Once Daily Tacrolimus Formulation: Monitoring of Plasma Levels, Graft Function, and Cardiovascular Risk Factors

Meçule, A.; Poli, L.; Nofroni, Italo; Bachetoni, A.; Tinti, Francesca; Umbro, I.; Barile, M.; Berloco, P.B.; Mitterhofer, Anna Paola

doi:10.1016/j.transproceed.2010.03.123

Cited by 45 publications

(26 citation statements)

References 8 publications

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“…The absence of acute events does not preclude subclinical graft rejection, which may compromise long-term graft survival. The decrease in nephrotoxicity was reported in non-randomized studies [29, 42] but not been confirmed in randomized control trials [43, 44]. …”

Section: Discussionmentioning

confidence: 99%

Conversion from twice- to once-daily tacrolimus in pediatric kidney recipients: a pharmacokinetic and bioequivalence study

et al. 2014

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BackgroundThe objectives of this study were to investigate pharmacokinetic and pharmacogenetic parameters during the conversion on a 1:1 (mg:mg) basis from a twice-daily (Prograf) to once-daily (Advagraf) tacrolimus formulation in pediatric kidney transplant recipients.MethodsTwenty-four-hour pharmacokinetic profiles were analyzed before and after conversion in 19 stable renal transplant recipients (age 7–19 years). Tacrolimus pharmacokinetic parameters [area under the concentration-time curve (AUC0–24), minimum whole-blood concentration (Cmin), maximum whole-blood concentration (Cmax), and time to achieve maximum whole-blood concentration (tmax)] were compared between Tac formulations and between CYP3A5 and MDR1 genotypes after dose normalization.ResultsBoth AUC0–24 and Cmin decreased after conversion (223.3 to 197.5 ng.h/ml and 6.5 to 5.6 ng/ml; p = 0.03 and 0.01, respectively). However, the ratio of the least square means (LSM) for AUC0–24 was 90.8 %, with 90 % CI limits of 85.3 to 96.7 %, falling within bioequivalence limits. The CYP3A5 genotype influences the dose-normalized Cmin with the twice-daily formulation only.ConclusionsBoth tacrolimus formulations are bioequivalent in pediatric renal recipients. However, we observed a decrease in AUC0–24 and Cmin after the conversion, requiring close pharmacokinetic monitoring during the conversion period.

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Section: Discussionmentioning

confidence: 99%

Conversion from twice- to once-daily tacrolimus in pediatric kidney recipients: a pharmacokinetic and bioequivalence study

et al. 2014

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“…25,26 Although an elevated C max has been associated with the worsening of glucose control and triglyceride levels, it is possible that despite achieving targeted tacrolimus trough concentrations and similar overall AUC values, increased exposure in the early period after dose administration may contribute to toxicities (e.g., tremor, headache) in some patients. 27,28 Unfortunately, given our inclusion criteria of enrolling only clinically stable patients and the use of a single time point after transplantation, our study did not capture clinical outcomes to test this hypothesis. Further pharmacokinetic studies comparing clinical measurements and individualization of therapy in patients receiving corticosteroid-free regimens may be warranted.…”

Section: Mean ± Sdmentioning

confidence: 99%

Pharmacokinetics of tacrolimus and mycophenolate mofetil in renal transplant recipients on a corticosteroid-free regimen

Greanya

Poulin²,

Partovi

et al. 2012

American Journal of Health-System Pharmacy

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Overall exposure and C(min) values for tacrolimus were similar but C(max) values were higher than those documented in renal transplant patients treated with corticosteroid-based regimens. This may have clinical implications in corticosteroid-free patients experiencing symptoms of tacrolimus toxicity despite trough levels within target ranges. Mycophenolic acid exposure increased with time, but AUC values fell within the range expected for patients receiving concurrent corticosteroids.

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“…Several conversion studies have demonstrated bioequivalence (10% lower systemic steady‐state exposure, comparable trough minimal concentrations, and slightly reduced peak levels) (10) between the two formulations, allowing 1: 1 (mg: mg) conversion in stable kidney transplant recipients previously treated with twice‐daily tacrolimus regardless of gender, race or presence of diabetes (4,11) with a comparable safety profile at 2‐year follow‐up (12). As stated by the manufacturer, conversion to the once‐daily prolonged‐release formulation on a 1: 1 (mg: mg) total daily dose basis in stable kidney transplant recipients can result in 10% lower systemic exposure to tacrolimus; highlighting the need to closely monitor tacrolimus trough levels, adjusting, if necessary, the dose (10%) in order to maintain the adequate systemic exposure (11,13–15).…”

Section: Introductionmentioning

confidence: 99%

Efficacy and Safety of Conversion from Twice-daily to Once-daily Tacrolimus in a Large Cohort of Stable Kidney Transplant Recipients

Guirado

Cantarell

Franco

et al. 2011

American Journal of Transplantation

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Group of new projects in transplantation (Grupo español de actualizaciones en trasplante).Prolonged-release tacrolimus was developed to provide a more convenient once-daily dosing that could improve patient adherence. We conducted a multicenter, prospective, observational, 12-month study to describe the efficacy, safety and patient preference of conversion from tacrolimus twice-daily to once-daily formulation in stable kidney transplant recipients in routine clinical practice. Conversion was made on a 1 mg : 1 mg basis (1 mg : 1.1 mg in patients with trough levels <6 ng/mL). The study included 1832 patients (mean age (±SD): 50.0 ± 13.4 years; 62.7% male). After conversion, a modest reduction in tacrolimus trough levels, necessitating an increase in daily dose, was observed (mean changes at 12 months of -9.1% and +1.24%, respectively; p < 0.0001). Mean glomerular filtration rate did not change significantly (56.5 ± 19.7 mL/min at conversion vs. 55.7 ± 20.6 mL/min at 12 months). Proteinuria, blood pressure, lipid, hepatic and glucose parameters remained stable. Eight patients (0.4%) had acute rejection and 34 patients (1.85%) discontinued treatment. Almost all patients (99.4%) preferred the once-daily formulation, because of less frequent dosing (66%) and improved adherence (34%). In conclusion, at similar doses to twice-daily tacrolimus, once-daily formulation provided stable renal function, a low acute rejection rate, and good tolerability in stable kidney transplant recipients in the routine clinical practice setting.

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Once Daily Tacrolimus Formulation: Monitoring of Plasma Levels, Graft Function, and Cardiovascular Risk Factors

Cited by 45 publications

References 8 publications

Conversion from twice- to once-daily tacrolimus in pediatric kidney recipients: a pharmacokinetic and bioequivalence study

Conversion from twice- to once-daily tacrolimus in pediatric kidney recipients: a pharmacokinetic and bioequivalence study

Pharmacokinetics of tacrolimus and mycophenolate mofetil in renal transplant recipients on a corticosteroid-free regimen

Efficacy and Safety of Conversion from Twice-daily to Once-daily Tacrolimus in a Large Cohort of Stable Kidney Transplant Recipients

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