Stereoisomers in Clinical Pharmacology

Abstract

Drugs are often marketed as racemic mixtures. Some surveys suggest that up to 75% of synthetic drugs are developed as racemates. In routine clinical practice we rarely give much thought to the problem despite the fact that many studies have reported differences in both pharmacokinetic and pharmacodynamic properties between enantiomers. Clearly, administration of a drug as a racemate rather than a single isomer is important if it affects the outcome of treatment. This occurs mainly when adverse effects are due to the less active enantiomer or if other drugs interact with one enantiomer to cause toxicity or reduced effect.