Fluocinolone (Fluocinolone Acetonide Topical) - Description and Clinical Pharmacology

FOR DERMATOLOGIC USE ONLY

NOT FOR OPHTHALMIC USE

Rx only

DESCRIPTION

Fluocinolone Acetonide Topical Solution USP, 0.01% contains fluocinolone acetonide USP (Pregna-1,4-diene-3,20-dione, 6,9-difluoro-11,21-dihydroxy-16,17-[(1-methylethylidene)bis(oxy)]-, (6α,11β,16α)-); it has an empirical formula of C ₂₄ H ₃₀ F ₂ O ₆ and a molecular weight of 425.49 (CAS Registry Number 67-73-2).

Each mL of the topical solution contains 0.1 mg fluocinolone acetonide in a base containing propylene glycol and citric acid.

CLINICAL PHARMACOLOGY

Topical corticosteroids share anti-inflammatory, anti-pruritic and vasoconstrictive actions. The mechanism of anti-inflammatory activity of the topical corticosteroids is unclear. Various laboratory methods, including vasoconstrictor assays, are used to compare and predict potencies and/or clinical efficacies of the topical corticosteroids. There is some evidence to suggest that a recognizable correlation exists between the vasoconstrictor potency and therapeutic efficacy in man.

Pharmacokinetics: 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 from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption. Occlusive dressings substantially increase the percutaneous absorption of topical corticosteroids. Thus, occlusive dressings may be a valuable therapeutic adjunct for treatment of resistant dermatoses. (See DOSAGE AND ADMINISTRATION). 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 metabolities are also excreted into the bile.