ABSTRACT

The British pharmacologist, Cushny, demonstrated differences in the pharmacological activity of atropine and (−)-hyoscyamine and (−)-and (+)-adrenaline in the early part of the last century.1 However, it is only relatively recently that the stereochemical nature of drug molecules has become a topic of concern and pharmacology has moved from a ‘flatland’ two-dimensional science to one of three-dimensional spatial awareness. This change in philosophy with respect to chiral pharmaceuticals, the majority of which are used

as racemic mixtures, has been brought about largely as a result of advances in chemical technologies for the analysis, synthesis and preparation of single stereoisomers. The ability to produce and determine the stereochemical purity of single stereoisomers has facilitated an evaluation of their pharmacological properties. As a result there has been an increased appreciation of the potential significance of the differential pharmacological properties of the enantiomers present in a racemate and the problems that may arise from the use of such mixtures.