Sublingual Tacrolimus as an Alternative to Intravenous Route in Patients With Thoracic Transplant: A Retrospective Study

Clinical Pharmacokinetics of Oral Versus Sublingual Administration of Tacrolimus in Adult Liver Transplant Recipients

“…Also, a preliminary study by Goorhuis 6 in pediatric liver transplant recipients showed that buccal administration of TAC is well tolerated, with similar resultant TAC trough levels compared with drug levels after TAC delivery through nasogastric tube. Collin 17 reported the potential safety of sublingual TAC as an alternative to the intravenous route in 16 patients with thoracic transplant: 90.4% of their TAC concentration samples were within the therapeutic range. In Collin's study, the powder content of the capsules was put directly under the patient's tongue; but in our study, to enhance drug absorption, the powder content of the capsules was dispersed in water before administration.…”

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

“…Only 7 patients were followed for more than 6 months; of these, 43% experienced biopsy-confirmed acute rejection. 20 A single-center, retrospective review of 16 hospitalized heart and lung transplant recipients who received sublingual tacrolimus for at least 5 consecutive days was conducted by Collin et al 21 The indication for lung transplantation was cystic fibrosis for the majority of patients. The mean sublingual tacrolimus dose of 0.116 ± 0.096 mg/kg daily corresponded to a mean AUC of 230 ± 74.1 ng · hr/ mL (n = 4), while a mean oral dose of 0.414 ± 0.246 mg/kg daily was needed to achieve a similar AUC of 252 ± 92.7 ng · hr/mL (n = 5).…”

“…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.…”

Use of sublingual tacrolimus in lung transplant recipients

“…2,3,7,8 Notably, the delivery vehicle of intravenous tacrolimus contains a castor oil derivative that can precipitate an anaphylactic reaction and should be avoided when possible. 8,9 Compared with intravenous administration, oral administration of tacrolimus is less expensive, more feasible in the outpatient setting, and is associated with a decreased risk of severe nephrotoxicity, neurotoxicity and anaphylaxis. 8,10 In some clinical situations, however, oral administration presents challenges.…”

“…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. Presently, an appropriate "universal" conversion ratio between oral and sublingual tacrolimus, independent of native disease, has yet to be defined.…”