Chemistry:Beclometasone

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Beclometasone or beclomethasone, sold under the brand name Vanceril among others, is a steroid medication.[1] It is available as an inhaler, cream, pills, and nasal spray.[2] The inhaled form is used in the long-term management of asthma.[1] The cream may be used for dermatitis and psoriasis.[3] The pills have been used to treat ulcerative colitis.[4] The nasal spray is used to treat allergic rhinitis and nasal polyps.[5]

Common side effects with the inhaled form include respiratory infections, headaches, and throat inflammation.[1] Serious side effects include an increased risk of infection, cataracts, Cushing's syndrome, and severe allergic reactions.[1] Long-term use of the pill form may cause adrenal insufficiency.[4] The pills may also cause mood or personality changes.[4] The inhaled form is generally regarded as safe in pregnancy.[6] Beclometasone is a glucocorticoid.[1]

Beclomethasone, as beclomethasone dipropionate, was first patented in 1962 and used medically in 1972.[7] It was approved for medical use in the United States in 1976.[1] It is a therapeutic alternative on the World Health Organization's List of Essential Medicines.[8] In 2023, it was the 351st most commonly prescribed medication in the United States, with more than 51,000 prescriptions.[9]

Medical uses

Beclometasone is indicated for maintenance treatment of asthma as prophylactic therapy;[10] for the treatment of nasal symptoms associated with seasonal and perennial allergic rhinitis;[11] and the relief of the symptoms of seasonal or perennial allergic and nonallergic (vasomotor) rhinitis.[12]

Side effects

Common side effects with the inhaled form include respiratory infections, headaches, and throat inflammation.[1] Serious side effects include an increased risk of infection, cataracts, Cushing's syndrome, and severe allergic reactions.[1] Long-term use of the pill form may cause adrenal insufficiency.[4] The pills may also cause mood or personality changes.[4] The inhaled form is generally regarded as safe in pregnancy.[6]

Occasionally, it may cause a cough upon inhalation. Deposition on the tongue and throat may promote oral candidiasis, which appears as a white coating, possibly with irritation.[13][14][15]

Nasal corticosteroids may be associated with central serous retinopathy.[16]

Pharmacology

Beclometasone is a glucocorticoid.[1] Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor[17] that is present in almost every vertebrate animal cell. The activated glucocorticoid receptor-glucocorticoid complex up-regulates the expression of anti-inflammatory proteins in the nucleus (a process known as transactivation) and represses the expression of proinflammatory proteins in the cytosol by preventing the translocation of other transcription factors from the cytosol into the nucleus (transrepression).[18]

Society and culture

Names

Beclometasone dipropionate is the international nonproprietary name modified and beclomethasone dipropionate is the United States Adopted Name and former British Approved Name. It is a prodrug of the free form, beclometasone (INN). The prodrug beclometasone is marketed in Norway and Russia.[19][20][21][22][23]

Clenil, Qvar, Cortis are brand names for the inhalers; Beconase, Alanase, Vancenase, Qnasl for the nasal spray or aerosol.

References

  1. 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 1.8 "Beclomethasone Dipropionate". The American Society of Health-System Pharmacists. https://www.drugs.com/monograph/beclomethasone-dipropionate.html. 
  2. "List of products: Beclometasone dipropionate". http://www.mhra.gov.uk/spc-pil/?subsName=BECLOMETASONE%20DIPROPIONATE&pageID=SecondLevel. 
  3. "Beclometasone dipropionate 0.25 mg/g Cream". http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1444971110586.pdf. 
  4. 4.0 4.1 4.2 4.3 4.4 "Clipper". http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1353302219931.pdf. 
  5. "Beclomethasone Dipropionate eent". The American Society of Health-System Pharmacists. https://www.drugs.com/monograph/beclomethasone-dipropionate-eent.html. 
  6. 6.0 6.1 Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. 2015. p. 349. ISBN 9781284057560. 
  7. "Beclomethasone dipropionate". Pharmaceutical Manufacturing Encyclopedia. (3rd ed.). Burlington: Elsevier. 2007. p. 539. ISBN 9780815518563. https://books.google.com/books?id=_J2ti4EkYpkC&pg=PA539. 
  8. The selection and use of essential medicines, 2025: WHO Model List of Essential Medicines, 24th list. Geneva: World Health Organization. 2025. 
  9. "Beclomethasone Drug Usage Statistics, United States, 2014 - 2023". https://clincalc.com/DrugStats/Drugs/Beclomethasone. 
  10. Cite error: Invalid <ref> tag; no text was provided for refs named Qvar Redihaler FDA label
  11. Cite error: Invalid <ref> tag; no text was provided for refs named Qnasl FDA label
  12. Cite error: Invalid <ref> tag; no text was provided for refs named Beconase FDA label
  13. "Beclomethasone dipropionate aerosol and oropharyngeal candidiasis". British Journal of Diseases of the Chest 70 (1): 32–38. January 1976. doi:10.1016/0007-0971(76)90004-8. PMID 1259918. 
  14. "Oropharyngeal candidiasis in patients treated with beclomethasone dipropionate delivered by metered-dose inhaler alone and with Aerochamber". The Journal of Allergy and Clinical Immunology 81 (2): 424–428. February 1988. doi:10.1016/0091-6749(88)90911-6. PMID 3339197. 
  15. "Oral candidiasis associated with inhaled corticosteroid use: comparison of fluticasone and beclomethasone". Annals of Allergy, Asthma & Immunology 90 (6): 646–651. June 2003. doi:10.1016/S1081-1206(10)61870-4. PMID 12839324. 
  16. "Central serous chorioretinopathy associated with inhaled or intranasal corticosteroids". Ophthalmology 104 (10): 1653–1660. October 1997. doi:10.1016/s0161-6420(97)30082-7. PMID 9331207. 
  17. Glucocorticoids: effects, action mechanisms, and therapeutic uses. Hauppauge, N.Y.: Nova Science. 2011. ISBN 978-1617287589. 
  18. "Antiinflammatory action of glucocorticoids--new mechanisms for old drugs". The New England Journal of Medicine 353 (16): 1711–1723. October 2005. doi:10.1056/NEJMra050541. PMID 16236742. 
  19. The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. 14 November 2014. pp. 123–. ISBN 978-1-4757-2085-3. https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA123. 
  20. Index Nominum 2000: International Drug Directory. Taylor & Francis. 2000. pp. 95–. ISBN 978-3-88763-075-1. https://books.google.com/books?id=5GpcTQD_L2oC&pg=PA95. 
  21. Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. 6 December 2012. pp. 46–. ISBN 978-94-011-4439-1. https://books.google.com/books?id=tsjrCAAAQBAJ&pg=PA46. Retrieved 17 March 2019. 
  22. European Drug Index: European Drug Registrations (Fourth ed.). CRC Press. 19 June 1998. pp. 141–. ISBN 978-3-7692-2114-5. https://books.google.com/books?id=2HBPHmclMWIC&pg=PA141. Retrieved 17 March 2019. 
  23. "Beclometasone". https://www.drugs.com/international/beclometasone.html.