naftidrofuryl

Action and Spectrum

Actions and Spectrum: 

naftidrofuryl is a medication primarily used in the treatment of peripheral vascular diseases, particularly intermittent claudication, which is a condition characterized by pain and cramping in the legs during physical activity due to reduced blood flow to the muscles. naftidrofuryl is classified as a vasodilator, which means it works by dilating (widening) blood vessels, thereby improving blood flow to affected areas.  

Action: 

Vasodilation: naftidrofuryl primarily acts as a vasodilator, which means it relaxes and also widens the blood vessels. This action helps increase blood flow to the limbs, particularly the legs, by reducing resistance to blood flow within the vessels. Improved blood circulation can alleviate the symptoms of intermittent claudication. 

Antiplatelet Effects: naftidrofuryl may also have mild antiplatelet effects, which means it can reduce the tendency of blood platelets to clump together and form blood clots. This property can further improve blood flow by preventing clot formation within narrowed blood vessels. 

Spectrum:  

naftidrofuryl is primarily used in the management of intermittent claudication, a condition that results from reduced blood flow to muscles in the legs during physical activity. It can help alleviate the pain and cramping associated with this condition, allowing individuals to engage in more physical activity and improving their overall quality of life. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Nausea 

Vomiting 

Diarrhoea 

Epigastric pain 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity: Individuals who have a known hypersensitivity or allergic reaction to naftidrofuryl or any of its components should not use this medication. 
• Severe Cardiovascular Conditions: naftidrofuryl may affect cardiovascular function. It should be used with caution or avoided in individuals with severe cardiovascular conditions, including: 
• Severe heart failure 
• Unstable angina pectoris 
• Recent myocardial infarction (heart attack) 
• Severe arrhythmias (abnormal heart rhythms) 
• Severe hypertension (high blood pressure) 
• Severe Liver or Kidney Impairment: naftidrofuryl is primarily metabolized in the liver and also excreted through the kidneys. Individuals with severe liver or kidney impairment may require dose adjustments or should avoid using this medication. 
• Pregnancy and Breastfeeding: The safety of naftidrofuryl during pregnancy and breastfeeding is not well-established. It should be used during pregnancy only if the potential benefits outweigh the potential risks, and it should generally be avoided during breastfeeding. 
• Children and Adolescents: naftidrofuryl’s safety and efficacy in children and adolescents have not been well studied, so its use in this population may be limited. 
• Interaction with Monoamine Oxidase Inhibitors (MAOIs): There is a potential for drug interactions between naftidrofuryl and monoamine oxidase inhibitors (MAOIs), a class of antidepressant medications. Concomitant use of naftidrofuryl and MAOIs should be avoided because of risk of hypertensive crisis. 
• Other Specific Conditions: In some cases, naftidrofuryl may need to be used with caution or avoided in individuals with specific medical conditions or a history of certain medical conditions.  

Caution 

• Cardiovascular Conditions: Individuals with underlying cardiovascular conditions, such as coronary artery disease, angina, arrhythmias, or a history of heart attack, should use naftidrofuryl with caution. This medication may have effects on heart function, and close monitoring is advisable in such cases. 
• Blood Pressure: naftidrofuryl may have mild effects on blood pressure. Individuals with uncontrolled hypertension (high blood pressure) should be monitored carefully while taking this medication. Dose adjustments or additional blood pressure management may be necessary. 
• Liver and Kidney Function: naftidrofuryl is metabolized in the liver and excreted by the kidneys. People with impaired liver/kidney function may require dosage adjustments or more frequent monitoring to ensure the drug is processed correctly. 
• Elderly Patients: Elderly individuals may be more sensitive to the effects of naftidrofuryl due to age-related changes in drug metabolism and elimination. Careful monitoring and dosage adjustments may be necessary in older adults. 
• Drug Interactions: naftidrofuryl may interact with other medications. Healthcare providers must review a patient’s medication list to identify potential drug interactions. For example, concomitant use with monoamine oxidase inhibitors (MAOIs) should be avoided due to the risk of hypertensive crisis. 
• Pregnancy and Breastfeeding: The use of naftidrofuryl during pregnancy and breastfeeding should be approached with caution. The safety of this medication in these situations is not well-established, and the potential risks and benefits should be carefully considered. 
• Allergic Reactions: While uncommon, allergic reactions to naftidrofuryl can occur. Individuals who develop signs of an allergic reaction, such as rash, itching, swelling, dizziness, or difficulty breathing, should seek immediate medical attention. 
• Side Effects: naftidrofuryl may cause side effects such as nausea, vomiting, headache, and gastrointestinal discomfort.  
• Children and Adolescents: naftidrofuryl’s safety and efficacy in pediatric populations have not been well-studied, so its use in children and adolescents may be limited. 
• Individual Health Status: The appropriateness of naftidrofuryl may vary depending on an individual’s overall health, medical history, and specific conditions. It should be prescribed by a healthcare professional who can assess these factors. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned. 

Lactation:   

Excreted into human milk: Not known. 

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: 

naftidrofuryl is a vasodilator medication with pharmacological actions centered on improving peripheral blood circulation. It acts by selectively dilating arterial vessels, particularly in the limbs, which helps reduce vascular resistance and increase blood flow to tissues. naftidrofuryl may enhance the release of endothelial nitric oxide, leading to vasodilation.

Additionally, it has mild antiplatelet effects, which reduce platelet aggregation and potentially prevent the formation of blood clots within narrowed blood vessels. These combined actions contribute to its efficacy in managing conditions like intermittent claudication and peripheral arterial disease by relieving symptoms related to impaired blood flow to the extremities. 

