Sulbutiamine: Nootropic Benefits, Uses, & Side Effects

Sulbutiamine, a synthetic derivative of thiamine (Vitamin B1), is a remarkable chemical compound with a rich history and a wide array of uses. Also known as Arcalion and Enerion, sulbutiamine was originally developed in Japan as a potent treatment for beriberi disease in the mid-60s.

Sulbutiamine is a fat-soluble thiamine disulfide variant that works as a nootropic by crossing the blood-brain barrier more efficiently than thiamine (b1 vitamin), which enhances neurotransmitter production and improves cognitive performance. 

Today, it’s commonly harnessed as a nootropic supplement due to its potential cognitive benefits.

Whether you’re familiar with this research chemical or have heard about it for the first time, this sulbutiamine review will delve into the fascinating world of this unique thiamine derivative.

We will discuss and its potential role as a nootropic with neuroprotective and antioxidant properties.

What is Sulbutiamine?

Sulbutiamine is a synthetic derivative of thiamine (vitamin B1) that functions as a nootropic compound, which crosses the blood brain barrier (BBB) faster than natural vitamin B1, allowing it to effectively and rapidly raise thiamine levels in the brain for enhanced cognitive function.⁽¹⁾ Sulbutiamine is similar to thiamine and shown potential as a treatment for beriberi, which is a disease caused by a vitamin B1 deficiency.

Other well-known names for sulbutiamine include bisibutiamine, bisibutiaminum, o-isobutyrylthiamine, sulbutiamina, and sulbutiaminum.

Sulbutiamine can also alleviate fatigue and weakness in athletes, allowing them to have higher endurance levels.⁽²⁾ This makes sulbutiamine an excellent nootropic for individuals looking to boost their athletic performance.⁽³⁾

Additionally, thanks to sulbutiamine’s ability to increase thiamine levels effectively, it also has a positive impact on cognitive performance and memory recall.

Overall, if you’re looking to boost your motivation, increase productivity and memory, or need help to beat chronic fatigue, then sulbutiamine is the perfect addition to your wellness routine.

Pros

• Crosses the blood-brain barrier and raises thiamine levels in the brain
• Can treat erectile dysfunction (ED)
• Improves focus and concentration
• Can improve memory formation and learning ability
• Suitable to treat thiamine deficiency
• Perfect nootropic for athletes looking for an edge

Cons

• Some people may need to take higher doses to achieve the desired results
• Banned in most competitive sports

Mechanism of Action

Sulbutiamine is an isobutyryl thiamine disulfide (a synthetic chemical compound that mimics vitamin B1, thiamine). Sulbutiamine is two thiamine molecules bonded together. It’s comparable to benfotiamine, another thiamine derivative with similar effects.

However, the difference between sulbutiamine and benfotiamine is that sulbutiamine is rapidly incorporated into cells and can cross plasma membranes, making it more effective in treating acute peripheral syndromes of thiamine deficiency, such as asthenia.⁽⁴⁾

Sulbutiamine is also well known for its unique mechanism of action that allows the B1 vitamin to cross the blood-brain barrier (BBB) and reach the brain cells faster and in higher concentrations than traditional thiamine.

Sulbutiamine induces an increase in neurotransmitters, such as dopamine and acetylcholine.

By using sulbutiamine to boost acetylcholine (ACh), you may experience improved short-term and long-term term memory, learning, and overall cognition.⁽⁵⁾ Additionally, by increasing levels of dopamine, sulbutiamine improves your ability to focus and give attention, further adding to the cognitive effects of sulbutiamine.

Sulbutiamine is also more bioavailable than thiamine, giving it a number of clinical benefits for your cognitive and physical performance.

In the brain, Sulbutiamine works in two specific ways:

1. Sulbutiamine is a fat-soluble molecule that more easily crosses the blood-brain barrier than thiamine. In your brain, it leads to higher levels of Thiamine Pyrophosphate (TPP). Thiamine Pyrophosphate (TPP) is an essential cofactor for numerous enzymes in the brain, including acetylcholine and dopamine.
2. Sulbutiamine plays a role in creating Pyruvate Dehydrogenase (PDH), an enzyme essential to making acetylcholine (ACH). This leads to better cognitive function and explains how treatment with sulbutiamine improves memory recall and reduces some amnesic effects.
3. Sulbutiamine plays a direct role in the citric acid cycle, providing energy in the form of adenosine triphosphate (ATP) within your mitochondria. This leads to more efficient brain and nervous system function, which can help improve memory, attention, alertness, and focus.
4. Sulbutiamine is also essential for maintaining optimal levels of the neurotransmitters glutamate and gamma-aminobutyric acid (GABA).

