The Enantiomers: Revolution or Evolution

Authors: Ekatodramis, G.; Borgeat, A.

Source: Current Topics in Medicinal Chemistry, Volume 1, Number 3, 1 August 2001 , pp. 205-206(2)

Publisher: Bentham Science Publishers

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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

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1568026013395254

Publication date: 2001-08-01