Lipoic acid is a natural antioxidant and anti-inflammatory compound that protects the brain, helps with weight loss, improves diabetes, decreases the risk of cardiovascular disease and alleviates pain. And these are only some of the numerous benefits of this “universal antioxidant”. Read on to learn more about how lipoic acid helps increase your wellbeing.

Contents

Introduction

Lipoic acid (LA), also known as alpha-lipoic (ALA) acid, R-lipoic acid, or thioctic acid, is a disulphide-containing compound (R), found inside every cell of the body (R).

It is called the “universal antioxidant” (R).

Important functions of lipoic acid:

  • Lipoic acid acts as a powerful antioxidant both inside and outside of the cells (R, R).
  • Lipoic acid scavenges several reactive oxygen species (ROS) (R).
  • Lipoic acid helps to regenerate both fat and water soluble antioxidant vitamins (such as vitamins C and E) (R, R).
  • Lipoic acid improves sugar and fat metabolism (R).
  • Lipoic acid is an essential cofactor for mitochondrial respiratory enzymes that improves mitochondrial function (R). Lipoic acid exerts a “rejuvenating” impact on mitochondria by protecting them against the higher levels of ROS they produce during the aging process (R).
  • Lipoic acid also has anti-inflammatory action, independently of its antioxidant activity (R).

A healthy body makes enough lipoic acid to supply its energy requirements; therefore, there is no daily requirement for this supplement. However, several medical conditions appear to be accompanied by low levels of lipoic acid – specifically, diabetes, liver cirrhosis, and heart disease (R).

In Europe, lipoic acid is licensed for the treatment of diabetic neuropathy. It has been shown to enhance insulin sensitivity, improve microcirculation in the limbs, and reduce neuropathic symptoms (R, R).

Also, lipoic acid produced in the body decreases with age, which could increase free radical-induced damage. Lipoic acid supplementation in animal models can prolong life, has neuroprotective effects, and has positive effects against cancer (R).

The Lipoic Acid That I Recommend

Health Benefits of Lipoic Acid

lipoic acid
http://journal.frontiersin.org/article/10.3389/fphar.2011.00069/full

1) Lipoic Acid Acts as a Powerful Antioxidant

Lipoic acid neutralizes free radicals and associated oxidative cellular damage  (R, R).

Lipoic acid scavenges several reactive oxygen species (ROS) (R).

Lipoic acid also helps regenerate antioxidant vitamins C and E (R, R).

In addition, lipoic acid promotes the activity of other antioxidants such as glutathione and coenzyme Q10, which are two essential anti-aging health-promoting compounds (R).

Lipoic acid increases tissue GSH levels, which otherwise decline with age, by restoring glutathione peroxidase activity (R).

2) Lipoic Acid Can Help with Weight Loss

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In healthy overweight/obese women on a calorie-restricted diet, lipoic acid supplementation increases weight loss (R).

Even without dieting, lipoic acid can greatly improve glucose and fat metabolism. As a result, more of the sugars and fats in foods will be broken down and used for energy instead of being stored as fat. This will also cause the consumer to feel the need to eat less (R).

In several other studies with overweight or obese subjects, lipoic acid induced mild but significant weight loss accompanied by a reduction in waist circumference (R, R, R).

In obese patients with type 2 diabetes, people treated with lipoic acid lost significantly more weight and had lower triglyceride levels (R).

Lipoic acid inhibits the production of chemerin, a molecule that is associated with obesity and metabolic syndrome. This may be how lipoic acid helps combat obesity and diabetes (R).

3) Lipoic Acid Promotes Muscle Regeneration After Exercise

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Short-term lipoic acid supplementation can protect DNA and cells against exercise-induced oxidative stress (R), and increase muscle regeneration (R).

Lipoic acid supplementation decreases oxidative damage in the muscles in men who perform muscle-damaging exercises, regardless of whether they are trained or untrained (R, R).

By increasing blood total antioxidant capacity, lipoic acid protects DNA and fatty acids from oxidative stress due to exercise (R).

Lipoic acid helps shift chemicals inside the cells and cytokines towards favoring the regeneration of injured muscles (R). In physically active males, lipoic acid significantly elevates H2O2 but reduced NO generation before or after exercise. Lipoic acid increases IL-6 and IL-10 levels at 20 min after exercise and decreases IL-1β and TNF-α before and after exercise.

