Adult Dosing
Heart transplant rejection prophylaxis
- 0.01 mg/kg/day IV as a continuous infusion. Titrate dose to achieve recommended blood concentration
- Administer 1st dose >6 hrs post transplantation
- Convert to oral therapy as soon as possible, usually within 2-3 days
- Give first oral dose 8-12 hrs after discontinuing IV infusion
Kidney transplant rejection prophylaxis
- 0.03-0.05 mg/kg/day IV as a continuous infusion. Titrate dose to achieve recommended blood concentration
- Wait at least 6 hours after transplantation to initiate and 8 to 12 hours if converting from IV to oral therapy. Administer 1st dose within 24 hrs of transplantation if renal function has recovered
- Convert to oral therapy as soon as possible
Liver transplant rejection prophylaxis
- 0.03-0.05 mg/kg/day IV as a continuous infusion. Titrate dose to achieve recommended blood concentration
- Administer 1st dose >6 hrs post transplantation
- Convert to oral therapy as soon as possible
Notes- Tacrolimus must be diluted with 0.9% NaCl or 5% dextrose to a concentration of 0.004 mg/mL and 0.02 mg/mL prior to use
- Therapeutic blood levels: 5-20 ng/mL
Pediatric Dosing
Liver transplant rejection prophylaxis
Child
- 0.03-0.05 mg/kg/day IV as a continuous infusion
- Administer 1st dose >6 hrs post transplantation
- Convert to oral therapy as soon as possible
Notes- Tacrolimus must be diluted with 0.9% NaCl or 5% dextrose to a concentration of 0.004 mg/mL and 0.02 mg/mL prior to use
- Therapeutic blood levels: 5-20 ng/mL
[Outline]
- Reserve IV use for patients unable to take oral formulation
- Anaphylaxis has been reported. Carefully observe patients for at least 30 mins following start of infusion. If symptoms of anaphylaxis occur, stop infusion and institute appropriate measures
- Risk of opportunistic infections, lymphomas & other malignancies, particularly of the skin
- Insulin-dependent post-transplant diabetes mellitus has been reported in kidney transplant patients without pretransplant history of diabetes mellitus
- Risk of nephrotoxicity, particularly when used in high doses. Avoid co-administration of cyclosporine; allow 24 hrs to elapse between administration
- Concomitant use with sirolimus in heart transplant patients increases risk of renal function impairment; use not recommended
- When given in high doses, neurotoxicity manifested with tremors, headache, changes in motor function, mental status, and sensory function, may occur
- Myocardial hypertrophy manifested by echocardiographically demonstrated concentric increases in left ventricular posterior wall and interventricular septum thickness, has occurred
- Monitor serum K, creatinine, fasting glucose and serum drug levels
- Coadministration with CYP3A4-inhibitors and inducers should not be considered without dose adjustment and close monitoring of tacrolimus whole blood trough concentrations and associated adverse reactions
- Tacrolimus may prolong QT interval when administered with other substrates or inhibitors of CYP3A4. Monitoring for QT prolongation is recommended
- Use of live vaccines should be avoided during treatment with tacrolimus
- Cases of pure red cell aplasia (PRCA) have been reported in patients receiving tacrolimus. Consider discontinuation of therapy If PRCA is diagnosed
- Gastrointestinal perforation has been reported in patients treated with tacrolimus. If reported appropriate medical/surgical management should be instituted promptly
Cautions: Use cautiously in
- Renal impairment
- Hepatic impairment
- Diabetes mellitus
- CV disease
- Hypertension
Pregnancy Category:C
Breastfeeding: Tacrolimus is excreted in breast milk, however since the amounts administered are low, it is not expected to adversely affect the breastfed infants. Measurements of serum drug levels in infants may be required to rule out toxicity. This information is based upon LactMed database (available at http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT last accessed 17 September 2010)).
