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.