Sulbutiamine: Review of Nootropic Benefits, Uses, & Side Effects

Updated on February 29, 2024
 by — reviewed by Jason Williams, PhD (Contributor: George Collins / Editor: Yoko Hill)
An abstract representation of the cognitive enhancement and mental clarity associated with Sulbutiamine use.

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 has gained attention for its ability to cross the blood-brain barrier more efficiently than thiamine (b1 vitamin). 

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 man-made molecule that is a derivative of thiamine (vitamin B1). It can cross the blood brain barrier (BBB) faster than the natural vitamin B1 structure, which allows it to effectively and rapidly raise thiamine levels in the brain.(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 – specifically cholinergic, dopaminergic, and glutamatergic transmission.(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.

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, sulbutiamine dosage ranges between 200-600 mg per day. This dosage is usually split into two doses for optimal absorption and effectiveness.

  • 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.

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

How long does sulbutiamine take to work?

Sulbutiamine typically starts working within 30 minutes to 1 hour. Its peak effects are felt around 1.5 to 2 hours after ingestion, although this can vary between individuals.

What is the elimination half-life of sulbutiamine?

Sulbutiamine has a short half life, typically around 5 hours. This means that the concentration of the drug in your body will decrease by half every 5 hours.

Can I stack sulbutiamine with other nootropics?

Yes, sulbutiamine can be stacked with other nootropics. Be sure to research each stack thoroughly and understand the potential interactions and side effects.

How should I store sulbutiamine?

Sulbutiamine should be stored in a cool, dry place out of direct sunlight. It should also be kept out of reach of children.

Is sulbutiamine legal to purchase and use?

The legality of sulbutiamine varies by country. In the U.S., it’s a dietary supplement, so it’s legal to purchase. Always check your local regulations.


Sources, Studies, and Scientific Research
  1. Starling-Soares, Bernardo et al. “Role of the Synthetic B1 Vitamin Sulbutiamine on Health.” Journal of nutrition and metabolism vol. 2020 9349063. 20 Apr. 2020, doi:10.1155/2020/9349063 
  2. Shah, Siddharth N, and Sulbutiamine Study Group. “Adjuvant role of vitamin B analogue (sulbutiamine) with anti-infective treatment in infection associated asthenia.” The Journal of the Association of Physicians of India vol. 51 (2003): 891-5.  
  3. Sobolevsky, Tim, and Grigory Rodchenkov. “Sulbutiamine in sports.” Drug testing and analysis vol. 2,11-12 (2010): 643-6. doi:10.1002/dta.183 
  4. Bykov, Y V, and R A Bekker. Terapevticheskii arkhiv vol. 94,5 689-694. 17 Jun. 2022, doi:10.26442/00403660.2022.05.201533 
  5. Hasselmo, Michael E. “The role of acetylcholine in learning and memory.” Current opinion in neurobiology vol. 16,6 (2006): 710-5. doi:10.1016/j.conb.2006.09.002 
  6. Benton, D et al. “Thiamine supplementation mood and cognitive functioning.” Psychopharmacology vol. 129,1 (1997): 66-71. doi:10.1007/s002130050163 
  7. Lôo, H et al. “Etude des effets de la sulbutiamine (Arcalion 200) sur l’inhibition psychocomportementale des épisodes dépressifs majeurs” [Effects of sulbutiamine (Arcalion 200) on psycho-behavioral inhibition in major depressive episodes]. L’Encephale vol. 26,2 (2000): 70-5. 
  8. Tiev, K P et al. “Traitement de l’asthénie en période postinfectieuse: étude randomisée en double aveugle de deux doses de sulbutiamine (400-600 mg/j) versus placebo” [Treatment of chronic postinfectious fatigue: randomized double-blind study of two doses of sulbutiamine (400-600 mg/day) versus placebo]. La Revue de medecine interne vol. 20,10 (1999): 912-8. doi:10.1016/s0248-8663(00)80096-x 
  9. Bizot, Jean-Charles et al. “Chronic treatment with sulbutiamine improves memory in an object recognition task and reduces some amnesic effects of dizocilpine in a spatial delayed-non-match-to-sample task.” Progress in neuro-psychopharmacology & biological psychiatry vol. 29,6 (2005): 928-35. doi:10.1016/j.pnpbp.2005.04.035 
  10. Ollat, H et al. “Effets de l’association de la Sulbutiamine à un inhibiteur de l’acétylcholinestérase dans les formes légères à modérées de la maladie d’Alzheimer” [Effects of the association of sulbutiamine with an acetylcholinesterase inhibitor in early stage and moderate Alzheimer disease]. L’Encephale vol. 33,2 (2007): 211-5. doi:10.1016/s0013-7006(07)91552-3 
  11. Sevim, Serhan et al. “Sulbutiamine shows promising results in reducing fatigue in patients with multiple sclerosis.” Multiple sclerosis and related disorders vol. 16 (2017): 40-43. doi:10.1016/j.msard.2017.05.010 
  12. Dmitriev, D G et al. Urologiia (Moscow, Russia : 1999) ,1 (2005): 32-5. 
  13. Trovero, F et al. “Evidence for a modulatory effect of sulbutiamine on glutamatergic and dopaminergic cortical transmissions in the rat brain.” Neuroscience letters vol. 292,1 (2000): 49-53. doi:10.1016/s0304-3940(00)01420-8 
  14. Page, M G et al. “Brain glutamate and gamma-aminobutyrate (GABA) metabolism in thiamin-deficient rats.” The British journal of nutrition vol. 62,2 (1989): 245-53. doi:10.1079/bjn19890027 
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