Benfotiamine, orbenphothiamine, is a lipid soluble form of thiamine. Preliminary human studies indicate that benfotiamine may be helpful in diabetic neuropathy. 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.
   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 reducing tissue AGEs.

Benfotiamine supplement ( S-benzyolthiamine-O-monophosphate )
80 mg - 120 Veggie Caps
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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Benfotiamine 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.

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.

Benfotiamine Research Update
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.