All About Sulbutiamine: Benefits, Safety, and How to Use It - Neuropedia

All About Sulbutiamine: Benefits, Safety, and How to Use It

Sulbutiamine was originally discovered in the 1960s by researchers looking for more effective ways to address deficiencies of thiamine, an essential nutrient that’s required for energy production and nerve function.[1] 

Following its discovery and in the decades since, a growing body of research suggests that additional sulbutiamine benefits may include improved cognitive function, decreased fatigue, improved physical performance, and more.

In this guide, you’ll learn the underlying science, side effects and benefits, optimal dosage range, safety, side effects, and other essential facts about sulbutiamine.

What Is Sulbutiamine?

Sulbutiamine (isobutyryl thiamine disulfide) is a synthetically modified derivative of thiamine (vitamin B1) produced by linking together two thiamine molecules with a disulfide (double sulfur) group.[2] Unlike regular thiamine, the sulfur addition makes sulbutiamine lipophilic (fat soluble) and gives it other distinct properties.

Japanese researchers initially developed sulbutiamine in the mid-1960s as part of an effort to produce lipid-soluble thiamine derivatives to treat beriberi (thiamine deficiency), a common problem in Japan at the time.[3] In the 1970s, a French pharmaceutical company began producing sulbutiamine under the brand name Arcalion as a treatment for asthenia (fatigue with abnormal physical weakness).[4]

Today, sulbutiamine is widely available over the counter in many countries without a prescription and is sometimes sold as a nutritional supplement. Other common names for sulbutiamine besides Arcalion include Enerion, sulbuthiamine, isobutyrylthiamine disulfide, bisulbutiamine, and bisulbuthiamine.[5]

How Does Sulbutiamine Work?

As a synthetic analog of thiamine, the original purpose of sulbutiamine was to help correct thiamine deficiency.[6] Whereas thiamine is hydrophilic (water-soluble), sulbutiamine’s lipid-soluble properties appear to allow it to absorb into cells faster and cross the blood-brain barrier more readily compared to thiamine. 

Thiamine is an essential nutrient that your body requires for energy production and nerve function.[7] After absorption, the body metabolizes (breaks down) sulbutiamine into thiamine and thiamine derivatives by removing the isobutyryl groups[8] 

Some evidence suggests that sulbutiamine increases thiamine and thiamine metabolite levels in the brain and the central nervous system more effectively than thiamine itself.[9]

Additionally, some sulbutiamine researchers think that the free sulfur thiol group that’s released during sulbutiamine’s metabolism could also play a role in some of its effects by acting as an antioxidant in tissues.[10]

Effects and Potential Sulbutiamine Benefits

  • Cognitive Enhancement
  • Energy and Anti-fatigue
  • Athletic Performance
  • Antioxidant Effects
  • Mental Health
TakeThesis banner

Sulbutiamine May Have Nootropic Effect Benefits

Sulbutiamine may have nootropic or cognitive-enhancing properties.[11] Nootropics are compounds or supplements that enhance cognitive performance, including memory, creativity, motivation, or attention.[12]

How to Pronounce Nootropic: 

Some evidence suggests that sulbutiamine may modulate (affect) the brain’s cholinergic system, meaning it could support the formation of memories and other cognitive functions.[13][14]

A study published in Pharmacology Biochemistry and Behavior found that mice receiving sulbutiamine daily for 10 days showed greater performance in a measure of long memory formation compared to those who didn’t.[15]

Sulbutiamine Has Possible Anti-fatigue Benefits

Some studies suggest sulbutiamine may help people who struggle with fatigue, but the current evidence is mixed and also limited due to few studies and small sample sizes.[16] 

In a Russian study of patients with traumatic brain injury (TBI), sulbutiamine was more effective than the nootropic piracetam for improving fatigue associated with concussions[17]

In a small study of patients with multiple sclerosis (MS), 400 milligrams of oral sulbutiamine once per day for two months resulted in significant improvements in the Fatigue Impact Scale, a measure of fatigue.[18] However, sulbutiamine did not appear to improve fatigue in those MS patients who weren’t taking prescription drugs for their condition.

Sulbutiamine May Benefit Enhanced Physical Performance

According to a 2010 paper, some athletes may take sulbutiamine for its “ergogenic (performance-enhancing) and mild stimulating properties.”[19]

Although there are currently no peer-reviewed studies demonstrating any ergogenic effects, it’s possible that sulbutiamine might increase energy production and carbohydrate metabolism by elevating thiamine levels in tissues, which could in turn lead to an increase in athletic performance[20]

A small 1996 study found that when athletes took high-dose thiamine (vitamin B1) supplementation of 100 milligrams per day, they experienced less fatigue.[21] Because sulbutiamine increases tissue thiamine levels, it may function similarly in terms of any potential effects on fatigue or recovery.

Sulbutiamine Has Antioxidant Properties

Sulbutiamine contains thiols, which are molecules with a structure similar to alcohol but containing sulfur in place of oxygen.[22] 

Thiols act as antioxidants, helping to reduce damage from free radicals that would otherwise cause harm to cells.[23] When your body breaks down sulbutiamine, its thiols become available for use by cells. 

