diosmin

Action and Spectrum

Actions and Spectrum: 

diosmin is a naturally occurring flavonoid compound in citrus fruits like oranges and lemons. It is commonly used as a dietary supplement and medication due to its potential health benefits. diosmin is primarily known for its action on blood vessels and is often used to support vascular health.  

Action: 

• Vasoprotective Action: diosmin has vasoprotective properties, which help protect and strengthen the blood vessel walls.  
• Venotonic Effect: diosmin exhibits venotonic effects, which enhance the contraction of veins, promoting better blood flow. This action aids in reducing the pooling of blood in the lower extremities and helps to alleviate symptoms like leg heaviness, pain, and swelling associated with venous disorders. 
• Anti-Inflammatory Activity: diosmin has anti-inflammatory properties that can help to reduce inflammation in blood vessels.  
• Antioxidant Properties: As a flavonoid, diosmin acts as an antioxidant, neutralizing harmful free radicals in the body. Combating oxidative stress may contribute to overall vascular health and protect blood vessels from damage. 
• Lymphatic Support: diosmin also positively influences the lymphatic system, helping to improve lymphatic drainage. This action is relevant when lymphatic congestion contributes to edema and swelling. 

The Spectrum of Effects: 

Due to its actions on blood vessels and inflammation, diosmin is commonly used in the management of various vascular conditions, including: 

• Chronic Venous Insufficiency (CVI): diosmin is widely used to treat CVI, where blood pools in the veins, leading to symptoms like leg pain, heaviness, and swelling. 
• Varicose Veins: diosmin can help reduce symptoms and improve the appearance of varicose veins by enhancing venous tone and reducing inflammation. 
• Hemorrhoids: diosmin is used in combination with hesperidin to treat hemorrhoids, as it can help reduce swelling and discomfort. 
• Lymphedema: diosmin’s lymphatic support can be beneficial in managing lymphedema, a condition characterized by swelling due to impaired lymphatic drainage. 
• Vascular Protection: The antioxidant properties of diosmin may contribute to overall vascular health and potentially reduce the risk of vascular-related diseases. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Dizziness 

Skin rash 

Muscle pain 

Diarrhea 

Stomach pain 

Hives 

Headaches 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Allergy or Sensitivity: Individuals with a known allergy or sensitivity to diosmin or other flavonoids should avoid its use. Allergic reactions may include itching, rash, hives, swelling, or difficulty breathing. 
• Pregnancy and Breastfeeding: The safety of diosmin during pregnancy and breastfeeding has not been extensively studied. It is generally recommended to avoid using diosmin during these periods unless expressly advised by a healthcare professional. 
• Bleeding Disorders: diosmin may have mild anticoagulant (blood-thinning) effects. People with bleeding disorders or taking medications that affect blood clotting should use diosmin cautiously and under medical supervision. 
• Surgery: If you are scheduled for surgery, it is important to inform your healthcare provider about any diosmin supplementation, as it may interact with anesthesia or other medications used during the procedure. 
• Drug Interactions: diosmin may interact with certain medications, including blood thinners (anticoagulants) and antiplatelet drugs.  
• Liver and Kidney Conditions: People with liver or kidney conditions should use diosmin cautiously and only under medical supervision. Dose adjustments may be necessary in such cases. 
• Children: There is limited information on the safety of diosmin use in children, so it is typically not recommended without proper medical guidance. 
• Gastric Ulcers or Digestive Disorders: diosmin may cause mild gastrointestinal disturbances in some individuals. If you have a history of gastric ulcers or digestive disorders, consult your healthcare provider before using diosmin. 

