Sulbutiamine is a synthetic derivative of thiamine (vitamin B1). As a dimer combining two modified thiamine molecules, it readily crosses the blood–brain barrier thus increasing levels of thiamine and thiamine phosphate esters in the brain. Sulbutiamine was developed in Japan by Taisho Pharmaceutical in 1965.
For increasing mental energy, brain activity and stamina
> Sulbutiamine is a psychostimulant, the anti-asthenic and energising effects of which are the result of modification of the thiamine ring, formation of a disulphide bridge, creation of a lipophilic ester and opening of the thiazole cycle. The resulting new lipophilic compound is therefore responsible for its valuable properties.
Sulbutiamine’s main benefit lies in its ability to combat asthenia by selectively targeting the areas involved in the condition. Asthenia is essentially a form of chronic fatigue that is cerebral rather than neuromuscular in origin.
In trials conducted on this compound, in which sulbutiamine was given for 15 days to patients suffering from craniocerebral trauma or post-infectious chronic fatigue, 916 of the 1772 patients involved in the trial experienced complete recovery.
Following this positive result, scientists expanded their research to focus on other potential areas of activity.
Sulbutiamine acts as a caffeine-like energising agent, but without the latter’s stimulant effect. It can be compared to nootropic derivatives that increase mental energy, stamina and brain activity while facilitating the conversion of carbohydrates into energy directly usable by brain cells. This use of energy is specific to the brain, unlike other organs which are able to selectively use proteins or fats. The fact that it increases energy in the brain helps improve cognitive processes in general.
Memory recall and ability to reason occur more rapidly. The mind becomes clearer, and in some people, it also contributes to improved visual and auditory perception.
Taking sulbutiamine results in stimulation and upregulation of the reticular system, the brain’s attention and motivation centre, but with the added benefit that it does not lead to stress, nervous tension or hyperactivity.
Alleviates memory problems
Sulbutiamine improves memory by maximising cholinergic and dopaminergic activity in the hippocampus as well as glutamatergic transmission in the prefrontal cortex.
As a result of these mechanisms, mice have been observed to perform better in operant conditioning and object recognition tests.
Recent research showed sulbutiamine resulted in a significant improvement in daily activity in people with early-stage Alzheimer’s disease, especially when it was combined with an acetylcholinesterase-inhibitor. A randomised, double-blind study using donepezil hydrochloride as the anticholinesterase agent produced better results in patients than donepezil and a placebo.
Combats psycho-behavioural and physical inhibition
Sulbutiamine has a positive effect on behavioural inhibition ranging from fearfulness and timidity to symptoms associated with depression (even though it is not an anti-depressant as such).
In a double-blind, placebo-controlled study, a 600mg daily dose of sulbutiamine administered for two months, produced a greater improvement in psycho-behavioural inhibition after just four weeks’ treatment compared with placebo. These improvements were apparent in emotional, cognitive and behavioural inhibition.
The study’s authors concluded that sulbutiamine “facilitates the rehabilitation of patients in their social, professional and family lives”.
It can also be taken alongside conventional anti-depressants.
Combats erectile dysfunction
When administered at a dose of 600mg/day for 30 days, sulbutiamine was seen to improve erectile dysfunction in 16 out of 20 study participants. This was undoubtedly the result of its disinhibitory effect linked to fear of failure, but these positive results could perhaps lead to the prescription of lower doses of substances designed to address this problem - an important benefit given that such substances may have side-effects, particularly for cardiovascular health.
Sulbutiamine has negligible side-effects, the only exceptions being a rare allergic skin reaction or mild irritation in older people.