Lipoic acid, when co-ingested with creatine, enhances muscle total creatine content (R). This would help those wishing to gain muscle mass with creatine supplements to do it more efficiently.

4) Lipoic Acid Decreases Inflammation

Abnormal inflammatory responses contribute to diseases such as diabetes, Alzheimer’s disease and multiple sclerosis (R). Lipoic acid was shown to have an anti-inflammatory effect in subjects with multiple sclerosis (R), metabolic syndrome (R), and diabetes (R).

Lipoic acid can reduce inflammatory markers in subjects with organ transplants (R).

Lipoic acid alleviates acute inflammatory responses in animal models (R). (R).

In overweight/obese women, lipoic acid caused a greater reduction the marker of chronic inflammation CRP (R).

5) Lipoic Acid Prevents and Improves Diabetes

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Lipoic acid has beneficial effects both in the prevention and in the treatment of diabetes (R).

Lipoic acid has insulin-mimetic activity (R), in that it improves glucose handling/utilization (R).

In patients with type-2 diabetes, lipoic acid decreases blood glucose and improves insulin sensitivity (R, R, R), including in overweight adults with type 2 diabetes (R).

Glutathione, an important antioxidant, is usually decreased in diabetics. In children and adolescents with asymptomatic type 1 diabetes, lipoic acid increased glutathione (GSH) levels (R).

In type 2 diabetic patients, lipoic acid improved metabolic indices and erectile dysfunction. Lipoic acid supplementation reduced BMI, HbA1C, total cholesterol, HDL-cholesterol and triglycerides (R).

6) Lipoic Acid Helps with Diabetes-Associated Complications

People with diabetes are more prone to oxidative stress, which means there is an imbalance of free radicals to antioxidants. Oxidative damage plays a key role in the development of diabetes-associated disorders and diseases (R, R).

Lipoic acid has drawn considerable attention as an antioxidant for use in managing diabetic complications such as retinopathy, neuropathy and other vascular diseases (R).

Lipoic acid Helps with Neuropathies

In Europe, alpha-lipoic acid is licensed for the treatment of diabetic neuropathy (nerve damages due to high blood sugar in diabetics). It has been shown to enhance insulin sensitivity, improve microcirculation and reduce neuropathic symptoms (R, R).

Studies show that lipoic acid improves these nerve damage symptoms such as stabbing and burning pain, asleep numbness, and prickling sensations (R, R, R, R). Lipoic acid also improves the function of motor nerves and reduced blood glucose (R).

Lipoic acid is a well-tolerated and effective long-term treatment for diabetic neuropathy. In mild-to-moderate cases, lipoic acid treatment for four years improved symptoms and prevented progression of neuropathic impairments (R).

In type 1 diabetic patients with autonomic diabetic neuropathy (damages to the nerve that control vital functions of the autonomic nervous system, such as blood pressure and heart rate), lipoic acid improved systolic blood pressure, dizziness, instability upon standing, leg edema and erectile dysfunction (R).

In diabetics, lipoic acid improved cardiac autonomic neuropathy (R).

Lipoic Acid Prevents Cardiovascular Complications

People with impaired glucose metabolism have blood vessel damages and impaired blood vessel function. Lipoic acid can improve blood vessel function by decreasing oxygen-derived free radicals (R).

In adolescents with type 1 diabetes, lipoic acid improved blood vessel function (R).

In children and adolescents with asymptomatic type 1 diabetes, lipoic acid improved left ventricular (heart chamber that pumps the blood throughout the body) function, suggesting that it may help prevent cardiomyopathy (damage to the heart muscles) (R).

In aged type 2 diabetes complicated with acute brain infarction (tissue death from blood clots), lipoic acid significantly reduced the patient’s oxidative stress, blood glucose and cholesterol levels (R).

Elevated asymmetric dimethylarginine (ADMA) concentrations predict cardiovascular events in patients with type 2 diabetes. In patients with T2D, lipoic acid treatment reduces ADMA (R).

In patients with type 2 diabetes, lipoic acid increases vasodilatation (widening of blood vessels) in response to ACh (R).

