Sulbutiamine is a synthetic version of thiamine (B-1 Vitamin). Also known as Arcalion, Enerion, Bisibuthiamine, and Youvitan. Sulbutiamine was initially developed in Japan as a super-charged B-1 vitamin to offset the effects of chronic thiamine deficiency which is more common in Japan than in the West.
The B Vitamins are vital to a healthy nervous system and lack of thiamine (B-1 vitamin) in your diet can manifest in many ways. This includes acute memory issues, shortened attention span, decreased alertness regarding your surroundings and mood disturbances. Serious side effects of depression have also been found from B vitamin deficiencies in general and thiamine specifically. Fatigue is another possible side effect which can cause the negatives to further spiral due to lack of energy to stay fit through a regular exercise regimen.
What Is It?
Sulbutiamine isn’t just good for those with B-1 deficiencies. Some evidence suggests that it may offer benefits to otherwise healthy adults. Sulbutiamine should not be confused with Sibutramine (a dangerous pharmaceutical appetite suppressant). The sulbutiamine molecule is formed by fusing two Thiamine (B-1)molecules. This structure is similar to how Pyritinol is created. Pyritinol is two Pyridoxine (B-6) molecules bound together. Sulbutiamine’s full chemical name is isobutyryl thiamine disulfide. Sulbutiamine, like Pyritinol has the two B vitamins fused via the disulfide. It has been used for Asthenia, myopathic and/or neurological weakness and for somatic and psychic inhibition. It is believed to not be a psychostimulant though it does act centrally on the brain.
Regular supplementation may positively affect memory and recall. The ability to retain information and recall has been noted anecdotally as well as improvement in both short and long-term memory. The exact mechanisms for sulbutiamine’s actions are still being researched. But scientists have a few working theories on what makes it so effective.
Part of its efficacy seems owed to the enhancement of neuronal health. Specifically, sulbutiamine seems to benefit neuronal transmission and communication tasks. This is in part due to modulation of certain key neurotransmitters such as the primary excitatory neurotransmitter glutamate as well as the pleasure, focus and motivation neurotransmitter dopamine and the learning and memory molecule acetylcholine.
Increase Alertness, Focus, Fight Fatigue And Raise Energy Levels
Dopaminergic activity has been noted with sulbutiamine but more research is needed to fully understand how it affects the brain. The enhanced focus and some stimulation may be due to the fact that sulbutiamine enhances the density of certain dopaminergic receptors. This may result in improved perceptive capability. Added focus and concentration may work well with the cholinergic effect. This synergy makes sulbutiamine an excellent candidate as a study aid.
Mood Boosting Anxiolysis
There is also ample anecdotal evidence to suggest that sulbutiamine may improve mood and overall feelings of well-being. This has been theorized to be in part due to the upmodulation of dopamine. Focus, concentration, alertness, wakefulness, motivation, and feelings of pleasure are all closely tied to the dopaminergic response to the B-1 vitamin.
Depression is often tied to a foggy or fuzzy mind. One can cause the other or they can exacerbate each other. There is a possibility that sulbutiamine might work on both routes. There is even some ongoing scientific research into the potential of sulbutiamine as an anxiolytic compound. Some users have reported decreased levels of anxiety and stress. This is especially so for certain types of social anxiety and fear.
Mechanism Of Action
Sulbutiamine, as mentioned before, is technically classified as a synthetic analogue of Thiamine (B-1 vitamin). As a result, it has some of the same effects as thiamine, though since it is far more bioavailable, it may be more pronounced and dramatic in its effects. The greater bioavailability is primarily due to the fact that it more easily crosses the blood-brain barrier, the mesh that acts as a chemical filter near the brainstem.
Once past the blood-brain barrier sulbutiamine has a nearly instantaneous effect on several receptor groups. Cholinergic, glutamatergic and dopaminergic response is positively influenced which may have an effect on memory, mood, focus, concentration, wakefulness and energy levels. Sulbutiamine is also fat soluble, so it can circulate further through the body enhancing the strength of its effects.
As of yet, no optimal dosage has been determined. There are some general guidelines based on anecdotal data and research. Factors that will effect sulbutiamine dosages include your own personal biochemistry (everybody is different because every body is different), health, diet and tolerance. Some other substances or medications may also have an effect on sulbutiamine, so it is best to check for possible drug interactions before using as a supplement.
