Inter-individual variability in the response to numerous drugs can be traced to a number of sources. One source of variability in drug response is the variability associated with the metabolic capacity of an individual. The component of metabolic capacity that will be the focus of this article is that determined by heredity. Pharmacogenetics is frequently referred to as the study of the effects of heredity on the disposition and response to medications. This article will review the pharmacokinetic and pharmacodynamic significance of pharmacogenetics as it pertains to a select number of cardiovascular agents. The enzyme systems responsible for drug metabolism discussed in this article will be limited to the P-450IID6 and N-acetylation pathways. Given the extensive use of cardiovascular agents in clinical practice that are affected by this genetic polymorphism, it is important for the practicing pharmacist to be aware of this phenomenon and its implications. Hopefully, the knowledge gained from this article will help practicing pharmacists to appreciate the clinical significance of polymorphic drug metabolism and provide a basis for the application of this knowledge to a variety of practice settings.