Effects of Drug Metabolism, Metabolites, and Stereoselectivity on Antiarrhythmic Drug Action

Metabolism, Stereoselectivity, and Antiarrhythmic Drug Action . The notion that variability in response to a desired antarrhythmic drug therapy can he reduced by adjusting doses to produce a desired plasma concentration is well established. However, unexplained toxicity or efficacy at low plasma concentrations, or suhstantial variahility in concentration‐effect relations can still occur. This review addresses two major potential sources of such responses: stereoselective drug action and the formation of active drug metaholites. Intensive study of the role of these phar‐macokinetic factors can not only improve patient care hut also can provide major clues to the fundamental determinents of drug‐macromolecule interactions which mediate drug effects in man. ( J Cardiovasc Electrophysiol, Vol. 1, pp. 238–260, June 1990 )