Tacrolimus: Review of Pharmacokinetics, Pharmacodynamics, and Pharmacogenetics to Facilitate Practitioners' Understanding and Offer Strategies for Educating Patients and Promoting Adherence

Abstract

Kidney transplantation requires lifelong immunosuppression with agents that prevent allograft rejection. Immunosuppressive regimens typically include a steroid, an immune modulator (eg, azathioprine, mycophenolate mofetil, or mycophenolate sodium), and a calcineurin inhibitor, either cyclosporine or tacrolimus. Tacrolimus is metabolized by cytochrome P450 3A4 in both the liver and small intestine. Drugs that are substrates of cytochrome P450 3A4, as well as inhibitors and inducers of cytochrome P450 3A4, can cause significant interactions with tacrolimus. A review of the pharmacodynamics and pharmacokinetics of tacrolimus is important to enhance practitioners' understanding when using tacrolimus after kidney transplantation. It is also important to educate patients and their families about tacrolimus. Patients' adherence to this medication regimen is pivotal for allograft survival. A consistent and comprehensive approach to education and discharge teaching is a key component of adherence and the attainment of therapeutic drug levels. At Shands Jacksonville Transplant Center, discharge education and teaching tools aid the transplant professionals and facilitate patients' adherence. This in turn supports the goals of maintaining therapeutic serum levels of tacrolimus and improving renal allograft survival.