Chemistry:Daflon

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Short description: Micronized purified flavonoid fraction

Daflon is an oral micronized purified phlebotonic flavonoid fraction containing 90% diosmin and 10% hesperidin. It is manufactured by Laboratoires Servier and often used to treat or manage disorders of the blood vessels.[1][2] Flavonoids are a type of phytochemical that have been associated with various effects on human health and are a component of many different pharmaceutical, nutraceutical, and cosmetic preparations.[3] Diosmin is a flavone glycoside that is derived from hesperidin. Hesperidin is a flavone that is extracted from citrus fruits.[4]

Vein diseases and hemorrhoids

Daflon is not an FDA-approved medication, and therefore it cannot be advertised for treatment of diseases in the United States. Daflon is under preliminary research for its potential use in treating vein diseases,[5] or hemorrhoids.[6] It is sold as a drug in France ,[7][8] Spain,[9] Malaysia[10][11] and Belgium.

There is moderate certainty evidence for the effectiveness of daflon for slightly reducing oedema compared to placebo in the treatment of chronic venous insufficiency.[12] Little to no differences in quality of life after treatment with Daflon were found and there is low certainty evidence that this class of drugs do not influence ulcer healing.[12] Diosmiplex, a micronized purified flavonoid fraction of daflon, with similar venous insufficiency indication, is sold as a prescription medical food in the US.[13]

Pharmacological activity

Daflon plays a crucial role in the prevention of perivascular edema formation and treatment of venous stasis. This activity can be explained by its antagonist activity against prostaglandin E2 (PgE2) and thromboxane (TxA2) biosynthesis leading to inhibition of inflammatory process. Moreover, it also has a contraction activity on the lymphatic vessels which cause the lymphatic flow maximal.[14]

Dosage

For venous insufficiency, the dosage is 2 tablets of 500mg daily. For acute hemorrhoidal attack, the dosage is 6 tablets daily for 4 days, followed by 4 tablets daily over the next 3 days.[15] For chronic venous disease, the dosage is 2 tablets a day for at least 2 months.[16]

Side effects

Possible side effects include routine gastric disorders and neurovegetative disorders, however, toxicology studies indicate that diosmin is quite safe.[2] Diosmin interacts in an inhibitory manner with some metabolic enzymes so drug-interactions are probable.[2]

References

  1. "Offocial Monograph. Daflon 500: Summary of Product Characteristics". https://www.servier.com.ve/sites/default/files/spc-pil/spc-daflon500.pdf. 
  2. 2.0 2.1 2.2 Gerges, Samar H.; Wahdan, Sara A.; Elsherbiny, Doaa A.; El-Demerdash, Ebtehal (2021-10-23). "Pharmacology of Diosmin, a Citrus Flavone Glycoside: An Updated Review". European Journal of Drug Metabolism and Pharmacokinetics 47 (1): 1–18. doi:10.1007/s13318-021-00731-y. ISSN 2107-0180. PMID 34687440. https://pubmed.ncbi.nlm.nih.gov/34687440. 
  3. Panche, A. N.; Diwan, A. D.; Chandra, S. R. (2016). "Flavonoids: an overview". Journal of Nutritional Science 5: e47. doi:10.1017/jns.2016.41. ISSN 2048-6790. PMID 28620474. 
  4. Gerges, Samar H.; Wahdan, Sara A.; Elsherbiny, Doaa A.; El-Demerdash, Ebtehal (2021-10-23). "Pharmacology of Diosmin, a Citrus Flavone Glycoside: An Updated Review". European Journal of Drug Metabolism and Pharmacokinetics 47 (1): 1–18. doi:10.1007/s13318-021-00731-y. ISSN 2107-0180. PMID 34687440. https://pubmed.ncbi.nlm.nih.gov/34687440. 
  5. Lyseng-Williamson KA, Perry CM (2003). "Micronised purified flavonoid fraction: a review of its use in chronic venous insufficiency, venous ulcers and haemorrhoids". Drugs 63 (1): 71–100. doi:10.2165/00003495-200363010-00005. PMID 12487623. 
  6. Perera, Nirmal; Liolitsa, Danae; Iype, Satheesh; Croxford, Anna; Yassin, Muhammed; Lang, Peter; Ukaegbu, Obioha; van Issum, Christopher (15 August 2012). "Phlebotonics for haemorrhoids". Cochrane Database of Systematic Reviews (8): CD004322. doi:10.1002/14651858.cd004322.pub3. ISSN 1465-1858. PMID 22895941. https://www.cochranelibrary.com/cdsr/doi/10.1002/14651858.CD004322.pub3/full. 
  7. "Daflon - EurekaSanté par Vidal" (in fr-FR). https://eurekasante.vidal.fr/medicaments/vidal-famille/medicament-odaflo01-DAFLON.html. 
  8. "Notice patient - Daflon 500 mg, comprimé pelliculé - Base de données publique des médicaments" (in fr). http://base-donnees-publique.medicaments.gouv.fr/affichageDoc.php?typedoc=N&specid=60491130. 
  9. Spanish medicines agency (in Spanish)
  10. "Drug Formulary". 2011. http://htar.moh.gov.my/images/pdf/bluebookcomplete.pdf. 
  11. Norliza (2011-09-14). "Kehamilan & Perubatan" (in ms-MY). http://www.myhealth.gov.my/kehamilan-a-perubatan/. 
  12. 12.0 12.1 Martinez-Zapata, Maria José; Vernooij, Robin Wm; Simancas-Racines, Daniel; Uriona Tuma, Sonia Maria; Stein, Airton T.; Moreno Carriles, Rosa Maria M.; Vargas, Emilio; Bonfill Cosp, Xavier (November 3, 2020). "Phlebotonics for venous insufficiency". The Cochrane Database of Systematic Reviews 2020 (11): CD003229. doi:10.1002/14651858.CD003229.pub4. ISSN 1469-493X. PMID 33141449. 
  13. Bush, Ronald; Comerota, Anthony; Meissner, Mark; Raffetto, Joseph D.; Hahn, Steven R.; Freeman, Katherine (April 2017). "Recommendations for the medical management of chronic venous disease: The role of Micronized Purified Flavanoid Fraction (MPFF)". Phlebology 32 (1_suppl): 3–19. doi:10.1177/0268355517692221. ISSN 1758-1125. PMID 28211296. 
  14. Labrid, C. (June 1994). "Pharmacologic properties of Daflon 500 mg". Angiology 45 (6 Pt 2): 524–530. ISSN 0003-3197. PMID 8203782. https://pubmed.ncbi.nlm.nih.gov/8203782/. 
  15. "Diosmin Uses, Benefits & Dosage - Drugs.com Herbal Database" (in en). https://www.drugs.com/npp/diosmin.html. 
  16. Publishing, Licorn (2009-11-26). "Benefit of Daflon 500 mg in chronic venous disease-related symptoms" (in en-US). https://www.phlebolymphology.org/benefit-of-daflon-500-mg-in-chronic-venous-disease-related-symptoms/. 

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