Benfotiamine, or benphothiamine, is marketed as a lipid soluble form of thiamine. Preliminary human studies indicate that benfotiamine may be helpful in diabetic neuropathy and to reduce microvascular damage from high blood sugar.. Much more research is needed before we determine the appropriate dosage and whether long term use of benfotiamine has side effects that are of concern. There are some scientists who are skeptical of the benefits of benfotiamine.
   Advanced glycation and lipoxidation end products (AGEs / ALEs) have been implicated in the causation of some of the major microvascular complications of diabetes mellitus: diabetic neuropathy, nephropathy, and retinopathy. Benfotiamine is a transketolase activator that directs these substrates to the pentose phosphate pathway, thus perhaps reducing tissue AGEs.

Benfotiamine supplement ( S-benzyolthiamine-O-monophosphate )
80 mg - 120 Veggie Capsules
Doctor's Best

Benfotiamine ( S-benzyolthiamine-O-monophosphate ) is a synthetic derivative of thiamin, belonging to the family of compounds knows as "allithiamines." Benofotiamine is fat-soluble and more bioavailable and physiologically active than thiamin.* Benfotiamine raises the blood level of thiamin pyrophosphate (TPP, the biologically active co-enzyme of thiamin, and stimulates transkotelase, a cellular enzyme essential for maintenance of normal glucose metabolic pathways. Benfotiamine helps maintain healthy cells in the presence of blood glucose. Controls formation of Advanced Glycation End products (AGEs)


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Supplement Facts
Amount Per capsule:
Benfotiamine - 80 mg *

Suggested Use: One benfotiamine capsule a few times a week or as recommended by your health care provider.

Benfotiamine daily value not established.

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Benefit of benfotiamine pills
There is a possibility that benfotiamine pills may be helpful in diabetic neuropathy and other conditions due to high blood sugar levels but more research is needed. For more information on natural ways to treat diabetes.

Benfotiamine benefit for diabetes patients
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. Heart and Diabetes Center NRW, Georgstrasse 11, 32545 Bad Oeynhausen, Germany.
Thirteen people with type 2 diabetes were given a heat-processed test meal with a high advanced glycation end products content (HAGE; 15.100 AGE kU, 580 kcal, 54 g protein, 17 g lipids, and 48 g carbohydrates) before and after a 3-day therapy with benfotiamine (1,050 mg/day). Macrovascular flow-mediated dilatation (FMD) and microvascular reactive hyperemia, along with serum markers of endothelial disfunction (E-selectin, vascular cell adhesion molecule-1, and intracellular adhesion molecule-1), oxidative stress, AGE, and MG were measured during both test meal days after an overnight fast and then at 2, 4, and 6 h postprandially. The HAGE induced a maximum reactive hyperemia decrease of -60.0% after 2 h and a maximum FMD impairment of -35.1% after 4 h, without affecting endothelium-independent vasodilatation. The effects of HAGE on both FMD and reactive hyperemia were completely prevented by benfotiamine. Our study confirms micro- and macrovascular endothelial dysfunction accompanied by increased oxidative stress following a real-life, heat-processed, AGE-rich meal in individuals with type 2 diabetes and suggests benfotiamine as a potential treatment.
   Comments: For long term use, the dosage of benfotiamine may be much less than what the researchers used in this short term study.

Benfotiamine as an antioxidant
Benfotiamine exhibits direct antioxidative capacity and prevents induction of DNA damage in vitro.
Diabetes Metab Res Rev. 2008 April. Schmid U, Stopper H, Heidland A, Schupp N. Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany.
Owing to a reduced activity of the enzyme transketolase, which requires diphosphorylated thiamine (vitamin B(1)) as cofactor, an accumulation of deleterious glucose metabolites occurs in patients with diabetes. Benfotiamine, a lipophilic thiamine diphosphate medicine, prevented early renal and retinal changes in animal studies, and reduced neuropathic pain in clinical studies.We investigated for the first time direct antioxidant abilities of benfotiamine. Additionally, a potential DNA protective effect of benfotiamine was found. Benfotiamine shows a direct antioxidant action. This effect of benfotiamine may be involved in the improvement of diabetic late complications, including peripheral neuropathy.

Uveitis study in rodents
Uveitis -- an inflammation just below the outer surface of the eyeball which causes 10 percent to 15 percent of U.S. blindness and even higher rates of blindness globally -- is usually treated with antibiotics or steroid eye drops. Researchers at the University of Texas Medical Branch at Galveston found benfotiamene fed to laboratory rats with bacterial toxins that ordinarily produce a reaction mimicking uveitis, failed to develop any signs of the inflammatory disorder. The study, published in the Januuary 2009 issue of Investigative Ophthalmology and Visual Science, found benfotiamene works by suppressing the activation of a crucial signaling molecule called NF-kappa B, which is normally triggered by the stress caused by infection. Shutting down NF-kappa B prevents the runaway production of inflammatory proteins that generates uveitis.

