Parenteral Manual

Tacrolimus (NON-FORMULARY)

Disclaimer: Official controlled document is the CHEO online copy. It is the responsibility of user to ensure that any paper copy version is the same as the online version before use.

Alternate Name(s): 
Immunosuppressive Agent - NON-CYTOTOXIC HAZARDOUS
Original Date: 
August 2005
Revised Date: 
December 2019
  • Prevention and treatment of solid organ transplant rejection
  • Other autoimmune diseases and the prevention of graft-vs-host disease following bone marrow transplantation
Reconstitution and Stability: 
  • Available as tacrolimus 5 mg/mL in 1 mL ampoules
  • Store ampoules at room temperature
  • Dilute with NS or D5W to a concentration of 0.004-0.02 mg/mL in a glass polyethylene (non-PVC), or polypropylene container
  • Diluted solution is stable at room temperature for 24 hours
  • DEHP-free tubing and non-PVC containers must be used

- Solutions Compatible: D5W, NS

- Y-site Compatible: KCL, morphine, TPN (amino acids/dextrose)


(For approved routes of administration by nursing personnel, refer to Policy for the Administration of Intravenous Medications.)

IV Direct NO
IV Intermittent Infusion

YES; Not a recommended parenteral route due to increased risk of adverse effects associated with increased plasma tacrolimus concentrations

Usual dilution: 0.004-0.02 mg/mL
Infusion time: over 2-4 hours

IV Continuous Infusion

YES, recommended parenteral route
Usual dilution: 0.004-0.02 mg/mL




(For neonatal dosages, refer to Neonatal IV Drug Manual.)

  • The optimal dosage and interval of tacrolimus has not been firmly established in pediatrics
  • Suggested dosage range: 0.03-0.15 mg/kg/day as a continuous infusion
  • For patients with hepatic or renal insufficiency, doses at the lower end of the dosing range should be used
  • Conversion to oral therapy should occur as soon as possible

- Conversion from oral to IV:

  • Oral dose = 4 x IV dose; administer the first dose 8-12 hours after the IV has been discontinued
Potential hazards of parenteral administration: 
  • CNS (most common): headache, tremor, insomnia, paresthesia, hyperesthesia, numbness, nightmares (greater with IV than oral)
  • Blurred vision and photophobia have been reported with IV therpay
  • Anaphylaxis: most likely related to the IV vehicle (castor oil) since oral administration does not carry the same risk
  • Potential for higher risk or nephrotoxicity and CNS symptoms with infusion durations less than 24 hours (related to high peak concentration)
  • Other adverse effects: nephrotoxicity, neurotoxicity, nausea, vomiting, diarrhea, infectious complications, anemia, leukocytosis, thrombocytopenia, hyperglycemia, hyperkalemia, hyperuricemia, hypomagnesemia
  • Monitoring guidelines for the first dose: monitor vital signs Q 5 minutes for the first 15 minutes of infusion, then Q 30 minutes x 1, then Q 1 hour thereafter x 3 hours, then Q 4 hours while infusion
  • Monitor whole blood concentrations 2-3 times during the first week of therapy in the morning
  • Target concentration are 5-20 mcg/L (monoclonal assay); concentrations in excess of 25 mcg/L should be asessed prior to administering
  • If tacrolimus is being administered through a single lumen venous catheter, the sample should be drawn peripherally
  • Oral administration is the usual route
  • Do not administer to patients allergic to castor oil
  • DO NOT ADMINISTER WITH CYCLOSPORINE (increased risk of nephrotoxicity)
  • Cyclosporine must be discontinued 24-48 hours before starting tacrolimus and vice-versa; dosing may be further delayed in presence of high levels
  • Additive nephrotoxicity when administered with other nephrotoxic drugs (e.g. amphotericin B, aminoglycosides, acylcovir, ganciclovir)
  • Blood concentration of tacrolimus may be altered by drugs which increase or decrease hepatic microsomal enzyme activity (e.g. phenytoin, phenobarbital, cimetidine, rifampin, ketoconazole, erythromycin)

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