Sulbutiamine
A synthetic fat-soluble derivative of thiamine (vitamin B1) developed in Japan to treat chronic fatigue and asthenia. Unlike regular thiamine, sulbutiamine crosses the blood-brain barrier and significantly increases thiamine levels in the brain. It modulates dopaminergic, glutamatergic, and cholinergic systems, providing mild stimulation, improved memory, and reduced mental fatigue.
Dosage
Standard: 200-600 mg daily in 1-2 doses. Take with food (fat-soluble). Tolerance can develop with daily use — best cycled or used intermittently.
Dosages shown are for research reference only. Always consult a qualified healthcare provider.
Half-Life
5 hours
Administration
Oral (capsules, tablets). Fat-soluble — take with food.
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Mechanism of Action
Sulbutiamine consists of two thiamine (vitamin B1) molecules connected by a disulfide bridge, conferring lipophilicity and efficient blood-brain barrier penetration via passive diffusion. In the brain, it is hydrolyzed to thiamine and increases thiamine diphosphate (TDP) levels—the cofactor for pyruvate dehydrogenase, alpha-ketoglutarate dehydrogenase, and transketolase, enzymes critical for glucose metabolism and the Krebs cycle. Sulbutiamine upregulates D1 dopamine receptors in the prefrontal cortex, possibly through reduced receptor internalization or increased expression. It modulates glutamatergic transmission (affecting NMDA/AMPA receptor function) and enhances cholinergic transmission. The anti-fatigue and memory-enhancing effects likely stem from improved neuronal glucose oxidation, increased ATP production, and enhanced dopaminergic and cholinergic tone in cognitive circuits.
Regulatory Status
OTC supplement in most countries. Prescription medication in Japan (Arcalion) for chronic fatigue and asthenia.
Risks & Safety
Common
Headache, insomnia, irritability, nausea. Tolerance develops with daily use.
Serious
No serious adverse effects documented.
Rare
Skin rash, mood instability, agitation.
Compare Sulbutiamine With
Research Papers
10Published: April 19, 2020
AI Summary
Indeed, new mechanisms of action have been found, mainly associated with its derivatives. Nevertheless, and although the research on sulbutiamine started 50 years ago, only a limited number of studies were conducted during this time frame.
Published: July 31, 1985
AI Summary
Parallel neurochemical investigations showed that the treatment induced a slight (+ 10%) but significant increase in hippocampal sodium-dependent high affinity choline uptake. The present findings and previous results suggest that sulbutiamine improves memory formation and that this behavioral effect could be mediated by an increase in hippocamp...
Published: August 6, 2007
AI Summary
Compared to entry results, episodic memory decreased in group D + P but improved in group S + D. Daylife activities only improved in group S + D.
Published: April 1, 2007
AI Summary
The authors present the results of the complex study, which includes neuropsychological tests and scales. It was shown that enerion was more effective as compared with paracetam.
Published: August 8, 2017
AI Summary
There are no available effective therapies for fatigue associated with MS, and it is unclear whether a successful therapy of MS leads to clinical improvement. Whereas several clinical trials have demonstrated the beneficial effects of sulbutiamine in patients with asthenia, there have been no reports on the effects of sulbutiamine on fatigue in ...
Published: November 1, 2011
AI Summary
We find that exposure to OGD in the presence of sulbutiamine significantly increases neuronal viability and enhances electrophysiological properties such as excitatory synaptic transmissions and intrinsic neuronal membrane input resistance in a concentration-dependent manner.
Published: June 19, 2000
AI Summary
Psycho-behavioural inhibition is characteristic of major depressive disorder and frequently recedes after the other depressive symptoms. This may induce an important psychosocial impairment which could be a risk factor for relapse.
Published: October 27, 2020
AI Summary
We found these products were listed in Natural Medicines and Dietary Supplement Databases and being queried by Military Service Members for enhanced mental focus, alertness and energy. Only two supplements showed huperzine A content within 10% of the declared amount.
Published: October 21, 2010
AI Summary
It was found that of ca. 16 000 samples analyzed in the Russian laboratory during 2009, about 100 samples contained sulbutiamine. This may indicate that sulbutiamine was intentionally administered for its ergogenic and mild stimulating properties.
Published: January 24, 2020
AI Summary
HPLC analysis revealed that sulbutiamine and benfotiamine significantly increased intracellular thiamine and TPP concentrations in vitro, corresponding with reduced levels of PDH phosphorylation. Pharmacologic administration of benfotiamine, but not sulbutiamine, reduced tumor growth in a subcutaneous xenograft mouse model.
Frequently Asked Questions
What is Sulbutiamine used for?
A synthetic fat-soluble derivative of thiamine (vitamin B1) developed in Japan to treat chronic fatigue and asthenia. Unlike regular thiamine, sulbutiamine crosses the blood-brain barrier and significantly increases thiamine levels in the brain. It modulates dopaminergic, glutamatergic, and cholinergic systems, providing mild stimulation, improved memory, and reduced mental fatigue.
What are the side effects of Sulbutiamine?
Common: Headache, insomnia, irritability, nausea. Tolerance develops with daily use. Serious: No serious adverse effects documented. Rare: Skin rash, mood instability, agitation.
How is Sulbutiamine administered?
Sulbutiamine is administered via oral (capsules, tablets). fat-soluble — take with food..
What is the half-life of Sulbutiamine?
The half-life of Sulbutiamine is 5 hours.
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