Overview
Benfotiamine is an ally in the fight against tissue damage from diabetes, aging and Gastric bypass surgery
Benfotiamine is a substance that, when taken orally, is converted into thiamine (Vitamin B1). It is found in food in only small amounts.
Thiamine itself has been used for many years to treat neurological disorders but its poor absorption and rapid metabolic conversion makes it difficult to achieve therapeutic levels in the body.
Benfotiamine solves this bioavailability problem. Taken orally, it is well absorbed and remains in the body for days.
Benfotiamine is typically used to prevent:
- diabetes-induced damage to nerves, blood vessels, eyes, and kidneys
- neuropathy due to alcohol consumption
- tissue damage and aging due to protein cross-linking
- genetic damage in late-stage kidney disease
- nerve damage due to vitamin B-1 deficiency after gastric bypass surgery.
It is also used by bodybuilders to improve muscle flexibility and performance.
Read Benfotiamine Monograph
Benfotiamine is a substance that, when taken orally, is converted into thiamine (Vitamin B1). It is found naturally in plants of the onion family, but the amounts present are miniscule.
Thiamine has been used for many years to treat neurological disorders. But this form of the vitamin is poorly absorbed and rapidly metabolized, making it difficult to achieve therapeutic levels in the body.
Benfotiamine, being fat-soluble, solves this bioavailability problem.1 Taken orally, it is well absorbed and remains in the body for days.2 Consequently, benfotiamine can raise thiamine concentrations in the blood and tissues about 5 times higher than oral thiamine consumption can.3
What we can’t tell you
In the U.S. and some other industrialized countries, government agencies like the U.S. Food and Drug Administration have adopted censorship as a method for intensifying their control over supplement users and their suppliers. Thus, FDA regulations prohibit us from telling you that any of our products are effective as medical treatments, even if they are, in fact, effective.
Accordingly, we will limit our discussion of benfotiamine to a brief summary of relevant research, and let you draw your own conclusions about what medical conditions it may be effective in treating.
Applications
Benfotiamine is typically used to prevent:
- diabetes-induced vascular damage
- neuropathy due to diabetes4,5,6 or alcohol7 consumption
- diabetic retinopathy5,8 and nephropathy5
- tissue damage and aging due to protein cross-linking
- genetic damage in late-stage kidney disease9
- nerve damage due to vitamin B-1 deficiency after gastric bypass surgery
How does it work?
Generally speaking, benfotiamine supplements serve as a source of thiamine and therefore increase the concentrations of this vitamin in the body. Thiamine itself plays at least two biological roles:
- increasing the rate at which glucose is converted to other sugars;8
- maintaining conduction of information along nerve fibers.10,11,12
Thus, thiamine works to prevent high concentrations of glucose from developing in cells and thereby decreases the damaging effects which glucose has on the body’s tissues. And thiamine also helps to maintain nerve function.
How can glucose be damaging to the body? Isn’t it one of the body’s main sources of energy? Yes, glucose is the most common of all sugars — it is a basic constituent of honey and table sugar, and is the building block of starches and other carbohydrates. Nevertheless, glucose has two tragic down-sides:
- during the metabolism of glucose (i.e., when cells break down glucose to extract its energy), free radicals are produced which then proceed to damage the surrounding tissues;
- a small portion of the glucose molecules, instead of being metabolized, react chemically with proteins in the tissues, producing crosslinks (‘AGEs’) that impede or inactivate the proteins. The result is a loss of flexibility and function in skin, muscle, and all other living tissues.
