Hesperidin

Usage

• Hesperidin, a bioflavonoid commonly found in citrus fruits, is primarily used to treat symptoms related to chronic venous insufficiency (CVI), such as varicose veins, leg swelling, pain, and restless legs syndrome. It is also used for acute and chronic hemorrhoids. Some studies also support its use for conditions like high blood pressure and metabolic disorders.

• Pharmacological classification: Vascular-protecting agent, Phlebotonic, Antioxidant.

• Mechanism of Action: Hesperidin strengthens blood vessel walls, reduces capillary permeability and fragility, improves venous tone, and exhibits anti-inflammatory and antioxidant properties. It may also have beneficial effects on microcirculation, reducing edema.

Alternate Names

• Hesperidina, Hespéridine, Hesperidin Methyl Chalcone, Trimethylhesperidin-chalcon

• Brand Names: Daflon 500 (in combination with Diosmin)

How It Works

• Pharmacodynamics: Hesperidin and its aglycone metabolite, hesperetin, exert multiple effects on the vascular system, mainly through their antioxidant and anti-inflammatory properties. This leads to improved venous tone, reduced capillary permeability, and microcirculation improvement.

• Pharmacokinetics: Hesperidin is orally absorbed and metabolized by the gut microbiota into hesperetin, which has better bioavailability. Hesperetin is further metabolized into glucuronides and other phenolic acids before being excreted mainly in urine and feces. The half-life is relatively short, with a significant portion excreted within 48 hours.

• Mode of Action: Hesperidin reduces inflammation by inhibiting inflammatory mediators and improves venous tone by modulating vascular smooth muscle function.

• Elimination Pathways: Primarily renal and fecal excretion of metabolites.

Dosage

Standard Dosage

Adults:

• For CVI: 500mg twice daily or 1000mg once daily, taken with meals.
• For acute hemorrhoids: 3000mg daily (in divided doses) for 4 days, followed by 2000mg daily for 3 days.
• For chronic hemorrhoids: 1000mg daily for up to 3 months.

Children:

• Not recommended for children due to insufficient safety data.

Special Cases:

• Elderly Patients: No specific dose adjustments, but monitor for side effects.
• Patients with Renal Impairment: No specific dose adjustments are mentioned in the sources.
• Patients with Hepatic Dysfunction: Exercise caution and adjust the dose based on the patient’s condition.
• Patients with Comorbid Conditions: Caution is advised in patients with bleeding disorders or taking anticoagulants/antiplatelet drugs.

Clinical Use Cases

Dosage recommendations for specific clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations are not mentioned in the sources primarily because Hesperidin is not typically used in these settings.

Dosage Adjustments

Dose adjustments may be necessary in patients with liver dysfunction or taking interacting medications. Adjustments are made based on the patient’s condition, comorbid conditions, and concomitant medications.

Side Effects

Common Side Effects

• Stomach pain, diarrhea, headache, nausea.

Rare but Serious Side Effects

• Allergic reactions, Liver toxicity (rare), Anemia.

Long-Term Effects

Limited data is available on long-term effects beyond 6 months of use.

Adverse Drug Reactions (ADR)

Rare cases of hemolytic anemia and cardiac arrhythmias have been reported.

Contraindications

• Hypersensitivity to hesperidin or any component of the formulation.
• Active bleeding or high risk of hemorrhage.

Drug Interactions

• Anticoagulants/antiplatelet medications: Increased risk of bleeding.
• Antihypertensive medications: May cause additive blood pressure lowering.
• Calcium channel blockers: Potential for additive effects.
• Sedatives: May increase drowsiness.
• CYP450 substrates: May alter the metabolism of certain drugs.
• Felodipine, Nifedipine, Verapamil.

Pregnancy and Breastfeeding

• Possibly safe when taken orally with diosmin, but limited data is available. Consult a healthcare professional for advice.

Drug Profile Summary

• Mechanism of Action: Vascular-protecting, phlebotonic, antioxidant, anti-inflammatory.
• Side Effects: Stomach pain, diarrhea, headache.
• Contraindications: Hypersensitivity, active bleeding.
• Drug Interactions: Anticoagulants, antihypertensives, calcium channel blockers.
• Pregnancy & Breastfeeding: Possibly safe with diosmin, consult a healthcare professional.
• Dosage: See dosage section.
• Monitoring Parameters: Liver function tests, blood pressure.

Popular Combinations

• Diosmin: Commonly combined with hesperidin to enhance efficacy in treating CVI and hemorrhoids.

Precautions

• Pre-existing medical conditions: Use with caution in patients with bleeding disorders, low blood pressure, liver or kidney disease.
• Specific Populations:
  • Pregnant Women: Possibly safe when taken orally with diosmin. Consult a healthcare professional before use.
  • Breastfeeding Mothers: Limited data available, caution advised.
  • Children & Elderly: Not recommended for children. Monitor elderly patients for side effects.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Hesperidin?

A: For CVI in adults, 500mg twice daily or 1000mg once daily with meals. For acute hemorrhoids, 3000mg daily for 4 days, followed by 2000mg daily for 3 days. For chronic hemorrhoids, 1000mg daily for up to 3 months.

Q2: What are the common side effects of Hesperidin?

A: Common side effects include stomach pain, diarrhea, and headache.

Q3: Is Hesperidin safe during pregnancy?

A: Possibly safe when taken orally with diosmin. Consult a doctor before use.

Q4: What are the drug interactions with Hesperidin?

A: Hesperidin can interact with anticoagulants, antihypertensives, calcium channel blockers, and sedatives.

Q5: How does Hesperidin work?

A: Hesperidin strengthens blood vessels, improves venous tone, reduces inflammation, and has antioxidant properties.

Q6: Can Hesperidin be used for other conditions besides CVI and hemorrhoids?

A: Some studies suggest benefits for high blood pressure, metabolic disorders, and other conditions, but more research is needed. Consult with a physician for personalized advice.

Q7: What precautions should be taken before prescribing Hesperidin?

A: Screen for allergies, bleeding disorders, low blood pressure, liver or kidney disease.

Q8: What are the contraindications for Hesperidin?

A: Hypersensitivity to hesperidin and active bleeding.

Q9: What are some brand names for Hesperidin?

A: Daflon 500 (in combination with Diosmin).