Navigating Thiamine Supplements

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Thiamin(e), vitamin B1, is spelled with and without an ‘e’. Originally thought to be an amine, the ‘e’ was dropped when the formula became known, but the spelling using the ‘e’ is still used in many texts and across the internet. We spell it with the ‘e’ on this site because of the enhanced search characteristics e.g. thiamine ranks higher than thiamin on search engines. In addition to the discrepancies in spelling, there is quite a bit of confusion surrounding this vitamin and its derivatives used in supplements. Even the most astute readers will find navigating the world of thiamine supplements confusing. For that reason, this post will address some of the more important issues concerning these supplements.

Thiamine Chemistry

In order to understand the writing that follows, I must try to show this formula.

thiamine chemistry

Please excuse this presentation of the thiamine formula. It was made from the Apache Open Office Drawing file. Its representation is incomplete because it does not show the “double bonds”, but it illustrates that the atoms that bind together to form thiamine are in “two rings”. The 6-sided ring on the left is called a pyrimidine ring and the 5-sided one on the right is called a thiazole ring. The CH2 that joins them is called a methylene bridge. This is the naturally occurring thiamine that we must obtain from our diet. Its deficiency causes the classical disease known as beriberi. It is important to understand the atomic construction of thiamine in the discussion that follows concerning its derivatives.

Allithiamine

The Vitamin B Research Committee of Japan, a group of university-based researchers, set out to study beriberi in detail, trying to find the best method of treatment for this disease which had been a scourge in Japan for thousands of years. Without covering the specific details, they found that thiamine was converted to a disulfide derivative by an enzyme found in garlic. Because this occurred in other members of the allium species of plants, they called it allithiamine. Thinking at first that thiamine had lost its biologic activity, when tested in animals the new compound was found to have a greater biologic activity than the original thiamine. It was found that the thiazole ring had been opened, creating a disulfide. They began a research program to synthesize a whole group of thiamine disulfides, two of which are shown below.

TTFD

 

Although the arrangement of the atoms is different from the thiamine diagram, the important thing to notice is that the thiazole ring (right side) has been opened, creating a disulfide, including  what is known as a prosthetic attachment (the part attached to the disulfide). A disulfide is easily reduced (S-S becomes SH) when the molecule comes into contact with the cell membrane. The result is that the prosthetic group is removed and left outside the cell. The remainder of the molecule passes through the cell membrane into the cell. The thiazole ring closes to provide an intact thiamine molecule in the cell. It is inside the cell where thiamine has its activity and so this is an important method of delivering it to where it is needed. It is this ability to pass through the lipid barrier of the cell membrane that has caused allithiamine to be called fat-soluble. It only refers to this ability, however. It is soluble in water and can be given intravenously.

This “fat solubility” is extremely important because dietary thiamine has to be attached to a genetically determined protein, known as a transporter, to gain entry to cells. There are known to be diseases where the transporter is missing. Affected individuals have thiamine deficiency that does not respond to ordinary thiamine and are usually misdiagnosed. Therefore, a disulfide derivative that does not need the transporter is a method by which thiamine can be introduced to the cell when the transporter is missing. There is no difference between allithiamine and thiamine from a biological activity standpoint. It is this ability to pass the active vitamin through the cell membrane into the cell that provides the advantage.

I performed animal and clinical studies with thiamine tetrahydrofurfuryl (TTFD) for many years and found it to be an extremely valuable therapeutic nutrient. Any disease where energy deficiency is the underlying cause may respond to TTFD, unless permanent damage has accrued. Dr. Marrs and I believe that energy deficiency applies to any naturally occurring disease, even when a gene is at fault. For example, Japanese investigators found that TTFD protected mice from cyanide and carbon tetrachloride poisoning, an effect that was not shown by ordinary thiamine (Fujiwara, M. Absorption, excretion and fatal thiamine and its derivatives in the human body. In Shimazono, N, Katsura, E, eds. Beriberi and Thiamine. (pp 120-121) Tokyo, Igaku Shoin Ltd. 1965). They exposed a segment of dog’s intestine, disconnected it from its nerve supply and found that one of the disulfide derivatives stimulated peristalsis (the wavelike movement of the intestine). It is more than likely that TTFD could be used safely in patients with post operative paralysis of the intestine (paralytic ileus).

