Diosmin
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Diosmin
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| Systematic (IUPAC) name | |
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| Identifiers | |
| CAS number | |
| ATC code | C05 |
| PubChem | |
| Chemical data | |
| Formula | C28H32O15 |
| Mol. mass | 608.545 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
Diosmin is a semisynthetic phlebotropic drug, a member of the flavonoid family. It is used with Hesperidin to control internal symptoms of hemorrhoids (piles). It is an oral phlebotropic drug used in the treatment of venous disease, i.e., chronic venous insufficiency (CVI) and hemorrhoidal disease (HD), in acute or chronic hemorrhoids, in place of rubber-band ligation, in combination with fiber supplement, or as an adjuvant therapy to hemorrhoidectomy, in order to reduce secondary bleeding.
Clinical studies have been inconclusive and no review articles on its use in vascular disease have been published.[1][2] It is sold in the U.S as a dietary supplement without U.S. Food and Drug Administration approval.
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[edit] Mechanisms
Diosmin prolongs the vasoconstrictor effect of noradrenaline on the vein wall, increasing venous tone, and therefore reducing venous capacitance, distensibility, and stasis. This increases the venous return and reduces venous hyperpressure present in patients suffering from CVI.
Diosmin improves lymphatic drainage by increasing the frequency and intensity of lymphatic contractions, and by increasing the total number of functional lymphatic capillaries. Furthermore, Diosmin (with Hesperidine ) decreases the diameter of lymphatic capillaries and the intralymphatic pressure.
At the microcirculation level, Diosmin reduces capillary hyperpermeability and increases capillary resistance by protecting the microcirculation from damaging processes.
Diosmin reduces the expression of endothelial adhesion molecules (ICAM1, VCAM1), and inhibits the adhesion, migration, and activation of leukocytes at the capillary level. This leads to a reduction in the release of inflammatory mediators, principally oxygen free radicals and prostaglandins (PGE2, PGF2a).
[edit] Regulatory status
Diosmin is distributed in the U.S. by Nutratech, Inc. as a dietary supplement. The U.S. Food and Drug Administration does not approve dietary supplements, and cannot prevent a supplement from being marketed until there is strong evidence of harm. In response to Nutratech's premarket notification, the FDA concluded that there was an "inadequate basis for reasonable expectation of safety."[3] Nutratech argued that Diosmin has a long history of use in Europe.
Diosmin 95 is currently a prescription medication in Europe that has been used to treat Varicose and Spider veins. In May of 2006, Stragen International submitted an NDI with the FDA to market Diosmin 95 as a nutritional supplement. The NDI was approved and Diosmin 95 is now available exclusively through the Venacura brand daily supplement. (http://www.fda.gov/ohrms/dockets/dockets/95s0316/95s-0316-rpt0293-01-vol228.pdf)
[edit] References
- ^ Rozhl Chir. 2005 Aug;84(8):410-2, 414-6. [Analysis of surgical procedures on the vena saphena magna in the Czech Republic and an effect of Detralex during its stripping] [PMID 16218350]
- ^ Eur J Vasc Endovasc Surg. 2002 Jan;23(1):73-6. A randomised controlled trial of micronised purified flavonoid fraction vs placebo in patients with chronic venous disease. Danielsson G, Jungbeck C, Peterson K, Norgren L. [PMID 11748952]
- ^ New Dietary Ingredients in Dietary Supplements, U. S. Food and Drug Administration Center for Food Safety and Applied Nutrition Office of Nutritional Products, Labeling, and Dietary Supplements February 2001 (Updated September 10, 2001) [1], Memorandum [2]
[edit] External links
http://www.fda.gov/ohrms/dockets/dockets/95s0316/95s-0316-rpt0293-01-vol228.pdf www.venacura.com
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