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Fluticasone propionate

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For other uses, seeFluticasone.

Fluticasone propionate
Clinical data
Trade namesFlovent, Flixotide, Flonase, others
AHFS/Drugs.comMonograph
MedlinePlusa695002
License data
Pregnancy
category
Routes of
administration		Intranasal,[2]inhalation,[3]topical[4]
Drug classSteroids and steroid derivatives
ATC code
Legal status
Legal status
Pharmacokineticdata
Bioavailability0.51% (Intranasal)
Protein binding91%
MetabolismIntranasal
Liver(CYP3A4-mediated)
Eliminationhalf-life10 hours
ExcretionKidney
Identifiers
  • S-(fluoromethyl)-6α,9-difluoro-11β, 17-dihydroxy-16α-methyl-3-oxoandrosta-1, 4-diene-17β-carbothioate, 17-propanoate
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.129.097Edit this at Wikidata
Chemical and physical data
FormulaC25H31F3O5S
Molar mass500.57g·mol−1
3D model (JSmol)
  • CCC(=O)OC1(C(CC2C1(CC(C3(C2CC(C4=CC(=O)C=CC43C)F)F)O)C)C)C(=O)SCF
  • InChI=1S/C25H31F3O5S/c1-5-20(31)33-25(21(32)34-12-26)13(2)8-15-16-10-18(27)17-9-14(29)6-7-22(17,3)24(16,28)19(30)11-23(15,25)4/h6-7,9,13,15-16,18-19,30H,5,8,10-12H2,1-4H3/t13-,15+,16+,18+,19+,22+,23+,24+,25+/m1/s1checkY
  • Key:WMWTYOKRWGGJOA-CENSZEJFSA-NcheckY
(verify)

Fluticasone propionate,sold under the brand namesFloventandFlonaseamong others, is asteroidmedication.[8]When inhaled it is used for the long term management ofasthmaandCOPD.[8]In the nose it is used forhay feverandnasal polyps.[9][10]It can also be used formouth ulcers.[11]It works by decreasinginflammation.

Common side effects when inhaled includeupper respiratory tract infections,sinusitis,thrush,andcough.[8]Common side effects when used in the nose includenosebleedingand sore throat.[9]

Fluticasone propionate was patented in 1980, and approved for medical use in 1990.[12]It is available as ageneric medication.[10]In 2021, fluticasone was the 23rd most commonly prescribed medication in the United States, with more than 25million prescriptions.[13][14]

Medical uses[edit]

Fluticasone propionate is used by powder or aerosolinhalationfor the prophylaxis of asthma.[3][8]Thenasal sprayis used for prevention and treatment ofallergic rhinitis.[2]Nasal drops are used in the treatment ofnasal polyps.The nasal spray can also be used in the mouth formouth ulcers.[11]

Fluticasone propionate in a topical form can be used to treat skin conditions such aseczema,psoriasis,andrashes.[15][16]

Adverse effects[edit]

The nasal spray and oral inhaler formulation have fewer corticosteroid side effects than the tablet formulation because they limit systemic (blood) absorption.[2]However, systemic absorption is not negligible even with correct administration.[2][specify]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.[2][3]These side effects include weakenedimmune system,increased risk ofsystemic infections,osteoporosis,and elevatedpressure in the eyes.[17]

Nasal spray[edit]

Flonase brand 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, for example, fever, sore throat, and cough),vision problems,severe swelling,hoarse voice, anddifficulty breathing or swallowing.[18][9][2]

Inhaled[edit]

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.[19][8][3]

Pharmacology[edit]

Fluticasone propionate is a highly selectiveagonistat theglucocorticoid receptorwith negligible activity atandrogen,estrogen,ormineralocorticoid receptors,[4]thereby producinganti-inflammatoryandvasoconstrictioneffects. It has been shown to have a wide range of inhibitory effects on multiple cell types (e.g.mast cell,eosinophil,neutrophil,macrophages,andlymphocytes) and mediators (e.g.histamine,eicosanoids,leukotrienes,andcytokines) involved ininflammation.Fluticasone propionate is stated to exert a topical effect on the lungs without significant systemic effects at usual doses, due to its low systemicbioavailability.[18]

Interactions[edit]

Fluticasone propionate is broken down byCYP3A4(cytochrome P4503A4), and has been shown to interact with strong CYP3A4 inhibitors such asritonavirandketoconazole.[2][3]Coadministration of ritonavir and fluticasone may lead to increased levels of fluticasone in the body, which may lead toCushing's Syndromeandadrenal insufficiency.[20]Ketoconazole,anantifungal drug,has been shown to increase fluticasone concentration leading to systemic corticosteroid side effects.[2][3]

