Like other topical corticosteroids, mometasone furoate has antiinflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the antiinflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are thought to act by the induction of phospholipase A₂ inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A₂.

Pharmacokinetics: The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the vehicle and the integrity of the epidermal barrier. Occlusive dressings with hydrocortisone for up to 24 hours have not been demonstrated to increase penetration; however, occlusion of hydrocortisone for 96 hours markedly enhances penetration. Studies in humans indicate that approximately 0.7% of the applied dose of ELOCON Ointment, 0.1%, enters the circulation after 8 NDA 19-543 Page 6 of 14 Schering Corp. ELOCON® (mometasone furoate) Ointment, 0.1% hours of contact on normal skin without occlusion. Inflammation and/or other disease processes in the skin may increase percutaneous absorption.

Studies performed with ELOCON Ointment indicate that it is in the medium range of potency as compared with other topical corticosteroids.

In a study evaluating the effects of mometasone furoate ointment on the hypothalamicpituitary-adrenal (HPA) axis, 15 grams were applied twice daily for 7 days to six adult patients with psoriasis or atopic dermatitis. The ointment was applied without occlusion to at least 30% of the body surface. The results show that the drug caused a slight lowering of adrenal corticosteroid secretion.

In a pediatric trial, 24 atopic dermatitis patients, of which 19 patients were age 2 to 12 years, were treated with ELOCON Cream, 0.1%, once daily. The majority of patients cleared within 3 weeks.

Sixty-three pediatric patients ages 6 to 23 months, with atopic dermatitis, were enrolled in an open-label, hypothalamic- pituitary-adrenal (HPA) axis safety study. ELOCON Ointment was applied once daily for approximately 3 weeks over a mean body surface area of 39% (range 15% to 99%). In approximately 27% of patients who showed normal adrenal function by Cortrosyn test before starting treatment, adrenal suppression was observed at the end of treatment with ELOCON Ointment. The criteria for suppression were: basal cortisol level of δ5 mcg/dL, 30-minute post-stimulation level of δ18 mcg/dL, or an increase of < 7 mcg/dL. Follow-up testing 2 to 4 weeks after stopping treatment, available for 8 of the patients, demonstrated suppressed HPA axis function in 3 patients, using these same criteria.

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