Stereochemical Elements Associated with Drug Metabolism and Toxicity

Abstract

AbstractMany drugs used in clinical practice today are administered as a racemic mixture. As a consequence, these drugs can often be associated with complex pharmacokinetics and observed toxicities compared to drugs that are administrated as a single enantiomer. It is well established that two enantiomers of a chiral drug commonly possess different pharmacological properties. In addition to variable pharmacodynamic properties, numerous studies have shown that the individual enantiomers of a chiral drug often display stereoselectivity in pharmacokinetics, toxicity, and drug disposition, particularly in the area of drug metabolism. This chapter attempts to provide a representative appraisal of the various stereochemical aspects associated with the metabolism and toxicity of chiral drugs.