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Exp Dermatol ; 16(9): 753-61, 2007 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-17697148

RESUMEN

Although introduced more than 50 years ago, topical glucocorticoids are still the first line therapy for many inflammatory skin disorders such as atopic eczema, contact dermatitis and many others. Recently, significant improvements have been made to optimize the ratio of desired to unwanted effects. While with early compounds such as triamcinolone, topical side effects such as skin atrophy and telangiectasias can be observed rather frequently, newer drugs such as methylprednisolone aceponate or mometasone furoate have a significantly improved therapeutic index. The present study compared these two modern topical glucocorticoids, which possess the highest therapeutic index currently found, in terms of nuclear receptor selectivity in vitro and induction of the most important local side effects (skin atrophy and telangiectasias) in a relevant rodent model in vivo. We demonstrate that methylprednisolone aceponate displays higher specificity in nuclear receptor binding compared with mometasone furoate. Methylprednisolone aceponate was also markedly superior in terms of minimizing induction of skin atrophy or telangiectasias when compared with mometasone furoate. Based on these observations, methylprednisolone aceponate is expected to have a greater therapeutic index as compared with mometasone furoate, at least in the test systems used here. The degree to which this observation may translate into a clinical setting requires confirmation.


Asunto(s)
Antiinflamatorios/uso terapéutico , Metilprednisolona/análogos & derivados , Pregnadienodioles/uso terapéutico , Receptores Citoplasmáticos y Nucleares/fisiología , Administración Tópica , Animales , Antiinflamatorios/administración & dosificación , Antiinflamatorios/efectos adversos , Atrofia/inducido químicamente , Atrofia/patología , Modelos Animales de Enfermedad , Metilprednisolona/administración & dosificación , Metilprednisolona/efectos adversos , Metilprednisolona/uso terapéutico , Furoato de Mometasona , Pregnadienodioles/administración & dosificación , Pregnadienodioles/efectos adversos , Unión Proteica/efectos de los fármacos , Unión Proteica/fisiología , Ratas , Ratas Mutantes , Ratas Desnudas , Ratas Wistar , Receptores Androgénicos/efectos de los fármacos , Receptores Androgénicos/fisiología , Receptores Citoplasmáticos y Nucleares/efectos de los fármacos , Receptores de Mineralocorticoides/efectos de los fármacos , Receptores de Mineralocorticoides/fisiología , Receptores de Progesterona/efectos de los fármacos , Receptores de Progesterona/fisiología , Piel/irrigación sanguínea , Piel/patología , Telangiectasia/inducido químicamente , Telangiectasia/patología
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