Usage
- Diosmin is primarily prescribed for the treatment of chronic venous insufficiency (CVI) and acute hemorrhoidal attacks. CVI is a condition affecting the veins in the legs, causing symptoms such as swelling, pain, leg heaviness, and cramps. Hemorrhoids are swollen veins in the anus and rectum that can cause pain, itching, and bleeding.
- Pharmacological classification: Phlebotonic, Vasoprotective. Phlebotonics are agents that improve venous tone, while vasoprotectives protect blood vessels.
- Mechanism of action: Diosmin increases venous tone and reduces venous capacitance and distensibility, thereby improving venous return. It also improves lymphatic drainage, reduces capillary permeability and fragility, and exhibits anti-inflammatory effects.
Alternate Names
- Diosmine
- Brand names: Daflon 500, Detralex, DiosVein, Diosmed.
How It Works
- Pharmacodynamics: Diosmin enhances venous tone by increasing the frequency and reducing the duration of venous contractions, leading to improved venous return. It decreases capillary permeability and fragility, thereby reducing edema formation. It also possesses anti-inflammatory properties by inhibiting the production of inflammatory mediators.
- Pharmacokinetics: Diosmin is generally administered orally, often in combination with hesperidin (micronized purified flavonoid fraction, or MPFF). Following oral ingestion, diosmin is rapidly absorbed and extensively metabolized in the body. The primary metabolic pathway involves deglycosylation to diosmetin, which is further degraded to phenolic acids. These metabolites are eliminated in urine and feces. The predominant metabolite is 3-hydroxy-phenylpropionic acid, primarily excreted in its conjugated form. Elimination of diosmin is relatively rapid.
- Mode of action at the cellular level: Diosmin acts on the venous smooth muscle cells and endothelial cells, enhancing their function and contributing to improved venous tone and reduced capillary permeability.
- Receptor binding/enzyme inhibition: The precise molecular mechanisms underlying the actions of diosmin are not fully elucidated.
Dosage
Standard Dosage
Adults:
- Chronic Venous Insufficiency: 1000 mg daily (either as 500 mg twice daily or 1000 mg once daily) with meals.
- Acute Hemorrhoidal Attack: Initially, 3000 mg daily (divided into two or three doses) with meals for 4 days, followed by 2000 mg daily (divided into two doses) with meals for 3 days.
Children:
- The safety and efficacy of diosmin have not been established in children and adolescents under 18 years old. Use is not recommended.
Special Cases:
- Elderly Patients: No specific dosage adjustments are typically required. However, start with the lowest effective dose and monitor for side effects.
- Patients with Renal Impairment: No specific dosage adjustments are recommended, but monitor patients closely.
- Patients with Hepatic Dysfunction: No specific dosage adjustments are recommended, but monitor patients closely.
- Patients with Comorbid Conditions: Use cautiously in patients with bleeding disorders, as diosmin may slow blood clotting.
Clinical Use Cases
Diosmin is primarily used for CVI and hemorrhoidal attacks. It is not typically used in the context of intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
- Dosage adjustments may be necessary for patients with renal or hepatic impairment, bleeding disorders, and concomitant use of anticoagulant or antiplatelet medications.
Side Effects
Common Side Effects
- Stomach pain
- Diarrhea
- Headache
- Dizziness
- Skin rash, hives
- Muscle pain
Rare but Serious Side Effects
Long-Term Effects
- No significant long-term effects have been reported with diosmin use for up to 6 months. However, prolonged use beyond this period should be under medical supervision.
Adverse Drug Reactions (ADR)
- Severe allergic reactions (angioedema, anaphylaxis) are rare but require immediate medical attention.
Contraindications
- Hypersensitivity to diosmin or any component of the formulation.
- Severe bleeding disorders.
Drug Interactions
- Anticoagulants/Antiplatelet drugs: Diosmin may enhance the effects of these medications, increasing the risk of bleeding and bruising.
- Antihistamines (e.g., fexofenadine): Diosmin may increase the absorption of certain antihistamines.
- Anticonvulsants (e.g., carbamazepine, phenytoin): Diosmin may decrease the metabolism of these medications.
- Muscle Relaxants (e.g., chlorzoxazone): Diosmin may decrease the metabolism of certain muscle relaxants.
- Herbal supplements (e.g., garlic, ginger, ginkgo, ginseng, turmeric, fenugreek, feverfew): These supplements may interact with diosmin’s blood-thinning properties.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: There is insufficient data to determine the safety of diosmin during pregnancy. Avoid use.
- Diosmin excretion in breast milk is unknown. Avoid use during breastfeeding.
Drug Profile Summary
- Mechanism of Action: Increases venous tone, reduces capillary permeability and fragility, exhibits anti-inflammatory properties.
- Side Effects: Common: stomach pain, diarrhea, headache, dizziness, skin rash. Serious (rare): irregular heartbeat, angioedema.
- Contraindications: Hypersensitivity, severe bleeding disorders.
- Drug Interactions: Anticoagulants/antiplatelet drugs, certain antihistamines, anticonvulsants, muscle relaxants, some herbal supplements.
- Pregnancy & Breastfeeding: Not recommended.
- Dosage: CVI: 1000 mg daily; Hemorrhoids: Initially 3000 mg daily for 4 days, then 2000 mg daily for 3 days.
- Monitoring Parameters: Monitor for signs of bleeding, allergic reactions, and liver function tests for long-term use.
Popular Combinations
- Diosmin is frequently combined with hesperidin, a flavonoid with synergistic effects in improving venous tone and reducing capillary permeability.
Precautions
- General Precautions: Screen patients for bleeding disorders, allergies, and liver or kidney disease before initiating therapy.
- Specific Populations: Avoid use in pregnancy and breastfeeding. Use with caution in elderly patients and those with renal or hepatic impairment.
- Lifestyle Considerations: Encourage patients with CVI to adopt a healthy lifestyle, including regular exercise, weight management, and avoiding prolonged standing or sitting.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diosmin?
A: For CVI: 1000 mg daily (500 mg twice daily or 1000 mg once daily). For acute hemorrhoids: 3000 mg daily for 4 days, then 2000 mg daily for 3 days.
Q2: Is Diosmin safe to use during pregnancy or breastfeeding?
A: No, it is not recommended due to limited safety data.
Q3: What are the common side effects of Diosmin?
A: The most common side effects are gastrointestinal (stomach pain, diarrhea) and headache.
Q4: Can Diosmin interact with other medications?
A: Yes, it can interact with anticoagulants/antiplatelet drugs, some antihistamines, anticonvulsants, muscle relaxants, and certain herbal supplements.
Q5: How long can I take Diosmin?
A: For CVI, treatment typically lasts 2-6 months. For acute hemorrhoids, the course is generally 7 days. Long-term use should be under medical supervision.
Q6: Are there any contraindications to Diosmin use?
A: Yes, contraindications include hypersensitivity to diosmin and severe bleeding disorders.
Q7: What is the mechanism of action of Diosmin?
A: Diosmin enhances venous tone, reduces capillary permeability, and exhibits anti-inflammatory properties.
Q8: What is the difference between diosmin and hesperidin?
A: Although they are both flavonoids and are frequently used together, they possess different chemical structures and potentially different pharmacological profiles.
Q9: What should I do if I miss a dose of Diosmin?
A: Take the missed dose as soon as you remember. However, if it’s close to the next dose, skip the missed dose and resume your regular schedule. Do not double the dose to make up for the missed one.
Q10: Does diet affect the effectiveness of Diosmin?
A: Taking diosmin with food is recommended to improve its absorption and reduce the risk of gastrointestinal upset. A balanced diet can support overall vascular health.
