Utility of sublingual tacrolimus in cystic fibrosis patients after lung transplantation

Use of sublingual tacrolimus in lung transplant recipients

“…Although sublingual administration of tacrolimus has been reported to yield therapeutic drug concentrations in the blood, information on how to efficiently convert between sublingual and oral tacrolimus is limited. 7,12,13,15 Thus, our conversion ratio may serve as an important instrument to aid in the selection of the appropriate tacrolimus dose when converting lung transplant recipients between oral and sublingual routes. The paired-sample nature of our study eliminated the impact that tacrolimus dose variation between subjects would have had on the conversion ratio.…”

“…4,9,[11][12][13] Importantly, the risk of serious complications associated with sublingual administration of tacrolimus appears to be similar to that of oral administration. 9 Although previous findings showed that sublingual administration is feasible, it has been speculated that the bioavailability may be different from oral administration.…”

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

“…The first report of successful sublingual administration included 6 lung transplant recipients with cystic fibrosis. 19 During sublingual tacrolimus administration, 46% of tacrolimus trough concentrations were within the therapeutic range (10-17 ng/mL), 28% were supratherapeutic (>17 ng/mL), and 26% were subtherapeutic (<10 ng/mL). These patients were followed for a mean of 3.6 months (range, 1.5-5 months).…”

“…Because a sublingual formulation is not commercially available for tacrolimus, the most commonly reported method of sublingual tacrolimus administration in the aforementioned studies [19][20][21][23][24][25] involved placing the contents of capsules under the patient's tongue, avoiding swallowing for a period of 5-15 minutes and avoiding any oral intake for 15-30 minutes. However, alternative sublingual administration techniques have resulted in findings that make the clinical utility of sublingual tacrolimus less certain.…”

A novel approach to immunosuppression: targeting the alloimmune mechanisms of graft rejection

“…A pilot study showed that tacrolimus does achieve therapeutic levels in lung transplant patients with cystic fibrosis; however, comparative randomized trials are required to determine the long-term safety and efficacy of this route of administration [33,34].…”