ALA Brochure- Alpha Lipoic Acid with Biotin

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. The Ideal Universal Antioxidant and Free Radical Scavenger

. Active in All Body Tissues and All Cellular Compartments

. Recycles Both Fat and Water-Soluble Antioxidant Vitamins

. Improves Sugar Metabolism and Energy Production

. Promotes the Incorporation of Cysteine into Glutathione

What is Alpha Lipoic Acid ?

What is Alpha Lipoic Acid ? Alpha Lipoic Acid (a.k.a. lipoate, thioctic acid, alpha-lipoic acid) is an antioxidant and a cofactor in the body's production of energy. It has vitamin-like roles in the body. Alpha Lipoic Acid is a cofactor in the multi-enzyme complex that catalyzes the last stage of the process called glycolysis. Glycolysis is the first step in converting blood sugar (glucose), obtained from carbohydrates and proteins, into an energy form that the body can use.

Alpha Lipoic Acid is not considered to be a vitamin because it is assumed that it can be synthesized by the body in small amounts from essential fatty acids and the amino acid cysteine. Although Alpha Lipoic Acid is found in foods, such as liver and yeast, there are no foods rich enough in Alpha Lipoic Acid to serve as good sources.

Alpha Lipoic Acid is referred to as a disulfide molecule because it contains two sulfur units occurring as thiols. A thiol consists of one sulfur and one hydrogen atom. Not only does Alpha Lipoic Acid act as an antioxidant itself, it also stimulates the production of glutathione, another thiol-containing molecule and the most important antioxidant made by the body.

Why the Universal Antioxidant?

Once inside cells, Alpha Lipoic Acid is converted to its more potent form, dihydrolipoic acid. Alpha lipoic acid is unique in that, like vitamin C, it is effective as an antioxidant in water-based phases such as blood; yet as dihydrolipoic acid, it is also effective in protecting fatty tissues and membranes, a role it shares with vitamin E. Thus, Alpha Lipoic Acid and dihydrolipoic acid function together as a universal antioxidant, meaning an antioxidant that quenches free radicals in both lipid and water-soluble portions of tissues and cells.

Alpha Lipoic Acid and dihydrolipoic acid are extremely powerful quenchers of hydroxyl, singlet-oxygen, peroxynitrite and other free radicals. Smog and many other sources of environmental toxins either create or lead to the creation of free radicals in the body.

Alpha Lipoic Acid Recycles Both Fat- and Water-Soluble Vitamins

Dihydrolipoic acid, which the body routinely manufactures from Alpha Lipoic Acid , functions as a powerful direct chainbreaking antioxidant halting runaway lipid peroxidation reactions. It enhances the antioxidant potency of other antioxidants (e.g. vitamins C and E) in both the water-based (cytosol interior) and lipid (membranous) portions of cells. Alpha Lipoic Acid directly recycles vitamin C and indirectly recycles vitamin E. This ability is both unique and highly significant.

Several other distinctive properties are characteristic of Alpha Lipoic Acid 's universal antioxidant properties. ALA increases glutathione levels in cells, in part by improving the body's ability to use the amino acid L-cysteine in synthesizing its supply of glutathione. It also maintains a normal ratio of reduced-to-oxidized coenzyme Q10, which is especially important to the health of the mitochondria, the energy factories of the cells. As a further benefit, as dihydrolipoic acid, Alpha Lipoic Acid is one of very few antioxidant molecules small enough to penetrate the mitochondria directly.

The reduction of Alpha Lipoic Acid to dihydrolipoic acid and the role of Alpha Lipoic Acid in the production of glutathione are two of its several vitamin-like physiologic functions.

Alpha Lipoic Acid Improves Sugar (Carbohydrate) Metabolism and Increases Muscular Energy

Alpha Lipoic Acid is an important component in the production of energy from carbohydrates. Lipoate is involved throughout the complex multi-enzyme process which catalyzes glucose (blood sugar) into energy.

As part of the glycolytic pathway, Alpha Lipoic Acid both stimulates insulin activity and reduces insulin resistance. Lipoic acid enhances the burning of glucose in obese laboratory animals in a manner comparable to, but independent of, insulin.

One study of adult diabetic patients showed that alpha lipoic acid increased cellular uptake and oxidation (burning) of glucose by about 50%. This is important for athletes as well as those who are overweight. The efficient burning of glucose is essential for the normal production of energy in the muscles, and impaired muscle-energy metabolism interferes with exertion. Similar improvements in energy metabolism have been found in the brain.

Alpha Lipoic Acid Has Special Delivery Requirements for Maximal Benefits

Because it doesn't accumulate in tissues, alpha lipoic acid has no toxicity in the amounts usually taken (see Usage and Safety below). Because it is distributed throughout the tissues, it is useful in a wide variety of conditions. It is particularly protective of the brain (the most sensitive organ to free radical damage) and the eyes. However, animal experiments have shown that this protective effect is highly dependent upon the timing and the form of administration.

Alpha Lipoic Acid also rapidly clears from the blood by action of the liver. It also must be transformed into dihydrolipoic acid for maximal benefits both as an antioxidant and as a glucose disposal agent. Pharmaceutically designed Sustained Release Delivery better meets the known pharmacokinetic demands of Alpha Lipoic Acid than do the usual tablet and capsule delivery forms.

