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Battle of the Thiamines


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#1 Lufega

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Posted 15 November 2008 - 08:44 AM


I am interested in the use of thiamine derivatives for the treatment of Dysautonomia or autonomia system dysfunction. Working through terrible "brain fog", I read the works of Dr. Derrick Lonsdale on using B1 to treat this. He believes the use of allithiamines which are fat soluble derivatives of B1 serves this purpose a lot better than ordinary thiamine salts. So, I assumed Benfotiamine was the best choice. I've been using it for a few months and while I have seen minor improvements, such as less tremors in my hands, I have not noticed more pronounced effects as I was expecting. I just re-read the two articles and it seems there's a better form of fat soluble B1 than benfotiamine. I searched the forum but only found a couple of scant references.


Thiamine's Mood-Mending Qualities

http://www.newhope.c...99/thiamine.cfm


Dysautonomia, A Heuristic Approach to a Revised Model for Etiology of Disease
http://ecam.oxfordjo...t/full/nem064v1



A Review of the Biochemistry, Metabolism and Clinical Benefits of Thiamin(e) and Its Derivatives

http://ecam.oxfordjo...abstract/3/1/49


Thiamine tetrahydrofurfuryl disulfi de: a little known therapeutic agent


http://journals.inde....php?ICID=11763


The story goes something like this: There are two classes of fat soluble B1, disulfide "allithiamines" and S-acyl-thiamine derivatives. Benfotiamine is of the S-acyl form while tetrahydrofurfuryl disulfide (TTFD) obviously is a disulfide and the only one considered to be an "Allithiamine". According to the Japanese guys that discovered these derivatives way back when, it's the disulfides that are more biologically active. They both work, but the TTFD are better. I haven't looked this up, but if benfotiamine has AGEs inhibiting properties, allithiamines should possess this same quality. Also, allithiamines and NOT S-acyl derivatives also have additional actiona like heavy metal chelation, anti-inflammatory and detoxifying effects against trichloroethylene and potassium cyanide.

This is from the 3rd link above:

"Although a series of S-acyl derivatives were studied, these investigators found that the disulfides had the best therapeutic effect "

Benfotiamine is a S-acyl derivative while TTFD falls under the disulfides. TTFD is also called fursultiamine.

"They concluded that thiamine enhances elimination of lead from the body and that this feature may be beneficial in chelation therapy."

This is way cool, but....

"It was noted that S-acyl derivatives are devoid of the preventive effect against trichloroethylene, potassium cyanide or lead intoxication that characterized their investigation of thiamine propyl disulfide, one of the early disulfide derivatives."

So, only the TTFD form can also chelate lead and other nasties from the body while benfotiamine doesn't have this quality.

Thiamine DerivativesMany thiamine derivatives have been synthesized after the discovery of allithiamine (97) (Figs 2 and 3) Most of the original studies were performed in Japan and the details were published in 1965 (98). Although a series of S-acyl derivatives were studied, these investigators found that the disulfides had the best therapeutic effect (99). It was noted that S-acyl derivatives are devoid of the preventive effect against trichloroethylene, potassium cyanide or lead intoxication that characterized their investigation of thiamine propyl disulfide, one of the early disulfide derivatives. These early investigators ascribed this failure to prevent toxicity to the absence of the S–S bond. The disulfides are easily reduced to thiamine in the presence of cystine or glutathione while the S-acyl derivatives require enzymatic reduction in liver or kidney.


There is also a discussion whether or not benfotiamine delivers thiamine into the cell passively like TTFD or if it's dumped outside of it necessitating a transport vehicle.

Then it gets interesting....

In response to an AD for Benfotiamine by AOR, Dr. Lonsdale wrote this:

http://findarticles....ag=artBody;col1

AOR's response:

http://findarticles....ag=artBody;col1 (in my opinion, this reponse didn't say much)


The good Doc. then countered again:

http://findarticles....ag=artBody;col1

..and that's the last of this communication I could find.

I have read from other Dysautonomia sufferers that they only seem to benefit from using allithiamine (TTFD) transdermal cream

http://www.ourkidsas...CFRxNagodjS3JEg

and get no improvement from using Benfotiamine. A big problem with the cream is that it will make you and your clothes stink of garlic. Actually, this is a big problem and the main reason I went for benfotiamine instead. But now I wonder If I would benefit more from using the cream versus benfo.

