2003, Number 2
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Dermatología Cosmética, Médica y Quirúrgica 2003; 1 (2)
Calcineurin inhibitors. New therapeutic option in the topical treatment of inflammatory skin diseases
Gómez GM
Language: Spanish
References: 9
Page: 89-92
PDF size: 149.45 Kb.
ABSTRACT
Macrolactam derivatives pimecrolimus and tacrolimus are actually approved for topical treatment of
mild and moderate atopic dermatitis. Both inhibit calcineurin of T-activated lymphocytes, preventing
them to synthesize cytokines such as IL-2, IL-3, IL-4, and TNF-alfa. They also diminish activity from
Langerhan s cells and release of histamine and tryptase from basophils.
Their application (twice a day) is effective to alleviate eczema and pruritus, with the advantage of not causing
cutaneous atrophy as can happen with corticosteroids.
The most referred secondary effect is a burning sensation, which results less frequent with pimecrolimus (10%)
than tacrolimus (50%).
Given their immunomodulatory effect, there are reports of their use in other skin diseases such as lichen
planus, vitiligo, psoriasis, seborrheic dermatitis, alopecia areata, and contact dermatitis.
New studies, formulations, and combinations with other pharmacological agents will be of use in the near
future.
REFERENCES
Nghiem P, Pearson G, Langley RG. Tacrolimus and pime- crolimus: From clever prokaryotes to inhibiting calcineurin and treating atopic dermatitis. J Am Acad Dermatol 2002; 46: 228-241
Queille-Roussel C, Paul C, Duteil L et al. The new topical ascomycin derivate SDZ ASM 981 does not induce skin atrophy when applied to normal skin for 4 weeks: a randomized, doubleblind controlled study. Br J Dermatol 2001; 144: 507-513
Bornhövd E, Burgdorf WH, Wollengberg A. Macrolactam immunomodulators for topical treatment of inflammatory skin diseases. J Am Acad Dermatol 2001; 45: 736-743
Ruzicka T, Bieber T, Schopf E et al. A short-term trial of tacrolimus ointment for atopic dermatitis. European Tacrolimus Multicenter Atopic Dermatitis Study Group. N Engl J Med 1997; 337: 816-821
Eichenfield LF, Lucky AW, Boguniewicz M et al. Safety and efficacy of pimecrolimus (ASM981) cream 1% in the treatment of mild and moderate atopic dermatitis in children and adolescents. J Am Acad Dermatol 2002; 46: 495-504
Meingassner J, Fahrngruber H, Bavandi A. SDZ ASM 981, in contrast to CyA and FK 506, does not suppress the primary inmmune response in murine allergic contact dermatitis. J Invest Dermatol 2000; 114: 832
Meingassner JG, Hiestand P, Bigout M et al. SDZ ASM 981 is highly effective in animal models of skin inflammation, but has only low activity in models indicating immunosuppressive potential. J Invest Dermatol 2001; 117: 532
Allen A, Siegfried E, Silverman R et al. Significant absorp- tion of topical tacrolimus in 3 patient with Netherton syndrome. Arch Dermatol 2001; 137: 747-750
Ruzicka T, Assmann T, Homey B. Tacrolimus, the drug for the turn of the Millenium. Arch Dermatol 1999; 135: 574-580