How Diosmin Works
Diosmin works primarily by modulating venous tone, improving lymphatic drainage, and reducing inflammation in the microcirculation, making it effective for treating chronic venous insufficiency and hemorrhoids. 1
Mechanism of Action
Diosmin acts through several complementary mechanisms:
Effects on Venous System
- Enhances venous tone by:
- Prolonging post-synaptic response to norepinephrine (NE)
- Increasing sensitivity of vascular smooth muscle to NE and calcium
- Inhibiting the norepinephrine-degrading enzyme catechol-O-methyltransferase (COMT) 1
Effects on Lymphatic System
- Improves lymphatic drainage by:
- Increasing lymphatic vessel contraction frequency
- Enhancing lymphatic contraction amplitude
- Reducing edema through improved lymphatic flow 1
Anti-inflammatory Effects
- Reduces inflammation by:
Glycocalyx Restoration
- Preserves endothelial glycocalyx integrity which:
- Decreases vascular permeability
- Reduces vessel wall inflammation
- Improves vascular tone 2
Absorption and Bioavailability
After oral administration, diosmin is not directly absorbed but must first be:
- Hydrolyzed in the intestine to its aglycone form, diosmetin
- Diosmetin is then absorbed into systemic circulation
- Some formulations include buffering agents (Alka4-complex) that can enhance bioavailability by up to 9.4 times compared to standard micronized diosmin 3
Clinical Applications
Diosmin is primarily used for:
- Chronic venous insufficiency (CVI) - reduces symptoms like edema, pain, and heaviness in legs
- Hemorrhoids - decreases inflammation and improves venous tone
- Lymphedema - improves lymphatic drainage 4, 5
Dosage Forms
Diosmin is available in various formulations:
- Standard micronized diosmin
- Enhanced bioavailability formulations with buffering agents (e.g., μSmin® Plus)
- Combined with other flavonoids (e.g., hesperidin in Daflon) 3, 4
Potential Risks
While generally well-tolerated, diosmin may:
- Interact with anticoagulants due to its platelet aggregation inhibition properties
- Potentially increase risk of bleeding when combined with warfarin or other anticoagulants 6
- Cause gastrointestinal side effects in some patients
Clinical Evidence of Effectiveness
Research has demonstrated that diosmin:
- Alleviates venous injury in experimental models of venous disease 5
- Shows dose-dependent therapeutic effects on venous stenosis 5
- Reduces inflammatory markers in blood vessels 2
- Improves endothelial function through glycocalyx restoration 2
Understanding diosmin's multifaceted mechanism of action explains its effectiveness in treating venous disorders through its combined venotonic, anti-inflammatory, and lymphatic-enhancing properties.