I also found TTFD in pill form by Ecological formulas (who also makes the cream) and I would assume that it's as effective as the cream, but I can't find any data or anecdotes to support this.
http://www.fubaoheal...LITHIAMINE.html

Any thoughts on this?

#2 Lufega

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Posted 15 November 2008 - 08:57 AM

Found a study that puts these two head to head.

http://www.biomedcen.../1471-2210/8/10

Results
Benfotiamine that is practically insoluble in water, organic solvents or oil was solubilized in 200 mM hydroxypropyl-β-cyclodextrin and the mice received a single oral administration of 100 mg/kg. Though thiamine levels rapidly increased in blood and liver to reach a maximum after one or two hours, no significant increase was observed in the brain. When mice received a daily oral administration of benfotiamine for 14 days, thiamine derivatives were increased significantly in the liver but not in the brain, compared to control mice. In addition, incubation of cultured neuroblastoma cells with 10 μM benfotiamine did not lead to increased intracellular thiamine levels. Moreover, in thiamine-depleted neuroblastoma cells, intracellular thiamine contents increased more rapidly after addition of thiamine to the culture medium than after addition of benfotiamine for which a lag period was observed.


Conclusion
Our results show that, though benfotiamine strongly increases thiamine levels in blood and liver, it has no significant effect in the brain. This would explain why beneficial effects of benfotiamine have only been observed in peripheral tissues, while sulbutiamine, a lipid-soluble thiamine disulfide derivative, that increases thiamine derivatives in the brain as well as in cultured cells, acts as a central nervous system drug. We propose that benfotiamine only penetrates the cells after dephosphorylation by intestinal alkaline phosphatases. It then enters the bloodstream as S-benzoylthiamine that is converted to thiamine in erythrocytes and in the liver. Benfotiamine, an S-acyl derivative practically insoluble in organic solvents, should therefore be differentiated from truly lipid-soluble thiamine disulfide derivatives (allithiamine and the synthetic sulbutiamine and fursultiamine) with a different mechanism of absorption and different pharmacological properties.


This seems to support what Dr. Lonsdale stated. So, it appears Benfotiamine is better for the purposes or AGEs reduction while allithiamines (sulbutiamine and fursultiamine) are better for CNS repair.

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#3 Lufega

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Posted 15 November 2008 - 09:13 AM

There are some references that say TTFD added to chelating agents like DMSA enhance the chelating effect. This is good news because right now I've also started Cutler's chelation protocol.

http://onibasu.com/a.../am/118898.html

"Of course, you may have heard of Derrick Lonsdale's work with TTFD, a
thiamine-related compound. Some DAN! doctors have reported that when used
at the same time as a chelating agent, that it enhanced chelation, even
though the molecule itself is not a chelator."

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#4 Lufega

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Posted 15 November 2008 - 07:40 PM

If you attempt a heavy metal chelation without correcting a thiamin deficiency, you could do more damage than good. Without proper levels of thiamin, the BBB opens up and allows more mercury in...

http://onibasu.com/a.../am/122612.html

..and of course, you can't corrent a thiamin deficiency UNTIL you correct a Magnesium def.

http://www.mgwater.c.../chapter8.shtml

Thiamine loses enzymatic activity in magnesium-deficient rats, which exhibit signs of thiamine deficiency unless magnesium is repleted (Zieve et al., 1968a,b; Zieve, 1969). Furthermore, thiamine levels have been shown to fall in liver and kidneys of magnesium-deficient rats (Itokawa et al., 1974c). Magnesium-deficient alcoholics are unresponsive to vitamin B (and other B vitamins) until their magnesium is repleted (Zieve, 1975). Magnesium deficiency has long been recognized in alcoholism (Flink et al., 1954; Review: Rink, 1976/1980); it can be secondary to low intake, malabsorption, and, if cirrhosis develops, secondary aldosteronism (Review: Massry and Coburn, 1973). The dependence of thiamine activity on magnesium as a co-factor is relevant (not only to the psychoneurologic manifestations of alcohol withdrawal) but to at least three of the metabolic aberrations that affect the heart in alcoholism.



edited for Correction: allithiamine is the form derived from the garlic bulbs, when enzymes there react allicin with thiamine. Allithiamine (TTFD) is a synthetic form of this substance. The capital "A" indicated a commercial name.

