Once-Daily Tacrolimus Extended Release Formulation: Experience at 2 Years Postconversion From a Prograf-Based Regimen in Stable Liver Transplant Recipients

2007 ◽  
Vol 83 (12) ◽  
pp. 1639-1642 ◽  
Author(s):  
Sander Florman ◽  
Rita Alloway ◽  
Munci Kalayoglu ◽  
Jeffrey Punch ◽  
Thomas Bak ◽  
...  
Keyword(s):  
Liver Transplant ◽  
Extended Release ◽  
Transplant Recipients ◽  
Release Formulation ◽  
Once Daily ◽  
Extended Release Formulation ◽  
Liver Transplant Recipients

scholarly journals Effect of CYP3A5 on the Once-Daily Tacrolimus Conversion in Stable Liver Transplant Patients

2020 ◽  
Vol 9 (9) ◽  
pp. 2897
Author(s):  
Jong Man Kim ◽  
Je Ho Ryu ◽  
Kwang-Woong Lee ◽  
Suk Kyun Hong ◽  
Kwangho Yang ◽  
...  
Keyword(s):  
Liver Transplant ◽  
Extended Release ◽  
Trough Level ◽  
Pharmacokinetic Analysis ◽  
Transplant Recipients ◽  
Open Label ◽  
Once Daily ◽  
Transplant Patients ◽  
Liver Transplant Recipients ◽  
Cyp3a5 Polymorphism

Cytochrome P450 (CYP) 3A5 polymorphism influences tacrolimus metabolism, but its effect on the drug pharmacokinetics in liver transplant recipients switched to once-daily extended-release formulation remains unknown. The aim of this study is to analyze the effect of CYP3A5 polymorphism on liver function after once-daily tacrolimus conversion in liver transplant patients. A prospective open-label study included 60 stable liver transplant recipients who underwent 1:1 conversion from twice-daily tacrolimus to once-daily tacrolimus. All participants were genotyped for CYP3A5 polymorphism. The study was registered at ClinicalTrials.gov (NCT 02882113). Twenty-eight patients were enrolled in the CYP3A5 expressor group and 32 in the non-expressor group. Although there was no statistical difference, incidence of liver dysfunction was higher in the expressor group than in the non-expressor group when converted to once-daily extended-release tacrolimus (p = 0.088). No biopsy-proven acute rejection, graft failure, and mortality were observed in either group. The decrease in dose-adjusted trough level (−42.9% vs. −26.1%) and dose/kg-adjusted trough level of tacrolimus (−40.0% vs. −23.7%) was significantly greater in the expressor group than in the non-expressors after the conversion. A pharmacokinetic analysis was performed in 10 patients and tacrolimus absorption in the non-expressor group was slower than in the expressor group. In line with this observation, the area under the curve for once-daily tacrolimus correlated with trough level (Cmin) in the non-expressors and peak concentration (Cmax) in the expressors. CYP3A5 genotyping in liver transplant recipients leads to prediction of pharmacokinetics after switching from a twice-daily regimen to a once-daily dosage form, which makes it possible to establish an appropriate dose of tacrolimus.

scholarly journals Conversion from Twice-Daily to Once-Daily Tacrolimus Improves Graft Function but has no Influence on Proteinuria in Renal Transplant Recipients

2016 ◽  
Vol 14 (2) ◽  
pp. 73-76
Author(s):  
Nikolina Basic-Jukic ◽  
Ljubica Bubic-Filipi ◽  
Lea Katalinic ◽  
Judita Lelas
Keyword(s):  
Renal Transplant ◽  
Serum Creatinine ◽  
Extended Release ◽  
Graft Function ◽  
Renal Transplant Recipients ◽  
Transplant Recipients ◽  
Release Formulation ◽  
Once Daily ◽  
Extended Release Formulation

AbstractIntroduction. Tacrolimus extended-release formulation enables once-daily use. Although an increasing number of patients have been converted from twice-daily (Tac- BID) to once-daily (Tac-QD) formulation, the available information regarding the initiation and follow-up of Tac- QD is sparse. In the present study we investigated influence of switch from Tac-BID or cyclosporine to Tac-QD on renal allograf function, proteinuria and protein-creatinine (P/C) ratio. Methods. Between October 2012 and October 2014, the switch from Tac-BID or cyclosporine to tacrolimus extended-release formulation was done in 129(38% female, mean age 49 years) renal transplant recipients at different time after transplantation. The analysis focused on markers of graft function (GFR, serum creatinine, proteinuria, P/C ratio), liver function (AST, ALT, γGT, alkaline phosphatase) and blood glucose. Clinical data were obtained at baseline (before conversion), 1 month (V1), 6 months (V6) and 12 months (V12) after conversion. Results. Both serum creatinine and GFR showed a statistically significant improvement. With GFR, signifycant improvement was observed as early as V1 and it continued to increase throughout the study period up to V12 (all between-visit changes were statistically significant). With serum creatinine, mean levels were numerically decreasing throughout the follow-up period, but a significant improvement occurred at V6 and remained significant at V12 (both vs. V0 values). Proteinuria and P/C ratio did not show any significant change through the observation period. In the majority of patients, the baseline values of AST, ALT, GGT, AlP and glucose were within normal limits and did not change significantly through the observation period. Analysis of tacrolimus C0 showed a significant decrease throughout the follow-up period, at practically all visit. This finding was paralleled by a significant tacrolimus dose decrease from baseline to V6 and V12, as well as by a significant decrease of tacrolimus dose/body weight. Conclusions. Conversion from cyclosporine or Tac-BID to extended-release Tac-QD improves graft function in renal transplant recipients, without influence on proteinuria or P/C ratio.

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