Benfotiamine

benfotiamine

Benfotiamine is a synthetic, fat soluble version of vitamin B1, also known as thiamine. In its non-synthetic form, thiamine, like many types of vitamins, is water soluble. Water soluble vitamins dissolve in the body and supply cells with nutrients. However, unused fluids that carry these vitamins will filter through the liver and pass from the kidneys as waste. Fat soluble vitamins are different. When benfotiamine moves into the gastrointestinal tract, fat globules absorb and carry this vitamin into the blood supply. As the blood supply circulates through the body, cells will convert benfotiamine into thiamine as needed.

When comparing water soluble and fat soluble vitamin B1, the research found that administering a dosage of benfotiamine resulted in thiamine levels in blood plasma being five times higher when compared to the same dosage of thiamine.(1) This greater bioavailability is thought to allow individuals to reduce their vitamin intake without disrupting their daily nutritional intake, and may be ideal during internal challenges, or when nutritional needs change.

What Is The Role Of Benfotiamine In The Body?

The key role of benfotiamine is to help maintain thiamine levels in the body.(2) Thiamine, like all B vitamins, is essential. This means that the body cannot create B vitamins or any vitamin for that matter. Instead, humans need to eat foods that contain B vitamins or take a supplement. When present in the body, B vitamins act as a catalyst in enzymes that convert food into energy.

These enzymes, also known as coenzymes or “helper molecules,” are proteins that either begin a biochemical process in the body or help to complete a biochemical process.(3) Thousands of these processes occur in the body, and support everything from energy production in cells, hormone regulation in the brain, to the development of skin cells, and much more.

In particular, thiamine is necessary for the metabolism of carbohydrates.(4) Carbohydrates are nutrients that take the form of sugars, starches, and fiber. Each form of carbohydrate, except fiber, is essential to the production of glucose (blood sugar) in the body. Glucose is produced when simple or complex sugars are broken down into a molecular form that the body can utilize for energy production. However, as a result of internal challenges due to a diet high in calories from mostly carbohydrates, excess glucose and disruptions to the normal blood sugar regulating systems can occur.

Blood Sugar Regulation

Benfotiamine may be ideal to help maintain transketolase activity in the body. Transketolase is a key enzyme in the conversion of glucose in the body. Specifically, transketolase connects the pentose phosphate pathway to glycolysis.(5) Glycolysis is a metabolic pathway that converts glucose into pyruvate, which can then be recycled back into glucose or support fatty acid synthesis. Additionally, during the conversion of glucose into pyruvate, a release of free energy occurs. This energy then forms the molecules ATP and NADPH. Both of these molecules are essential for the production and transmission of energy in cells.(6)

The pentose phosphate pathway is unique in that it does not produce energy. Instead, it uses sugars as a structural element in the production of DNA and RNA. The pentose phosphate pathway also helps to create the NADPH molecule. Both the pentose phosphate pathway and glycolysis rely on thiamine as a regulator, but as a result of thiamine-linked deficiencies that result from high-calorie diets with excess carbohydrates, or a general nutrient deficiency, this process may not occur as intended.

When the creation of energy does not occur as intended, glycation can result.(7) Glycation occurs when a sugar molecule (glucose or fructose) bypasses enzyme regulators and binds to blood cells, proteins, or fat (lipids). In most of the population, around 4.5%-6% of glucose is linked to red blood cells, with similarly low levels found in protein and fat. Above this percentage, a negative health state related to excess blood sugar can occur.

This high sugar state either inhibits the function of the pentose phosphate pathway or disrupts glycolysis. As a result, cells may no longer develop as necessary to meet the needs of the body, or cells will cease to produce or transfer the energy needed to live. These disruptions may also affect the fatty acid synthesis and other cells that have no dependence on insulin. Without the function of these systems, a deprivation of oxygen and cell death can occur.

benfotiamine infographic

Nervous System Support

As mentioned previously, Thiamine plays a key role in the metabolism of blood sugar that directly impacts energy production. Individual cells and biological systems in the body generate energy using glucose to function normally. For example, the brain and central nervous system use energy to send and receive signals. Without this necessary energy, the function of these systems may become dull.(8)

This is believed to be the result of a build-up of pyruvic acid, which is generated during glycolysis. Pyruvic acid can either be recycled back into a carbohydrate or turned into lactic acid. According to research, the buildup of lactic acid, known as lactic acidosis, can result in potentially serious health problems.(9) When this happens, pathways that convert sugars to energy become blocked and the cells can no longer process oxygen. As a result, the pH of the brain can decrease and result in higher levels of acidity and damage tissue.