It’s important to understand that more research on Sulbutiamine (isobutyryl thiamine disulfide) is needed to understand long-term effects on neurotransmitter levels in the brain.

Benefits of Sulbutiamine

With so many powerful effects, using sulbutiamine appears to be a popular option for both athletes and academics.

To understand this, let’s take a closer look at the potential sulbutiamine benefits available.

Treatment for Major Depressive Episodes

A study from the University of Wales Swansea in the UK looked at thiamine supplementation for mood and cognitive functioning in non-depressed individuals.⁽⁶⁾

People who took 50 mg of thiamine every day for 2 months reported experiencing improved cognitive function with no brain fog, significantly improved mood, and higher energy levels.

Therefore, sulbutiamine (synthetic vitamin b1) may also aid in the resorption of psycho-behavioral inhibition that occurs during major depressive episodes.⁽⁷⁾

Beats Chronic Fatigue

Another randomized, double-blind study of two doses of sulbutiamine (400-600 mg of Sulbutiamine daily) versus placebo looked at treating acute fatigue.⁽⁸⁾ Those who took chronic treatment of sulbutiamine showed less fatigue, improved attention, and greater self-reported vigor than those who took the placebo.

Sulbutiamine in the treatment of diseases related to fatigue and weakness, such as beriberi and asthenia, has also been shown to be effective.⁽²⁾

Overall, evidence supports that sulbutiamine is one of the most powerful nootropics (smart drugs) for increased brain activity and reduced fatigue.

Improves Memory Recall

One study looked at how chronic treatment with sulbutiamine improves long-term memory formation in mice.⁽⁹⁾

The study aimed to test if large doses of sulbutiamine given over a long period would affect memory and central cholinergic activity in a rat brain. Each mouse in the study was given a 300 mg chronic administration of sulbutiamine for 10 days, and the results were promising.

Additionally, there is ongoing research to understand if sulbutiamine reduces some amnesic effects and how doctors can potentially use it to treat Alzheimer’s disease.⁽¹⁰⁾

The findings suggest that treatment with sulbutiamine improves memory formation. This behavioral effect is likely mediated by an increase in hippocampal cholinergic activity.

Improves Athletic Performance

Sulbutiamine use is associated with a reduction in the total score of the Fatigue Impact Scale (FIS) and in subscales assessing physical functioning in multiple sclerosis patients on disease-modifying treatment.⁽¹¹⁾

Additionally, sulbutiamine has been observed to increase levels of thiamine and thiamine phosphate esters in the brain, helping to treat asthenia and chronic fatigue. 

Improves Erectile Dysfunction

Sulbutiamine daily intake has shown to be successful and was used for the treatment of patients with psychogenic (functional) erectile dysfunction.⁽¹²⁾

A study done in Russia took 20 patients with psychogenic erectile dysfunction and gave them Enerion (sulbutiamine) daily. The average value of the international index for erectile function increased from 17.5 points to 24.8 points.

Increases Thiamine Levels in the Brain

Sulbutiamine is known for its ability to increase thiamine levels in the brain. Unlike regular thiamine, sulbutiamine can cross the blood-brain barrier effectively. Once inside the brain, it gets metabolized into two thiamine molecules.

Recent sulbutiamine studies have shown that this compound increases levels of both free and phosphorylated forms of thiamine.

Enhances Neurotransmitter Leves in The Brain

Sulbutiamine enhances neurotransmission levels in the brain – specifically cholinergic, dopaminergic, and glutamatergic transmission – which produces effects including improved memory formation, increased energy levels, reduced fatigue, enhanced mood, and better cognitive function.⁽¹³⁾

Thiamine deficiency leads to lower GABBA levels, and by fixing thiamine levels, sulbutiamine may help rectify low glutamine levels and increase GABBA transmission.⁽¹⁴⁾

Additionally, the possible cholinergic mediation by sulbutiamine may also help support improved memory performance.

Lastly, the sulbutiamine nootropic promotes D1 dopamine receptor activity (the D1 receptors are one of the five types of dopamine receptors in the brain). Enhancement in dopaminergic transmission levels in the brain has been linked to increased motivation and pleasure responses.

