Daflon

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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]

Contents

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]

Related Research Articles

<span class="mw-page-title-main">Hemorrhoid</span> Vascular structures in the anal canal

Hemorrhoids, also known as piles, are vascular structures in the anal canal. In their normal state, they are cushions that help with stool control. They become a disease when swollen or inflamed; the unqualified term hemorrhoid is often used to refer to the disease. The signs and symptoms of hemorrhoids depend on the type present. Internal hemorrhoids often result in painless, bright red rectal bleeding when defecating. External hemorrhoids often result in pain and swelling in the area of the anus. If bleeding occurs, it is usually darker. Symptoms frequently get better after a few days. A skin tag may remain after the healing of an external hemorrhoid.

<span class="mw-page-title-main">Flavonoid</span> Class of plant and fungus secondary metabolites

Flavonoids are a class of polyphenolic secondary metabolites found in plants, and thus commonly consumed in the diets of humans.

<span class="mw-page-title-main">Polyphenol</span> Class of chemical compounds

Polyphenols are a large family of naturally occurring phenols. They are abundant in plants and structurally diverse. Polyphenols include flavonoids, tannic acid, and ellagitannin, some of which have been used historically as dyes and for tanning garments.

<span class="mw-page-title-main">Rutin</span> Chemical compound

Rutin is the glycoside combining the flavonol quercetin and the disaccharide rutinose. It is a flavonoid glycoside found in a wide variety of plants, including citrus.

<span class="mw-page-title-main">Naringin</span> Chemical compound

Naringin is a flavanone-7-O-glycoside between the flavanone naringenin and the disaccharide neohesperidose. The flavonoid naringin occurs naturally in citrus fruits, especially in grapefruit, where naringin is responsible for the fruit's bitter taste. In commercial grapefruit juice production, the enzyme naringinase can be used to remove the bitterness (debittering) created by naringin. In humans naringin is metabolized to the aglycone naringenin by naringinase present in the gut.

<span class="mw-page-title-main">Hesperidin</span> Chemical compound

Hesperidin is a flavanone glycoside found in citrus fruits. Its aglycone is hesperetin. Its name is derived from the word "hesperidium", for fruit produced by citrus trees.

<span class="mw-page-title-main">Hesperetin</span> Chemical compound

Hesperetin is the 4'-methoxy derivative of eriodictyol, a flavanone. Hesperetin's 7-O-glycoside, hesperidin, is a naturally occurring flavanon-glycoside, the main flavonoid in lemons and sweet oranges. Hesperetin are not found to a significant extent in Citrus spp.

<span class="mw-page-title-main">Apigenin</span> Chemical compound

Apigenin (4′,5,7-trihydroxyflavone), found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally occurring glycosides. It is a yellow crystalline solid that has been used to dye wool.

<span class="mw-page-title-main">Diosmin</span> Chemical compound

Diosmin, a flavone glycoside of diosmetin, is manufactured from citrus fruit peels as a phlebotonic non-prescription dietary supplement used to aid treatment of hemorrhoids or chronic venous diseases, mainly of the legs.

<span class="mw-page-title-main">Flavones</span> Class of flavonoid chemical compounds

Flavones are a class of flavonoids based on the backbone of 2-phenylchromen-4-one (2-phenyl-1-benzopyran-4-one).

Sulodexide, traded as Aterina, is a highly purified mixture of glycosaminoglycans composed of heparan sulfate (80%) and dermatan sulfate (20%).

<span class="mw-page-title-main">Hidrosmin</span> Chemical compound

Hidrosmin is a flavone, a type of flavonoid. It is a vasoprotective.

<span class="mw-page-title-main">Calcium dobesilate</span> Chemical compound

Calcium dobesilate is a vasoprotective. It is the calcium salt of dobesilic acid. It is a synthetic molecule with the ability to reduce capillary permeability in the body. In Switzerland the drug is sold by the pharmaceutical company OM Pharma under the trade name of Doxium in capsules containing 500 mg of active ingredient.

