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Sublingual tacrolimus as an alternative to oral administration for solid organ transplant recipients

PURPOSE:

Available data regarding sublingual tacrolimus were analyzed to provide recommendations for solid organ transplant recipients.

SUMMARY:

Tacrolimus is an immunosuppressive agent with a narrow therapeutic range that is commonly used in solid organ transplantation. Achieving and maintaining appropriate tacrolimus exposure are critical for preventing rejection and minimizing toxicity. A variety of clinical situations requiring nonoral medication delivery arise, presenting the need for reliable alternative routes of tacrolimus administration. A review of the currently available literature revealed nine reports of sublingual tacrolimus use in human subjects. Seven reported that sublingual administration could achieve comparable tacrolimus trough concentrations to oral administration, but none investigated the correlation between tacrolimus trough concentration and exposure. One study of lung transplant recipients found that approximately 50% of the oral dose was needed to obtain therapeutic trough concentrations when converted to sublingual administration. Another study of patients with end-stage renal disease identified a similar sublingual:oral dosing ratio of 1:2. When converted from oral tacrolimus in combination with clotrimazole to sublingual administration, the sublingual:oral dosing ratio was 1:1.

CONCLUSION:

In addition to enteral tube and i.v. tacrolimus dosing, sublingual administration may be considered for short-term use in patients who are unable to receive medications orally. Based on the available data, it is reasonable to initiate sublingual tacrolimus at 50% of the current or anticipated oral dose in the absence of interacting medications. Dosing must be individualized, taking into consideration concomitant interacting medications, and adjusted to target levels based on therapeutic drug monitoring.

Related Products

Cat.No. Product Name Information
S5003 Tacrolimus (FK506) Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.

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