Diosmin: Benefits, Dosage, Contraindications
Other name(s)
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Scientific name(s)
Diosmin
Family or group:
Phytosubstances
Indications
Rating methodology
EFSA approval.
Venous Insufficiency ✪✪✪✪✪
Numerous clinical studies support the efficacy of diosmin, alone or in combination, to improve symptoms of chronic venous insufficiency. The most studied product, Daflon 500 mg, combines 450 mg of micronized diosmin and 50 mg of other flavonoids, mainly hesperidin. Taken at a dosage of 2 to 3 tablets per day for 2 to 6 months, it significantly reduces pain, heaviness, edema, and cramps compared to placebo or baseline. In an observational study among patients with advanced chronic venous insufficiency, taking 1000 mg of a Micronized Purified Flavonoid Fraction (MPFF) for 6 months, in addition to compression therapy, reduced symptoms (edema, varicose veins, pain) and subcutaneous adipose tissue thickness, although the absence of a comparator group limits these results. Research comparing diosmin alone and in combination with other flavonoids shows that micronized diosmin is more effective than the non-micronized form for symptom reduction. However, in some cases, non-micronized diosmin (Flebodia 600 mg) showed equivalent efficacy to Daflon 1000 mg. Overall, diosmin is a treatment of choice in chronic venous insufficiency, particularly in micronized formulation.
Posologie
Oral
450 - 1000 mg
Micronized Purified Flavonoid Fraction
Synergies
Clinical Efficacy of Conservative Treatment with Micronized Purified Flavonoid Fraction in Female Patients with Pelvic Congestion Syndrome
Micronized purified flavonoid fraction-based conservative treatment of chronic venous disease in a real-world setting
Analysis of the effects of micronized purified flavonoid fraction versus placebo on symptoms and quality of life in patients suffering from chronic venous disease: from a prospective randomized trial
MPFF 1000 mg chewable once daily vs. MPFF 500 mg twice daily in chronic venous disease: the double-blind, randomized, non-inferiority CHEWY trial
Is Nonmicronized Diosmin 600 mg as Effective as Micronized Diosmin 900 mg plus Hesperidin 100 mg on Chronic Venous Disease Symptoms? Results of a Noninferiority Study
Efficacy of a Low-Dose Diosmin Therapy on Improving Symptoms and Quality of Life in Patients with Chronic Venous Disease: Randomized, Double-Blind, Placebo-Controlled Trial
Hemorrhoids ✪✪✪✪✪
Clinical studies and a meta-analysis confirm the efficacy of Micronized Purified Flavonoid Fraction (MPFF) containing 450 mg of diosmin and 50 mg of flavonoids (Daflon 500) in managing internal hemorrhoids. Taken as three tablets twice a day for 4-5 days, followed by two tablets twice a day for 3 months, this treatment reduces acute bleeding in up to 92% of patients within 4 days and improves symptoms such as pain, anal discomfort, and discharge in just 2 days. Post-operatively, MPFF also accelerates recovery after hemorrhoidopexy or hemorrhoidectomy. A maintenance treatment with one tablet twice a day for 2-3 months reduces the relapse rate and improves persistent symptoms including pain, itching, edema, and bleeding. A combination of diosmin, troxerutin, and hesperidin showed promising results in acute hemorrhoidal crises. Administered in tapering doses over 43 days, it significantly reduces pain (88% of patients), bleeding (64%), and anal itching (56%) compared to placebo. The protocol includes an initial phase of 3 days with three sachets per day containing diosmin 300 mg, troxerutin 300 mg, and hesperidin 300 mg, followed by reduced doses over 40 days. Another combination with bulk laxatives, including diosmin 600 mg three times per day for 4 days then 300 mg twice per day for 10 days with psyllium 11 g/day, modestly improves symptoms after 4 days, although it is less effective than MPFF.
Posologie
Oral
300 mg
Micronized Purified Flavonoid Fraction
Double-blind, placebo-controlled evaluation of clinical activity and safety of Daflon 500 mg in the treatment of acute hemorrhoids
Micronized Purified Flavonoid Fraction in Hemorrhoid Disease: A Systematic Review and Meta-Analysis
Micronized flavonoid therapy in internal hemorrhoids of pregnancy
Flavonoids mixture (diosmin, troxerutin, hesperidin) in the treatment of acute hemorrhoidal disease: a prospective, randomized, triple-blind, controlled trial
Leg Ulcers ✪✪✪✪✪
Venous leg ulcers result from chronic venous insufficiency, where blood reflux and venous hypertension damage skin tissues, causing painful open lesions. These ulcers, often located on the lower leg, are difficult to heal without appropriate treatment. Clinical studies show that taking two tablets daily of a Micronized Purified Flavonoid Fraction (MPFF, Daflon 500) containing 450 mg of diosmin and 50 mg of other flavonoids, in addition to a compression bandage, doubles the number of patients achieving complete healing of ulcers measuring up to 10 cm in diameter, compared to a placebo. Moreover, the healing time is significantly reduced. However, this combination has not shown significant effects on ulcers larger than 10 cm in terms of surface reduction, symptoms, or healing rate.
