Many of the drugs currently used in medical practice are mixtures of enantiomers (racemates). Many a times, the two enantiomers differ in their pharmacokinetic and pharmacodynamic properties. Replacing existing racemates with single isomers has resulted in improved safety and/or efficacy profile of various racemates. In this review, pharmacokinetic and pharmacodynamic implications of chirality are discussed in brief, followed by an overview of some important chiral switches that have yielded safer alternatives. These include levosalbutamol, S-ketamine, levobupivacaine, S-zopiclone, levocetirizine, S-amlodipine, S-atenolol, S-metoprolol, S-omeprazole, S-pantoprazole and R-ondansetron. Few potential chiral switches under evaluation and some chiral switches that have not been successful are also discussed.