Sulbutiamine, made in Japan, is a synthetic derivative of thiamine (vitamin B1) used in the treatment of Beri-Beri, a result of an extreme deficiency of vitamin B1. Thiamine Pyrophosphate, the biologically active form of thiamine, works as a coenzyme of the enzymes connected to the metabolism and synthesis of acetyl-CoA, which is necessary for the synthesis of the neurotransmitter acetylcholine. Thiamine deficiency leads to the disfunction of the central nervous system (chronic fatigue, general weakness, nystagmus, memory and concentration impairment, cognitive impairment, depression) , the weakening of cholinergic activity, as well as the insufficiency of the cardiovascular and digestive systems.2
Sulbutiamine is characterized by its high bioavailability resulting from the highly lipophilic nature of the molecule. In contrast to hydrophilic thiamine; which, requires a membrane transporter in order to pass through the cell membrane, Sulbutiamine easily passes through the cell membrane, through the blood-brain barrier, and penetrates the brain structures where it is metabolized into thiamine and its phosphate esters. Because of its chemical properties, Sulbutiamine is the only compound used in the treatment of asthenia, and any other disorders of the central nervous system connected to vitamin B1 deficiency, which are manifested in the form of physical and psychological weakness present in the course of neurosis, depression, and schizophrenia.1
Facilitates social functioning Vitamin B1 deficiency reduces acetyltransferase activity in the hippocampus and in consequence leads to memory impairment. Sulbutiamine's cholinergic activity is due to its inhibition of acetylocholinesterase activity, the enzyme which breaks down acetylcholine into choline and acetic acid residue, and its increase in sodium-dependent choline uptake in the hippocampus.4-6 Studies suggest that long-term (10 days) Sulbutiamine intake has a positive influence on working, episodic, and long-term memory.4,5 It was also shown that Sulbutiamine combats the effects of scopolamine (drowsiness, stupor, amnesia) and has a subtly stimulating effect on the facitilating and maintaining of the waking state, which is most likely the result of the increased activity in the reticular system, which regulates sleeping and waking states, and provides impulses to subcortical motivational centers.6,7
Like many antidepressant drugs, Sulbutiamine modifies glutaminergic and dopaminergic neurotransmission in the prefrontal cortex (responsible for the operation of the working memory, action planning, consequence prediction) and the cingulate cortex (a structure belonging to the limbic system, partly responsible for emotional behavior regulation, as well as certain emotional sates such as satisfaction, pleasure, or fear).8-10 Clinical studies involving patients suffering from depression have shown that Sulbutiamine, despite its lack of anti-depressant effects, reduces various aspects of behavioral inhibition (affective, cognitive, emotional, behavioral) which in turn facilitates a return to social life, work, and family after heavy depression.11
Vitamin B1 deficiency leads to an increased usage of glucose by neurons, which in turn leads to an increased concentration of lactic acid in the cell area. It is believed that lactic acidosis is a major cause of irreversible damage to nerve cells with an extreme deficiency of thiamine. Studies have shown that thiamine improves cognitive function and slows down the progression of dementia in patients suffering from Alzheimer's disease.12,13 Additionally, Sulbutiamine induces the activity of catalase, an enzyme that breaks down hydorgen peroxide, and the activity of the transcription factor Nrf2, which is responsible for the induction of protein genes as a celluar response to oxidative stress.14
Studies on the potential use of Sulbutiamine in the treatment of psychogenic erectile disfunction have shown an improvement in blood flow to the corpus cavernosum in 80% of patients. Additionally, 40% of patients have shown a total normalization of sexual function.15
A daily dose of 12.5-25 mg/kg of body weight was administered in basic research.
A typical pharmocological dose is 400 mg per day. It is not recommended to exceed 60 mg in less than 24 hours. In order to avoid an increase in tolerance to Sulbutiamine, it is not recommended to take for longer than 2 weeks.
Not recommended for pregnant or breast-feeding women.
Noopept, Phenylpiracetam, Coluracetam, Pyritinol
May increase sensitivity to alcohol.16
1. Volvert, M.-L. et al. Benfotiamine, a synthetic S-acyl thiamine derivative, has different mechanisms of action and a different pharmacological profile than lipid-soluble thiamine disulfide derivatives. BMC Pharmacol. 8, 10 (2008).
2. Dreyfuss, P. M. & Victor, M. Effects of Thiamine Defficiency on the Central Nervous System. Am. J. Clin. Nutr. 9, 414–25 (1961).
3. Bettendorff, L., Weekers, L., Wins, P. & Schoffeniels, E. Injection of sulbutiamine induces an increase in thiamine triphosphate in rat tissues. Biochem. Pharmacol. 40, 2557–2560 (1990).
4. Bizot, J. C. 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. Prog. Neuro-Psychopharmacology Biol. Psychiatry 29, 928–935 (2005).
5. Micheau, J., Durkin, T. P., Destrade, C., Rolland, Y. & Jaffard, R. Chronic administration of sulbutiamine improves long term memory formation in mice: possible cholinergic mediation. Pharmacol. Biochem. Behav. 23, 195–198 (1985).
6. Meador, K. J. et al. Evidence for a central cholinergic effect of high-dose thiamine. Ann. Neurol. 34, 724–726 (1993).
7. Balzamo, E. & Vuillon-Cacciuttolo, G. Facilitation of a state of wakefulness by semi-chronic treatment with sulbutiamin (Arcalion) in Macaca mulatta. Rev Electroencephalogr Neurophysiol Clin. Dec;12(4), 373–8. (1982).
8. Trovero, F. et al. Evidence for a modulatory effect of sulbutiamine on glutamatergic and dopaminergic cortical transmissions in the rat brain. Neurosci. Lett. 292, 49–53 (2000).
9. Permoda-Osip, A. & Rybakowski, J. Koncepcja glutaminergiczna chorób afektywnych. Psychiatr. Pol. 45, 875–888 (2011).
10. Permoda-Osip, A. & Rybakowski, J. Rola układu glutaminergicznego w mechanizmie działania przeciwdepresyjnego i normotymicznego w chorobach afektywnych. Farmakoter. w Psychiatr. i Neurol. 2, 57–65 (2011).
11. Lôo, H., Poirier, M., Ollat, H. & Elatk, S. Effects of sulbutiamine (Arcalion 200) on psycho-behavioral inhibition in major depressive episodes. Encephale 26(2), 70–5 (2000).
12. Nakagawasai, O. Behavioral and neurochemical alterations following thiamine deficiency in rodents: relationship to functions of cholinergic neurons. Yakugaku Zasshi 125, 549–554 (2005).
13. Lu’o'ng, K. V. Q. & Nguy n, L. T. H. Role of Thiamine in Alzheimer’s Disease. Am. J. Alzheimers. Dis. Other Demen. 26, 588–598 (2011).
14. Majid, A. S. A., Yin, Z. Q. & Ji, D. Sulphur antioxidants inhibit oxidative stress induced retinal ganglion cell death by scavenging reactive oxygen species but influence nuclear factor (erythroid-derived 2)-like 2 signalling pathway differently. Biol. Pharm. Bull. 36, 1095–110 (2013).
15. Dmitriev, D., Gamidov, S. & Permiakova, O. Clinical efficacy of the drug enerion in the treatment of patients with psychogenic (functional) erectile dysfunction. Urologiia Jan-Feb;(1, 32–5. (2005).
16. Gauvin, D. V. et al. Influence of thiamine on the behavioral sensitivity to ethanol. Alcohol. Clin. Exp. Res. 18, 1398–1405 (1994).
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