Overall, these receptors influence a variety of cognitive processes, including attention, working memory, and decision-making. By promoting activity at these receptors, sulbutiamine may contribute to improved cognitive function in these areas.

Uses of Sulbutiamine

Sulbutiamine, a synthetic derivative of vitamin B1, has numerous applications in the medical field.

Here are some key uses of sulbutiamine to consider:

1. Improving Athletic Performance: Sulbutiamine increases energy levels, thereby improving endurance. This gives it the ability to enhance athletic performance.
2. Improving Cognitive Function: Sulbutiamine has been found to increase hippocampal cholinergic activity, which is associated with memory formation.
3. Treating Thiamine Deficiency: The effect of thiamine deficiency is irritability, loss of appetite, poor memory, insomnia, weight loss, and abdominal discomfort. Sulbutiamine can be transformed into thiamine derivatives in the body, making it an effective treatment for reducing these symptoms.

Sulbutiamine Stacks

Sulbutiamine can be effectively combined with other nootropics to enhance its benefits and create synergistic effects. One particularly popular combination is the sulbutiamine and noopept stack.

Sulbutiamine and Noopept Stack

Combining sulbutiamine with noopept creates a powerful cognitive enhancement stack that addresses multiple aspects of brain function:

• Complementary Mechanisms: While sulbutiamine primarily works by increasing thiamine levels and enhancing dopaminergic and cholinergic transmission, noopept operates through different pathways, including BDNF and NGF stimulation. This complementary action creates a more comprehensive cognitive enhancement effect.
• Recommended Dosages: When stacking these compounds, typical dosages are 200-400mg of sulbutiamine with 10-30mg of noopept daily. It’s advisable to start with lower doses of each and gradually increase as needed.
• Potential Benefits: Users report this specific stack provides enhanced focus, improved memory formation, better mental clarity, and reduced mental fatigue beyond what either supplement can provide alone.
• Safety Considerations: As both compounds affect neurotransmitter systems, start with lower doses to assess tolerance. Some users may experience increased stimulation, so it’s best to take this stack earlier in the day to avoid sleep disruption.

This stack is particularly beneficial for students and professionals requiring extended periods of mental performance and focus.

Where To Buy Sulbutiamine

Sulbutiamine powder (which also goes by two brand names: Arcalion and Enerion) is available over the counter without a prescription.

When looking for where to buy sulbutiamine, it’s important to remember to look at sulbutiamine reviews and customer experiences to gain insights into the best retailers.

Our top pick is Science.bio because of its numerous third-party tested, high-quality nootropics and known reputation as a trustworthy retailer.

It’s important to understand that sulbutiamine is not yet approved by the FDA.

Sulbutiamine is still a research chemical, so it’s vital to stay on the safe side when it comes to finding reliable suppliers.

Sulbutiamine Dosage

The optimal dosage of sulbutiamine varies from person to person. It’s important to consider factors like tolerance level and the effects of long-term use when deciding on your ideal daily dose.

For most people, the recommended sulbutiamine dosage ranges between 200-600 mg per day, which should be split into two doses for optimal absorption and effectiveness, with a morning dose to increase energy and focus and an afternoon dose to maintain these benefits.

• A morning dose helps kickstart your day with increased energy and focus.
• An afternoon dose can help maintain these benefits throughout the day.

It’s wise to start with a lower dose of sulbutiamine. This allows you to assess your tolerance level before gradually increasing the dosage if necessary. Starting low might mean beginning with a 100 mg or 200 mg sulbutiamine dose.

Sulbutiamine Side Effects & Safety

Sulbutiamine, like many other products, has a potential for negative side effects to occur.

It’s important to look at all the information available about reported side effects before people take sulbutiamine. This is especially the case if you have pre-existing medical conditions and known health problems.

Some users of sulbutiamine have reported nausea, irritability, and insomnia after taking this supplement. Additionally, sulbutiamine is a synthetic b vitamin, making it possible for some users to experience an allergic response.

Here are some more considerations:

• Long-Term Use Risks: Regular long-term use of sulbutiamine may lead to tolerance and dependence, leading to withdrawal symptoms when sulbutiamine use is discontinued.
• Medication Interactions: Sulbutiamine may interact with certain medications which could lead to unwanted side effects or reduce medication effectiveness.

