Table 1. Summary of Initial Oral Dosage Recommendations and Observed Whole Blood Trough Concentrations in Adults
Patient Population Recommended Tacrolimus Initial Oral Dosage Note: daily doses should be administered as two divided doses, every 12 hours Observed Tacrolimus Whole Blood Trough Concentrations
Adult kidney transplant patients
In combination with azathioprine
In combination with MMF/IL-2 receptor antagonist a
0.2 mg/kg/day
0.1 mg/kg/day
month 1 to 3: 7 to 20 ng/mL
month 4 to 12: 5 to 15 ng/mL
month 1 to 12: 4 to 11 ng/mL
Adult liver transplant patients 0.10 to 0.15 mg/kg/day month 1 to 12: 5 to 20 ng/mL
Adult heart transplant patients 0.075 mg/kg/day month 1 to 3: 10 to 20 ng/mL
month ≥4: 5 to 15 ng/mL
In a second smaller trial, the initial dose of Tacrolimus was 0.15 to 0.2 mg/kg/day and observed Tacrolimus concentrations were 6 to 16 ng/mL during month 1 to 3 and 5 to 12 ng/mL during month 4 to 12 [seeClinical Studies (14.1)]. Dosing should be titrated based on clinical assessments of rejection and tolerability. Lower Tacrolimus capsule dosages than the recommended initial dosage may be sufficient as maintenance therapy. Adjunct therapy with adrenal corticosteroids is recommended early post-transplant. The data in kidney transplant patients indicate that the Black patients required a higher dose to attain comparable trough concentrations compared to Caucasian patients (Table 2).
Table 2. Comparative Dose and Trough Concentrations Based on Race
Time After Transplant Caucasian
n=114 Black
n=56
Dose(mg/kg) Trough Concentrations(ng/mL) Dose (mg/kg) Trough Concentrations(ng/mL)
Day 7 0.18 12.0 0.23 10.9
Month 1 0.17 12.8 0.26 12.9
Month 6 0.14 11.8 0.24 11.5
Month 12 0.13 10.1 0.19 11.0
Initial Dose – Injection
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Tacrolimus injection should be used only as a continuous IV infusion and when the patient cannot tolerate oral administration of Tacrolimus capsules.Tacrolimus injection should be discontinued as soon as the patient can tolerate oral administration of Tacrolimus capsules, usually within 2 to 3 days. In a patient receiving an IV infusion, the first dose of oral therapy should be given 8 to 12 hours after discontinuing the IV infusion.
The observed trough concentrations described above pertain to oral administration of Tacrolimus only; while monitoring Tacrolimus concentrations in patients receiving Tacrolimus injection as a continuous IV infusion may have some utility, the observed concentrations will not represent comparable exposures to those estimated by the trough concentrations observed in patients on oral therapy.
The recommended starting dose of Tacrolimus injection is 0.03 to 0.05 mg/kg/day in kidney and liver transplant and 0.01 mg/kg/day in heart transplant given as a continuous IV infusion. Adult patients should receive doses at the lower end of the dosing range. Concomitant adrenal corticosteroid therapy is recommended early post-transplantation.
Anaphylactic reactions have occurred with injectables containing castor oil derivatives, such as Tacrolimus injection [see Warnings and Precautions (5.11)].
2.2 Dosage in Pediatric Liver Transplant Patients
The initial oral dosage recommendations for pediatric patients with liver transplants along with recomm