Also, sustained release may be helpful to those who are affected by the very low pH (i.e. very acid quality) of Jarrow FORMULAS® Alpha Lipoic Acid when taken in regular dosage forms.

The Multiple Benefits of Alpha Lipoic Acid

. A natural antioxidant that has a high reactivity to specific free radicals, including oxygen radicals and ionizing metals such as iron.

. Well absorbed via the stomach and is easily supplemented orally. It does not accumulate in tissue, and therefore has no toxicity in the amounts taken to support blood sugar metabolism.

. Because it is distributed throughout all tissues, it is useful for a wide variety of tissues, particularly the protection of the brain, which is the most sensitive organ to free radical damage.

. Synergistically interacts with other antioxidants to regenerate both vitamins C and E and maintain the proper ratio of reduced-to-oxidized Co-Q10 in the mitochondria. Therefore, alpha lipoic acid can buffer periodic deficiencies in these and other antioxidants due to improper diet and/or elevated stress.

. Increases tissue levels of glutathione, one of the principal antioxidants that decline with age. Protects the mitochondria; mitochondrial decay is associated with aging.

. In addition to its benefits as an antioxidant, Alpha Lipoic Acid functions as a co-vitamin or coenzyme by enhancing the utilization and disposal of glucose.

The Importance of Biotin

Anyone likely to be severely biotin-deficient should take supplemental biotin if Alpha Lipoic Acid is used regularly. Since biotin (vitamin H) and Alpha Lipoic Acid are chemically similar and are transported into cells by the same mechanism, elevated dietary alpha lipoic acid can interfere with biotin absorption. Additionally, Alpha Lipoic Acid may decrease the efficacy of biotin's role in the function of certain enzymes. To prevent the possibility of biotin deficiency, all Jarrow FORMULAS' ALA products contain over 100% of the daily value of biotin.

Usage and Safety

No serious side effects have been associated to date with the ingestion of Alpha Lipoic Acid . Side effects are very rare, but include allergic skin reactions and possible hypoglycemia in diabetics as a consequence of improved glucose utilization with high levels of intake.

Note: Individuals who are diabetic, being treated for glucose control, pregnant or lactating should consult a health care professional before using this product.

One hundred milligrams supplemented once or twice a day is considered adequate for most purposes. Clinical studies typically have employed 300 mg taken twice daily.

Jarrow FORMULAS® Sustained Release Formula is intended to match the known metabolism of alpha lipoic acid in the body and may be helpful to those who suffer gastric distress from ordinary Alpha Lipoic Acid supplements due to the very low pH of the compound.

Pharmaceutical Controlled Release

Under normal circumstances, Alpha Lipoic Acid is taken up very rapidly from the gastrointestinal tract. Capsules and tablets release their contents into the system within less than a two hour period. As already noted, however, such rapid release leads to similarly rapid clearance by the liver.

Blood levels of Alpha Lipoic Acid quickly rise and fall to match this release and clearance pattern, leading to gaps in antioxidant coverage after only a few hours. By extending the release of Alpha Lipoic Acid , Jarrow FORMULAS® ALA Sustain 300 eliminates gaps in coverage, and ensures optimal antioxidant protection. Multi-hour protection matches the body's needs for continuous control of free radicals and other oxidants.

. The Ideal Universal Antioxidant and Free Radical Scavenger

References

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Radical Biology & Medicine (1995) 19:227-250.
Whiteman M, et. al. Protection against peroxynitrite-dependent
tyrosine nitration and alpha-antiproteinase inactivations by
oxidized and reduced lipoic acid. FEBS Letters (1996) 379:74-76.
Kagan VE, et. al. Dihydrolipoic acid, a universal antioxidant
both in the membrane and in the aqueous phase. Biochemical
Pharmacology (1992) 44:1637-1649.
Kagan VE, et. al. Recycling of vitamin E in human low density
lipoproteins. Journal of Lipid Research (1992) 33:385-397.
Dusse E, et. al. Influence of Alpha Lipoic Acid on intracellular
glutatione in vitro and in vivo. Arzneimittel-Forschung (1992)
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Gotz ME et. al. Effect of lipoic acid on redox state of coenzyme Q in
mice treated with 1-methyl-1-4-phenyl-1,2,3,4-tetrahydropyridine
and diethyl-dithiocarbamate. European Journal of Pharmacology
(1994) 266:291-300.
Haugaard N, Haugaard ES. Stimulation of glucose utilization by
thioctic acid in rat diaphragm incubated in vitro. Biochemica et
Biophysica Acta (1970) 222:583-586.
Jacob S, et. al. Enhancement of glucose disposal in patients
with type 2 diabetes by Alpha Lipoic Acid . Arzneimittel-Forschung
(1995) 45:872-874.
Henriksen EJ. et. al. Chronic thioctic acid treatment increases
insulin stimulated glucose transport activity in skeletal muscle of
obese zucker rats. Diabetes (Suppl.) (1994) 1:122A.
Barbirolli B, et. al. Lipoic (thioctic acid) increases brain energy
availability and skeletal muscle performance as shown by in vivo
31P-MRS in a patient with mitochondrial cytopathy. Journal of
Neurology (1995) 242:472-477.
Wolz P, Krieglstein J. Neuroprotective effects of Alpha Lipoic Acid
and its enantiomers demonstrated in rodent models of focal
cerebral ischemia. Neuropharmacology (1996) Mar, 35(3):69-75.

Source: Jarrow Formulas