Benfotiamine, or benphothiamine, is marketed as a lipid soluble form
of thiamine. Preliminary human studies indicate that it 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 has side effects
that are of concern. There are some scientists who are skeptical of the benefits
of this nutrient.
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.
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Early research indicates benofotiamine is fat-soluble and more bioavailable and physiologically active
than thiamin. This nutrient 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.
It helps maintain healthy cells in the presence of blood glucose and controls formation of advanced glycation end products (AGEs).
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Supplement Facts
Amount Per capsule:
Benfotiamine 80 mg each pill
Suggested Use: One capsule a few times a week or as recommended by your health
care provider.
Benefits
Antioxidant
Benfotiamine exhibits direct antioxidative capacity and prevents induction of
DNA damage in vitro.
Diabetes Metab Res Rev. 2008.
Benfotiamine,
a lipophilic thiamine diphosphate medicine, prevented early renal and retinal
changes in animal studies, and reduced neuropathic pain in clinical studies. A
potential DNA protective effect was found.
Benfotiamine alleviates diabetes-induced cerebral oxidative damage
independent of advanced glycation end-product, tissue factor and TNF-alpha.
Neurosci Lett. 2005. Division of Pharmaceutical Sciences and Center for
Cardiovascular Research and Alternative Medicine, University of Wyoming,
Laramie, WY.
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-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.
Diabetes
patients benefit
There is a possibility that benfotiamine pills may be helpful in diabetic
neuropathy and other conditions due to high blood sugar levels in those who have
diabetes but more research
is needed.
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. Heart and Diabetes Center NRW, Georgstrassen, Germany.
Thirteen people with type 2 diabetes were given a heat-processed test meal
with a high advanced glycation end products content 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. 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 may be much
less than what the researchers used in this short term study.
Diabetic nephropathy, not of
benefit
A Double-Blind, Randomized, Placebo-Controlled Clinical Trial on Benfotiamine
Treatment in Patients with Diabetic Nephropathy.
Diabetes Care. 2010. Alkhalaf A, Klooster A, van Oeveren W, Achenbach
U, Kleefstra N, Slingerland RJ, Mijnhout GS, Bilo HJ, Gans RO, Navis GJ, Bakker
SJ. Department of Internal Medicine, University Medical Center Groningen,
Groningen, the Netherlands.
To investigate the effect of benfotiamine on urinary excretion of albumin (UAE)
and the tubular damage marker kidney injury molecule-1 (KIM-1) in patients with
type 2 diabetes and nephropathy. Patients with type 2 diabetes and UAE
equivalent to 15-300 mg/24h despite angiotensin-converting enzyme inhibitors
(ACE-Is) or angiotensin-receptor blockers (ARBs), were randomly assigned to
12-week benfotiamine (900mg/day) or placebo. Results - In 39 patients on
benfotiamine versus 43 patients on placebo, benfotiamine treatment resulted in
significant improvement of thiamine status. Benfotiamine treatment did neither
result in significant decrease in 24h-UAE nor in significant decrease in
24h-KIM-1 excretion. In patients with type 2 diabetes and nephropathy, high-dose
benfotiamine treatment for 12 weeks as add-on to ACE-Is or ARBs did not reduce
UAE or KIM-1 excretion despite improvement of thiamine status.
Diabetic neuropathy
Benfotiamine in the treatment of diabetic
polyneuropathy -- a three-week randomized, controlled pilot study (BEDIP
study).
Int J Clin Pharmacol Ther. 2005.
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 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. 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 were observed.
Effectiveness of different benfotiamine dosage
regimens in the treatment of painful diabetic neuropathy.
Arzneimittelforschung. 1999.
The therapeutic effectiveness of a benfotiamine-vitamin B combination (Milgamma-N), administered in high (4 x
2 capsules / day, = 320 mg / day) and medium doses (3 x 1
capsules / day), was compared to a monotherapy with benfotiamine (Benfogamma)
(3 x 1 tablets / day, = 150 mg / day) in diabetic patients
suffering from painful peripheral diabetic neuropathy. In a 6-week open clinical
trial, 36 patients (aged 40 to 70 yrs) having acceptable metabolic control
(HbA1c < 8%) were randomly assigned to three groups, each of them comprising 12
participants. 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.
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.
Diabetic retinopathy studies
Benfotiamine blocks three major pathways of
hyperglycemic damage and prevents experimental diabetic retinopathy.
Natural Medicine. 2003.
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. In retinas of diabetic animals, benfotiamine treatment inhibited these three pathways and NF-kappaB
activation by activating transketolase, and also prevented experimental
diabetic retinopathy.
Insect bites
I believe in taking extra vitamin B-1
because it reputedly helps to discourage biting insects, specifically
mosquitoes and black-flies. I
wonder if it would follow that it could also produce that
effect?
We have not seen any research regarding the role of benfotiamine
supplements in discouraging insect bites.
Neuropathy pain research
Benfotiamine relieves inflammatory and neuropathic pain in rats.
Eur J Pharmacol. 2006. 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 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.
Bendotiamine efficacy in alcoholic polyneuropathy
therapy
Zh Nevrol Psikhiatr Im S S Korsakova. 2001.
Benfogamma efficacy in alcoholic polyneuropathy therapy with pain
syndrome and other sensor disorders has been studied. Fourteen males with stage
II-III chronic alcoholism have been examined. Clinical neurophysiological
examination was conducted at the beginning and at the end of 6-week therapy, 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.
Prostate cancer
Please advise if it is safe to take benfotiamine and
alpha lipoic acid for diabetes if one already has prostate cancer.
A doctor has to know the full history, do a medical exam, and
review lab studies before making any recommendations regarding combinations and
interactions. The dosage makes a huge effect on tolerance and interactions.
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 January 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.
Safety, side effects, risk
Is it possible that a daily dose of 600 mg benfotiamine could have a negative effect on red and
white blood cells? Just wondered because a perfect blood test three
months ago turned into a bad one and the only thing I took
since the previous test was the mentioned doseage of this vitamin.
I am not aware of human studies that have evaluated the
influence of this supplement in high dosages on red or white blood
cells. Unexpected side effects could occur with certain supplements.
Questions
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 it 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
it 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,
2008.
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.