Other Derivatives

The Japanese investigators made many disulfide derivatives, testing them individually for their biologic activity. They found that thiamin propyl disulfide gave the best results, but unfortunately gave both treated animals and human subjects a pervasive body odor of garlic. They went on to create TTFD with a deliberate attempt to remove the garlic odor and the commercial product was named Alinamin F (odorless). This is by far the best of the disulfide derivatives. Besides the trade name of Alinamin, the Japanese product, TTFD is sold as Lipothiamine in the United States.

S-acyl derivatives

The Japanese investigators synthesized a whole series of thiamine derivatives where the prosthetic group was attached to the carbon atom (bottom right C on the thiazole ring). They are all so-called open ring derivatives but the prosthetic group has to be separated by an enzyme in the body for the thiazole ring to close. The best known of these is known as Benfotiamine and several papers have been published concerning its benefits in the treatment of neuropathy. It has also been published that it does not cross into the brain, whereas TTFD does and this seems to be the major difference between Benfotiamine and Lipothiamine. Benfotiamine, a synthetic S-acyl thiamine derivative, has different mechanisms of action and a different pharmacological profile than lipid-soluble thiamine disulfide derivatives. It is predictable that TTFD would be the best choice since it has beneficial effects both inside and outside the brain and it certainly needs to be explored and researched further as a very valuable therapeutic agent.

Thiamine Salts

Thiamine is found in health food stores as thiamine hydrochloride and thiamine mononitrate. These are known as “salts” of thiamine. Like dietary thiamine, they require a protein transporter to get the vitamin into the cell. Their absorption used to be thought to be extremely limited, but megadoses are effective in some situations. The absorption of salts is therefore inferior to that of the thiamine derivatives discussed above. They are all so-called “open ring (thiazole)” forms of thiamine and represent the most useful way of getting big doses of thiamine into the cell. The reader should be aware that when we talk about big doses of a vitamin, it is being used as a drug. Although they can be used for simple vitamin deficiency, their medical use goes far beyond that because they can be effective sometimes when thiamine absorption is genetically compromised.

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7 Comments

  1. I’ve been having problems waking up with a dry mouth for years, and recently air hunger, I thought was due to apena, however ENT could not diagnose me with sleep apnea after reading sleep study. He could not figure out way I was suffocating at night as he never had a skinny patient before. I found your article about pusedo-hypoxia after I talked to the ENT.

    This spring I was diagnosed with a B1 genetic deficiency homozygous SLC19. I ordered B1 Benfotiamine, HCI, and sulbtiamine and have been experimenting in dosages up to 500 mg with regular dosing of the other multi- B’s. I just ordered the TPP form. The 500 mg B1 dose was recommended by a hypothyroid clinician, who has seen marvelous energy improvements. At this large dose my suffocating went away immediately on the first night, and now I wake up only 2 times a night instead of 6 times. I have been on this protocol for only 7 days and surprised with the fast results.

    I have Hashimoto’s and have not felt well under all the different meds I’ve tried over the past 5 years. I believe my condition is due to B1 deficiency, and the symptoms are getting more severe now that I’m 52.

    I would like to try IV injections until my breathing problem is cured. There isn’t a lot of information on B1 IVs. Is there a therapeutic dose or IV drip to start with muscle shots as maintenance to continue? Or would you just recommend I use oral B1? I eventually develop tolerance to oral supplements and they stop working all together.

    Thank you for sharing your work with us all.

