Fluticasone propionate is a highly selective agonist at the glucocorticoid receptor with negligible activity at androgen , estrogen , or mineralocorticoid receptors , thereby producing anti-inflammatory and vasoconstriction effects. It has been shown to have a wide range of inhibitory effects on multiple cell types (. mast cell , eosinophil , neutrophil , macrophages , and lymphocytes ) and mediators (. histamine , eicosanoids , leukotrienes , and cytokines ) involved in inflammation . Fluticasone propionate is stated to exert a topical effect on the lungs without significant systemic effects at usual doses, due to its low systemic bioavailability .
Fluticasone propionate is a synthetic (man-made) corticosteroid that is used on the skin (topically). The naturally-occurring corticosteroid is cortisol or hydrocortisone produced by the adrenal gland. Corticosteroids have potent anti-inflammatory actions and also suppress the immune response. Similar drugs include betamethasone dipropionate (Diprolene), clobetasol propionate (Temovate), halobetasol propionate (Ultravate), betamethasone dipropionate (Diprosone), desoximetasone (Topicort), halcinonide (Halog), amcinonide (Cyclocort), triamcinolone acetonide (Kenalog), fluocinolone acetonide (Synalar), hydrocortisone butyrate (Locoid), hydrocortisone valerate (Westcort), and mometasone furoate (Elocon). The FDA approved topical fluticasone propionate in December, 1990.
In rabbits, fetal weight reduction and cleft palate were observed at a fluticasone propionate dose approximately times the MRHDID for adults (on a mg/m² basis at a maternal subcutaneous dose of 4 mcg/kg/day). However, no teratogenic effects were reported at fluticasone propionate doses up to approximately 20 times the MRHDID for adults (on a mg/m² basis at a maternal oral dose up to 300 mcg/kg/day). No fluticasone propionate was detected in the plasma in this study, consistent with the established low bioavailability following oral administration [see CLINICAL PHARMACOLOGY ].