Benfotiamine Research studies
Benfotiamine relieves inflammatory and neuropathic pain in rats.
Eur J Pharmacol. 2006 Jan 13;530(1-2):48-53. Departamento de Farmacobiologia, Centro de Investigacion y de Estudios Avanzados-Coapa, Calzada de los Tenorios 235, Colonia Granjas Coapa, DF, Mexico.
Benfotiamine has shown therapeutic efficacy in the treatment of painful diabetic neuropathy in human beings. However, so far there is no evidence about the efficacy of this drug in preclinical models of pain. The purpose of this study was to assess the possible antinociceptive and antiallodynic effect of benfotiamine in inflammatory and neuropathic pain models in the rat. Inflammatory pain was induced by injection of formalin in non-diabetic and diabetic (2 weeks) rats. Reduction of flinching behavior was considered as antinociception. Neuropathic pain was induced by either ligation of left L5/L6 spinal nerves or administration of streptozotocin (50 mg/kg, i.p.) in Wistar rats. Benfotiamine significantly reduced inflammatory (10-300 mg/kg) and neuropathic (75-300 mg/kg) nociception in non-diabetic and diabetic rats. Results indicate that oral administration of benfotiamine is able to reduce tactile allodynia from different origin in the rat and they suggest the use of this drug to reduce inflammatory and neuropathic pain in humans.

Benfotiamine alleviates diabetes-induced cerebral oxidative damage independent of advanced glycation end-product, tissue factor and TNF-alpha.
Neurosci Lett. 2005 Oct 27; Wu S, Ren J.
Division of Pharmaceutical Sciences and Center for Cardiovascular Research and Alternative Medicine, University of Wyoming, Laramie, WY 82071
Diabetes mellitus leads to thiamine deficiency and multiple organ damage including diabetic neuropathy. This study was designed to examine the effect of benfotiamine, a lipophilic derivative of thiamine, on streptozotocin (STZ)-induced cerebral oxidative stress. Benfotiamine alleviated diabetes-induced cerebral oxidative stress without affecting levels of AGE, protein carbonyl, tissue factor and TNF-alpha. Collectively, our results indicated benfotiamine may antagonize diabetes-induced cerebral oxidative stress through a mechanism unrelated to AGE, tissue factor and TNF-alpha.

High-Dose Benfotiamine Rescues Cardiomyocyte Contractile Dysfunction in Streptozotocin-Induced Diabetes Mellitus.
J Appl Physiol. 2005 Sep 15; Ceylan-Isik AF, Wu S, Li Q, Li SY, Ren J.
Diabetic cardiomyopathy is characterized by cardiac dysfunction. This study was designed to examine the effect of benfotiamine, a lipophilic derivative of thiamine, on streptozotocin (STZ)-induced cardiac contractile dysfunction in mouse cardiomyocytes. Diabetes triggered oxidative stress, measured by GSH/GSSG ratio and formation of advanced glycation end-product (AGE) in the hearts. Benfotiamine treatment alleviated oxidative stress without affecting AGE or protein carbonyl formation. Collectively, our results indicated benfotiamine may rescue STZ-induced cardiomyocyte dysfunction but unlikely AGE formation in short-term diabetes.

Benfotiamine in the treatment of diabetic polyneuropathy -- a three-week randomized, controlled pilot study (BEDIP study).
Int J Clin Pharmacol Ther. 2005 Feb;43(2):71-7.
The aim of the study was to evaluate the efficacy of benfotiamine administered over three weeks (allithiamine; a lipid-soluble vitamin B1 prodrug with high bioavailability) to patients with diabetic polyneuropathy in a randomized, placebo-controlled, double-blind, two-center pilot study. Forty inpatients (23 male, 18 female, age range 18 - 70 years) with a history of type 1 or 2 diabetes and polyneuropathy of not longer than two years, were included in the study. Twenty Patients received two 50 mg benfotiamine tablets four times daily and 20 patients received placebo over the three-week study period. Two clinical units were involved with 10 patients receiving placebo and 10 patients benfotiamine in each. The neuropathy score according to Katzenwadel et al. [1987] was used to evaluate symptoms of polyneuropathy, vibration perception threshold and both the physician's and the patient's own assessment were documented. A statistically significant improvement in the neuropathy score was observed in the group given active drug when compared to the placebo-treated controls. There was no statistically significant change observed in the tuning fork test. The most pronounced effect on complaints was a decrease in pain. More patients in the benfotiamine-treated group than in the placebo group considered their clinical condition to have improved. No side effects attributable to benfotiamine were observed. The differences between the groups cannot be attributed to a change in metabolic parameters since there were no significant alterations in the HbA1 levels and blood sugar profiles. The body mass index of the two groups did not differ. This pilot investigation (BEDIP Study) has confirmed the results of two earlier randomized controlled trials and has provided further evidence for the beneficial effects of benfotiamine in patients with diabetic neuropathy.