Posologie
Oral route
450 mg
Micronized Purified Flavonoid Fraction
Efficacy of Daflon 500 mg in venous leg ulcer healing: a double-blind, randomized, controlled versus placebo trial in 107 patients
Benefit of a 2-month treatment with a micronized, purified flavonoidic fraction on venous ulcer healing. A randomized, double-blind, controlled versus placebo trial
Venous Thromboses ✪✪✪✪✪
In a clinical study, adding 600 mg of diosmin daily to rivaroxaban and compression stockings for 12 months significantly reduced the incidence of post-thrombotic syndrome in patients with femoropopliteal deep vein thrombosis (DVT) compared to standard treatment alone. Diosmin also accelerated venous recanalization and slowed the progression of chronic venous disease, while improving the quality of life of patients, measured by the CIVIQ-20 score.
Posologie
Oral route
600 mg
Micronized Purified Flavonoid Fraction
Properties
Venotonic
Diosmin improves vascular health by strengthening venous tone and reducing blood stasis. It acts by increasing intracellular cAMP levels through phosphodiesterase inhibition, which reduces the production of inflammatory prostaglandins (PGE2, PGF2) and thromboxanes (A2, B2). It also decreases the expression of endothelial adhesion molecules, reducing neutrophil infiltration and free radical formation. In a clinical study on patients with chronic venous insufficiency, the administration of diosmin (Daflon 500 mg) for 60 days significantly reduced symptoms like edema and pain, while improving capillary permeability and lymphatic drainage. These anti-inflammatory and pro-angiogenic effects also promote the healing of venous ulcers.
Usages associés
Anti-inflammatory
Diosmin reduces inflammation by modulating pro-inflammatory mediators and limiting oxidative damage. It inhibits phosphodiesterase, increasing intracellular cAMP levels, which decreases the production of prostaglandins (PGE2, PGF2) and thromboxanes (A2, B2).
Hepatoprotective
Diosmin and its metabolite, diosmetin, exhibit promising hepatoprotective properties. Diosmetin acts as a direct antioxidant, increasing glutathione (GSH) levels and reducing lipid peroxidation, thus limiting liver damage. Preclinical studies have shown that diosmin protects the liver against the toxic effects of heavy metals like cadmium and lead. It mitigates hepatic lesions by reducing inflammation and oxidative stress induced by these substances. These mechanisms include a decrease in pro-inflammatory cytokines and an improvement in antioxidant markers such as superoxide dismutase (SOD) and glutathione.
Safety dosage
Adult: 450 mg - 1350 mg (Micronized Purified Flavonoid Fraction)
Diosmin is generally used alone or in combination with other flavonoids, at doses of 450 to 1350 mg per day for 1 to 6 months, depending on the indication.
Interactions
Médicaments
Diclofenac: moderate interaction
Diosmin may increase the blood levels and clinical effects of diclofenac by inhibiting its metabolism. A human pharmacokinetic study showed that taking diosmin (Venex 500, 500 mg/day) for 9 days before an oral dose of diclofenac 100 mg increased the plasma concentrations of diclofenac while reducing its clearance. This effect is related to inhibition of cytochrome P450 2C9 (CYP2C9), responsible for the metabolism of diclofenac.
Fexofenadine: moderate interaction
Diosmin may increase the blood concentrations and clinical effects of fexofenadine. A human pharmacokinetic study showed that taking diosmin (Venex, 500 mg/day) for 10 days before the oral administration of fexofenadine 120 mg increased the plasma levels by 49% and decreased its apparent oral clearance by 41%. These effects seem related to inhibition of intestinal P-glycoprotein by diosmin, without affecting the kidney or liver. Other pharmacokinetic parameters, such as time to reach maximum plasma concentration and half-life, are not affected.
Carbamazepine: moderate interaction
Diosmin may reduce the therapeutic effects of carbamazepine while increasing the risk of seizures. A human pharmacokinetic study showed that taking diosmin (Venex, 500 mg/day) for 10 days before an oral dose of carbamazepine 200 mg increased plasma concentrations of carbamazepine by 58% while decreasing its clearance by 42%. Additionally, the formation of the active metabolite of carbamazepine was reduced, likely due to inhibition of cytochrome P450 3A4 (CYP3A4) by diosmin.
Precautions
Pregnant women: use with caution
Diosmin is taken during pregnancy at doses up to 900 mg per day, in combination with hesperidin, for a maximum of 30 days. However, its use in the third trimester could be associated with placental insufficiency.
Breastfeeding women: use with caution
During breastfeeding, diosmin does not seem to affect the growth or feeding of infants, but medical advice is recommended before use.
