Tacrolimus: review of pharmacokinetics, pharmacodynamics, and pharmacogenetics to facilitate practitioners' understanding and offer strategies for educating patients and promoting adherence.
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.
Vicari-Christensen
Michele
M
University of Florida and Shands Jacksonville Medical Center, USA. michele.vicari-christensen@jax.ufl.edu
Repper
Suzanne
S
Basile
Sharon
S
Young
Danella
D
D051544:Cytochrome P-450 CYP3A / Q000187:drug effects; D065692:Cytochrome P-450 CYP3A Inhibitors; D004347:Drug Interactions; D016903:Drug Monitoring; D006084:Graft Rejection / Q000276:immunology / Q000517:prevention & control; D006085:Graft Survival / Q000187:drug effects / Q000276:immunology; D006801:Humans; D007165:Immunosuppression Therapy / Q000009:adverse effects / Q000379:methods / Q000523:psychology; D007166:Immunosuppressive Agents / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D016030:Kidney Transplantation / Q000276:immunology*; D008499:Medical Records; D055118:Medication Adherence / Q000523:psychology; D008657:Metabolic Clearance Rate; D010351:Patient Discharge; D010353:Patient Education as Topic / Q000458:organization & administration*; D010597:Pharmacogenetics; D016559:Tacrolimus / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D014181:Transplantation Immunology / Q000187:drug effects / Q000276:immunology
D065692:Cytochrome P-450 CYP3A Inhibitors; D007166:Immunosuppressive Agents; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human; D016559:Tacrolimus