Benfotiamine blocks three major pathways of hyperglycemic damage and prevents experimental diabetic retinopathy.
Nat Med. 2003 Mar;9(3):294-9. Epub 2003 Feb 18.
Three of the major biochemical pathways implicated in the pathogenesis of hyperglycemia induced vascular damage (the hexosamine pathway, the advanced glycation end product (AGE) formation pathway and the diacylglycerol (DAG)-protein kinase C (PKC) pathway) are activated by increased availability of the glycolytic metabolites glyceraldehyde-3-phosphate and fructose-6-phosphate. We have discovered that the lipid-soluble thiamine derivative benfotiamine can inhibit these three pathways, as well as hyperglycemia-associated NF-kappaB activation, by activating the pentose phosphate pathway enzyme transketolase, which converts glyceraldehyde-3-phosphate and fructose-6-phosphate into pentose-5-phosphates and other sugars. In retinas of diabetic animals, benfotiamine treatment inhibited these three pathways and NF-kappaB activation by activating transketolase, and also prevented experimental diabetic retinopathy. The ability of benfotiamine to inhibit three major pathways simultaneously might be clinically useful in preventing the development and progression of diabetic complications.

Bendotiamine efficacy in alcoholic polyneuropathy therapy
Zh Nevrol Psikhiatr Im S S Korsakova. 2001;101(12):32-6.
Benfogamma efficacy in alcoholic polyneuropathy therapy with pain syndrome and other sensor disorders has been studied. Fourteen males with stage II-III chronic alcoholism (mean age 41.2 +/- 9 years, mean alcoholism duration 20.6 +/- 6 years, mean alcoholic polyneuropathy therapy duration 6.8 +/- 4.9 years) have been examined, 93% of the cases having positive family history of alcoholism. Clinical neurophysiological examination was conducted at the beginning and at the end of 6-week therapy, 450 mg/day (2 weeks) and 300 mg/day (4 weeks). During the treatment the regress of algic, other sensor and movement disorders, as well as some neuropathy symptoms has been observed. The evidence of positive dynamics at peripheral and segmental nerve system level was supported by neurophysiological data.

Effectiveness of different benfotiamine dosage regimens in the treatment of painful diabetic neuropathy.
Arzneimittelforschung. 1999 Mar;49(3):220-4.
The therapeutic effectiveness of a benfotiamine (CAS 22457-89-2)-vitamin B combination (Milgamma-N), administered in high (4 x 2 capsules/day, = 320 mg benfotiamine/day) and medium doses (3 x 1 capsules/day), was compared to a monotherapy with benfotiamine (Benfogamma) (3 x 1 tablets/day, = 150 mg benfotiamine/day) in diabetic patients suffering from painful peripheral diabetic neuropathy (DNP). In a 6-week open clinical trial, 36 patients (aged 40 to 70 yrs) having acceptable metabolic control (HbA1c < 8.0%) were randomly assigned to three groups, each of them comprising 12 participants. Neuropathy was assessed by five parameters: the pain sensation (evaluated by a modified analogue visual scale), the vibration sensation (measured with a tuning fork using the Riedel-Seyfert method) and the current perception threshold (CPT) on the peroneal nerve at 3 frequencies: 5, 250 and 2000 Hz). Parameters were registered at the beginning of the study and at the end of the 3rd and 6th week of therapy. An overall bneneficial therapeutic effect on the neuropathy status was observed in all three groups during the study, and a significant improvement in most of the parameters studied appeared already at the 3rd week of therapy. The greatest change occurred in the group of patients receiving the high dose of benfotiamine, compared to the othr groups). Metabolic control did not change over the study. It is concluded that benfotiamine is most effective in large doses, although even in smaller daily dosages, either in combination or in monotherapy, it is effective.

