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Mechanism of Action
Topical corticosteroids share anti-inflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the antiinflammatory activity of the topical corticosteroids 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.
The extent of percutaneous absorption of topical corticosteroids is determined by many factors, including the vehicle, the integrity of the epidermal barrier, and the use of occlusive dressings.
Topical corticosteroids can be absorbed through normal intact skin. Inflammation and/or other disease processes in the skin, occlusive dressings, or widespread application may increase percutaneous absorption and increase the risk of HPA Axis suppression.
The vasoconstrictor assay showed that Locoid Lipocream (hydrocortisone butyrate) had a more pronounced skin blanching effect than Locoid Cream, suggesting greater percutaneous absorption from the former.
Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids.
Corticosteroids are bound to plasma proteins in varying degrees.
Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys.
Some of the topical corticosteroids and their metabolites are also excreted into the bile.
Pediatric Atopic Dermatitis
In a multicenter, randomized, vehicle-controlled trial of 264 pediatric subjects 3 months to 18 years of age with mild to moderate atopic dermatitis, Locoid Lipocream (hydrocortisone butyrate) or vehicle was applied twice daily for up to four weeks. Treatment success was assessed at day 29 (after 28 days of treatment) and was defined as the proportion of patients who achieved both “clear” or “almost clear” and at least a two grade improvement from baseline on a 5-point Physician's Global Assessment (PGA) scale.
Study results are shown in Table 3.
TABLE 3 : Efficacy Results at Day 29 in Pediatric Subjects
|Number (%) successes||82 (63%)||37 (28%)|
Last reviewed on RxList: 11/6/2009
This monograph has been modified to include the generic and brand name in many instances.
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