2015
DOI: 10.2146/ajhp140322
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Sublingual tacrolimus as an alternative to oral administration for solid organ transplant recipients

Abstract: 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.

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Cited by 30 publications
(15 citation statements)
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“…Although some studies are promising, contradictive results exist [ 12 , 14 , 28 , 33 , 45 ]. Tacrolimus has been used as an immunosuppressant drug in transplantations and granulomatous disease [ 73 ]. Alijotas-Reig et al investigated its use in series of seven patients with late-onset adverse events after silicone injection, finding good clinical response [ 33 ].…”
Section: Discussionmentioning
confidence: 99%
“…Although some studies are promising, contradictive results exist [ 12 , 14 , 28 , 33 , 45 ]. Tacrolimus has been used as an immunosuppressant drug in transplantations and granulomatous disease [ 73 ]. Alijotas-Reig et al investigated its use in series of seven patients with late-onset adverse events after silicone injection, finding good clinical response [ 33 ].…”
Section: Discussionmentioning
confidence: 99%
“…TAC, IR capsules may be opened and administered sublingually by placing the powder contents underneath the tongue for 10–15 minutes. Of note, a sublingual dose may double TAC exposure compared with oral/enteral administration; thus, close therapeutic drug monitoring is necessary and a dose reduction may be warranted 61,62 . Immediate‐release products and SR products are not interchangeable and SR products are not interchangeable with each other 63 .…”
Section: Maintenance Immunosuppression In Pediatric Kidney Transplantmentioning
confidence: 99%
“…Tacrolimus remains the mainstay in the majority of transplantation drug regimens. The mechanism of action of tacrolimus as an immunosuppressant has been extensively studied [79] and mainly driven by calcineurin phosphatase inactivation [80] via binding to the intracellular protein FKBP12 [81]. This inactivation prevents the transport of nuclear factor of activated T cells (NF-AT), which is required for T-cell activation and expression of several cytokines, including IL-2.…”
Section: Tacrolimusmentioning
confidence: 99%
“…Distribution after absorption appears to vary drastically with representative sites being erythrocytes, lungs, liver, kidneys, pancreas, heart and spleen. Tacrolimus is metabolized in the liver via the CYP3A4 and CYP3A5 isoenzymes in addition to the P-gp efflux pump [81] in the intestinal wall to eight possible metabolites, with the 31-demethyl tacrolimus being the most common which has similar efficacy as tacrolimus [83]. The half-life of tacrolimus is extremely variable from patient to patient (2.1-36 h) with a time to peak onset of 0.5-6 h. Tacrolimus is primarily excreted at an average rate of 30 ml/min/kg in the feces (93%) and <1% is found to be excreted via the kidney in the active form of the drug [84].…”
Section: Tacrolimusmentioning
confidence: 99%