Society and culture[edit]

In 2024,GSK plcremoved Flovent from the market and replaced it with an authorized generic.[21][22]

References[edit]

  1. ^"Fluticasone Use During Pregnancy".Drugs.com.9 January 2019.Archivedfrom the original on 26 March 2019.Retrieved31 January2020.
  2. ^abcdefgh"Flonase Allergy Relief- fluticasone propionate spray, metered".DailyMed.30 May 2019.Archivedfrom the original on 2 December 2020.Retrieved31 January2020.
  3. ^abcdef"Flovent Diskus- fluticasone propionate powder, metered".DailyMed.7 January 2019.Archivedfrom the original on 7 December 2019.Retrieved31 January2020.
  4. ^abc"Cutivate- fluticasone propionate lotion".DailyMed.8 August 2018.Archivedfrom the original on 20 February 2022.Retrieved19 February2022.
  5. ^"Prescription medicines: registration of new generic medicines and biosimilar medicines, 2017".Therapeutic Goods Administration (TGA).21 June 2022.Retrieved30 March2024.
  6. ^"Respiratory health".Health Canada.9 May 2018.Retrieved13 April2024.
  7. ^"Flixonase Aqueous Nasal Spray - Summary of Product Characteristics (SmPC)".(emc).25 October 2019.Archivedfrom the original on 31 January 2020.Retrieved31 January2020.
  8. ^abcde"Fluticasone Propionate Monograph for Professionals".Drugs.com.American Society of Health-System Pharmacists.Archivedfrom the original on 28 February 2019.Retrieved27 February2019.
  9. ^abc"Fluticasone Propionate eent Monograph for Professionals".Drugs.com.American Society of Health-System Pharmacists.Archivedfrom the original on 28 February 2019.Retrieved27 February2019.
  10. ^abBritish national formulary: BNF 76(76 ed.). Pharmaceutical Press. 2018. pp. 262, 1172.ISBN9780857113382.
  11. ^ab"Flixonase aqueous spray"(PDF).Sheffield Teaching Hospitals.June 2018. Archived fromthe original(PDF)on 25 September 2019.Retrieved31 January2020.
  12. ^Fischer J, Ganellin CR (2006).Analogue-based Drug Discovery.John Wiley & Sons. p. 487.ISBN9783527607495.Archivedfrom the original on 28 November 2023.Retrieved19 September2020.
  13. ^"The Top 300 of 2021".ClinCalc.Archivedfrom the original on 15 January 2024.Retrieved14 January2024.
  14. ^"Fluticasone - Drug Usage Statistics".ClinCalc.Retrieved14 January2024.
  15. ^"Drugs & Medications".www.webmd.com.Archivedfrom the original on 22 October 2020.Retrieved13 April2020.
  16. ^Lax SJ, Harvey J, Axon E, Howells L, Santer M, Ridd MJ, et al. (Cochrane Skin Group) (March 2022)."Strategies for using topical corticosteroids in children and adults with eczema".The Cochrane Database of Systematic Reviews.2022(3): CD013356.doi:10.1002/14651858.CD013356.pub2.PMC8916090.PMID35275399.
  17. ^"Prednisone and other corticosteroids: Balance the risks and benefits".Mayo Clinic.Archivedfrom the original on 25 May 2017.Retrieved4 March2018.
  18. ^ab"Fluticasone Nasal Spray: MedlinePlus Drug Information".MedlinePlus.Archivedfrom the original on 5 September 2023.Retrieved14 October2023.
  19. ^"Fluticasone Oral Inhalation".AHFS Consumer Medication Information [Internet].Bethesda (MD): American Society of Health-System Pharmacists, Inc. 1 September 2010 [2008].Archivedfrom the original on 3 November 2014.Retrieved2 November2014.
  20. ^Foisy MM, Yakiwchuk EM, Chiu I, Singh AE (July 2008). "Adrenal suppression and Cushing's syndrome secondary to an interaction between ritonavir and fluticasone: a review of the literature".HIV Medicine.9(6): 389–96.doi:10.1111/j.1468-1293.2008.00579.x.PMID18459946.S2CID40502127.
  21. ^Sydney Lupkin (30 December 2023)."A popular asthma inhaler is leaving pharmacy shelves. Here's what you need to know".NPR.
  22. ^Tirrell M (28 December 2023)."'A huge shock to the system': Doctors warn about asthma inhaler switch coming in January ".CNN.Retrieved10 January2024.

External links[edit]

Retrieved from "https://en.wikipedia.org/w/index.php?title=Fluticasone_propionate&oldid=1225226489"