Side effects may vary, and it’s essential to stick to medical dose instructions to avoid adverse effects and health concerns.

Managing Sulbutiamine Tolerance

One important consideration when using sulbutiamine regularly is the potential development of tolerance. With continued use, some users find they need higher doses to achieve the same effects they initially experienced.

How Tolerance Develops

Tolerance to sulbutiamine develops relatively quickly with daily use, which typically occurs within 1-2 weeks of consistent supplementation, requiring users to cycle their intake with breaks between usage periods to maintain effectiveness.

Tolerance to sulbutiamine typically begins to develop after 1-2 weeks of continuous use. This occurs primarily due to the downregulation of dopamine receptors in response to the increased dopaminergic activity that sulbutiamine promotes.

Signs of Tolerance

You may be developing tolerance if you notice:

• Diminished cognitive enhancement effects
• Reduced energy and motivation benefits
• Need for higher doses to achieve the same results
• Return of fatigue symptoms despite continued use

Recommended Cycling Protocol

To minimize tolerance development, consider implementing a cycling regimen:

• 2 weeks on, 1 week off is a commonly recommended protocol
• Some users prefer a 5 days on, 2 days off weekly cycle
• During off periods, focus on baseline nutrition including natural B-vitamin sources

Reversing Tolerance

Tolerance to sulbutiamine is generally reversible. After a break of 1-2 weeks, most users report that sensitivity to sulbutiamine’s effects returns to baseline levels. During this period, supporting overall brain health with adequate rest, hydration, and nutrition can help accelerate the reset process.

By implementing a strategic cycling approach, you can maintain sulbutiamine’s effectiveness for longer periods while minimizing the risk of dependence.

User Experiences with Sulbutiamine

While clinical studies provide valuable scientific data, real-world user experiences offer additional insights into sulbutiamine’s effects across different individuals and scenarios.

Cognitive Enhancement

Many users report noticeable improvements in mental clarity and focus within 30-60 minutes after taking sulbutiamine:

“After taking 400mg of sulbutiamine daily for two weeks, I noticed a significant improvement in my ability to concentrate during long study sessions. The mental fatigue I typically experienced after 2-3 hours was substantially reduced.” – Graduate student, age 28

“As someone who works night shifts, I found sulbutiamine helped maintain my mental sharpness during the challenging hours between 2-5 AM when alertness typically plummets. The effect was subtle but consistent.” – Healthcare professional, age 34

Fatigue Reduction

The anti-fatigue effects are among the most consistently reported benefits:

“Having dealt with chronic fatigue for years, sulbutiamine has been a game-changer. At 600mg daily, I experienced a gradual but significant improvement in my energy levels over the course of 3 weeks. Unlike caffeine, there’s no crash or jitters.” – Office worker, age 42

Memory and Learning

Users frequently note improvements in information retention and recall:

“I noticed that information seemed to ‘stick’ better when studying while taking sulbutiamine. Concepts that previously required multiple reviews became clearer after fewer repetitions.” – College student, age 22

Timeframe for Results

User experiences suggest varying timeframes for experiencing benefits:

• Acute effects: Most users report feeling initial effects within 30-60 minutes
• Peak effects: Typically occur 2-3 hours after administration
• Cumulative benefits: Many users report that certain benefits, particularly for memory and fatigue reduction, become more pronounced after 1-2 weeks of consistent use

Comparative Experiences

When compared to other nootropics, users often describe sulbutiamine’s effects as:

• More subtle but longer-lasting than caffeine
• Less stimulating but more mood-enhancing than racetams
• More effective for physical fatigue than most other cognitive enhancers

These real-world experiences complement the clinical research and provide a more complete picture of what new users might expect when adding sulbutiamine to their nootropic regimen.

Summary

In conclusion, sulbutiamine is a thiamine derivative that has been studied for its potential benefits in various areas. Sulbutiamine works as an anti-fatigue nootropic, with the ability to increase levels of thiamine in the body and stimulate increased brain activity.

Sulbutiamine has a unique mechanism of action and a low incidence of reported adverse effects that make it an excellent option for people seeking to optimize their mental and physical performance. This synthetic thiamine derivative is especially beneficial for athletes looking for an effective vitamin b1 (thiamine) treatment to improve energy levels and beat deficiency.

Remember to discuss effective dose instructions and supplementation information with your doctor before you use sulbutiaminein order to get the best results out of this fascinating nootropic.

FAQs

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