As a result, sulbutiamine may help to preserve the function and integrity of the cells and tissues of the nervous system by protecting them from damage.[24]

In its capacity as an antioxidant, sulbutiamine also appears to influence redox status,[25] or the balance between pro-oxidants (bad) and antioxidants (good). By supporting redox potential in tissues of the central nervous system (CNS), sulbutiamine may increase the available electrons and the negative electrical charge of neurons, which could support the functioning of the CNS.[26]

Some evidence also suggests that thiols from sulbutiamine can increase the available levels of glutathione, one of the most important antioxidants in your body’s endogenous antioxidant defense system.[27] Increased glutathione availability resulting from sulbutiamine supplementation could help protect brain cells from oxidative stress.[28]

Sulbutiamine and Mental Health

Early evidence suggests sulbutiamine may affect glutaminergic and dopaminergic functioning in the brain and central nervous system, which could relate to potential mental health benefits.[29]

A randomized, double-blind, placebo-controlled trial of inpatients with major depression who took 600 milligrams of sulbutiamine per day for 8 weeks found that they experienced improvements in areas of previous incapacitation including affect (mood), emotion, cognition, and behavior.[30] However, the researchers didn’t document a direct antidepressant effect in the patients.

Sulbutiamine Dosage and How to Take It

The most common sulbutiamine dosages used in scientific studies range from 100 to 600 milligrams per day, usually in a single daily dose.[31] 

You can take sulbutiamine on an empty stomach, with fats like olive oil, coconut oil, or MCT oil, or with a full meal. It’s possible that sulbutiamine will act faster when consumed on an empty stomach, but may absorb better with fats or a meal because it’s fat soluble. 

Lipid-soluble thiamine analogs like sulbutiamine are more bioavailable compared to thiamine, but currently, there’s no research to say for certain whether you should take them with or without food  — so it’s probably best to experiment and see what works for you.[32]

Because sulbutiamine may have mild stimulating effects and can rarely cause difficulties with sleep, it’s probably a good idea to take it in the morning rather than later in the day or before bedtime.[33][34] 

Sulbutiamine Side Effects and Safety

Large-scale and long term safety data for sulbutiamine is currently lacking. However, in human studies and clinical trials with sulbutiamine, adverse effects are rare and are usually mild in nature.[35] 

In one of the largest clinical trials of sulbutiamine, 10 out of 1,722 participants reported side effects including nausea (5), headache (1), insomnia (1), diarrhea (1), tremor (1), and drowsiness (1).[36] In total, 0.6% of the subjects experienced adverse effects while taking sulbutiamine for 15 days. 

In a randomized controlled trial investigating the effects of sulbutiamine on diabetic neuropathy, no adverse effects or interactions with prescription drugs were mentioned.[37]

Other evidence from randomized studies shows no serious adverse effects from taking sulbutiamine, or a rate of side effects that is comparable to the placebo group.[38]

In one published case history, a team of psychiatrists reported a case where the use of sulbutiamine may have interfered with a patient’s therapy for bipolar disorder.[39]

On the other hand, a study examining the effects of sulbutiamine in patients who were receiving inpatient treatment for major depressive episodes did not find any increase in mania or suicide attempts or any decrease in the effectiveness of treatment.[40]

There isn’t a proven link between sulbutiamine use and these types of difficulties, but individuals who take medication for bipolar disorder or who have a history of mania should ask their doctor or therapist before taking sulbutiamine to be on the safe side.

Athletes who participate in sanctioned sports with drug tests should probably use caution when considering taking sulbutiamine. While it’s not an anabolic steroid and doesn’t actually have steroid-like effects, sulbutiamine use may trigger a false positive or alert for the performance-enhancing steroid boldenone.[41]

Frequently Asked Questions (FAQs) About Sulbutiamine

Should You Take Sulbutiamine with Food?

Sulbutiamine can work on an empty stomach or when taken with dietary fats or a meal. There’s currently no research to demonstrate which approach is most effective. It most likely absorbs faster without food, but may absorb more effectively with food.

What’s the Difference Between Sulbutiamine and Thiamine? (Sulbutiamine vs Thiamine)

When it comes to their molecular structure, sulbutiamine and thiamine are related but different. While thiamine (vitamin B1) is a naturally occurring essential nutrient, sulbutiamine is a synthetic analog of thiamine that’s designed to absorb better and cross the blood-brain barrier.[42]

Is Sulbutiamine a Stimulant?

Although sulbutiamine is definitely not a stimulant in the traditional sense of the word, some people do report mildly stimulating effects when taking sulbutiamine. These effects may be due to sulbutiamine’s ability to cross the blood-brain barrier and affect the brain’s dopamine functioning.[43]

Do You Need to Take Breaks from Sulbutiamine?

As with most supplements, taking occasional breaks from sulbutiamine is a good idea. Unlike thiamine, sulbutiamine isn’t an essential nutrient, so you don’t need to take it all the time. While sulbutiamine appears safe from clinical trials lasting up to a few months, there’s currently no data on long term usage. 

TakeThesis banner


Share your love