Significant Systemic Absorption of Tacrolimus After Topical Application in a Patient With Lamellar Ichthyosis

Netherton syndrome: Successful use of topical tacrolimus and pimecrolimus in four siblings

“…Tacrolimus and pimecrolimus have been approved by many agencies for atopic dermatitis 3,39 . There have been several reports of the efficacy of tacrolimus and pimecrolimus in a variety of other inflammatory dermatoses including psoriasis, lamellar ichthyosis and NS 4–6,29,47,48 . Because patients with NS may be particularly vulnerable to increased percutaneous absorption owing to a defective epidermal barrier, it is recommended to monitor the blood drug level closely 5,6,49 .…”

“…They bind cytoplasmic proteins and the resulting complex binds calcineurin, inhibiting its ability to dephosphorylate the nuclear factor of activated T cells (NF‐AT), thus suppressing gene transcription 3 . There have been conflicting reports of the usefulness of tacrolimus in NS patients, with systemic absorption being the main adverse outcome 4–6 . We report four Saudi siblings (two boys and two girls) with NS who were treated with topical tacrolimus and pimecrolimus with good control of their skin disease without any toxic effect.…”

Toxic absorption of pimecrolimus in a patient with severe acute graft-versus-host disease

“…In patients with primary dermatologic diseases, levels as high as 37.2 ng/ml have been reported. [6][7][8][9][10] The patients achieving elevated levels all had relatively rare dermatologic diseases, with a breakdown of the epidermal barrier, leading to an increase in percutaneous absorption of topical tacrolimus. 11,12 In vitro studies show percutaneous absorption by healthy skin of 0.03, 0.1, and 0.3% topical tacrolimus ointments was 3.1, 4.9, and 6.8 ng/cm 2 /h, respectively, while damaged skin absorbed an average of 40 ng/cm 2 /h.…”

Safety of dermatologic drugs used in pregnant patients with psoriasis and other inflammatory skin diseases

“…48,49 Systemic absorption of tacrolimus after topical administration is very low, except in patients who have defective dermal barrier function. [50][51][52] Blood concentrations of patients with atopic dermatitis treated topically with tacrolimus were 7 to 17 times lower than those observed in transplantation recipients after oral administration. 52 In a large series of 71 transplantation recipients who were treated orally with tacrolimus during pregnancy and delivered live infants, there were 3 (4%) perinatal deaths and 4 (6%) infants born with congenital anomalies.…”