Xanthinol Nicotinate
Also known as: Xanthinol Nicotinate, Xantinol Nicotinate, Nicotinic acid xanthinol ester
Overview
Xanthinol Nicotinate is a synthetic compound combining xanthinol (a derivative of theophylline) and nicotinic acid (vitamin B3). It is primarily used to improve peripheral blood flow in conditions like peripheral vascular disease (PVD) and chronic lower limb ischemia. As a vasodilator, it enhances microcirculation and oxygen delivery to tissues. Research suggests potential cognitive benefits, but evidence is limited. It is orally bioavailable and acts through adenosine receptors (via xanthinol) and nicotinic acid receptors. While generally well-tolerated, common side effects include mild gastrointestinal discomfort and flushing. Evidence supporting its use is moderate, consisting mainly of small clinical trials and observational studies. Systematic reviews and meta-analyses are lacking, highlighting the need for more robust research to confirm its efficacy and safety.
Benefits
Xanthinol Nicotinate has demonstrated benefits in improving symptoms of peripheral vascular disease. Studies show that it can relieve claudication pain in a significant percentage of patients (87.9%) and reduce rest pain (49.8%). Additionally, it may improve limb temperature and capillary filling (22.4%). Some research suggests cognitive benefits, specifically improvements in sensory register and short-term memory in healthy adults, although these effects are modest and require further validation. The most substantial evidence supports its use in patients with inoperable peripheral vascular disease or chronic lower limb ischemia, where it can enhance overall well-being and potentially reduce analgesic use. However, the quality of evidence is limited by small sample sizes and observational study designs.
How it works
Xanthinol Nicotinate functions primarily as a vasodilator, enhancing blood flow to peripheral tissues. This effect is likely mediated through a combination of mechanisms. Xanthinol, a theophylline derivative, interacts with adenosine receptors, while nicotinic acid contributes its own vasodilatory properties. By improving microcirculation, Xanthinol Nicotinate increases oxygen delivery to tissues, which is particularly beneficial in conditions such as peripheral vascular disease. The compound primarily affects the cardiovascular system, improving blood flow and oxygenation in peripheral areas. Specific pharmacokinetic data are limited, but it is known to be orally bioavailable.
Side effects
Xanthinol Nicotinate is generally well-tolerated, but it can cause several side effects. Common side effects, affecting more than 5% of users, include mild gastrointestinal discomfort and flushing, the latter due to the nicotinic acid component. Less common side effects (1-5%) are headache and dizziness. Rare side effects (less than 1%) include allergic reactions and hypotension. It may interact with other vasodilators or antihypertensives, potentially leading to additive effects. It is contraindicated in individuals with hypersensitivity to xanthinol or nicotinic acid, as well as those with severe hypotension. Caution is advised in patients with liver or kidney impairment, and there is limited data on its safety during pregnancy or lactation. Long-term safety data are also limited, necessitating careful monitoring during extended use.
Dosage
The minimum effective dose of Xanthinol Nicotinate is around 150 mg per day, but most clinical trials use higher doses. Optimal dosage ranges typically fall between 300 and 900 mg per day, divided into multiple doses. Some studies have used a common regimen of 500 mg three times daily. While doses up to 1,500 mg per day have been used without major adverse effects, the maximum safe dose is not definitively established. It is typically administered in divided doses throughout the day. Xanthinol Nicotinate is available in oral tablet or capsule form, and absorption is generally good without the need for specific cofactors. It is often recommended to take it with meals to minimize gastrointestinal discomfort.
FAQs
What is Xanthinol Nicotinate primarily used for?
It's mainly used for peripheral vascular disease to improve blood flow and alleviate symptoms like claudication. It is not a first-line treatment for cognitive enhancement.
Is Xanthinol Nicotinate safe for long-term use?
It is generally safe for short-term use, but long-term safety data are limited. Consult a healthcare provider for extended use.
How should I take Xanthinol Nicotinate?
It's best taken with meals to reduce gastrointestinal discomfort. Follow your healthcare provider's instructions for dosage and timing.
What results can I expect from taking Xanthinol Nicotinate?
You might see improvement in claudication pain and possibly cognitive function, but effects are modest and not guaranteed. It's not a substitute for lifestyle changes.
Can Xanthinol Nicotinate replace surgery for vascular disease?
No, it is not a substitute for lifestyle changes or surgical interventions in severe vascular disease. Consult with your doctor about appropriate treatments.
Research Sources
- https://pubmed.ncbi.nlm.nih.gov/3936095/ – This double-blind, placebo-controlled study investigated the effects of Xanthinol Nicotinate on cognitive function in 96 healthy adults. The study found that Xanthinol Nicotinate (500 mg t.i.d.) improved sensory register and short-term memory compared to placebo, suggesting potential cognitive benefits.
- https://pubmed.ncbi.nlm.nih.gov/23450533/ – This systematic review of oral vasoactive medications for intermittent claudication found insufficient evidence to draw strong conclusions about Xanthinol Nicotinate. The review cited methodological limitations and heterogeneity in included studies as reasons for the inconclusive findings, highlighting the need for more robust research.
- https://academicmed.org/Uploads/Volume6Issue1/235.%20%5B2543.%20JAMP_Rohin%5D%201187-1190.pdf – This prospective observational study of 350 patients with inoperable peripheral vascular disease found that Xanthinol Nicotinate provided relief of claudication pain in 87.9% of patients. Additionally, 49.8% experienced reduced rest pain, and 22.4% showed improved limb temperature and capillary filling, suggesting benefits for PVD symptoms.
- https://academicmed.org/Uploads/Volume6Issue5/151.%20%5B4072.%20JAMP_Dinesh%5D%20791-793.pdf – This observational study on patients with chronic lower limb ischemia found that Xanthinol Nicotinate improved ankle-brachial pressure index (ABPI) and was beneficial in early-stage disease. The results suggest that Xanthinol Nicotinate may be effective in managing early-stage chronic lower limb ischemia.
- http://www.crd.york.ac.uk/CRDWeb/ShowRecord.asp?ID=12000001441 – This record describes a systematic review of oral vasoactive drugs for intermittent claudication. The review concluded that there was insufficient evidence to support the use of Xanthinol Nicotinate due to methodological limitations and heterogeneity in the included studies.
