Sublingual administration of tacrolimus: A pilot study

摘要

The immunosuppressant tacrolimus has a narrow therapeutic index and high inter- and intra-individual variability of its pharmacokinetics. Oral bioavailability is low and highly variable (25%(4-93%)). A pilot study by Reams et al. [1, 2] demonstrated that lung transplant patients achieve therapeutic blood levels after sublingual administration comparable with oral administration. Inspired by these results, we have measured 0-12 hour blood concentration time curves after sublingual administration of tacrolimus to kidney transplant patients before transplantation.