|Systematic (IUPAC) name|
|S-(fluoromethyl)-6α,9-difluoro-11β, 17-dihydroxy-16α-methyl-3-oxoandrosta-1, 4-diene-17β-carbothioate, 17-propanoate|
|Routes||Intranasal, Inhaled, Topical Cream or Ointment|
|ATC code||D07 & D07 (topical)|
|Mol. mass||500.57 g/mol|
|(what is this?)|
Fluticasone propionate belongs to a class of drugs known as corticosteroids, specifically glucocorticoids, which are hormones that predominantly affect the metabolism of carbohydrates and, to a lesser extent, fat and protein. It is used to treat asthma, allergic rhinitis, nasal polyps, various skin disorders and Crohn’s disease and ulcerative colitis. It is also used to treat eosinophilic esophagitis.
Fluticasone propionate is a highly selective agonist at the glucocorticoid receptor with negligible activity at androgen, estrogen, or mineralocorticoid receptor thereby producing anti-inflammatory and vasoconstriction effects. It has been shown to have a wide range of inhibitory effects on multiple cell types (e.g. mast cell, eosinophil, neutrophil, macrophages, and lymphocytes) and mediators (e.g. 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.
Medical uses & administration
Fluticasone is used by powder or aerosol inhalation for the prophylaxis of asthma. Typical initial doses in the UK range from 100 to 250 micrograms twice daily in mild asthma up to 1 mg twice daily in severe asthma, adjusted according to response. Children over 4 years of age may be given initial doses of 50 to 100 micrograms twice daily, increased to 200 micrograms twice daily if necessary. The drug may also be given via a nebuliser in severe chronic asthma. Usual adult doses are 0.5 to 2 mg twice daily. Children aged 4 to 16 years may be given 1 mg twice daily.
Nasal spray preparation of Fluticasone propionate is used in the prophylaxis and treatment of allergic rhinitis. The usual dose is 100 micrograms into each nostril once daily, increased if necessary to 100 micrograms into each nostril twice daily. Children over 4 years of age may be given half these doses.
Fluticasone propionate nasal drops are used in the treatment of nasal polyps, 200 micrograms should be instilled into each nostril once or twice daily for at least 4 to 6 weeks.
Creams and ointments containing 0.05% and 0.005% Fluticasone propionate, respectively, are available and applied topically in the treatment of various skin disorders. It can be given orally in the treatment of Crohn’s disease and ulcerative colitis. Some benefit was also reported in coeliac disease. The dose is 5 mg four times daily but some consider higher doses necessary.