Tacrolimus Dosage

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Usual Adult Dose for:

Usual Pediatric Dose for:

Additional dosage information:

Usual Adult Dose for Organ Transplant - Rejection Prophylaxis

For use in the prophylaxis of allograft rejection in transplant recipients:

INTRAVENOUS INJECTION:
-Kidney and Liver Transplant:
Initial Dose: 0.03 to 0.05 mg/kg/day as a continuous IV infusion
-Heart Transplant: 0.01 mg/kg/day as a continuous IV infusion

-Doses as high as 0.1 mg/kg/day as a continuous IV infusion may be appropriate.
-Continuous IV infusion of tacrolimus injection should be continued only until the patient can tolerate oral administration of the capsules. This usually occurs within 2 to 3 days.

IMMEDIATE RELEASE CAPSULE:
-Kidney Transplant:
In combination with azathioprine: 0.2 mg/kg/day orally
In combination with MMF/IL-2 receptor antagonist: 0.1 mg/kg/day orally
-Liver Transplant: 0.1 to 0.15 mg/kg/day orally
-Heart Transplant: 0.075 mg/kg/day orally

-Daily doses should be administered as two divided doses, every 12 hours.
-Doses as high as 0.3 mg/kg/day administered every 12 hours in 2 divided doses may be appropriate.
-The initial dose of should be administered no sooner than 6 hours after transplantation in liver and heart transplant patients. In kidney transplant patients, the initial dose may be administered within 24 hours of transplantation, but should be delayed until renal function has recovered.
-It is important to take immediate release capsules consistently every day either with or without food because the presence and composition of food decreases the bioavailability.
-Patients should not eat grapefruit or drink grapefruit juice.

EXTENDED RELEASE CAPSULE:
Kidney Transplant only:
-With basiliximab induction: 0.15 mg/kg/day orally as a single daily dose. Give first dose prior to or within 48 hours after transplant completion; may delay therapy initiation until renal function has recovered.
-Without induction:
0.1 mg/kg/day orally, preoperatively, as a single daily dose. Give preoperative dose within 12 hours prior to reperfusion.
0.2 mg/kg/day orally, postoperatively, as a single daily dose. Give first postoperative dose within 12 hours after reperfusion but not less than 4 hours after preoperative dose.

-Take tacrolimus extended release capsules once daily in the morning, preferably on an empty stomach; do not take with an alcoholic beverage or grapefruit juice; do not chew, divide or crush capsules.

Comments:
-Adult patients should receive doses at the lower end of the dosing range.
-Dosing of tacrolimus should be titrated based on clinical assessments of rejection and tolerability, and to maintain recommended trough concentration ranges. Monitoring of whole blood tacrolimus trough concentrations is recommended.
-Typical whole blood trough concentrations usually range from 5 to 20 ng/mL. Monitoring of tacrolimus blood levels is considered an essential component of toxicity evaluation. The incidence of adverse effects increase as blood levels rise above the typical range. Extra caution and closer monitoring are recommended when graft function changes or drug interactions are suspected.
-In a patient initially receiving an IV infusion of tacrolimus, the first dose of oral therapy should be given 8 to 12 hours after discontinuing the IV infusion.
-African-American kidney transplant patients may require higher doses of tacrolimus to attain comparable trough concentrations compared to Caucasian patients.
-Tacrolimus should not be used simultaneously with cyclosporine. Tacrolimus or cyclosporine should be discontinued at least 24 hours before initiating the other.
-Extended-release capsules are not interchangeable or substitutable with tacrolimus immediate-release capsules.

Usual Adult Dose for Graft Versus Host Disease

(Not approved by FDA)
Prevention:
Initial dose: 0.03 mg/kg/day (based on lean body weight) as a continuous infusion. Treatment should begin at least 24 hours prior to stem cell infusion and continued only until oral medication can be tolerated.

Treatment:
Initial dose: 0.03 mg/kg/day (based on lean body weight) as a continuous infusion.

Conversion from IV to oral dose (1:4 ratio): Multiply total daily IV dose times 4 and administer in 2 divided oral doses per day, every 12 hours.

Usual Pediatric Dose for Organ Transplant - Rejection Reversal

Liver transplant:
Oral: Initial dose: 0.15 to 0.2 mg/kg/day divided every 12 hours
IV: 0.03 to 0.05 mg/kg/day as a continuous infusion
Dose adjustments may be required. Doses as high as 0.15 mg/kg/day IV or 0.3 mg/kg/day orally have been used.

Heart transplant:
Oral: Initial dose: 0.1 to 0.3 mg/kg/day divided every 12 hours
IV: 0.01 to 0.03 mg/kg/day as a continuous infusion

Kidney transplant:
Oral: Initial dose: 0.2 to 0.3 mg/kg/day divided every 12 hours
IV: 0.06 mg/kg/day as a continuous infusion

Usual Pediatric Dose for Graft Versus Host Disease

(Not approved by FDA)
Prevention:
Initial dose: 0.03 mg/kg/day (based on lean body weight) as continuous infusion. Treatment should begin at least 24 hours prior to stem cell infusion and continued only until oral medication can be tolerated.
Conversion from IV to oral dose (1:4 ratio): Multiply total daily IV dose times 4 and administer in 2 divided oral doses per day, every 12 hours.

Renal Dose Adjustments

Due to the potential for nephrotoxicity, patients with renal impairment should receive doses at the lowest value of the recommended IV and/or oral dosing ranges. Further reductions in dose below these ranges may be required.

Liver Dose Adjustments

Due to the reduced clearance and prolonged half-life, patients with severe hepatic impairment (Child Pugh score of 10 or greater) may require lower doses of tacrolimus. Close monitoring of blood concentrations is warranted.

The use of tacrolimus in liver transplant recipients experiencing post-transplant hepatic impairment may be associated with increased risk of developing renal insufficiency related to high blood levels of tacrolimus. Monitor these patients closely and consider dosage adjustments as warranted. Some evidence suggests that lower doses should be used in these patients.

Precautions

In kidney transplant patients with postoperative oliguria, tacrolimus therapy should be given no sooner than 6 hours and within 24 hours of transplantation, but may be delayed until renal function recovers.

The safety and efficacy of the extended release capsule formulation in pediatric patients less than 16 years of age has not been established.

Dialysis

Data not available

Other Comments

Younger children generally require higher maintenance doses on a mg/kg basis than older children, adolescents, or adults.

Tacrolimus should be used concomitantly with adrenal corticosteroids.

Because of the risk of anaphylaxis, tacrolimus injection should be reserved for patients unable to take the capsules orally.

Typical whole blood trough concentrations usually range from 5 to 20 ng/mL. Monitoring of tacrolimus blood levels is considered an essential component of toxicity evaluation. The incidence of adverse effects increase as blood levels rise above the typical range. Extra caution and closer monitoring are recommended when graft function changes or drug interactions are suspected.

Serum creatinine and potassium should be monitored regularly during tacrolimus therapy. In addition, a complete blood count with differential, platelet count, liver function tests, and metabolic tests should be routinely monitored during tacrolimus therapy if clinically indicated.

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