Edited by Lufega, 15 November 2008 - 08:00 PM.

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#5 neogenic

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Posted 20 November 2008 - 03:06 PM

Found a study that puts these two head to head.

http://www.biomedcen.../1471-2210/8/10

Results
Benfotiamine that is practically insoluble in water, organic solvents or oil was solubilized in 200 mM hydroxypropyl-β-cyclodextrin and the mice received a single oral administration of 100 mg/kg. Though thiamine levels rapidly increased in blood and liver to reach a maximum after one or two hours, no significant increase was observed in the brain. When mice received a daily oral administration of benfotiamine for 14 days, thiamine derivatives were increased significantly in the liver but not in the brain, compared to control mice. In addition, incubation of cultured neuroblastoma cells with 10 μM benfotiamine did not lead to increased intracellular thiamine levels. Moreover, in thiamine-depleted neuroblastoma cells, intracellular thiamine contents increased more rapidly after addition of thiamine to the culture medium than after addition of benfotiamine for which a lag period was observed.


Conclusion
Our results show that, though benfotiamine strongly increases thiamine levels in blood and liver, it has no significant effect in the brain. This would explain why beneficial effects of benfotiamine have only been observed in peripheral tissues, while sulbutiamine, a lipid-soluble thiamine disulfide derivative, that increases thiamine derivatives in the brain as well as in cultured cells, acts as a central nervous system drug. We propose that benfotiamine only penetrates the cells after dephosphorylation by intestinal alkaline phosphatases. It then enters the bloodstream as S-benzoylthiamine that is converted to thiamine in erythrocytes and in the liver. Benfotiamine, an S-acyl derivative practically insoluble in organic solvents, should therefore be differentiated from truly lipid-soluble thiamine disulfide derivatives (allithiamine and the synthetic sulbutiamine and fursultiamine) with a different mechanism of absorption and different pharmacological properties.


This seems to support what Dr. Lonsdale stated. So, it appears Benfotiamine is better for the purposes or AGEs reduction while allithiamines (sulbutiamine and fursultiamine) are better for CNS repair.

To me, those are the two preferential forms and I use both, sulbutiamine and benfotiamine.
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#6 Lufega

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Posted 25 November 2008 - 08:12 AM

Update:

I just finished my first bottle of Doctor's Best Benfotiamine, 150 mg. I started using it for the AGEs reduction benefits but then I read from many sources including wikipedia that essential tremors can be treated with magnesium and B1. Upon learning this, I upped my dose to 6 pill per day spread out to 2 per meal. I've been using magnesium for a while now.

I've had a problem with essential tremor since I was 19. I am now 29. In those 10 years it progressively worsened to were people would point it out to me. Anyways, I must say that after using Benfotiamine, my tremors have improved a good 90%. I really wasn't expecting this to work but it's quite a miracle. For me, doing simple things like using a screwdriver, drawing blood, or even helping someone with a necklace or bracelet was impossible without making my disability obvious. Heck, holding my girlfriends hand she would feel my hands shaking.

Just yesterday I was tightening a tiny loose screw on my laptop and this is when I noticed I had absolutely no tremor. Benfotiamine is pretty amazing stuff!

#7 bdelfin

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Posted 22 October 2009 - 08:15 PM

Given the greater bioavailability of TTFD, approximately how many mg. of TTFD would it take to equal the effect of 500 mg. daily of benfotiamine?

#8 neogenic

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Posted 23 October 2009 - 05:46 PM

Given the greater bioavailability of TTFD, approximately how many mg. of TTFD would it take to equal the effect of 500 mg. daily of benfotiamine?

The two aren't comparable. Sulbutiamine and TTFD are. Benfotiamine is a fat soluble one and works differently, more anti-glycation.

#9 Lufega

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Posted 23 October 2009 - 08:51 PM

I couldn't find any studies or references comparing them. TTFD and sulbutiamine works mainly in the CNS. Benfo works mostly peripherally, but there is conflicting evidence whether it crosses the CNS.

