Benfotiamine

Uses

Benfotiamine is primarily marketed as an over-the-counter drug to treat diabetic polyneuropathy. A 2021 review described two clinical trials with positive results for diabetic polyneuropathy and concluded that more research is needed.

As of 2017, benfotiamine was marketed as a pharmaceutical drug in many countries 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.

Adverse effects

There is little published data on adverse effects. In one study of a combination of benfotiamine, pyridoxine, and cyanocobalamin, around 8% of people taking the drug experienced nausea, dizziness, stomach ache and weight gain.

Pharmacology

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. providing higher levels of thiamine in muscle, brain, liver, and kidney.

Benfotiamine mainly acts on peripheral tissues through an increase in transketolase activity.

Chemistry

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

Research

Benfotiamine has been studied in laboratory models of diabetic retinopathy, neuropathy, and nephropathy. A 2021 review of its use for diabetic polyneuropathy described two clinical trials which showed improvements in neuropathic pain and neuropathic symptoms scores, the latter of which showed a dose-response effect. The authors concluded that it could potentially serve as an economical supplement to enhance neuropathy treatment and that more research is needed.

Administration of benfotiamine may increase intracellular levels of thiamine diphosphate, a cofactor of transketolase. Based on metabolic theories of Alzheimer's disease, since thiamine-dependent processes are critical in glucose metabolism and are diminished in brains of Alzheimer's disease patients at autopsy, and since treatment of mouse models of Alzheimer's disease with benfotiamine diminishes plaques, decreases phosphorylation of tau and reverses memory deficits, benfotiamine administration has been proposed as a possible intervention to reverse biological and clinical processes of Alzheimer's disease.

References

References

1. (July 1961). "A new thiamine derivative, S-benzoylthiamine O-monophosphate". Science.
2. (May 2021). "Neuroprotective Effects of Thiamine and Precursors with Higher Bioavailability: Focus on Benfotiamine and Dibenzoylthiamine". International Journal of Molecular Sciences.
3. (2008). "Nutraceuticals, glycemic health and type 2 diabetes". Wiley-Blackwell/IFT Press.
4. (April 2021). "A Review of Alternative Treatment Options in Diabetic Polyneuropathy". Cureus.
5. "Benfotiamine International brands". Drugs.com.
6. (1991). "Bioavailability assessment of the lipophilic benfotiamine as compared to a water-soluble thiamin derivative". Annals of Nutrition & Metabolism.
7. (1968). "Studies on the absorption of ''S''-benzoylthiamine ''O''-monophosphate: (I) Metabolism in tissue homogenates". Vitamins.
8. (March 2012). "Solubility enhancement of benfotiamine, a lipid derivative of thiamine by solid dispersion technique". J Pharm Bioallied Sci..
9. (June 2010). "The multifaceted therapeutic potential of benfotiamine". Pharmacological Research.
10. (July 2013). "Abnormal thiamine-dependent processes in Alzheimer's Disease. Lessons from diabetes". Molecular and Cellular Neurosciences.