Usage
- Diosmin + Hesperidin is prescribed for the treatment of chronic venous insufficiency (CVI), hemorrhoids (piles), and venous leg ulcers. It is also used to alleviate symptoms associated with CVI, such as heavy legs, pain, nocturnal leg cramps, and early morning restless legs.
- Pharmacological classification: Phlebotonic, venoprotective, vasculoprotective, capillary stabilizing agent.
- Mechanism of action: Diosmin + Hesperidin improves venous tone by inhibiting the breakdown of norepinephrine. It also strengthens capillaries and reduces capillary permeability, thereby decreasing microcirculation damage and inflammation.
Alternate Names
- Micronized Purified Flavonoid Fraction (MPFF)
- Brand Names: Daflon 500, Detralex, Diovenor, Barosmin, Flebosten, Litosmil, Venosmine
How It Works
- Pharmacodynamics: Diosmin + Hesperidin enhances venous tone, reduces venous capacitance and distensibility, normalizes capillary permeability and resistance, and increases venous emptying time. It also exhibits anti-inflammatory effects by reducing leukocyte activation and inhibiting the release of inflammatory mediators (free radicals and prostaglandins).
- Pharmacokinetics: Diosmin is metabolized in the intestine to diosmetin, its active aglycone metabolite. Diosmetin is then further degraded into phenolic acids and their glycine conjugates. It’s primarily eliminated through renal excretion (urine), with some elimination through the feces.
- Mode of action: Improves venous tone by inhibiting the breakdown of norepinephrine. Reduces capillary permeability and fragility. Exerts anti-inflammatory actions by decreasing leukocyte activation and inhibiting the release of inflammatory mediators.
- Receptor binding/Enzyme inhibition/Neurotransmitter modulation: Inhibits the breakdown of norepinephrine.
- Elimination pathways: Primarily renal excretion (urine) with some elimination through the feces.
Dosage
Standard Dosage
Adults:
- Chronic Venous Insufficiency: 1000 mg daily, either as two 500 mg doses (one midday and one evening) or a single 1000 mg dose in the morning.
- Acute Hemorrhoidal Attack: Initially, 3000 mg daily (in divided doses) for four days, then 2000 mg daily (in divided doses) for three days, followed by maintenance doses as needed.
Children:
- Not recommended for use in children and adolescents under 18 years old due to insufficient safety and efficacy data.
Special Cases:
- Elderly Patients: No specific dose adjustment is typically required unless there is significant renal or hepatic impairment.
- Patients with Renal Impairment: Dose adjustment may be necessary in severe renal impairment.
- Patients with Hepatic Dysfunction: Use with caution in patients with hepatic impairment.
- Patients with Comorbid Conditions: Caution advised in patients with bleeding disorders. Consult with a physician for patients with comorbidities like diabetes, cardiovascular diseases, or IBD.
Clinical Use Cases
- Intubation: No specific dosage recommendations.
- Surgical Procedures: For preoperative use in cardiac surgery, 3000 mg daily for four days, followed by 1000 mg daily for three days before the surgery.
- Mechanical Ventilation: No specific dosage recommendations.
- Intensive Care Unit (ICU) Use: No specific dosage recommendations.
- Emergency Situations: No specific dosage recommendations.
Dosage Adjustments:
- Dose adjustments may be required based on patient-specific factors, including renal and hepatic function and presence of bleeding disorders.
Side Effects
Common Side Effects:
- Abdominal discomfort
- Nausea
- Vomiting
- Diarrhea or constipation
- Headache
- Dizziness
Rare but Serious Side Effects:
- Angioedema
- Allergic reactions (swollen face/eyes/lips/tongue, difficulty breathing, itchy skin rashes)
- Cardiac arrhythmias (tachycardia)
Long-Term Effects:
- Limited data are available on long-term effects beyond six months of continuous use.
Adverse Drug Reactions (ADR):
- Angioedema
- Allergic reactions
Contraindications
- Hypersensitivity to diosmin, hesperidin, or any component of the formulation.
- Pregnancy and breastfeeding (due to insufficient safety data).
- Active bleeding disorders.
Drug Interactions
- Some cancer drugs (e.g., doxorubicin, vincristine)
- Immunosuppressants (e.g., sirolimus)
- Some heart medications (e.g., digoxin)
- Colchicine (for gout)
- CNS depressants
- Medications metabolized by CYP450 2E1 or 2C9 enzymes or by P-glycoprotein
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Insufficient data available. Avoid use as a precautionary measure.
- Fetal risks: Unknown.
- Breastfeeding: Avoid use due to lack of data.
- Safer alternatives may be available.
Drug Profile Summary
- Mechanism of Action: Enhances venous tone, reduces capillary permeability, exhibits anti-inflammatory properties.
- Side Effects: Common: GI disturbances, headache, dizziness. Rare but serious: angioedema, allergic reactions.
- Contraindications: Hypersensitivity, pregnancy, breastfeeding, bleeding disorders.
- Drug Interactions: Certain cancer drugs, immunosuppressants, heart medications, colchicine, CNS depressants, CYP450 2E1/2C9 substrates/P-glycoprotein substrates.
- Pregnancy & Breastfeeding: Avoid use.
- Dosage: CVI: 1000 mg daily; Acute hemorrhoids: Up to 3000 mg initially, then tapered down.
- Monitoring Parameters: Leg circumference, pain levels, CVI-related symptoms, signs of bleeding.
Popular Combinations
- Often combined with troxerutin (for hemorrhoids).
Precautions
- General Precautions: Evaluate for allergies, bleeding disorders, renal/hepatic impairment before initiating therapy. Monitor for adverse reactions.
- Specific Populations: Pregnant/breastfeeding women: Avoid use. Children/elderly: Not recommended for children under 18. Use with caution in the elderly, especially those with renal/hepatic impairment.
- Lifestyle Considerations: Encourage healthy lifestyle modifications, such as regular exercise, weight management, avoiding prolonged standing/sitting.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diosmin + Hesperidin?
A: For CVI, 1000 mg daily. For acute hemorrhoids, up to 3000 mg daily initially, then tapered.
Q2: What are the common side effects?
A: Common side effects include gastrointestinal upset (nausea, vomiting, diarrhea/constipation), headache, and dizziness.
Q3: Is Diosmin + Hesperidin safe during pregnancy?
A: No. Its use is not recommended during pregnancy or breastfeeding due to lack of safety data.
Q4: How long can a patient take Diosmin + Hesperidin?
A: Treatment duration varies depending on the condition. For CVI, it can be taken for several months. For acute hemorrhoids, treatment is generally shorter. Consult the prescribing information or a healthcare professional for specific recommendations.
Q5: Does Diosmin + Hesperidin interact with any other medications?
A: Yes. It can interact with various medications, including some cancer drugs, immunosuppressants, and heart medications. Consult a doctor or pharmacist to check for potential interactions.
Q6: What is the mechanism of action of Diosmin + Hesperidin?
A: It improves venous tone, reduces capillary permeability and fragility, and has anti-inflammatory effects.
Q7: What conditions is Diosmin + Hesperidin used to treat?
A: Primarily used for chronic venous insufficiency, hemorrhoids, and venous leg ulcers.
Q8: Are there any contraindications for using Diosmin + Hesperidin?
A: Yes. Contraindications include hypersensitivity to the drug, pregnancy, breastfeeding, and active bleeding disorders.
Q9: Can children take Diosmin + Hesperidin?
A: No. It is not recommended for children and adolescents under 18 years old.