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#10 hamishm00

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Posted 25 October 2009 - 06:10 AM

I just noticed a month or so ago that I have no tremors whatsoever. This coincided with supplementation with Benfo. Anecdotal, but supports what others are saying here.

#11 Lufega

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Posted 25 October 2009 - 07:28 AM

I just noticed a month or so ago that I have no tremors whatsoever. This coincided with supplementation with Benfo. Anecdotal, but supports what others are saying here.


How much are you using? I got this effect from using the LEF product three times a day with magnesium plus 500 mg thiamine mononitrate. Very annoying, so I stopped. Recently, I noticed that Arginine rids my tremors completely. I haven't figured out the mechanism.

#12 pycnogenol

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Posted 25 October 2009 - 10:39 PM

I must say that after using Benfotiamine, my tremors have improved a good 90%.
I really wasn't expecting this to work but it's quite a miracle. Benfotiamine is pretty amazing stuff!


Good to hear, Lufega.

I really like taking Benfotiamine as it definitely helps lower blood glucose.

Sometimes as little as 250 mg does the trick but sometimes I gotta bump it up to 500 mg.

Low dosages under 250 mg don't do jack to lower my blood glucose.

I don't take it every day though. Not yet anyway. Yeah, good stuff.

I take the Life Extension brand.

Edited by pycnogenol, 25 October 2009 - 11:34 PM.


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#13 Nate-2004

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Posted 06 November 2017 - 02:14 PM

Found a study that puts these two head to head.

http://www.biomedcen.../1471-2210/8/10
 

Results
Benfotiamine that is practically insoluble in water, organic solvents or oil was solubilized in 200 mM hydroxypropyl-β-cyclodextrin and the mice received a single oral administration of 100 mg/kg. Though thiamine levels rapidly increased in blood and liver to reach a maximum after one or two hours, no significant increase was observed in the brain. When mice received a daily oral administration of benfotiamine for 14 days, thiamine derivatives were increased significantly in the liver but not in the brain, compared to control mice. In addition, incubation of cultured neuroblastoma cells with 10 μM benfotiamine did not lead to increased intracellular thiamine levels. Moreover, in thiamine-depleted neuroblastoma cells, intracellular thiamine contents increased more rapidly after addition of thiamine to the culture medium than after addition of benfotiamine for which a lag period was observed.


Conclusion
Our results show that, though benfotiamine strongly increases thiamine levels in blood and liver, it has no significant effect in the brain. This would explain why beneficial effects of benfotiamine have only been observed in peripheral tissues, while sulbutiamine, a lipid-soluble thiamine disulfide derivative, that increases thiamine derivatives in the brain as well as in cultured cells, acts as a central nervous system drug. We propose that benfotiamine only penetrates the cells after dephosphorylation by intestinal alkaline phosphatases. It then enters the bloodstream as S-benzoylthiamine that is converted to thiamine in erythrocytes and in the liver. Benfotiamine, an S-acyl derivative practically insoluble in organic solvents, should therefore be differentiated from truly lipid-soluble thiamine disulfide derivatives (allithiamine and the synthetic sulbutiamine and fursultiamine) with a different mechanism of absorption and different pharmacological properties.


This seems to support what Dr. Lonsdale stated. So, it appears Benfotiamine is better for the purposes or AGEs reduction while allithiamines (sulbutiamine and fursultiamine) are better for CNS repair.

 

 

Resurrecting this because of a reddit post.  I wonder what would happen if you took benfotiamine or sulbutiamine sublingually instead. It was posted earlier on another thread that fat solubility helps with sublingual absorption. Not sure if they're saying benfotiamine is lipid soluble or not.

 

 


Lipophilicity of drug: For a drug to be absorbed completely through sublingual route, the drug must have slightly higher lipid solubility than that required for GI absorption is necessary for passive permeation

 

pH and pKa of the saliva: As the mean pH of the saliva is 6.0, this pH favors the absorption of drugs which remain unionized. Also, the absorption of the drugs through the oral mucosa occurs if the pKa is greater than 2 for an acid and less than 10 for a base.

 

http://www.ijddr.in/...on.php?aid=5669


Edited by Nate-2004, 06 November 2017 - 02:16 PM.





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