Many dihydropyridine calcium antagonists are widely used for the treatment of angina and hypertension, and many more are under development. Most of these drugs have one or more chiral centre, and the pharmacological activity between the enantiomers for these drugs is known to be markedly different. First, the stereospecific assay methods for these drugs in plasma or serum are reviewed with emphasis on chiral stationary phase high-performance liquid chromatography for their determination. Next, the stereoselective pharmacokinetics of these drugs (nilvadipine, nitrendipine, felodipine, nimodipine, manidipine, benidipine and nisoldipine) in animals, healthy subjects and patients with hepatic disease is reviewed. Enantiomer-enantiomer interaction, enantiomeric inversion and the stereochemical aspects of pharmacokinetic drug interactions in these drugs are also described.