Stable Position of Micronized Diosmin in the Treatment of Chronic Venous Insufficiency and Hemorrhoids

Introduction

Diosmin is a flavonoid produced for medical purposes by extracting hesperidin from citrus fruits and subsequently dehydrogenating hesperidin. The European Pharmacopoeia allows certain amounts of other flavonoids in the final product. The unreacted hesperidin constitutes the dominant component (max. 4%), with other flavonoids including isorhoifolin and linarin (max. 3% each), diosmetin (max. 2%), 6-iododiosmin (max. 0.6%), and acetoisoavanillon (max. 0.5%).

Pharmacokinetic Properties of Diosmin

When administered orally, diosmin is converted in the intestines into the active metabolite diosmetin, which has a plasma half-life of 26-43 hours. Hesperidin is similarly metabolized to hesperetin, which has a plasma half-life of approximately 3 hours and a bioavailability of 3.26%. This value is significantly higher for micronized diosmin. Micronization is a technological process that reduces the particle size of the medicinal product in order to increase its solubility and thus intestinal absorption.

Pharmacodynamic and Clinical Effects of Diosmin

The pharmacodynamic effect of diosmin is complex. Studies have demonstrated its positive impact on microcirculation, lymphatic drainage, capillary filtration, fragility, and permeability of the venous wall. In preclinical experiments, it has been shown to significantly influence the increase in the tone of the venous wall, lymphatic drainage, and suppression of the inflammatory response. In addition to its venotonic effect, its antioxidant and anti-inflammatory properties are also important, for example through the inhibition of prostaglandin PGE₂ and thromboxane TxA₂, thereby reducing migration, adhesion, and activation of leukocytes. Plethysmographic parameters have shown a statistically significant and dose-dependent effect of diosmin on reducing venous capacity, distensibility, and emptying time.

Diosmin is indicated for the treatment of chronic venous insufficiency of the lower limbs and acute attacks of hemorrhoidal disease. In chronic venous insufficiency, diosmin has been reported to have a beneficial effect on alleviating the feeling of heavy legs, limb swelling, pain, cramps, and trophic changes including venous ulcers.

Conclusion

Diosmin is defined by the European Pharmacopoeia as a substance with a certain proportion of other flavonoids, whose total amount must not exceed 8.5%. Diosmin represents the dominant active ingredient in terms of its favorable pharmacological properties. Its role in the treatment of chronic venous insufficiency and hemorrhoids remains important even after several decades of use.

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Sources:
1. Slíva J. Diosmin – still an important modality in the treatment of venous insufficiency. Internal Medicine 2019; 65 (7–8): 524–526.
2. European Pharmacopoeia (Ph. Eur.) 8.3 (01/2015): 4297–4298.