Fluticasone Furoate (Flonase Sensimist®, Arnuity Ellipta®)

Overview

Fluticasone furoate is a synthetic corticosteroid with clinical applications in the treatment of asthma and allergy symptoms.  Fluticasone furoate is a potent agonist of the glucocorticoid receptor (GR). Like many of the synthetic corticosteroids, fluticasone furoate demonstrates minimal activity at the mineralocorticoid receptor. Binding of the GR results in receptor dimerization and nuclear translocation, leading to transcription of glucocorticoid responsive elements.  Upregulation of these genes increases the production and release of anti-inflammatory cytokines, chemokines, and adhesion molecules.  Glucocorticoids also appear to inhibit the transcription of pro-inflammatory genes via interactions with other transcription factors in the cytoplasm and nucleus.

Fluticasone furoate nasal spray is approved for the treatment of nasal and ocular allergy symptoms and is available over-the-counter in the United States.  Inhaled formulations of the drug are often prescribed as add-on therapy for asthma unresponsive to bronchodilators alone.

Fluticasone furoate generally demonstrates little systemic absorption following intranasal or inhaled administration.  Prolonged use, however, can result in local and systemic adverse effects including hypercorticism and hyperglycemia, osteoporosis and avascular necrosis, cataracts and glaucoma, hypothalamic-pituitary axis (including adrenal) suppression, and eosinophilia (inhaled formulation).

A closely related drug with a propionate (rather than furoate) ester substituent on the fluticasone base is also approved for the treatment of persistent asthma in the inhaled form, and seasonal rhinitis in the intranasal form.

In Plain English

Fluticasone furoate alters how your cells read DNA and make proteins.  This results in fewer inflammatory molecules and helps control asthma and allergy symptoms like runny nose and red eyes.

Clinical Considerations

fluticasone_furoate_intranasal

Figure 1. Fluticasone furoate intranasal spray clinical considerations at a glance.

fluticasone_furoate_inhaled

Figure 2.  Fluticasone furoate inhaled powder clinical considerations at a glance.

Evidence Basis

Fluticasone furoate in the News

Citations

  1. Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M. DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2017 Nov 8. doi: 10.1093/nar/gkx1037
  2. Epocrates Rx Online [Internet database]. San Mateo (CA): Epocrates, Inc. 2003. Retrieved at mobile.epocrates.com. Web-based; continuous content updates. Accessed 2018 May 21.
  3. “Prescription Prices, Coupons & Pharmacy Information – GoodRx.” Prescription Prices, Coupons & Pharmacy Information – GoodRxhttp://www.goodrx.com
  4. “DailyMed.” U.S. National Library of Medicine, National Institutes of Health, dailymed.nlm.nih.gov/dailymed/.
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