Pharmacokinetic and clinical study of FK506
YU Li-xin
LIU Xiao-you
HU Min-yan
Abstract：Objective To explore the relationship of the whole blood concentrations of FK506 with the occurrence of acute rejection after renal transplantation and further, with the toxicity of this medication. Methods Ten patients with renal transplantation were given FK506-based immunosuppressive regimen 24 h after the operation. Heparinized blood samples were obtained after the initial oral administration of the drug for the pharmacokinetic evaluation. The FK506 dosage, the episodes of acute rejection and the toxicity of the medication were recorded in detail. Results t(peak) was (1.4797±1.2174) h，t1/2 beta was (10.8065±12.0799) h, and the mean residence time (MRT) was (8.0535±4.4750) h. Within the first postoperative month, 2 patients experienced acute rejection and 2 others developed diabetes which necessirare insulin therapy. The blood concentrations of the drug were not significantly different between patients with acute rejection and those without, but were significantly different between diabetic and non-diabetic patients. Conclusions FK506 is an effective prophylactic immunosuppressant for renal transplantation. The whole blood concentrations, in a certain range, are not corresponding to the episode of acute rejection. There was a significant tendency for side effects with increase of the dose concentrations, and small dose low concentrations of Fk506 can achieve good effect and reduce its toxicity.
Keywords：Fk506pharmacokineticskidney transplantation toxicityside effect
Publication Date：2000-01-01
Online Publishing Date：2025-08-15(First online date of this platform, not the publication date of the document)
Pages：3( 539 )