|AHFS/Drugs.com||International Drug Names|
|Biological half-life||5 hours|
|Chemical and physical data|
|Molar mass||702.89 g/mol|
|3D model (JSmol)|
|(what is this?)|
Sulbutiamine (brand name: Arcalion) is a synthetic derivative of thiamine (vitamin B1). It is used in France to treat symptoms of weakness or fatigue, but there is not good data to support this. It is sold as a dietary supplement. Sulbutiamine was discovered in Japan as part of an effort to develop more useful thiamine derivatives.
Adverse effects in clinical trials have included diarrhea, bladder infections, bronchitis, arthritic pain, back pain, asthma, abdominal pain, insomnia, constipation, gastroenteritis, diffuse pain, sinusitis, headache, kidney pain, vertigo, and sore throat.
Efforts to develop thiamine derivatives with better bioavaiability than thiamine were conducted in the 1950s, mainly in Japan. These efforts led to the discovery of allicin (diallyl thiosulfinate) in garlic, which became a model for medicinal chemistry efforts to create other thiamine disulfides. The results included sulbutiamine, fursultiamine (thiamine tetrahydrofurfuryl disulfide) and benfothiamine. These compounds are hydrophobic, easily pass from the intestines to the bloodstream, and are reduce to thiamine by cysteine or glutathione.:302
It was first marketed in France by Servier in 1973 under the brand name Arcalion. The drug registration went through a validation procedure in France in the 1980s, which found that the use for treatment of fatigue was not supported by data.
Sulbutiamine is sold as a dietary supplement; it appears that endurance athletes may use it to try to enhance their performance.
Because thiamine deficiency causes problems with memory and other cognitive functions, thiamine and analogs like sulbutiamine have been studied in clinical trials in the 1980s and 1990s for age-associated cognitive decline.
The pharmacology of subutiamine has been studied in various mice and rats; as of 2014 it appeared that subutiamine might be more effective than in raising thiamine phosphate levels in the brain than benfotiamine and fursultiamine, but this was not certain.:303
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