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Pharmacokinetics of prolonged‐release tacrolimus and implications for use in solid organ transplant recipients
Author(s) -
Tanzi Maria G.,
Undre Nasrullah,
Keirns James,
Fitzsimmons William E.,
Brown Malcolm,
First M. Roy
Publication year - 2016
Publication title -
clinical transplantation
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.918
H-Index - 76
eISSN - 1399-0012
pISSN - 0902-0063
DOI - 10.1111/ctr.12763
Subject(s) - medicine , tacrolimus , pharmacokinetics , organ transplantation , intensive care medicine , solid organ , pharmacology , transplantation
Abstract Prolonged‐release tacrolimus was developed as a once‐daily formulation with ethylcellulose as the excipient, resulting in slower release and reduction in peak concentration ( C max ) for a given dose compared with immediate‐release tacrolimus, which is administered twice daily. This manuscript reviews pharmacokinetic information on prolonged‐release tacrolimus in healthy subjects, in transplant recipients converted from immediate‐release tacrolimus, and in de novo kidney and liver transplant recipients. As with the immediate‐release formulation, prolonged‐release tacrolimus shows a strong correlation between trough concentration ( C min ) and area under the 24‐hour time–concentration curve ( AUC 24 ), indicating that trough whole blood concentrations provide an accurate measure of drug exposure. We present the pharmacokinetic similarities and differences between the two formulations, so that prescribing physicians will have a better understanding of therapeutic drug monitoring in patients receiving prolonged‐release tacrolimus.