Nafodil100 mg

Nafodil is a peripheral vasoactive agent used mainly for symptomatic relief of circulatory disorders.

Guideline-supported / established use

• Intermittent claudication due to peripheral arterial disease (PAD): Nafodil is used to improve walking distance in patients with stable, mild-to-moderate intermittent claudication, as an adjunct to standard PAD management (structured exercise therapy, smoking cessation, and cardiovascular risk-factor control), particularly when lifestyle measures alone have not sufficiently improved symptoms. The symptomatic benefit is generally modest, and Nafodil should be presented as a symptom-relief option rather than a disease-modifying or vascular risk-reducing therapy.

Other / regionally-used indications (evidence more limited)

• Cerebrovascular insufficiency: in some markets, Nafodil has been used for symptomatic relief of complaints attributed to cerebral circulatory insufficiency (e.g. dizziness, reduced concentration in the elderly). Evidence for this use is weaker and less consistent than for intermittent claudication, and it is not a universally accepted indication.
• Raynaud's phenomenon / other peripheral circulatory complaints: occasionally used off-label for symptomatic relief in some countries; this is not a well-established, guideline-endorsed indication and should only be considered on a physician's advice.

Nafodil is not a treatment for acute limb ischemia, critical limb ischemia, or established cardiovascular disease, and does not replace revascularization or standard secondary-prevention therapy when these are indicated.

Each capsule/tablet contains Naftidrofuryl Oxalate as the active ingredient, commonly available in strengths such as 100 mg and 200 mg for oral use. Exact strength, dosage form, and inactive ingredients vary by manufacturer and brand; refer to the specific product label for the confirmed composition.

Nafodil is a synthetic peripheral and cerebral vasodilator belonging to the naftidrofuryl class of vasoactive agents. It is used orally for the symptomatic management of circulatory disorders, most notably to improve pain-free and maximum walking distance in people with intermittent claudication caused by peripheral arterial disease.

Nafodil works at the level of the blood vessel wall and tissue metabolism rather than by simple mechanical dilation, and its clinical effect on walking distance, while statistically demonstrated in trials, is generally modest. It is intended to be used alongside, not instead of, standard measures such as supervised exercise and control of cardiovascular risk factors.

Peripheral and cerebral vasodilator — Nafodil belongs to the class of vasoactive agents used in peripheral vascular disease.

Mechanism of action

Naftidrofuryl Oxalate acts as a selective antagonist of 5-hydroxytryptamine type-2 (5-HT2) receptors, with inverse agonist activity at the 5-HT2A receptor subtype found on vascular smooth muscle and platelets. By blocking serotonin-mediated vasoconstriction, Naftidrofuryl Oxalate promotes vasodilation and improves blood flow in affected tissues.

Beyond its vascular effects, Naftidrofuryl Oxalate is also believed to improve cellular oxidative metabolism in ischemic tissue — increasing tissue resistance to hypoxia, improving red blood cell deformability, and mildly reducing platelet aggregation — which together are thought to contribute to improved tissue perfusion and exercise tolerance in intermittent claudication.

Pharmacokinetics

After oral administration, Naftidrofuryl Oxalate is absorbed with variable bioavailability, reaches peak plasma concentration within about 1 hour, is highly protein-bound (~80%), is metabolized in the liver, and has a relatively short elimination half-life (approximately 1–2 hours in healthy adults, prolonged in the elderly), which is why it is typically dosed multiple times per day.

Take Nafodil by mouth, swallowing the capsule/tablet whole with a glass of water. Taking it with or immediately after food may reduce the chance of stomach upset. Take doses at evenly spaced intervals through the day as directed by the prescriber, and do not stop treatment abruptly without medical advice, especially before the response has been assessed.

Documented, clinically significant drug interactions with Nafodil are limited compared with many other vasoactive drugs, but the following should be considered:

• Antiplatelet agents / anticoagulants (e.g. aspirin, clopidogrel, warfarin, DOACs): Nafodil has mild antiplatelet activity; theoretically this could add to bleeding risk when combined with other drugs that affect hemostasis. Use with caution and monitor for signs of bleeding if co-administered.
• Other hepatotoxic drugs: Because rare hepatotoxicity has been reported with Nafodil (see Precautions and Warnings), caution is advised when combining it with other medicines known to affect the liver, and liver function should be monitored if such combinations are necessary.
• Other antihypertensive/vasodilator drugs: Concomitant use may theoretically add to blood-pressure-lowering or vasodilatory effects; clinically significant interactions are not well established, but caution is reasonable in patients on multiple vasoactive agents.