Pharmacodynamics: 

Mechanism of action: The exact mechanism of action of naftidrofuryl is not fully understood, but it is thought to exert its therapeutic effects through several pharmacological actions. naftidrofuryl is primarily used in the treatment of peripheral vascular diseases, particularly intermittent claudication, and it is known for its vasodilatory properties.  

• Vasodilation: naftidrofuryl acts as a vasodilator, which means it relaxes and widens blood vessels, particularly the arterial vessels. This vasodilatory effect reduces the resistance to blood flow within the vessels, which can be particularly beneficial in improving circulation to the limbs affected by conditions like intermittent claudication. By increasing blood flow, it helps alleviate the symptoms of reduced blood flow, such as leg pain and cramping during physical activity. 
• Enhancement of Endothelial Function: naftidrofuryl may enhance the function of the endothelium, the inner lining of blood vessels. This enhanced function can lead to the production of nitric oxide, a molecule that further promotes vasodilation. Nitric oxide helps relax the smooth muscle cells in the blood vessel walls. 
• Antiplatelet Effects: naftidrofuryl has mild antiplatelet effects, which means it can reduce the tendency of blood platelets to aggregate and form clots. This property may contribute to the drug’s ability to improve blood flow by preventing clot formation within narrowed blood vessels. 
• Improvement in Hemorheology: naftidrofuryl may also have a beneficial impact on blood rheology, which refers to the flow properties of blood. By reducing blood viscosity and improving its flow characteristics, the drug may help blood circulate more effectively through narrowed vessels. 
• Cellular Effects: Some studies suggest that naftidrofuryl may have direct effects on cellular energy metabolism within tissues, potentially improving cellular function and reducing tissue damage caused by reduced blood flow. 

Pharmacokinetics: 

Absorption 

naftidrofuryl is typically administered orally in the form of tablets or capsules. After oral administration, it is absorbed through the gastrointestinal tract. The absorption process may vary among individuals, and taking it with meals may help reduce gastrointestinal side effects. 

Distribution 

Once absorbed, naftidrofuryl is distributed throughout the body via the bloodstream. It can cross cell membranes and is distributed to various tissues, including those in the limbs, where it exerts its vasodilatory effects. The extent of distribution and tissue-specific concentrations may depend on factors such as the formulation of the drug and individual patient characteristics. 

Metabolism 

naftidrofuryl undergoes hepatic (liver) metabolism, primarily through cytochrome P450 enzymes. The specific metabolic pathways and metabolites involved in the metabolism of naftidrofuryl are not extensively documented in the available literature.  

Elimination and Excretion 

The elimination of naftidrofuryl and its metabolites is primarily through renal (kidney) excretion. Some of the metabolites and the unchanged drug are excreted in urine. The exact excretion pathways and the proportions of metabolites excreted in urine are not well-documented in the literature. 

Adminstartion

Administration: 

naftidrofuryl is typically administered orally in the form of tablets or capsules. The specific dosing instructions for naftidrofuryl may vary depending on the brand, formulation, and the patient’s medical condition.  

• Dosage: The recommended dosage of naftidrofuryl can vary, but it is typically taken two to three times a day. Your healthcare provider will determine the exact dosage and frequency based on your condition and response to the medication. 
• Timing: naftidrofuryl is often taken with meals to reduce the risk of gastrointestinal side effects. Taking it at the same time each day can help maintain consistent blood levels of the medication. 
• Swallow Whole: Swallow the tablets or capsules whole with a glass of water.  
• Compliance: To benefit most from naftidrofuryl, take it regularly as your healthcare provider prescribes. Missing doses or stopping the medication prematurely may reduce its effectiveness. 
• Duration of Treatment: The duration of therapy with naftidrofuryl will depend on your medical condition and response to the medication. Your healthcare provider will generally determine how long you should continue taking it. 
• Follow-Up: Your healthcare provider may schedule follow-up appointments to monitor your progress and assess the effectiveness of naftidrofuryl. Be sure to attend these appointments and report any side effects or concerns. 
• Special Instructions: If you have specific medical conditions/are taking other medications, inform your healthcare provider before starting naftidrofuryl. Some adjustments to your treatment plan may be necessary to ensure safety and efficacy. 
• Overdose: If you suspect an overdose of naftidrofuryl, seek immediate medical attention.

Patient Information Leaflet

Patient information leaflet 

Generic Name: naftidrofuryl 

Why do we use naftidrofuryl? 

naftidrofuryl is a medication with several potential uses, primarily related to improving blood circulation. Its primary and most common use is in the treatment of peripheral vascular diseases, particularly intermittent claudication.  

• Intermittent Claudication: naftidrofuryl is primarily prescribed to individuals with intermittent claudication, a condition characterized by cramping leg pain and discomfort during physical activity due to diminished blood flow to the leg muscles. naftidrofuryl helps improve blood circulation to the affected limbs, which can alleviate the symptoms and allow individuals to engage in more physical activity. 
• Peripheral Arterial Disease (PAD): Peripheral arterial disease is a condition in which blood flow to the extremities, typically the legs, is reduced due to the narrowing of arteries. naftidrofuryl is used to manage the symptoms of PAD, including pain and cramping. 
• Cerebrovascular Disorders: In some cases, naftidrofuryl may be prescribed for the management of cerebrovascular disorders. It can generally improve blood flow to the brain, potentially benefiting individuals with conditions such as vascular dementia and certain types of stroke. However, its use in these conditions may vary depending on the country and medical guidelines. 
• Raynaud’s Disease: naftidrofuryl may be used as part of the treatment for Raynaud’s disease. By promoting vasodilation, naftidrofuryl can help improve blood flow to these extremities.