Benfotiamine


Benfotiamine is a synthetic S-acyl derivative of thiamine that sold as a medication or dietary supplement to treat diabetic neuropathy. Combination drugs with pyridoxine or cyanocobalamin are also marketed.
Benfotiamine was developed and invented in Japan then reported internationally by Wada, Takagi, Minakami et al. in 1961.

Uses

Benfotiamine is primarily marketed as an over-the-counter drug to treat diabetic neuropathy; clinical trials results are mixed, finding it mildly useful or no different from placebo.

Adverse effects

There is little published data on adverse effects; in one study of a combination drug of benfotiamine, pyridoxine, and cyanocobalamin, around 8% of people taking the drug experienced nausea, dizziness, stomach ache and weight gain, all of which are strongly associated with the common, normal aging process.

Pharmacology

Benfotiamine is more bioavailable than thiamine salts, providing higher levels of thiamine in muscle, brain, liver, and kidney.
Benfotiamine is dephosphorylated to S-benzoylthiamine by ecto-alkaline phosphatases present in the intestinal mucosa, and is then hydrolyzed to thiamine by thioesterases in the liver.
Benfotiamine mainly acts on peripheral tissues through an increase in transketolase activity.

Chemistry

Benfotiamine is a synthetic S-acyl Vitamin B1 analogue; its chemical name is S-benzoylthiamine O-monophosphate. Benfotiamin is a lipid derivative of thiamine vitamin. It has very low solubility in water or other aqueous solvents.

Society and culture

As of 2017, benfotiamine was marketed as a pharmaceutical drug in Argentina, Bosnia & Herzegowina, Bulgaria, Colombia, Czech Republic, Estonia, Georgia, Germany, Hong Kong, Hungary, India, Indonesia, Japan, Latvia, Lithuania, Poland, Portugal, Romania, Serbia, Slovakia, Slovenia, Russian Federation, Taiwan, and Vietnam under the following brand names: Benalgis, Benfogamma, Benforce, Benfotiamina, Biotamin, Biotowa, Milgamma, and Vilotram.
It was also marketed in some jurisdictions as a combination drug with cyanocobalamin as Milgamma, in combination with pyridoxine as Milgamma, in combination with metformin as Benforce-M, and with thiamine as Vitafos.

Research

Benfotiamine has been studied in laboratory models of diabetic retinopathy, neuropathy, and nephropathy. As of 2015 there had been one clinical study of benfotiamine in diabetic nephropathy.
Administration of benfotiamine may increase intracellular levels of thiamine diphosphate, a cofactor of transketolase, and based on metabolic theories of Alzheimer's disease, it has been studied in preclinical models of Alzheimer's disease.