Always inform the physician or pharmacist about all prescription, over-the-counter, and herbal products being used before starting Nafodil.

Most people tolerate Nafodil well. Reported side effects include:

Common

• Nausea, vomiting, epigastric or abdominal discomfort
• Diarrhea or other mild gastrointestinal upset
• Skin rash

Rare but serious

• Hepatotoxicity, including hepatitis and, very rarely, liver failure — see Precautions and Warnings for monitoring advice and warning signs that require immediate medical attention.
• Hypersensitivity reactions (e.g. urticaria, angioedema) — discontinue and seek medical care if these occur.

This is not an exhaustive list. Report any unusual or persistent symptom to a physician.

Pregnancy: Data on the use of Nafodil in pregnant women are limited. As a precaution, Nafodil should be used during pregnancy only if clearly needed and if the potential benefit to the mother justifies the potential risk to the fetus. Consult a physician before use in pregnancy.

Lactation: It is not well established whether Nafodil or its metabolites pass into human breast milk. Because safety data in breastfeeding are limited, Nafodil should be used during breastfeeding only on medical advice, weighing the benefit of treatment against any potential risk to the infant.

Hepatotoxicity (main safety concern)

Rare but serious cases of liver injury, including hepatitis and liver failure, have been reported with Nafodil. Patients should be advised to stop Nafodil and seek prompt medical attention if they notice symptoms suggestive of liver dysfunction, such as jaundice (yellowing of skin/eyes), dark urine, pale stools, unusual fatigue, loss of appetite, nausea, or right upper abdominal pain. Nafodil should not be restarted in a patient who has developed such symptoms while on treatment, and it is contraindicated in severe hepatic impairment (see Contraindications).

Modest and evidence-appropriate expectations

The symptomatic benefit of Nafodil in intermittent claudication is modest; it should be used as an adjunct to, not a substitute for, supervised exercise therapy and control of cardiovascular risk factors (smoking cessation, blood pressure, lipid, and glycemic control). Response should be reassessed periodically (see Duration of Treatment).

Gastrointestinal tolerability

Mild gastrointestinal upset is relatively common; taking Nafodil with food can help reduce this.

Renal and hepatic caution

Use with caution in patients with renal impairment or mild hepatic impairment, with clinical monitoring as appropriate.

Limited specific data exist on Nafodil overdose. In case of a suspected overdose, seek immediate medical attention or contact a poison control center/emergency services rather than attempting home treatment. Expected effects of overdose would generally relate to an extension of known side effects (e.g. gastrointestinal upset, hypotension). Management is supportive and symptomatic, and should be carried out by trained medical personnel; do not induce vomiting or attempt any specific antidote without professional medical guidance.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

• Elderly: Nafodil is commonly used in older adults, who make up much of the population with intermittent claudication; because elimination half-life may be prolonged with age, the lowest effective dose should be used and patients monitored for tolerability.
• Renal impairment: Use with caution; well-established dose-adjustment data are limited, so clinical monitoring is advised.
• Hepatic impairment: Avoid in severe hepatic impairment (contraindicated); use with caution and monitoring in milder impairment (see Precautions and Warnings for hepatotoxicity monitoring).
• Pregnancy and breastfeeding: See Pregnancy and Lactation section.
• Children: Not recommended; safety and efficacy have not been established (see Pediatric Uses).

Treatment with Nafodil for intermittent claudication should be reviewed after approximately 3 to 6 months. If there is no meaningful improvement in walking distance or claudication symptoms by this point, continuation should be reconsidered with the prescribing physician, since ongoing use without benefit is not justified. When used for other indications, duration should follow the prescriber's individualized assessment of ongoing benefit versus risk.

Peripheral vasodilators; 5-HT2 (serotonin) receptor antagonists — Naftidrofuryl Oxalate is classified within this pharmacological group.

Naftidrofuryl Oxalate selectively antagonizes 5-HT2 (serotonin type-2) receptors, particularly the 5-HT2A subtype, on vascular smooth muscle and platelets, reducing serotonin-mediated vasoconstriction and platelet aggregation while improving cellular oxidative metabolism in ischemic tissue — together promoting vasodilation and better tissue perfusion.

The safety and efficacy of Nafodil have not been established in children and adolescents. Nafodil is not recommended for use in the pediatric population, as peripheral arterial disease with intermittent claudication and the other indications for which Nafodil is used are conditions that occur almost exclusively in adults, particularly older adults.