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Many synthetic drugs that contain a chiral center are marketed as racemates. Taking into account the composite nature of chiral drugs has improved our understanding of the dose/effect relationship of these compounds. It is widely accepted that drug metabolism is often responsible for stereoselective disposition and hence factors modulating the activity of drug-metabolizing enzymes can modify this effect. The present article highlights the influence of some of these factors (induction and inhibition of drug-metabolizing enzymes) on stereoselective drug disposition. The latter topic includes an enantiomer/enantiomer interaction that alters drug disposition and drug action.