1. Pharmacokinetics of prolonged-release tacrolimus and implications for use in solid organ transplant recipients.
- Author
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Tanzi, Maria G., Undre, Nasrullah, Keirns, James, Fitzsimmons, William E., Brown, Malcolm, and First, M. Roy
- Subjects
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PHARMACOKINETICS , *TACROLIMUS , *TRANSPLANTATION of organs, tissues, etc. , *ETHYLCELLULOSE , *LIVER transplantation , *KIDNEY transplant patients , *DRUG monitoring , *PATIENTS - 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 ( Cmax) 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 ( Cmin) and area under the 24-hour time-concentration curve ( AUC24), 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. [ABSTRACT FROM AUTHOR]
- Published
- 2016
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