Benfotiamine supplement questions
Q. I am 73 years of age and have suffered with neuropathy for the past 5 years, I am not diabetic. Awhile back I gave in and went on "Lyrica", it did work but in the seven weeks I was on it, I put on 7 pounds and in my life span I at one time was 240 lbs. and at 6'3'' tall I thought I could handle it, always keep myself in fair shape, got myself down to 240 lbs. and had a heart attack (1997) it has taken me 10 years to get down to 180 lbs. so when I put the 7 lbs. on, off of Lyrica I went. I must say it did work! I am a believer in vitamins and take quite a few a day, so when I put into the computer," a vitamin for neuropathy, benfotiamine came up. I started the benfotiamine capsules this week, I am taking 300 mg. a day. Do you think this is enough? I have only been on benfotiamine capsules now for 2 days. If I am right in what I read, they will not have any reaction to the other 14 vitamins I take. At 73 I am very active.
   A. As of May 2008, not enough long term research is available with benfotiamine to know what percentage of patients with diabetic neuropathy it may help, what the appropriate dosage would be and whether benfotiamine has side effects or interactions with other supplements, herbs, vitamins, or medications.

Q. I have question regarding benfotiamine supplement, specifically, 'Doctor's Best benfotiamine (S-benzyolthiamine-O-monophosphate) 80 mg - 120 Veggie Caps. I have always believed in taking 'extra' B-1 because it reputedly helps to 'discourage biting insects', specifically mosquitoes and black-flies. If in fact you also adhere to that belief, I wonder if it would follow, that benfotiamine could also produce that effect?
   A. We have not seen any research regarding the role of benfotiamine supplements in discouraging insect bites.

Q. I was previously using benfotiamine 150 mg tablets (four per day) and got great relief for my diabetic neuropathy feet (I'm diabetic). I believe the formula was a synthetic form of of vitamin B1. As your product is 80 mg per tablet, should I continue at 600 mg per day?
   A. Sometimes it takes a higher dosage of a supplement or medication to work but once the benefits begin often a lower dosage can be just as helpful.
      Q. I was taking the benfotiamone for around eight months for diabetic neuropathy - tingling, burning and numbness in my legs and feet. Three weeks after commencing the dosage of 600 mg, I noticed improvement. I felt a slight reversal when I ran out recently. Is the dosage equivalent in natural and synthetic formulas?
         A. I have not studied benfotiamine in detail but I do not think there is a natural form. To the best of my knowledge, benfotiamine is made synthetically.

Q. Your site is beyond fantastic, your decrying of megadoses admirable! The below link is to this June '08 article downplaying benefits of Benfotiamine. Comments?
Vitamin Supplement Little More Than 'Snake Oil,' Researcher Claims. Science Daily (June 13, 2008) — A popular vitamin supplement is being advertised with claims that are demonstrably untrue, as revealed by research published in the open access journal BMC Pharmacology. Benfotiamine is a synthetic derivative of thiamine (vitamin B1). It is marketed heavily as a dietary supplement using a selection of unsubstantiated, 'not-quite-medical' claims that tend to characterize this field. A large part of this campaign has been built around the belief that benfotiamine is lipid-soluble and, therefore, more physiologically active. Scientific research led by Dr Lucien Bettendorff of the Center for Cellular and Molecular Neurobiology at the University of Liège, Belgium, has entirely disproved these claims. According to Lucien Bettendorff, "We suspect that those companies selling benfotiamine have poisoned much of the recent literature in an attempt to bestow it with properties that it does not have". Benfotiamine has been previously shown to prevent several diabetic complications in experimental animal models. The researchers carried out experiments in mice in which benfotiamine was administered using several different techniques and the resulting levels of thiamine were measured in various parts of the body. Contrary to other claims about its solubility, the results show that benfotiamine is only sparingly soluble in water under physiological conditions and cannot be dissolved in octanol or oils. As Lucien Bettendorff explains, "Benfotiamine is very often considered a 'lipid-soluble' thiamine precursor from the disulfide derivative family though it is neither lipid-soluble, nor a disulfide. Sometimes, it is considered to have more biological activity than thiamine disulfides, but our study shows that it does not even penetrate cell membranes, except in those cells containing an ecto-alkaline phosphatase. There is no evidence that benfotiamine would be more effective than other precursors as a therapeutic agent for complications of diabetes." Journal reference: Marie-Laure Volvert, Sandrine Seyen, Marie Piette, Brigitte Evrard, Marjorie Gangolf, Jean-Christophe Plumier and Lucien Bettendorff. Benfotiamine, a synthetic S-acyl thiamine derivative, has different mechanisms of action and a different pharmacological profile than lipid-soluble thiamine disulfide derivatives. BMC Pharmacology.
   A. As with many supplements or medications, it often takes many years of research from various centers to finally have a good understanding of whether the supplement or medication works or whether is is ineffective. We happen to be in the early stages in terms of benfotiamine research and it is not easy for me to predict the outcome.

This benfotiamine supplement page was last updated in 2008.