Both of these side effects of glucose consumption are destructive to the body. They are considered major contributors to the aging process as well as to the failure of organs and tissues in diabetes.13,14,15
But this damage can be limited if glucose levels in the body’s cells can be kept low. And they can be kept low if excess glucose can be rapidly converted to less harmful substances. Thiamine is a biological cofactor that does exactly this16 — it promotes the conversion of glucose into other, less harmful sugars, as well as promoting the breakdown of glucose into carbon dioxide, water, and energy. Since benfotiamine is converted into thiamine in the body, benfotiamine supplementation is equivalent to dramatically increasing the bioavailability of thiamine.17
Diabetic applications
Diabetes causes tissue damage in many — perhaps all — bodily tissues. This is to be expected, since the hallmark of diabetes is a failure to limit the body’s exposure to high glucose levels — levels that will cause damage to any type of tissue. However, some kinds of glucose-related damage can be prevented, or even reversed, by benfotiamine. Among these are:
- vascular damage due to protein cross-linking;18
- damage to limbs caused by wounds and inadequate blood supply;19
- damage to retina and other tissues by free radical production;20
- dysfunction of nerves and kidneys due to a variety of mechanisms.5
Alcoholism
Alcoholics absorb thiamine poorly, and often show symptoms of thiamine deficiency.21 One of the results of such deficiencies is nerve damage, especially in the extremities. Benfotiamine supplements can reverse some of these neuropathic symptoms. For example, in a 2001 study, patients with alcoholic polyneuropathy were given benfotiamine at 450 mg/day for 2 weeks followed by 300 mg/day for 4 weeks. The researchers reported a regression in sensor and movement disorders, as well as some neuropathy symptoms.22
Nerve conduction
Indirect
evidence suggests that thiamine plays a fundamental, but still-obscure,
role in cell signalling — not only in mammals, but throughout the
biological world. During the evolution of nerves as specialized
communication cells, this role of thiamine evolved, too. For example,
thiamine came to be involved in controlling the pores in nerve cell
membranes through which ions pass during neural activity.12 Thus, thiamine levels seem to be correlated with the efficiency with which nerves conduct information.
Gastric bypass surgery
Gastric bypass surgery can leave some patients with nutritional deficiencies because certain vitamins, such as vitamin B-1, normally get absorbed in the parts of the digestive tract that have been bypassed.27 Symptoms of such B-1 deficiencies include numbness and weakness in arms and legs, and cognitive failures.28
Injections of vitamin B-1 are sometimes used to correct such B-1 shortages, but benfotiamine offers a more convenient approach that can — and should — be followed soon after surgery rather than waiting for symptoms of nerve damage to appear.
Why not just take oral B-1 supplements after gastic bypass surgery? Because benfotiamine’s ability to raise B-1 levels in the body is 5 times greater than that of oral B-1 supplements or of other B-1 derivatives.3,26Bodybuilding
Because of benfotiamine’s reputation for improving nerve conduction and preserving tissue flexibility, it has become popular with body-builders. Bodybuilders know from experience that muscles perform better when the nerves controlling them work better and when the muscle tissue itself is flexible.23
Safety
Benfotiamine has an excellent safety record. No reports of toxicity can be found in the medical literature.24
Reviews
A good overview of Benfotiamine and its uses is the one by Thorne Research.24 Another good Thorne Research review is their discussion of peripheral neuropathy.25
Conclusion
Is benfotiamine useful for the conditions and purposes mentioned above? We aren’t allowed to tell you, so you should take
a look at some of the references cited here, and then decide for yourself.
References
[1] Bioavailability assessment of the lipophilic benfotiamine as compared to a water-soluble thiamin derivative. Ann Nutr Metab. 1991; 35(5):292-6 Bitsch R, Wolf M, Möller J, Heuzeroth L, Grüneklee D
[2] Comparative autoradiographic investigations on the tissue distribution of benfotiamine versus thiamine in mice. Arzneimittelforschung. 1998 May; 48(5):461-8 Hilbig R, Rahmann H
