Benfotiamine? Benefits, Uses, and More

Benfotiamine is a derivative of thiamine (vitamin B1), whose greater lipid solubility allows it to penetrate much deeper into the nervous tissues. After oral intake, it shows much more bioavailability than the equivalent amount of water-soluble thiamine. Thus, it is a better choice to treat thiamine deficiency than its natural counterpart. 

Thiamine has a role in energy metabolism by degrading the carbon skeleton and sugars. It also activates the immune system and improves neuronal communication. These functions make thiamine an essential nutritional element, and its lower levels result in neurological side effects, cellular oxidative stress, and poor energy metabolism. 

The mechanism of action of Benfotiamine  

Benfotiamine modulates the advanced glycation end products (AGEs) and functions through pathways that are independent of AGEs. The advanced glycation end products are the modified lipids and proteins that are non-enzymatically modified after exposure to sugars, e.g., adipose. These AGEs generate reactive oxygen species, form specific cross-linkages, and bind to specific receptors. 

These AGEs are present in diabetics' vasculature and are involved in the pathogenesis of atherosclerosis. Benfotiamine improves metabolism by inhibiting the AGEs' synthesis, thus lowering metabolic stress. 

Likewise, it regulates various non-AGE pathways, such as glycogen synthase kinase-3β (GSK-3β), vascular endothelial growth factor receptor 2, and nuclear transcription factor kB. It also modulates the mechanisms related to apoptosis, cellular survival, and repair. 

We have detailed the nine health benefits of Benfotiamine in another must-read article. Click here to read it. It details some additional health benefits than this article. 

Benefits and uses of Benfotiamine 

Benfotiamine has several health benefits, and several such benefits are being studied. Some proven health benefits of Benfotiamine are; 

Improvement in diabetic retinopathy  

Benfotiamine is a potential therapy for the prevention of diabetic retinopathy, a pathological and severe complication of diabetes that is linked to a higher risk of mortality and heart disease. 

More glucose concentration in the blood causes the accumulation of triose phosphates, which increases the risk of developing diabetic retinopathy by causing biochemical dysfunction. 

Various preclinical studies in rat models have shown that Benfotiamine helps prevent the accumulation of triose phosphates in people with diabetes, thus inhibiting neuropathy development. 

Reduction of alcohol dependence 

Chronic alcohol intake is linked with a severe deficiency of vitamins and other vital nutrients. The alcohol-associated deficiency of thiamine causes a neurological disease by the progressive loss of peripheral and central white matter. 

Although thiamine therapy is necessary for patients with alcohol-associated CNS damage, Benfotiamine is not yet proven to be effective in crossing the CNS system from the periphery. 

Better cognitive health in Alzheimer's patients 

Various preclinical studies have shown that benfotiamine has beneficial effects on cognitive health in Alzheimer's patients. It reduces amyloid deposition in animal models of Alzheimer's disease. Although these effects have yet to be proven for humans, better results are expected. 

A clinical trial in phase 2 is being undertaken to assess if Benfotiamine halts the cognitive decline in patients with mild to moderate cognitive decline. Better results are expected.

Beneficial effects for smoking  

Smoking is associated with endothelial dysfunction, an early indicator of cardiovascular health risk. This risk is exacerbated by inflammation and oxidative stress. 

Benfotiamine is known to prevent nicotine-induced vascular dysfunction in preclinical rat models. A clinical trial conducted on normal volunteers has shown that short-term treatment using benfotiamine partly restored microvasculature in otherwise healthy smokers. More research is needed on this topic to explore its health effects on smoking better and devise specific suggestions for users. 

Antioxidant Potential  

Benfotiamine has anti-inflammatory and antioxidant properties resulting from leukotriene synthesis and prostaglandins. It reduces oxidative stress by neutralising free radicals. This antioxidant potential reduces inflammation and improves cellular functions, thus avoiding the health damage associated with free radicals. 

Antitumor properties 

In vitro trials have shown that benfotiamine helps prevent leukaemia by parasitosis cell death, a type of programmed cell death that involves vacuole formation in the cytoplasm. A cell culture analysis by scientists at Kanazawa University in Japan published by PLOS ONE in 2015 showed that benfotiamine is a potent agent for people with acute myeloid leukaemia who are eligible to receive standard therapy. 

Benfotiamine has positive and synergetic activity with cytarabine, a chemotherapeutic agent known to eliminate myeloid leukaemia cells. 