    1. This is a marvelous example of thiamine deficiency. Notice that the symptoms were confused with sleep apnea and probably with Hashimoto. If you read and understand the post above, you will come to the conclusion that the best supplement is the one that has the chemical name of thiamine tetrahydrofurfuryl disulfide (TTFD) and sold in the United States as Lipothiamine available from Ecological Formulas. Notice also that Karen got immediate relief for some of her symptoms but not all.She expected her “breathing problem” to be relieved. All she needs to do is continue with the large doses of oral thiamine derivatives because they do not need the transporter protein that she tells us is missing. She should also add large doses of magnesium because that works with thiamine. A well-rounded multivitamin is also a good idea because thiamine does not work on its own. It is a team member. I must emphasize here that the compromise of automatic breathing is due to thiamine deficiency in the lower part of the brain. The dry mouth in the morning is almost certainly because thiamine deficiency stimulates the sympathetic component of the autonomic nervous system so I would expect some components of the fight or flight reflex.Treatment of long-term thiamine deficiency is quite different from the use of a pharmaceutical drug. It is relatively slow as the system reconstitute itself and patience is required

      1. I read you comments on increasing magnesium potassium aspartate and magnesium salt.

        Could you comment on foods and supplements that destroys B1 transport? My lab cited blueberries and raw fish as antithiminase. I was eating berries everyday because of low sugar content and taking resveratrol and 88% dark chocolate, which happen to be the only two of the few foods that I like that I’m not allergic to. I do not eat sushi anymore, because of toxins and white rice. I have an intolerance or sensitivity to many common foods. I’m paleo 80% of the time and do not eat dairy or gluten. Whenever I eat too much of one food, I develop a IGE or IGG response, I’m sure this is due to the B1 deficiency and hoping the inflammation will go down in time. I don’t have enzyme activity to breakdown sulfur, SOD and histamine nor transport folate, so vegetable nutrients aren’t being absorbed. I read
        Vitamin C foods help with absorbstion, but I’m allergic to citrus fruits and nightshades. Would something like Perque Vitamin C powder compensate for times I ingest polyphenols?

        I try to stay at 20-25 grams of sugar a day, I have insulin resistance. Is this still too high?

        I was able to wipe out Candida Krusei but I do still have yeast overgrowth (white toungue) due to IBS-C. I had elevated oxalates but not sure if I still have it. Would taking calcium citrate help breakdown oxalate foods? It’s been extremely difficult eradicating my yeast infections.

        An interesting topic would be the quality of lab testing available. I have taken Genova OAT and Great Plains labs in the past, I took the Spectrecell lab most recently which was the one that measured my B1 and aspartate deficiency and low glutathione, big markers in my case.

        I will be taking your articles to my Orthomolecular doctor that is out of state in a few months, and he will be extremely pleased at the information available here. My GP is excited to monitor this new way of treating my thyroid problem.

        1. Point number 1: there is obvious confusion here. Thiaminase is an enzyme that occurs in certain bacteria that live in the human intestine. It has the capacity to break down dietary thiamine. It has nothing to do with transporters. Thiaminase also occurs in the intestines of fish and in several plants. Note that when we eat sushi we do not consume the intestines of a fish. As far as I know blueberries do not contain thiaminase. Point number 2. There are several proteins known as transporters, several of which transport thiamine into our cells. They are made in the body and are under genetic control. If one or more of the thiamine transporters is missing, it is a source of body and brain cellular thiamine deficiency.Point number 3. A level teaspoonful of sugar would be 5 g. So taking 20 to 25 g would be the equal of 4 to 5 teaspoonfuls. This would easily be the cause of thiamine deficiency, particularly if there is a transporter problem.Point number 4. For those interested, there are many posts on this website that discuss various aspects of thiamine metabolism and I do not need to repeat them here.

  2. Dr. Lonsdale, your blog changed my life – and probably extended it. Thiamine deficiency plagued me for many years and supplementation with Benfotiamine was a rapid miracle cure for me. By chance, a person mentioned Sulbutiamine to me today. Apparently, it’s benefits are getting attention from doctors. You may wish to add it to this important article.

  3. Dr. Lonsdale, your blog changed my life – and probably extended it. Thiamine deficiency plagued me for many years and supplementation with Benfotiamine was a rapid miracle cure for me. This is another important post. By chance, a person mentioned Sulbutiamine to me today. Apparently, it’s benefits are getting attention from doctors.

    1. Sulbutiamine is a disulfide derivative of thiamine. I recommend reading the post above carefully to see why the disulfide derivatives are the best

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