R Alpha Lipoic Acid: Uses, Side Effects, Interactions, Dosage

What is R Alpha Lipoic Acid and Alpha Lipoic Acid?

Alpha Lipoic Acid (ALA) is an organosulfur compound. ALA a natural substance found in certain foods and also produced in the human body, and is essential for aerobic metabolism. However, it is usually present in low concentrations and has low bio-availability. It is also manufactured and is available as a dietary supplement in some countries and as a pharmaceutical drug in other countries.

Alpha Lipoic acid is found naturally in mitochondria as the coenzyme for pyruvate dehydrogenase and a-ketoglutarate dehydrogenase. Lipoic acid is a cofactor for at least five enzyme systems, two of which are in the citric acid cycle through which our cells turn nutrients into energy.

Synthetic Alpha lipoic acid (ALA) exists in two forms, R-alpha-lipoic acid and S-alpha-lipoic acid. These two forms contain the same number and composition of atoms but have different arrangements of the atoms in their respective molecules. Natural lipoic acid is R Alpha lipoic acid. Synthetic lipoic acid contains a 50/50 mixture of the two forms. Studies with the mixture demonstrated beneficial effects in treating a number of diseases and conditions. More recent research has shown that the R Alpha Lipoic acid alone is far more effective than S Alpha Lipoic acid or the mixture. Recently, pure R Alpha Lipoic acid has become available as a nutritional supplement.

R Alpha Lipoic Acid as an Antioxidant

R Alpha Lipoic acid is regarded by many as the supreme antioxidant. R-Lipoic acid is unique in that it functions as both a fat and water-soluble antioxidant that can easily cross cell membranes. Thus, it can confer free radical protection to both interior and exterior cellular structures.

Vitamin E is a potent biological antioxidant that acts to stabilize highly reactive free radicals in lipid (fatty) tissues and cell membranes. In the process of quenching fatty free radicals, vitamin E becomes a free radical itself. The vitamin E radical is then regenerated by vitamin C (ascorbic acid). This process recycles vitamin E from a radical back into an antioxidant again, but results in the formation of a new free radical in the form of unstable vitamin C. Vitamin C is next recycled by glutathione. Up to this point vitamins E, C and glutathione work in concert to control free radicals and prevent cellular damage. But this is also an important stage where the antioxidant regeneration cycle runs into a limiting factor determined by the availability of glutathione. The concentration of these key antioxidants, vitamins E,C and glutathione diminishes with age and the individual becomes more susceptible to oxidative damage and inflammation. Cell membrane integrity, the immune system, organs and DNA integrity all go down hill as antioxidants diminish.

Glutathione is an important free-radical deactivator. Cellular glutathione levels are considered by many life extension experts to be the single best predictor of how long an individual will live. Glutathione also plays a vital role in protecting against cataract formation, enhancing immune function, preventing liver damage, slowing the initiation of cancers and eliminating heavy metals. Glutathione is quickly depleted when the body experiences high levels of oxidative stress from causes such as illness, infection, trauma, medication, environmental toxins and surgery. Glutathione deficiency is also associated with low protein intake, diabetes, liver disease, cataracts, HIV infection, respiratory distress syndrome, cancer, and idiopathic pulmonary fibrosis.

R-Lipoic acid boosts glutathione levels. Alpha lipoic acid enhances glutathione (GSH) levels. Glutathione is the most important water-soluble antioxidant and is linked to detoxification of xenobiotics, modulation of signal transduction, prostaglandin metabolism, regulation of immune response, control of enzyme activity and peptide hormones, etc. The availability of the amino acid Cysteine is known as the rate-limiting factor in glutathione synthesis. Lipoic acid is taken up rapidly by the cell and reduced to DHLA, which in turn reduces cystine to cysteine and accelerates the biosynthesis of GSH.

In summary, R Lipoic Acid acts as a potent anti-oxidant on its own, serves to regenerate other anti-oxidants like vitamin E, Vitamin C and glutathione, and increases the production of glutathione.

R Alpha Lipoic acid in Mitocondrial Function

The mitochondria are structures inside each individual cell that produce the energy that the cell needs to function. The mitochondria are analagous to an engine, boiler room or furnace. As the cells age, the activity of the mitochondria decreases, resulting in lower energy production, slower metabolism and and increased oxidative stress and damage. Clinical studies with rats have demonstrated that supplementation with R Alpha Lipoic acid improved mitocondrial function, increases metabolic rate and decreases oxidative damage. Ambulatory activity, a measure of general metabolic activity was almost threefold lower in untreated rats compared to treated rats. The decline was reversed in old rats fed R Alpha Lipoic Acid.

