Clinical Pharmacology of Melacare Hydroquinone Tretionoin Mometasone Furoate Cream

 

 

Similar to other topical corticosteroids, mometasone furoate contains anti-inflammatory, antipruritic, and vasoconstrictive properties. The method of the anti- inflammatory activity of the topical steroids, usually, has not been examined. On the other hand, corticosteroids are supposed to work by the initiation of phospholipase A 2 inhibitory proteins, commonly called lipocortins. It is suggested that these proteins control the biosynthesis of potent mediators of inflammation including prostaglandins and leukotrienes. They do it by reducing the release of their common precursor arachidonic acid. Phospholipase A 2 releases arachidonic acid from membrane phospholipids.

Pharmacokinetics

Many factors together with the vehicle and the integrity of the epidermal barrier determine the degree of percutaneous absorption of topical corticosteroids. Occlusive dressings with hydrocortisone for up to 24 hours have not been reported to enhance penetration; but, occlusion of hydrocortisone for 96 hours noticeably enhances penetration. Studies in humans show that around 0.4% of the applied dose of Mometasone Cream enters the circulation after 8 hours of contact on normal skin without occlusion. Inflammation and/or other disease processes in the skin may enhance percutaneous absorption.

Studies made on Mometasone Cream reveals that it is in the medium range of effectiveness as compared with other topical corticosteroids.

In another study 15 grams were applied twice daily for 7 days to 6 adult patients with psoriasis or atopic dermatitis. The cream was applied without occlusion to at least 30% of the body surface. The study was made to assess the effects of mometasone furoate cream on the hypothalamic- pituitary-adrenal (HPA) axis. The treatment led to a slight lowering of adrenal corticosteroid secretion.

In a study made on pediatric patient, 24 atopic dermatitis patients, of whom 19 patients were age 2 to 12 years, were administered mometasone cream, once daily. The majority of patients cleared within 3 weeks.

In an open-label, hypothalamic-pituitary-adrenal (HPA) axis safety study, around 16% of pediatric patients, ages 6 to 23 months, who showed normal adrenal function by Cortrosyn test before starting treatment revealed HPA axis suppression. They had been treated for about 3 weeks over a mean body surface area of 41% (range 15% to 94%). The criteria for suppression were: basal cortisol level of ≤ 5 mcg/dL, 30-minute post-stimulation level of ≤ 18 mcg/dL, or an increase of <7 mcg/dL. Follow-up testing 2 to 4 weeks after study completion, available for 5 of the patients, demonstrated suppressed HPA axis function in one patient, using these same criteria. Long-term use of topical corticosteroids has not been studied in this population.