The average daily recommended dosage may be between 200 and 600mg in a day. Taking more than 800mg in any 24 hour period is strongly discouraged. Always start low and adjust as needed to determine your minimum effective dosage. Sulbutiamine has an extraordinarily bitter taste even for those accustomed to compounds like piracetam or pramiracetam. For this reason, capsules may be a a great solution for getting past the taste and will make measuring doses more convenient.
Additional B-1 Vitamin Benefits
Sulbutiamine has benefits unrelated to thiamine as well. For instance, the potential neuroprotection of hippocampal cells from oxygen and/or glucose deprivation is theorized in one study. In the study in question, a staining protocol was used to identify neurons oblated or killed due to glucose/oxygen deprivation. In the control group, a 6.1-fold increase was seen. It was then attenuated to 4.1-fold increase with sulbutiamine supplementation. Conditions like these can lead to synaptic transmission disruption that is due to nutrient deprivation, including B-1 vitamin deficiency.
Even neuropathy may benefit from sulbutiamine according to the results of a 6 week human trial involving patients with type II diabetes and diabetic neuropathy. In the study the patients took 400mg daily and reported their signs and symptoms based on a subjective score for constriction sensations, paraesthesia, pain, weakness and other symptoms. Though there was an improvement over baseline with sulbutiamine, there was no major improvement against the placebo, so the study is somewhat inconclusive. Other research is underway to confirm the possibility of its effectiveness. Nerve conduction velocity, compound motor action, and other neuropathic measures were improved according to electrophysical measurements.
Glutamate is the primary excitatory neurotransmitter in the body. The excitatory neurotransmitters cause the activation that results in the firing of neurons. Inhibitory neurotransmitters like GABA do the opposite. Both glutaminergic and dopaminergic transmission in the brain have been noted. This is especially so in the prefrontal cortex and cingular cortex. These areas are involved in organizing and decision making strategies which may result in improvement in overall thinking. A study involving daily injections of 12.5mg/kg sulbutiamine in rodents for two weeks noted a decrease in kainate receptors in tested areas and decreased dopamine levels but no change in dopamine receptor content. Sulbutiamine effect on dopaminergic and glutamergic receptors in the nuclear accumbens in a model of glucose/oxygen deprivation showed that there was no modulation of neuron excitability in the hippocampus.
Sulbutiamine was tested on laboratory animals at 300mg/kg for 10 days. A 10.1% increase in hippocampal choline uptake was noted against the control. Another mice study showed significant improvement in retention of memory which resulted in increased performance in operant tasks. Another animal study showed sulbutiamine was able to reverse some of the amnesic effects of dizocilpine (an NMDA agonist). NMDA is a glutamate subreceptor. The reversal of the NMDA agonism resulted in improved task performance in the study.
Sulbutiamine was even implicated in an overall improvement in object-recognition memory in mice. A study on chronic post-infectious fatigue (CPIF) related to sulbutiamine supplementation at 400-600mg daily for 28 days suggested that sulbutiamine may be effective at fighting fatigue. Both the 400 and 600mg groups had significantly less fatigue than the control (placebo) group. That said, the improvement was not considered statistically significant. The 600mg group also was inconsistent in performance, occasionally better than the 400mg group. A similar human trial involving infection related fatigue with a large (uncontrolled, unblinded) sample of patients resulted in a complete resolution of asthenic symptoms in 51.7% of the sample group following the completion of the 15 day study.
There has even been some evidence that sulbutiamine could be a beneficial supplement for those living with Multiple Sclerosis. The study involved a sample of 60 MS patients. 91.37% of those tested reported less fatigue, 74.13% reported “substantial” improvement in fatigue symptoms. The study was, once again, subjectively scored and self-reported by patients. To sulbutiamine’s credit, there were no reports of exacerbation of symptoms of fatigue in the study. There has even been a study that suggests sulbutiamine as possibly effective at combatting psychogenic erectile dysfunction. Increased performance from 17.5 to 24.8 on the International Index of Erectile Function was noted on average.
Sulbutiamine may impact circadian rhythms and sleep cycles just like thiamine (B-1 vitamin). For those who are prone to sleep disturbances, it is best to dose low and only in the morning. A primate study showed increased wakefulness and reduced phase 2 sleep but increased phase 1 sleep and showed no effect on REM.
Remember to always check with your primary care practitioner before undergoing any new supplement regimen. This is especially important if you’re currently under a doctor’s care for any pre-existing condition or are taking any over-the-counter or prescription medications. Sulbutiamine may build up tolerance after some time, so it is best used on an as needed basis.
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