R Alpha Lipoic Acid as a Chelating Agent

Studies with rats and mice have shown that R Alpha Lipoic Acid provided protection against the toxic effects of arsenic, cadmium and mercury. It may also bind to other metals including iron, copper and zinc. The chelating action of R Alpha Lipoic Acid is considered to be relatively weak compared to other chelating agents. Some of the harmful effects of heavy metal poisoning are associated with oxidative damage. In addition, lipoic acid's antioxidant properties reduce the harmful effects of heavy metals.

Reduction of Aging from Glycation by R Alpha Lipoic Acid

Glycation is the formation of chemical bonds between protein molecules and glucose. This process impairs the physiological function of those proteins and contributes to the effects of aging and many disease processes, especially those associated with diabetes. These sugar-damaged proteins are referred to as advanced glycosylation end products (AGEs). AGEs increase with the length of hyperglycemia and are thought to be responsible for the kidney damage and advanced atherosclerosis seen in diabetes. Researchers have found that noncovalent binding of alpha-lipoic acid to albumin protected proteins against glycation. Thus R Alpha Lipoic Acid acts as an anti-aging nutrient by both its anti-oxidant properties and its anti glycation properties.

Clinical Uses for R Alpha Lipoic Acid

Large amounts of free radicals are created in tissue that has been injured by trauma or ischemia. Ischemia is caused by low oxygen levels from blood clots, stroke, etc. Treatment of this type of injury with anti-oxidants could be expected to reduce the effects of the damage. These types of injuries include heart attack, stroke, burns, sprains, strains, contusions, etc. The treatment of some of these entities with alpha lipoic acid have been documented in the literature and some have not.

Because alpha lipoic acid helps to conserve and increase production of glutathione, it may be beneficial in treating certain diseases that affect the liver. These include exposure to various toxins, alcoholic liver disease, aminita mushroom poisoning, hepatitis, etc.

Alpha lipoic acid is beneficial to individuals with type II diabetes. First, it improved the overall control of blood sugar and reduced blood sugar and insulin levels. Second, its anti-oxidant and anti-glycation effects reduce the damage caused by high blood sugar levels.

Alpha lipoic acid acts as an anti-oxidant, anti-glycation agent, blood sugar normalizer, mitochondria activator and glutathione enhancer. All of these effects counter the effects of a variety of diseases and conditions including but not limited to diabetes, pre-diabetes, neuropathy and inflammatory diseases and conditions.

Dosage of R Alpha Lipoic Acid

As a nutritional supplement, doses of 50 to 100 mg. per day have been recommended. As a Therapeutic agent, higher doses have been used. Dosages of 600 mg. per day have been used for preventing the damaging effects of hyperglycemia in diabetes. Larger doses, 1200 mg. given intravenously, have been used to treat aminita mushroom poisoning.

R Alpha Lipoic Acid Side Effects and Precautions

Always consult with your physician or pharmacist before combining supplements and medications.

Clinical research has shown no evidence of carcinogenic effects with administration of alpha lipoic acid. Serious side effects have not been observed, even at high doses. Minor side effects include skin reactions and gastrointestinal effects, such as nausea and vomiting. However, these effects have only been observed in a small percentage of subjects who received intravenous infusions of 1,200 mg or more of alpha lipoic acid per day.

Alpha Lipoic Acid supplementation may reduce glucose and insulin levels in diabetics. Diabetics taking insulin or glucose lowering drugs will have to monitor their sugar levels and adjust medication as needed. Diabetics taking alpha lipoic acid supplements should work with their physician to monitor and and adjust any medication that they may be using.

There is a lack of available data regarding use of alpha lipoic acid during pregnancy. During more than three decades of scientific research and clinical usage no serious adverse effects have been reported as a consequence of alpha lipoic acid supplementation. The LD50 is approximately 400-500 mg/kg after oral dosing in dogs.

High doses of alpha lipoic acid should be accompanied ty thiamine administration. An experiment done with rats showed that administration of alpha lipoic acid in extremely high doses (20 mg./kg) in the presence of a thiamine deficiency proved fatal. It would probably be beneficial to include a B-complex supplement in a regimen containing alpha lipoic acid.

Should you take R Alpha Lipoic Acid Supplements

The summary is that there is abundant evidence for using R alpha lipoic acid supplements when certain conditions including but not limited to diabetes, pre-diabetes, neuropathy, and some inflammatory conditions are present. There is a lack of evidence supporting the use of R alpha lipoic acid for life extension and health improvement by healthy individuals. When used, the R version should be used exclusively. Do your own extensive research, then make your choices based on medical advise.