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Many psychotropic drugs are marketed and prescribed as a racemate form in a mixture of the stereoisomers. A chiral center or a center of unsaturation of carbon atoms in the chemical structures creates various stereoisomers of the psychotropic drugs, including antidepressants such as fluoxetine and venlafaxine, etc. The stereochemical significances of enantiomers on the pharmacokinetics and pharmacodynamics of several psychotropic drugs and their relationships with pharmacogenetic polymorphisms were reviewed. The single enantiomer drugs will be increasing more in the market shares replacing the racemic drugs by chiral switching, which is driven by the development of the analytical and preparative resolution techniques and will be of much benefit to the treatment from low dosages, simple dose-response curve, few adverse reactions, and so on.


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