DIFLORASONE DIACETATE- diflorasone diacetate cream
Taro Pharmaceuticals U.S.A., Inc.
Rx only
For External Use Only - Not for Ophthalmic Use.
DESCRIPTION
Diflorasone diacetate cream USP, 0.05% contains the active compound diflorasone diacetate, a synthetic corticosteroid for topical dermatological use.
Chemically, diflorasone diacetate is 6?, 9?-difluoro-11?,17,21-trihydroxy-16-methylpregna-1,4-diene-3,20-dione 17,21 diacetate, with the empirical formula C26 H32 F2 O7 , a molecular weight of 494.5, and the following structural formula:
Chemical Structure
(click image for full-size original)
Each gram of diflorasone diacetate cream USP, 0.05% contains 0.5 mg diflorasone diacetate in a cream base consisting of butylated hydroxytoluene, cetyl alcohol, citric acid, glyceryl stearate/PEG 100 stearate, isopropyl myristate, lanolin alcohol, mineral oil, monobasic sodium phosphate, polyoxyl 40 stearate, polysorbate 60, propylene glycol, purified water, sorbitan monostearate and vegetable oil.
CLINICAL PHARMACOLOGY
Like other topical corticosteroids, diflorasone diacetate has anti-inflammatory, anti-pruritic, and vasoconstrictive actions. The mechanism of the anti-inflammatory activity of the topical corticosteroids, 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. Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin may increase percutaneous absorption. Studies performed with diflorasone diacetate cream indicate that it is in the high range of potency as compared with other topical corticosteroids.
INDICATION AND USAGE
Diflorasone diacetate cream USP, 0.05% is a high potency corticosteroid indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.