STEREOSELECTIVE PHARMACOKINETICS OF DIHYDROPYRIDINE CALCIUM-ANTAGONISTS

Many dihydropyridine calcium antagonists are widely used for the treat ment of angina and hypertension, and many more are under development. Most of these drugs have one or more chiral centre, and the pharmacolo gical 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 stationa ry phase highperformance liquid chromatography for their determination . Next, the stereoselective pharmacokinetics of these drugs (nilvadipi ne, nitrendipine, felodipine, nimodipine, manidipine, benidipine and n isoldipine) in animals, healthy subjects and patients with hepatic dis ease is reviewed. Enantiomer-enantiomer interaction, enantiomeric inve rsion and the stereochemical aspects of pharmacokinetic drug interacti ons in these drugs are also described.