Caution 

• Dosage and Administration: Follow the recommended dosage and instructions provided by your healthcare professional or as indicated on the product label. Taking excessive diosmin may lead to adverse effects or interactions with other medications. 
• Allergic Reactions: While rare, some individuals may be allergic to diosmin or other flavonoids found in citrus fruits. If you experience itching, rash, hives, swelling, or difficulty breathing. 
• Drug Interactions: diosmin may interact with certain medications, including blood thinners (anticoagulants) and antiplatelet drugs. Inform your healthcare provider about all your medications and supplements before starting diosmin to prevent potential interactions. 
• Bleeding Disorders: diosmin may have mild anticoagulant effects, potentially increasing the risk of bleeding, especially in individuals with bleeding disorders. If you have a bleeding disorder or are taking blood-thinning medications, consult your healthcare provider before using diosmin. 
• Pregnancy and Breastfeeding: The safety of diosmin during pregnancy condition and breastfeeding has not been fully established. It is advisable to avoid diosmin during these periods unless specifically recommended by a healthcare professional. 
• Surgery: If you are scheduled for the surgery, inform your healthcare provider about any diosmin supplementation, as it may interact with anesthesia or other medications used during the procedure. 
• Gastric Sensitivity: Some individuals may experience mild gastrointestinal disturbances, such as stomach upset or nausea when using diosmin. If you have a history of gastric ulcers or digestive disorders, use diosmin cautiously and under medical guidance. 
• Liver and Kidney Conditions: If you have liver or kidney conditions, consult your healthcare provider before using diosmin, as dose adjustments may be necessary. 
• Children: The safety and effectiveness of diosmin in children have not been extensively studied. Therefore, it is generally not recommended for pediatric use without medical guidance. 
• Monitoring and Side Effects: While diosmin is generally considered safe, it’s essential to be aware of any possible side effects and to monitor your response to the supplement.

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Avoid 

Lactation:   

Excreted into human milk: Avoid. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

diosmin, a naturally occurring flavonoid compound found in citrus fruits, exhibits pharmacological actions primarily on the vascular system. Upon oral administration, diosmin is absorbed from the gastrointestinal tract and is converted into its active metabolite, diosmetin, in the body.

diosmin’s main pharmacological effects include vasoprotective and venotonic actions, which strengthen blood vessel walls and improve venous tone, reducing symptoms associated with chronic venous insufficiency and varicose veins.

Additionally, diosmin displays anti-inflammatory and antioxidant properties, mitigating inflammation in blood vessels and protecting them from oxidative damage. Its positive influence on lymphatic drainage is also beneficial in conditions like lymphedema. 

Pharmacodynamics: 

Mechanism of action: The mechanism of action of diosmin is multifaceted and involves various pharmacological effects on the vascular system.  

• Vasoprotective Action: diosmin helps protect the integrity of blood vessel walls. It increases the synthesis and secretion of various substances, such as collagen and elastin, which are crucial components of the blood vessel structure. By enhancing the strength and elasticity of blood vessels, diosmin reduces their permeability and fragility, thereby preventing fluid leakage into the surrounding tissues. 
• Venotonic Effect: diosmin exhibits venotonic properties, which means it enhances the contraction of veins, especially in the lower extremities. This action improves the efficiency of venous blood flow, reducing blood pooling and congestion in the veins. As a result, symptoms associated with chronic venous insufficiency (CVI), such as leg heaviness, pain, and swelling, are alleviated. 
• Anti-Inflammatory Activity: diosmin possesses anti-inflammatory properties, which help reduce inflammation in blood vessels. Chronic venous insufficiency and related conditions involve inflammation of the vein walls, which can exacerbate symptoms. diosmin’s anti-inflammatory action helps mitigate this inflammatory response, relieving symptoms. 
• Antioxidant Properties: As a flavonoid, diosmin acts as an antioxidant, neutralizing harmful free radicals in the body. Oxidative stress can damage blood vessel walls and other tissues, contributing to vascular disorders. diosmin’s antioxidant effects protect blood vessels from such damage and promote overall vascular health. 
• Lymphatic Support: diosmin supports the lymphatic system by improving lymphatic drainage. This action is particularly relevant in conditions where lymphatic congestion contributes to edema and swelling, such as lymphedema. 

Pharmacokinetics: 

Absorption 

diosmin is orally administered as tablets or capsules. Upon ingestion, it is absorbed from the gastrointestinal tract into the bloodstream. The absorption of diosmin is relatively low, with approximately 10-15% of the ingested dose being absorbed. 

