strategies. It suggests that a better understanding of the stereoselective effects of drugs can lead to more targeted and effective therapies. Additionally, this research underscores the need for further investigation into the potential benefits and risks of using individual enantiomers rather than racemic mixtures.

Dr.Camel's Conclusion

Imagine a camel traversing the desert, facing a fork in the road. Just like each path leads to a different destination, different enantiomers of a drug can have distinct effects. This research sheds light on the subtle differences between these molecular twins, emphasizing the importance of understanding their individual actions for optimizing treatment outcomes.

Date :
  1. Date Completed 2001-08-16
  2. Date Revised 2018-11-30
Further Info :

Pubmed ID

11400186

DOI: Digital Object Identifier

10.1002/chir.1042

Related Literature

SNS
PICO Info
in preparation
Languages

English

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