糠酸氟替卡松为源自氟替卡松的一种人工合成皮质类固醇,可治疗过敏性鼻炎用。
糠酸氟替卡松(GW685698)是一种吸入性皮质类固醇/长效的β肾上腺素能受体激动剂的复方治疗药物,能延长支气管扩张剂的作用时间。它被用于非过敏性和过敏性皮炎的治疗。
Kd: 0.3 nM (Corticosteroid)
Fluticasone furoate comes in a nasal spray, as an aqueous suspension of micronized fluticasone furoate for topical administration to the nasal mucosa by means of a metering, atomizing spray pump. Fluticasone furonate displays great potency in inhibiting tumor necrosis factor synthesis and action. Fluticasone furonate is also potent in preventing damage to cultured human lung epithelial cells by different stimulus.
Fluticasone furonate is 99.4% bound to plasma protein in vitro and other research indicated extensive first-pass metabolism of the absorbed drug. Protein binding is highly relevant because only the unbound free drug can exert an effect at the receptor site. Clearance of Fluticasone furonate is primarily by hydrolysis in the liver by the cytochrome P450 isozyme (CYP) 3A4 that converts the drug to the 17β-carboxylic acid metabolite (M10), which displays low glucocorticoid receptor agonist potency. Fluticasone furonate is excreted mainly in the feces, with only minor amounts in the urine.