AHFS Class:

90:28.28.92 Calcineurin Inhibitors, Miscellaneous

Generic Name

• Tacrolimus

Tacrolimus concentrate for injection is available in 1-mL ampuls containing the equivalent of 5 mg of anhydrous tacrolimus per mL.³¹²⁷ In addition to tacrolimus, each mL contains polyoxyl 60 hydrogenated castor oil (surfactant) 200 mg and dehydrated alcohol, USP, 80% (v/v).¹⁶⁸³; ³¹²⁷ The product is a concentrate that must be diluted in sodium chloride 0.9% or dextrose 5% prior to administration.³¹²⁷

Trade Name(s)

Prograf

Tacrolimus is administered only by continuous intravenous infusion following dilution to a final concentration of 0.004 to 0.02 mg/mL (4 to 20 mcg/mL) in sodium chloride 0.9% or dextrose 5%.³¹²⁷ Intravenous solution containers should be composed of glass or polyethylene; polyvinyl chloride (PVC) containers should be avoided due to potential leaching of diethylhexyl phthalate (DEHP) plasticizer and decreased stability of the drug.³¹²⁷ For more dilute solutions of tacrolimus, non-PVC tubing also should be used to minimize the potential for significant drug adsorption onto the tubing.³¹²⁷

Intact ampuls should be stored at temperatures between 5 and 25°C.³¹²⁷ Diluted solutions for infusion in glass or polyethylene containers should be discarded after 24 hours.³¹²⁷ Solutions should be visually inspected for particulate matter and discoloration prior to administration.³¹²⁷

Tacrolimus exhibits a minimum rate of decomposition at pH values between 2 and 6; the rate of decomposition increases substantially at higher pH values¹⁹²⁶ and is unstable above pH 9.²²¹⁶ The manufacturer recommends that tacrolimus not be mixed with or even co-infused with solutions having a pH of 9 or greater (e.g., solutions containing acyclovir or ganciclovir).³¹²⁷

Syringes

Tacrolimus (Fujisawa) 100 mcg/mL in sodium chloride 0.9% was packaged as 20 mL in 30-mL plastic syringes (Becton Dickinson) and stored at 24°C exposed to normal room light and protected from light. No decrease in tacrolimus concentration was found after storage for 24 hours.¹⁸⁶⁴

Sorption

Tacrolimus (Fujisawa) 100 mcg/mL in dextrose 5% was delivered through PVC anesthesia extension tubing (Abbott), PVC intravenous administration set tubing (Venoset, Abbott), and lipid emulsion tubing (Abbott). The delivered solutions had no loss of tacrolimus using the PVC administration set tubing and the lipid emulsion tubing and only 2.5% drug loss from the PVC anesthesia extension tubing.¹⁸⁶⁴

Tacrolimus 50 mcg/mL delivered through 100 cm of PVC tubing at a rate of 5 mL/hr resulted in the delivery of 76% of the tacrolimus concentration. No loss due to sorption occurred when the tacrolimus solution was delivered through polyolefin tubing.²⁴⁵²

Plasticizer Leaching

Parenteral products containing a large amount of surfactant in the formulation, such as tacrolimus injection, will extract the plasticizer DEHP from PVC containers and administration sets.¹⁶⁸³; ³¹²⁷ Consequently, use of PVC containers with tacrolimus should be avoided.³¹²⁷ Instead, glass or polyethylene containers and PVC-free tubing are recommended.¹⁶⁸³; ³¹²⁷

Tacrolimus 50 mcg/mL delivered through 100 cm of PVC tubing at a rate of 5 mL/hr leached 12 mcg/mL of DEHP into the drug solution. No plasticizer leached when the tacrolimus solution was delivered through similar polyolefin tubing.²⁴⁵²

Tacrolimus 0.02 mg/mL in dextrose 5% in VISIV polyolefin bags was tested at room temperature near 23°C for 24 hours. No leached plastic components were found within the 24-hour study period.²⁶⁶⁰; ²⁷⁹²

Standardize 4 Safety

One or more standardized concentrations for this drug have been established through Standardize 4 Safety (S4S), a national patient safety initiative to reduce medication errors, especially during transitions of care. (See Standardize 4 Safety in Users Guide.) Recommendations developed to date through this initiative are available at www.ashp.org/pharmacy-practice/standardize-4-safety-initiative.

Table 1. Standardize 4 Safety Continuous IV Infusion Standard Concentrations for Tacrolimus³⁶³⁵

Solution Compatibility

Y-Site Injection Compatibility (1:1 Mixture)

For a list of references cited in the text of this monograph, search the monograph titled References.

ASHP^® Injectable Drug Information^TM. Selected Revisions December 5, 2024. © Copyright, 2025. American Society of Health-System Pharmacists^®, 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.