Kidney health benefits 

Studies in rat models show that benfotiamine protects the remnant kidney and peritoneal membrane in uremia and peritoneal dialysis. Research published by the Journal of the American Society of Nephrology in 2011 shows that the inclusion of benfotiamine in the diet increases transketolase activity and lowers the expression of advanced glycation end products and related end products. 

A Study published by Frontiers in Neuroscience by Dr Iva Bozic and colleagues (University of Belgrade, Serbia) noted that benfotiamine supplementation helps attenuate antibiotic-linked nephrotoxicity by soothing renal tubular cells' inflammation and oxidative stress. 

Side effects and tolerability of Benfotiamine 

Benfotiamine's multiple health benefits make it helpful in treating a range of medical illnesses. Side effects and severe reactions are very rare. Nevertheless, most of these effects were observed in the pilot preclinical studies on humans. It is well tolerated, and no severe side effects or adverse events have been reported in humans.

Nevertheless, clinical trials on humans are needed to establish the long-term side effects and efficacy in humans. Although long-term side effects are limited, extremely high doses are ill-advised and expose the users to some side effects. The data about its long-term safety is limited at best. 

A tolerability and safety study published by BMJ Open in 2022 noted that the rate of adverse events for its short-term use in healthy young volunteers is similar to that of the placebo group. The highest doses in the study group were 1200 mg daily for ten days. The side effects observed were proteinuria, increased white blood cell (WBC) count, slow heart rate or sinus bradycardia, increased pulse rate & blood pressure, and increased liver enzymes. Safety data is only available for the short term as it is used only in the short term.  

Dosage and safety precautions  

No dosage guidelines are available for its practical and safe use, and it is not recommended for treating any health condition. Most human studies on people with diabetes have used regular doses of up to 300 mg twice daily and doses as high as 900-1200 mg without any severe side effects. Moreover, it doesn't cause toxicity. 

You should consult a healthcare provider for safety precautions and information if you plan to use it. Its safety is currently not established for people taking medications, having specific medical conditions, children, nursing women, and pregnant women. It contains sulphur, and those sensitive to sulphur are not advised to take it. 

Frequently Asked Questions 

Does Benfotiamine help memory? 

In animal models of amyloid formation, it reduces the patients' phosphorylated tau levels and the number of amyloid plaques. It also improves memory and increases the phosphorylation of glycogen synthase kinase, 3-beta & 3-alpha. 

Which time of the day is best to take Benfotiamine? 

Due to its fat-soluble nature, it is recommended to take it with food for better absorption. It helps minimise the gastrointestinal disadvantages that people often experience after taking the supplements on an empty stomach. There are no specific guidelines about the time of the day. 

Does Benfotiamine cause sleepiness? 

Benfotiamine is a potent B vitamin that improves sleep by reducing stress, enhancing neurotransmitter functions, and improving the health of the nervous system. It does make a person sleepy and relaxed, but it is not used to treat insomnia and related sleeping disorders. 

How much Benfotiamine must be taken daily? 

Various dosages of Benfotiamine are recommended for multiple purposes. For diabetic retinopathy, 50-100mg must be taken thrice daily. The daily dose of 150-600mg must not be exceeded without consulting the doctor. Clinical and preclinical studies have used doses as high as 900-1200 mg daily. Consult the doctor for better and safer doses.

Is Benfotiamine safe and effective for liver health? 

Benfotiamine is well tolerated, but due to its long elimination time, it causes accumulation in chronic users. The adverse effects in chronic users include elevated liver enzymes. 

What are the situations that need Benfotiamine? 

Benfotiamine is recommended for those with Alzheimer's disease and chronic nerve pain. However, the chronic use of Benfotiamine for months has potential disadvantages, and it must not be used without consultation. 

How does Benfotiamine differ from vitamin B1? 

Benfotiamine is the synthetic form of B1, which is better absorbed by the body. It also has better fat solubility than thiamine and raises thiamine levels more quickly. 

Summary 

Benfotiamine is a valuable health supplement that quickly increases thiamine levels. It is a water-soluble vitamin that is in the body. It also helps those with Alzheimer's disease and diabetic retinopathy. Nevertheless, more research is needed to understand its benefits and health effects.

Side effects are rare, but they are possible. Most studies have used daily doses of as high as 300-900 mg, and guidelines still need to be developed. Consult the healthcare provider for safety precautions and dosages to determine whether it suits you.

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