[3] Pharmacokinetics of thiamine derivatives especially of benfotiamine. Int J Clin Pharmacol Ther. 1996 Feb; 34(2):47-50 Loew D
[4] Diabetic neuropathy: new strategies for treatment. Diabetes Obes Metab. 2008 Feb; 10(2):99-108 Várkonyi T, Kempler P
[5] The potential role of thiamine (vitamin B(1)) in diabetic complications. Curr Diabetes Rev. 2005 Aug; 1(3):287-98 Thornalley PJ
[6] Effectiveness of different benfotiamine dosage regimens in the treatment of painful diabetic neuropathy. Arzneimittelforschung. 1999 Mar; 49(3):220-4 Winkler G, Pál B, Nagyb
[7] Benfotiamine in treatment of alcoholic polyneuropathy: an 8-week randomized controlled study (BAP I Study). Alcohol Alcohol. 1998 Nov-Dec; 33(6):631-8 Woelk H, Lehrl S, Bitsch R, Köpcke W
[8] Vitamin B1 blocks damage caused by hyperglycemia. Sci Aging Knowledge Environ. 2003 Mar 12; 2003(10):PE6 Obrenovich ME, Monnier VM
[9] New approaches for the treatment of genomic damage in end-stage renal disease. J Ren Nutr. 2008 Jan; 18(1):127-33 Schupp N, Schmid U, Heidland A, Stopper H
[10] Lipid soluble forms of thiamine for prevention and treatment of age-related cognitive impairment of the nervous system United States Patent 5885608; 1999 Mcentee, William J
[11] A non-cofactor role of thiamine derivatives in excitable cells? Arch Physiol Biochem. 1996 Oct; 104(6):745-51 Bettendorff L
[12] Thiamine triphosphate and thiamine triphosphatase activities: from bacteria to mammals. Cell Mol Life Sci. 2003 Jul; 60(7):1477-88 Makarchikov AF, Lakaye B, Gulyai IE, Czerniecki J, Coumans B, Wins P, Grisar T, Bettendorff L
[13] Effects of antioxidant supplementation on the aging process. Clin Interv Aging. 2007; 2(3):377-87 Fusco D, Colloca G, Lo Monaco MR, Cesari M
[14] Receptor for Advanced Glycation Endproducts (RAGE): a formidable force in the pathogenesis of the cardiovascular complications of diabetes & aging. Curr Mol Med. 2007 Dec; 7(8):699-710 Yan SF, D'Agati V, Schmidt AM, Ramasamy R
[15] Cross-link breakers as a new therapeutic approach to cardiovascular disease. Biochem Soc Trans. 2007 Nov; 35(Pt 5):853-6 Susic D
[16] Detection Of Transketolase In Bone Marrow-Derived Insulin Producing Cells: Benfotiamine Enhances Insulin Synthesis And Glucose Metabolism. Stem Cells Dev. 2008 Apr 7; Oh SH, Witek RP, Bae SH, Darwiche HA, Jung Y, Pi L, Brown A, Petersen BE
[17] Regulation of intracellular glucose and polyol pathway by thiamine and benfotiamine in vascular cells cultured in high glucose. J Biol Chem. 2006 Apr 7; 281(14):9307-13 Berrone E, Beltramo E, Solimine C, Ape AU, Porta M
[18] Benfotiamine prevents macro- and microvascular endothelial dysfunction and oxidative stress following a meal rich in advanced glycation end products in individuals with type 2 diabetes. Diabetes Care. 2006 Sep; 29(9):2064-71 Stirban A, Negrean M, Stratmann B, Gawlowski T, Horstmann T, Götting C, Kleesiek K, Mueller-Roesel M, Koschinsky T, Uribarri J, Vlassara H, Tschoepe D
[19] Benfotiamine accelerates the healing of ischaemic diabetic limbs in mice through protein kinase B/Akt-mediated potentiation of angiogenesis and inhibition of apoptosis. Diabetologia. 2006 Feb; 49(2):405-20 Gadau S, Emanueli C, Van Linthout S, Graiani G, Todaro M, Meloni M, Campesi I, Invernici G, Spillmann F, Ward K, Madeddu P
[20] Benfotiamine counteracts glucose toxicity effects on endothelial progenitor cell differentiation via Akt/FoxO signaling. Diabetes. 2006 Aug; 55(8):2231-7 Marchetti V, Menghini R, Rizza S, Vivanti A, Feccia T, Lauro D, Fukamizu A, Lauro R, Federici M
[21] Inability of chronic alcoholics with liver disease to use food as a source of folates, thiamin and vitamin B6. Am J Clin Nutr. 1975 Dec; 28(12):1377-80 Baker H, Frank O, Zetterman RK, Rajan KS, ten Hove W, Leevy CM
[22] [Bendotiamine efficacy in alcoholic polyneuropathy therapy] Zh Nevrol Psikhiatr Im S S Korsakova. 2001; 101(12):32-6 Anisimova EI, Danilov AB
[23] Anyone know good diabetic body building supplements? Bodybuilding.com Forums
[24] Benfotiamine. Monograph. Altern Med Rev. 2006 Sep; 11(3):238-42
[25] Peripheral neuropathy: pathogenic mechanisms and alternative therapies. Altern Med Rev. 2006 Dec; 11(4):294-329 Head KA
[26] Comparative bioavailability of various thiamine derivatives after oral administration. Int J Clin Pharmacol Ther. 1998 Apr; 36(4):216-21 Greb A, Bitsch R
[27] Gastric bypass surgery. Wikipedia website
[28] A Case of Polyneuropathy After Gastric Bypass Surgery. MedGenMed. 2005; 7(2): 21 Teitleman M
