Abstract
The use of single stereoisomers are gaining popularity in the world of anesthesiology. The reduced costs of production have made these compounds available for clinical application. The majority of drugs used in anesthesiology such as ketamine, isoflurane, etomidate, atracurium, bupivacaine and ropivacaine have an asymmetric carbon, and are still used primarily as racemic mixtures (1:1 mixture of R and S enantiomers). Among local anesthetics, the S enantiomers often have favorable biological properties. This insight has led to the development of ropivacaine. Ropivacaine is the first local anesthetic marketed as pure S-(-) enantiomer. Its pharmacodynamic and pharmacokinetic profile is similar to that of bupivacaine, but in vitro and in vivo studies have shown that ropivacaine is less cardiotoxic. Clinical data suggests that ropivacaine has a greater margin of safety than bupivacaine, which is necessary for further expanding the application of regional anesthesia. The time has come for the use of single enantiomers in regional and general anesthesia
Keywords: The Enantiomers, Revolution, Evolution, ketamine, chiral drugs
Current Topics in Medicinal Chemistry
Title: The Enantiomers: Revolution or Evolution
Volume: 1 Issue: 3
Author(s): G. Ekatodramis and A. Borgeat
Affiliation:
Keywords: The Enantiomers, Revolution, Evolution, ketamine, chiral drugs
Abstract: The use of single stereoisomers are gaining popularity in the world of anesthesiology. The reduced costs of production have made these compounds available for clinical application. The majority of drugs used in anesthesiology such as ketamine, isoflurane, etomidate, atracurium, bupivacaine and ropivacaine have an asymmetric carbon, and are still used primarily as racemic mixtures (1:1 mixture of R and S enantiomers). Among local anesthetics, the S enantiomers often have favorable biological properties. This insight has led to the development of ropivacaine. Ropivacaine is the first local anesthetic marketed as pure S-(-) enantiomer. Its pharmacodynamic and pharmacokinetic profile is similar to that of bupivacaine, but in vitro and in vivo studies have shown that ropivacaine is less cardiotoxic. Clinical data suggests that ropivacaine has a greater margin of safety than bupivacaine, which is necessary for further expanding the application of regional anesthesia. The time has come for the use of single enantiomers in regional and general anesthesia
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Cite this article as:
Ekatodramis G. and Borgeat A., The Enantiomers: Revolution or Evolution, Current Topics in Medicinal Chemistry 2001; 1 (3) . https://dx.doi.org/10.2174/1568026013395254
DOI https://dx.doi.org/10.2174/1568026013395254 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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