Distribution 

Once absorbed, diosmin is distributed throughout the body via the bloodstream. It primarily accumulates in the blood vessels and tissues of the lower extremities, where it exerts its effects on venous health. diosmin’s distribution to target tissues is facilitated by its lipophilic nature, which allows it to pass through cell membranes. 

Metabolism 

diosmin undergoes metabolism in the body, primarily in the liver. It is converted into its active metabolite called diosmetin, which is responsible for most of the pharmacological actions of diosmin. Diosmetin is metabolized into various metabolites, some of which are conjugated with glucuronic acid to facilitate their elimination. 

Elimination and Excretion 

diosmin and its metabolites are eliminated from the body primarily through bile and feces. Some portion of the metabolites may undergo enterohepatic circulation, where they are reabsorbed from the intestines back into the bloodstream and excreted again through the bile. A smaller amount of diosmin and metabolites are also excreted in the urine. 

Adminstartion

Administration: 

Oral administration 

diosmin is available in various forms, including oral tablets and capsules. The administration of diosmin typically involves taking it by mouth.  

• Dosage: The appropriate dosage of diosmin can vary based on the specific product and the condition it is being used to treat. The typical dosage for venous insufficiency and related conditions is usually between 500 mg to 1000 mg daily, divided into two doses. However, always follow the dosage instructions provided by your healthcare professional or as indicated on the product label. 
• Timing: diosmin is commonly taken orally with meals. Taking it with food can improve its absorption and minimize the risk of gastrointestinal discomfort. 
• Swallowing: Swallow the diosmin tablets or capsules whole with a glass of water. Do not crush, chew, or break them unless specifically instructed by your healthcare provider. 
• Duration of Use: The duration of diosmin use will based on the medical condition being treated. It may be used for short-term relief or management of acute symptoms or longer-term chronic condition. Follow the recommended duration of use as advised by your healthcare professional. 
• Consistency: Taking diosmin consistently as prescribed is crucial for optimal results. Missing doses or irregular use may reduce its effectiveness. 
• Special Instructions: If your healthcare provider has given you specific instructions regarding the use of diosmin, such as dose adjustments or timing, follow them carefully. 
• Combination with Hesperidin: In some cases, diosmin may be combined with another flavonoid called hesperidin to enhance its effects. If your diosmin supplement contains hesperidin, follow the dosage instructions accordingly. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: diosmin 

Why do we use diosmin? 

diosmin is a naturally occurring flavonoid compound found in citrus fruits, and it is commonly used for various health purposes.  

• Management of Chronic Venous Insufficiency (CVI): diosmin is widely used to support vascular health and manage symptoms associated with chronic venous insufficiency. It is a condition where blood pools in the veins, leading to symptoms like leg pain, heaviness, swelling, and varicose veins. diosmin helps improve venous tone and reduce inflammation, thereby alleviating these symptoms. 
• Treatment of Hemorrhoids: diosmin, often in combination with another flavonoid called hesperidin, is used to treat hemorrhoids, which are swollen and also inflamed blood vessels in the anal and rectal area. diosmin’s venotonic and anti-inflammatory properties can help reduce hemorrhoidal symptoms, such as pain, itching, and discomfort. 
• Vascular Protection: Due to its antioxidant properties, diosmin may protect blood vessels from oxidative stress and damage caused by free radicals. This potential vascular protection can contribute to overall cardiovascular health. 
• Lymphedema Management: diosmin’s influence on the lymphatic system helps improve lymphatic drainage, making it helpful in managing conditions like lymphedema, characterized by swelling due to impaired lymph flow. 
• Circulatory Health: diosmin is believed to improve microcirculation, which refers to blood flow in the smallest vessels (capillaries). Better microcirculation can benefit various organs and tissues in the body. 
• Venous Ulcers: diosmin’s ability to support vascular health may also help heal venous ulcers and open sores due to poor leg circulation. 
• Sports Injuries: Some studies suggest that diosmin may positively impact sports-related injuries, especially those related to muscle strains and contusions. Its anti-inflammatory properties may aid in the recovery process.