Fluticasone propionate

Fluticasone propionate, sold under the brand names Flovent and Flonase among others, is a steroid medication.[1] When inhaled it is used for the long term management of asthma and COPD.[1] In the nose it is used for hay fever and nasal polyps.[2][3] It can also be used for mouth ulcers.[4]

Fluticasone propionate
Clinical data
Trade namesFlovent, Flixotide (inhaled)
Flixonase, Flonase (nasal)
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • US: C (Risk not ruled out)
    Routes of
    administration    		Intranasal, inhaled, topical
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Bioavailability0.51% (Intranasal)
    Protein binding91%
    MetabolismIntranasal
    Liver (CYP3A4-mediated)
    Elimination half-life10 hours
    ExcretionKidney
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    ChEBI
    ChEMBL
    ECHA InfoCard100.129.097
    Chemical and physical data
    FormulaC25H31F3O5S
    Molar mass500.57 g/mol g·mol−1
    3D model (JSmol)
      (verify)

    Common side effects when inhaled include upper respiratory tract infections, sinusitis, thrush, and cough.[1] Common side effects when used in the nose include nosebleeding and sore throat.[2] It works by decreasing inflammation.[1]

    Fluticasone propionate was patented in 1980 and approved for medical use in 1990.[5] It is available as a generic medication.[3] In the United States the wholesale cost per spray is about 0.33 USD as of 2018.[6] In the United Kingdom, it costs the NHS about 0.13 GBP per spray as of 2019.[3] In 2016 it was the 16th most prescribed medication in the United States with more than 29 million prescriptions.[7]

    Medical uses

    Fluticasone is used by powder or aerosol inhalation for the prophylaxis of asthma. The nasal spray is used for prevention and treatment of allergic rhinitis. Nasal drops are used in the treatment of nasal polyps. The nasal spray can also be used in the mouth for mouth ulcers.[4]

    Adverse effects

    If taken correctly, the nasal spray and oral inhaler formulation have fewer corticosteroid side effects than the tablet formulation because they limit systemic (blood) absorption.[8] However, the systemic absorption is not negligible even with correct administration.[8] Using the spray or inhaler at higher than recommended doses or with other corticosteroids can increase the risk for serious, systemic corticosteroid induced side effects.[8][9] These side effects include weakened immune system, increased risk of systemic infections, osteoporosis, and elevated pressure in the eyes.[10]

    Nasal spray

    Common side effects may include nasal irritation (burning, stinging, bleeding), headache, upset stomach (nausea, vomiting), and diarrhea. Rare side effects include infection (evidenced by, e.g., fever, sore throat, and cough), vision problems, severe swelling, hoarse voice, and difficulty breathing or swallowing.[11]

    Inhaled

    Common side effects may include upper respiratory tract infection, throat irritation, thrush, cough, and headache. Rare side effects include bruising, swelling of the face/neck, depression, tiredness, and shortness of breath.[12]

    Pharmacology

    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 (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.

    Interactions

    Fluticasone propionate is broken down by CYP3A4 (Cytochrome P450 3A4), and has been shown to interact with strong CYP3A4 inhibitors such as ritonavir and ketoconazole.[8][9]

    Ritonavir is a common drug used in the treatment of HIV. Coadministration of ritonavir and fluticasone may lead to increased levels of fluticasone in the body, which may lead to Cushing’s Syndrome and adrenal insufficiency.[13]

    Ketoconazole, an antifungal drug, has also been shown to increase fluticasone concentration leading to systemic corticosteroid side effects.[8][9]

    References
    1. "Fluticasone Propionate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 27 February 2019.
    2. "Fluticasone Propionate eent Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 27 February 2019.
    3. British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 262, 1172. ISBN 9780857113382.
    4. "Flixonase aqueous spray" (PDF).
    5. Fischer, János; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 487. ISBN 9783527607495.
    6. "NADAC as of 2018-12-19". Centers for Medicare and Medicaid Services. Retrieved 22 December 2018.
    7. "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
    8. Flonase [package insert]. Research Triangle Park, NC: GlaxoSmithKline; 2003.
    9. Flovent [package insert]. Research Triangle Park, NC: GlaxoSmithKline; 2014.
    10. "Prednisone and other corticosteroids: Balance the risks and benefits". Retrieved 4 March 2018.
    11. AHFS Consumer Medication Information [Internet]. Bethesda (MD): American Society of Health-System Pharmacists, Inc.; ©2008. Fluticasone Nasal Spray; [revised 2010 Sept 1; reviewed 2010 Sept 1; cited 2014 Nov 2]; [about 1 p.]. Available from: https://www.nlm.nih.gov/medlineplus/druginfo/meds/a695002.html
    12. AHFS Consumer Medication Information [Internet]. Bethesda (MD): American Society of Health-System Pharmacists, Inc.; ©2008. Fluticasone Oral Inhalation; [revised 2010 Sept 1; reviewed 2010 Sept 1; cited 2014 Nov 2]; [about 1 p.]. Available from: https://www.nlm.nih.gov/medlineplus/druginfo/meds/a601056.html
    13. Foisy, M., Yakiwchuk, E., Chiu, I. and Singh, A. (2008). "Adrenal suppression and Cushing's syndrome secondary to an interaction between ritonavir and fluticasone: a review of the literature". HIV Medicine, 9: 389–396. {{doi:|10.1111/j.1468-1293.2008.00579.x}}.
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