If lactic acidosis during ischemia or hypoxia reaches these excessive levels, metabolic and functional restitution is severely hampered upon subsequent recirculation and reoxygenation. In these circumstances, cell morphology shows signs of irreversible damage.

However, the research goes on to note that “there is less damage if severe tissue lactic acidosis can be hindered. In a medical case involving an ill patient, doctors found “profound lactic acidosis” when the individual was administered to the hospital.(10) Alcohol consumption and weight loss were noted as a potential cause of the patient's condition. After initial treatments had failed to reverse the patient's level of consciousness, 300 mg of thiamine were administered intravenously, which helps to normalize lactate levels during the next 24 hours.

It is also important to recognize that thiamin helps to maintain sodium and potassium, which are required to conduct the sending and receiving of signals from nerves. These nerves are important to things such as sensory touch, feeling, and other forms of stimuli.

The Effect Of Glucose On The Brain During Aging

The insufficient conversion of available blood sugar may also be attributed to cognitive challenges during the different stages of life. A study that examined the link between blood sugar and cognition found that key systems were involved in the delivery of glucose across the blood-brain barrier. However, excess glucose was found to have a negative effect on this process.(11)

In the brain, endothelial cells contain GLUT1, which is a type of protein that helps glucose move into the brain. The study notes that “a GLUT1 reduction could reduce glucose uptake and limit the brain’s supply of energy, and akin to a kink in the fuel line of a combustion engine, could impair neuronal activity and, in the long run, result in neurodegeneration.”

Another study examined thiamine dependent enzymes that are essential to glucose metabolism in the brain, and even plaque formation, which is associated with several neurological disorders.(12) The study notes that thiamine “has been implicated in neurological problems, delirium, and dementia.” Although the role of thiamine and its potential benefits to cognition during normal aging is not entirely known, researchers note that they will continue to look at symptoms associated with thiamine deficiency, including Alzheimer’s disease (AD). Although studies related to AD, potential causes, and treatments are still very much in the early stages of research and benfotiamine is not a clear-cut solution at this point.

As noted, a thiamine deficiency may “dull” the central nervous system and brain, but research from the World Health Organization (WHO) suggests other disorders may result from a thiamine deficiency.(13)

The most striking clinical signs of thiamine deficiency are related to the nervous system. Polyneuritis and paralysis of the peripheral nerves predominate. In the sensory system tactile sensation is first affected, then there is the pain, and finally, temperature sensitivity is altered. They include loss of vibratory sense over the big toe and the ankle and disturbances in peripheral sensation such as paresthesia (tingling, burning, numbness) in the legs and toes and superficial hyperesthesia (increased sensitivity) beginning in the lower extremities, then in the finger tips, lower abdomen, and perioral areas and gradually expanding. The sensory effects are usually symmetrical although the side that is in greater use may be affected first.

The WHO also reports that similar “disturbances” may occur in motor nerves after they affect the sensory system. However, unlike the sensory systems, these new issues ascend progressively, starting with lower extremities like the legs or toes, and moving upwards, until “foot drop and, later, wrist drop may also develop.” Additionally, if treatment is not sought, “advanced neurological changes may result in great difficulty in walking and may even lead to complete paralysis.”

The WHO writes that these symptoms can go by the names: “atrophic beriberi; dietetic neuritis (in part); dry beriberi; endemic polyneuritis; panneuritis endemica; paralytic beriberi; and polyneuritis endemica.”

Cardiovascular Support

The heart is made up of muscle cells known as cardiac myocytes.(14) Molecules in cells that produce energy, known as adenosine, rely on the ability for glucose to cross the blood-brain barrier. Given that thiamine is essential to this function, as a result of a deficiency, the myocytes found in tissue are unable to regulate adenosine monophosphate. This can lead to the body using fat stores to produce energy, which can cause an increase in lactic acid production, and finally result in potential health consequences. The research notes:

The increased production of lactate, in turn, can lead to lactic acidosis. This entire process severely disturbs the mechanics of the normal cardiovascular system. The ventricular filling pressures are increased along with increased oxygen consumption. The resistance vessels are damaged, which causes decreased peripheral vascular resistance, leading to arteriovenous shunting of blood, increased cardiac output, and venous congestion.

