Pharmacokinetic principles of immunosuppressive drugs

A basic tenet of clinical pharmacology is that the pharmacologic activity of an exogenously administered agent is related to the free drug concentration available at its receptor or ligand-binding site. The discipline of pharmacokinetics can be defined as the study of the processes that lead to the availability of an agent to its site of action. In this review we will discuss basic principles of pharmacokinetics that govern the absorption, distribution, metabolism, elimination and binding of immunosuppressive drugs commonly utilized in whole organ transplantation. In a discipline such as organ transplantation, where the agents utilized carry significant toxicity and where failure of efficacy can have dire consequences, knowledge of the pharmacokinetics of the agents utilized has become a basic skill for all transplant professionals. In this review we describe some of the underlying principles that govern the disposition of the agents commonly utilized in solid organ transplantation. In addition, we hope this review will help in understanding some of the basic drug interactions encountered in transplant practice.