<span class="mw-page-title-main">Chronic venous insufficiency</span> Medical condition

Chronic venous insufficiency (CVI) is a medical condition in which blood pools in the veins, straining the walls of the vein. The most common cause of CVI is superficial venous reflux which is a treatable condition. As functional venous valves are required to provide for efficient blood return from the lower extremities, this condition typically affects the legs. If the impaired vein function causes significant symptoms, such as swelling and ulcer formation, it is referred to as chronic venous disease. It is sometimes called chronic peripheral venous insufficiency and should not be confused with post-thrombotic syndrome in which the deep veins have been damaged by previous deep vein thrombosis.

<span class="mw-page-title-main">Apiin</span> Chemical compound

Apiin is a natural flavonoid, a diglycoside of the flavone apigenin found in the winter-hardy plants parsley and celery, and in banana leaf. The glycoside moiety at carbon-7 of apigenin, O-β-D-apiofuranosyl(→)2-β-D-glucosyl, is carried by several other flavones in parsley plant and seed. The sugar apiose possibly play a role in winter hardiness of celery, duckweed and parsley.

<span class="mw-page-title-main">Diosmetin</span> Chemical compound

Diosmetin, also known as 5,7,3′-trihydroxy-4′-methoxyflavone, is an O-methylated flavone, a chemical compound that can be found in the Caucasian vetch.

<span class="mw-page-title-main">Chronic cerebrospinal venous insufficiency controversy</span> Medical condition

Chronic cerebrospinal venous insufficiency is a term invented by Italian researcher Paolo Zamboni in 2008 to describe compromised flow of blood in the veins draining the central nervous system. Zamboni hypothesized that it might play a role in the cause or development of multiple sclerosis (MS). Zamboni also devised a surgical procedure which the media nicknamed a liberation procedure or liberation therapy, involving venoplasty or stenting of certain veins. Zamboni's ideas about CCSVI are very controversial, with significantly more detractors than supporters, and any treatments based on his ideas are considered experimental.

Hydroxyethylrutosides are hydroxyethyl derivatives of rutosides. Examples include:

<span class="mw-page-title-main">Paolo Zamboni</span>

Paolo Zamboni is an Italian doctor and scientist. He is full Professor and Director of the School of Vascular Surgery at the University of Ferrara in Italy.

Venalex is a micronized purified flavonoid fraction containing 90% diosmin and 10% hesperidin.

References

  1. ↑ "Offocial Monograph. Daflon 500: Summary of Product Characteristics" (PDF). www.servier.com.ve. Archived (PDF) from the original on 2016-12-28. Retrieved 2018-12-09.
  2. 1 2 3 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. S2CID   239473375.
  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. PMC   5465813 . 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. S2CID   239473375.
  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. S2CID   46982572.
  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. S2CID   28445593.
  7. ↑ "Daflon - EurekaSanté par Vidal". EurekaSanté (in French). Retrieved 2018-02-17.
  8. ↑ "Notice patient - Daflon 500 mg, comprimé pelliculé - Base de données publique des médicaments". base-donnees-publique.medicaments.gouv.fr (in French). Retrieved 2018-02-17.
  9. ↑ Spanish medicines agency (in Spanish)
  10. ↑ "Drug Formulary" (PDF). Hospital Tengku Ampuan Rahimah. 2011. Archived (PDF) from the original on 2017-05-17.
  11. ↑ Norliza (2011-09-14). "Kehamilan & Perubatan". Portal MyHealth (in Malay). Retrieved 2020-01-17.
  12. 1 2 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. PMC   8094625 . 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. S2CID   24389276.
  14. ↑ Labrid, C. (June 1994). "Pharmacologic properties of Daflon 500 mg". Angiology. 45 (6 Pt 2): 524–530. ISSN   0003-3197. PMID   8203782.
  15. ↑ "Diosmin Uses, Benefits & Dosage - Drugs.com Herbal Database". Drugs.com. Retrieved 2020-01-17.
  16. ↑ Publishing, Licorn (2009-11-26). "Benefit of Daflon 500 mg in chronic venous disease-related symptoms". Servier - Phlebolymphology. Retrieved 2020-01-17.
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