In a 2013 study that examines the importance of thiamine as a micronutrient in connection with systolic heart failure, researchers sought to identify the administering of thiamine to help improve left ventricular ejection fraction (LVEF), a known condition of congestive heart failure (CHF).(15)

Following the evaluation of the patient's conditions, dosages of 200-300 mg/d of thiamine were administered by mouth and intravenously in a clinical setting. The study states that “thiamine supplementation in patients with HF include improvements in end-systolic volume and New York Heart Association (NYHA) functional class.” NYHA is classification system that places patients in one of four categories based on how much they are limited during physical activity as a result of their condition.(16)

It is important to note with this research that “current CHF guidelines do not recommend thiamine supplementation, the evidence discussed above seems to indicate that a large, multicenter trial should be performed to verify the benefit of thiamine in systolic HF patients.” Additionally, the study identifies the limitations of a small sample size, writing that “a larger, randomized, double-blind, placebo-controlled trial should be performed to confirm the results of this meta analysis, as well as to assess the potential of thiamine on major cardiovascular events, including mortality in patients with systolic HF.”

Eyes Support

Benfotiamine may have a clinical use for support of eye health. In a report that details visual loss following a gastrointestinal illness that may have resulted in a disruption to the uptake of vitamins, a patient developed “visual loss and bilateral optic nerve head swelling.”(17) This is believed to have resulted in what is known as optic neuropathy, which can manifest as a result of a thiamine deficiency. The research notes:

Visual loss is often severe, including loss of light perception, and significant visual improvement may occur after thiamine replacement. Optic disc edema is present in most cases, ranging from peripapillary retinal nerve fiber layer thickening with retinal hemorrhage to marked optic disc swelling with peripapillary hemorrhage to pale edema.

In this case, 100 mg of thiamine was administered into the muscle daily for 2 weeks. At the end of treatment, visual acuity improved from 2/200 in the right eye and 4/200 in the left eye, to 20/25 and 20/50. In the event of visual loss, a number of treatments may be available, but recognizing the potential of thiamine may help to identify the cause.

Sources of Benfotiamine

While thiamine may always be present in the body as a result of a healthy diet, certain conditions may increase the demand for vitamin B1. Some potential causes of an increased need include pregnancy, lactation, fever, illness, aging, alcohol use, and diet. To help fill nutrition gaps, you can choose foods that are high in thiamine content, or you can use a benfotiamine supplement.

Foods that contains thiamine:

  • Fortified breakfast cereal
  • Beans: soy, lima
  • Potatoes with skin
  • Enriched white or brown rice
  • Enriched egg noodle
  • Meat: pork, turkey, chicken, beef
  • Seafood: trout, mussels, tuna, salmon
  • Acorn squash
  • Whole wheat bread
  • Orange juice
  • Toasted sunflower seeds
  • Yogurt
  • Oatmeal
  • Corn
  • Milk
  • Cheese

There are many foods available with thiamine. Choosing any of these may help to fill nutrition gaps. Although, it may be important to recognize when digestive challenges interfere with a healthy diet and normal absorption of nutrients.

In situations where supplementation is necessary, benfotiamine may provide optimal levels of thiamine in the body. As noted earlier, research indicates that benfotiamine stays in the body longer than thiamine, and when given the same dose of both forms of vitamin B1, benfotiamine increases levels of thiamine in blood plasma by up to 500%. Notably, some benfotiamine supplements also contain thiamine, which may provide a more immediate uptake as benfotiamine is absorbed in the lower intestine and may take longer to move through the body. If you are unsure about an appropriate dosage, consult with your personal health care practitioner, because too much benfotiamine or any vitamin or mineral may have a potentially adverse effect on health and wellness.

Sources

  1. https://www.ncbi.nlm.nih.gov/pubmed/8929745
  2. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1375232/
  3. http://orthomolecular.org/nutrients/b1.html
  4. https://www.hsph.harvard.edu/nutritionsource/carbohydrates/
  5. https://www.khanacademy.org/test-prep/mcat/biomolecules/carbohydrate-metabolism/a/pentose-phosphate-pathway
  6. https://www.tamu.edu/faculty/bmiles/lectures/Pentose%20Phosphate%20Pathway.pdf
  7. http://www.diabetesincontrol.com/glycosylation/
  8. http://healthresearchfunding.org/understanding-the-pyruvic-acid-blood-test-results/
  9. https://www.ncbi.nlm.nih.gov/pubmed/3927794
  10. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3388689/
  11. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4731873/
  12. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4846521/
  13. http://www.who.int/nutrition/publications/en/thiamine_in_emergencies_eng.pdf
  14. http://onlinelibrary.wiley.com/doi/10.1111/chf.12037/full
  15. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3865826/
  16. http://www.heart.org/HEARTORG/Conditions/HeartFailure/AboutHeartFailure/Classes-of-Heart-Failure_UCM_306328_Article.jsp#.WXoLdojyvmE
  17. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4039400/