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January 2007

By Dale Kiefer

When treating diabetes, today’s doctors focus on establishing blood glucose control, but often overlook the need to protect against common diabetic complications such as blindness, stroke, endothelial dysfunction, and loss of limb.1

Fortunately, benfotiamine, a little-known fat-soluble form of vitamin B1, has been shown to help prevent the development and progression of many diabetic complications. As a result, benfotiamine has become a critical nutrient for those seeking to ward off the potentially lethal impact of sustained high blood sugar levels.

Used for decades in Europe as a prescription medication, benfotiamine ameliorates the progression of diabetic nerve, kidney, and retinal damage, and relieves the painful symptoms of diabetic neuropathy.2-8 Diabetic neuropathy makes it difficult for nerves to carry messages to the brain and also impairs the function of the microvasculature (tiny blood vessels) in the extremities. The result of this pathological blood-vessel damage is numbness and painful tingling in the feet (and hands) that can eventually result in amputation of the lower extremities.

Benfotiamine acts through a novel mechanism, blocking the biochemical pathways by which high blood sugar damages cells throughout the body.8 Now available as a low-cost dietary supplement, benfotiamine can help diabetes sufferers protect their nerves, kidneys, eyes, blood vessels, and heart. Benfotiamine’s multifaceted effects in preventing dangerous diabetic complications make it an essential supplement for people with elevated blood sugar levels.

Benfotiamine Differs from Conventional Diabetes Drugs

Diabetes drugs are among the most widely prescribed pharmaceuticals on the market today. Current medications for type II diabetes seek to reduce the dangerous buildup of excess sugar (glucose) in the bloodstream by either increasing insulin production or enhancing its effectiveness.

Benfotiamine is one of the most effective yet overlooked treatments for preventing the debilitating complications of diabetes. Benfotiamine is a chemical sibling of the essential nutrient thiamine (vitamin B1). Thiamine helps to convert fats and carbohydrates into glucose, a form of fuel for the body. As such, thiamine is essential for the proper regulation of glucose metabolism.9

However, while thiamine is soluble only in water, benfotiamine is fat soluble, a characteristic that allows it to enter cells far more readily than thiamine and thus help to prevent diabetes-related dysfunction within the cells. This enhanced bioavailability makes benfotiamine particularly effective in treating hyperglycemia-related damage to tissues and organs.10-12

Benfotiamine’s Biochemical Response to High Blood Sugar

Diabetes treatments that seek to increase insulin output or improve the cells’ response to insulin do not provide adequate protection against the many complications of the disease. While diabetes medications help tackle the problem of inordinately high levels of plasma glucose, only benfotiamine reduces elevated levels of intracellular glucose and alters the body’s biochemical response to the toxic breakdown products of excess sugar. Benfotiamine stimulates the production of transketolase, a naturally beneficial enzyme that efficiently converts these potentially toxic glucose breakdown products into harmless compounds that can be safely eliminated by the body.

Numerous studies have shown that benfotiamine inhibits three major pathways that lead to the formation of toxic substances such as advanced glycation end products (AGEs).5,8,13

AGEs have been implicated in the development and progression of numerous disorders in diabetics. These include:

  • Cardiovascular disease14
  • Diabetic neuropathy (nerve disorders)15,16
  • Retinopathy (affecting vision)15,16
  • Peripheral vascular disease (affecting blood vessels of the extremities)15,16
  • Nephropathy (kidney disease).15,16

Interestingly, AGE-associated damage to the cardiovascular system is also seen in aging adults without diabetes. In fact, aging itself is considered a major risk factor for the development of cardiac dysfunction, due to the accumulation of AGEs over time, even in non-diabetics. AGEs are believed to act through several mechanisms to promote vascular damage, scar tissue formation, and inflammation.14 Unfortunately, this process is simply accelerated in diabetics,17 which suggests that even non-diabetics can benefit from benfotiamine’s ability to inhibit AGE formation.

Years of use as a prescription drug in Europe have shown that benfotiamine is safe and well tolerated.3,6,7,18,19 Now that it is available in the United States as a low-cost dietary supplement, researchers are turning their attention to benfotiamine and uncovering evidence that it helps to offset the dangers of numerous complications of diabetes and high blood sugar.

Benfotiamine Protects Delicate Nerve and Brain Tissue

The nervous system can suffer in numerous ways from the damaging effects of high blood sugar. Comprising brain, spinal cord, and peripheral nerves, the nervous system controls the functions of muscles and organs, coordinates thoughts and actions, and conveys sensory information.

Neuropathy, or nerve disease, is one of the most prevalent and painful complications of diabetes. Characteristics of diabetic neuropathy include:

  • Damage to the peripheral nerves of the extremities
  • Pain that may be unresponsive to conventional pain relievers
  • Numbness and altered sensation affecting the limbs
  • Nerves of the extremities may malfunction simultaneously, causing polyneuropathy.

Clinical trials demonstrate that benfotiamine effectively relieves diabetic polyneuropathy. A recent random, double-blind study in Germany found that diabetes patients with polyneuropathy who supplemented with 100 mg of benfotiamine four times daily for three weeks demonstrated statistically significant improvement in nerve function scores. A decrease in pain was the most pronounced effect noted. The study authors said their findings support the results of two earlier randomized, controlled trials, which also found evidence of benfotiamine’s beneficial effects in patients with diabetic neuropathy.3 Diabetes has been associated with increased oxidative stress, a contributor to many age-related disease processes. Delicate brain tissue is especially susceptible to the damaging effects of oxidative stress. As a result, diabetes is increasingly associated with cognitive decline, including dementia and Alzheimer’s. (See “The Deadly Connection Between Diabetes and Alzheimer’s,” Life Extension, December 2006.)

A newly released study indicates that benfotiamine may protect the brain against oxidative stress associated with diabetes. Investigators experimentally induced diabetes in a group of test subjects. Following two weeks of induced high blood sugar levels, the subjects received two weeks of benfotiamine supplementation. Benfotiamine alleviated the oxidative stress in the brain that typically occurs with diabetes, leading the research team to conclude that benfotiamine may avert diabetes-induced cerebral oxidative stress through a novel mechanism.20

This important finding means that benfotiamine offers critical protection for the delicate nervous system by shielding the peripheral nerves and brain from damage caused by diabetes.

Benfotiamine: What You Need to Know
  • Currently, there is no drug available to diminish the toxic effects of the breakdown products of excess glucose.
  • Long used as a prescription drug for diabetes in Europe, benfotiamine is now readily available as a dietary supplement in the US. A fat-soluble derivative of vitamin B1, benfotiamine works by a novel mechanism to prevent the development and progression of diabetic complications.
  • Benfotiamine helps relieve polyneuropathy, pain, and dysfunction affecting multiple nerves in the extremities, while also protecting against tissue-damaging oxidative stress in the brain.
  • Benfotiamine preserves healthy endothelial function, which is associated with optimal cardiovascular health and protection against diabetic peripheral vascular disease. Benfotiamine also supports the function of muscle cells in the heart.
  • Benfotiamine protects the kidneys against oxidative stress and loss of filtering capability, thus helping to prevent diabetic kidney disease.
  • Benfotiamine helps prevent or delay the development of diabetic retinopathy, a cause of vision loss.