Buflomedil

Buflomedil synthesis

Buflomedil is a vasodilator that has been used in the treatment of peripheral vascular disease, including claudication and other conditions resulting from poor blood circulation to the limbs. It works by improving blood flow, which helps to relieve symptoms such as pain and cramps during exercise in patients suffering from these conditions.

Mechanism of Action

Buflomedil acts primarily by inhibiting the uptake of adenosine, which is a potent vasodilator, leading to increased concentrations of adenosine in the blood and thus causing dilation of the blood vessels. This action helps to improve blood flow to the areas of the body that are not receiving adequate blood supply. Additionally, Buflomedil has been shown to have antiplatelet properties, which further aids in improving circulation.

Indications

Buflomedil is indicated for the treatment of various forms of peripheral arterial disease (PAD), including:

• Intermittent claudication: Pain caused by insufficient blood flow to the muscles during exercise.
• Critical limb ischemia: A severe blockage in the arteries which markedly reduces blood flow to the extremities and can lead to pain and ulcers.

Pharmacokinetics

The pharmacokinetic properties of Buflomedil include rapid absorption from the gastrointestinal tract, with peak plasma concentrations occurring within 1 to 2 hours after oral administration. It is metabolized in the liver and excreted primarily through the kidneys. The half-life of Buflomedil is approximately 2 to 3 hours, which may be prolonged in patients with renal impairment.

Side Effects

While Buflomedil is generally well tolerated, it can cause side effects in some patients. Common adverse effects include:

• Nausea and vomiting
• Headache
• Dizziness
• Palpitations

Serious side effects are rare but may include cardiac arrhythmias and seizures, especially in cases of overdose or in patients with severe renal impairment.

Contraindications

Buflomedil is contraindicated in patients with:

• Hypersensitivity to Buflomedil or any of its components
• Severe renal impairment
• Severe hepatic impairment
• History of seizures

Regulatory Status

The use of Buflomedil has been restricted in some countries due to concerns over its safety profile, particularly the risk of seizures and cardiac arrhythmias in patients with renal impairment. It is important for healthcare providers to carefully assess the risk-benefit ratio of Buflomedil in their patients and to monitor for any adverse effects during treatment.