FLUTICASONE PROPIONATE � fluticasone propionate cream
G & W LABORATORIES, INC.
Chemical structure for fluticasone propionateCarton Label for Fluticasone Propionate Cream 0.05%, 15g
DESCRIPTION
Fluticasone Propionate Cream 0.05% contains fluticasone propionate [(6?,11?,16?,17?)-6,9,-difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)androsta-1,4-diene-17-carbothioic acid, S-fluoromethyl ester], a synthetic fluorinated cortico-steroid, for topical dermatologic use. The topical cortico-steroids constitute a class of primarily synthetic steroids used as anti-inflammatory and antipruritic agents.Chemically, fluticasone propionate is C25 H3 F3 O5 S. It has the following structural formula:
Chemical structure for fluticasone propionate
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Fluticasone propionate has a molecular weight of 500.6. It is a white to off-white powder and is insoluble in water.
Each gram of Fluticasone Propionate Cream contains fluticasone propionate 0.5 mg in a base of propylene glycol, mineral oil, cetostearyl alcohol, Ceteth-20, isopropyl myristate, dibasic sodium phosphate, citric acid, purified water, and methylparaben as preservative.
CLINICAL PHARMACOLOGY
Like other topical corticosteroids, fluticasone propionate has anti-inflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the anti-inflammatory 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 .
Fluticasone propionate is lipophilic and has a strong affinity for the glucocorticoid receptor. It has weak affinity for the progesterone receptor, and virtually no affinity for the mineralocorticoid, estrogen, or androgen receptors. The therapeutic potency of glucocorticoids is related to the half-life of the glucocorticoid-receptor complex. The half-life of the fluticasone propionate-glucocorticoid receptor complex is approximately 10 hours.
Studies performed with Fluticasone Propionate Cream indicate that it is in the medium range of potency as compared with other topical corticosteroids. INDICATIONS & USAGE
Fluticasone Propionate Cream is a medium potency corticosteroid indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. Fluticasone Propionate Cream may be used with caution in pediatric patients 3 months of age or older. The safety and efficacy of drug use for longer than 4 weeks in this population have not been established. The safety and efficacy of Fluticasone Propionate Cream in pediatric patients below 3 months of age have not been established.