7) Lipoic Acid Helps Combat Metabolic Syndrome

Lipoic acid reduces blood pressure and insulin resistance, improves cholesterol, and reduces body weight. These are all components of the metabolic syndrome (R).

In patients with metabolic syndrome, lipoic acid improves blood vessel cell function and reduces proinflammatory markers (R).

In obese subjects with impaired glucose tolerance, lipoic acid improved insulin sensitivity and decreased free fatty acids, triglycerides, total cholesterol, and LDL cholesterol. Lipoic acid also decreased proinflammatory markers and increased adiponectin (R).

Lipoic acid significantly reduced ROS and improved HDL cholesterol in men with metabolic syndrome, especially those treated with blood sugar-reducing drugs (R).

8) Lipoic Acid Helps Lower Blood Pressure

Lipoic acid may have a beneficial effect in preventing the development of hypertension (elevated blood pressure) by lowering the level of inflammatory cytokines in the blood, thus preventing pathological changes to blood vessel cells and normalizing changes in blood pressure (R).

Several clinical trials have shown that lipoic acid inhibits the overproduction of endothelin I, the main vasoconstrictor (narrower of blood vessels) (R). Furthermore, lipoic acid significantly increases the synthesis of NO, the main vasodilator (widener of blood vessels) (R).

Lipoic acid improves blood vessel cell function (R).

However, clinical studies show that lipoic acid is not very effective in lowering blood pressure on its own. However, it can more effectively reduce blood pressure when used in combination with other antioxidants such as L-carnitine (R).

A combination of lipoic acid with acetyl-L-carnitine reduced blood pressure and improved the function of various arteries (R).

9) Lipoic Acid Decreases Bad Cholesterol

Clinical studies confirm that lipoic acid reduces LDL cholesterol and triglycerides, but increases HDL (good) cholesterol (R).

10) Lipoic Acid Prevents Atherosclerosis

Many studies suggest the potential role of lipoic acid in prevention and treatment of atherosclerosis (hardening of the arteries) and related cardiovascular disease (R).

Lipoic acid improves blood vessel structure and function (R, R). Lipoic promotes anti-inflammatory and antithrombotic (blood clot-reducing) pathways, and increases nitric oxide-mediated vasodilatation (blood vessel widening) (R).

Lipoic acid can decrease atherosclerotic plaque burden (R).

Lipoic acid reduces circulating inflammatory risk markers, such as CRP and leukocyte (white blood cell) count in healthy overweight or obese women independently of weight loss (R).

Lipoic acid counteracts ROS, such as superoxide anions, normalizes NADPH oxidase activity, and can prevent Angiotensin II-induced macrophage, monocyte, and T cell infiltration (R).

Lipoic acid reduces NF-κB-mediated inflammatory responses (R).

Lipoic acid may also prevent LDL oxidation (R). Oxidized LDL is more detrimental to cardiovascular health.

One study indicates that lipoic acid may increase the atherogenicity of LDL, but when it’s combined with exercise, this atherogenic effect is abolished (R).

11) Lipoic Acid Protects the Brain

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Because of its antioxidant properties, lipoic acid acts as a potent neuroprotective agent. It promotes neuronal regeneration (R) and can combat neurodegenerative disease (R).

In rats, urgent lipoic acid treatment given after stroke has a significant neurorestorative effect and promotes long-term functional recovery through enhanced anti-inflammatory and antioxidant actions (R).

Another study in rats showed that lipoic acid reduces brain damage and increase survival rate after a stroke (R).

Among other mechanisms, lipoic acid improves brain function by increasing glutathione (GSH) (R).

12) Lipoic Acid Improves Alzheimer’s

Oxidative stress, inflammation, and increased cholesterol levels have been associated with Alzheimer‘s disease (AD) pathology (R). Lipoic acid helps with all of these.

When lipoic acid was given daily to patients with AD (receiving a standard treatment with cholinesterase inhibitors) the treatment led to a stabilization of cognitive functions (R).

In another study, in AD patients with dementia, lipoic acid slowed down the progression of the disease (R).

Similarly, a combination of omega-3 fatty acids + lipoic acid slowed cognitive and functional decline in AD (R).

Levels of acetylcholine (Ach) are significantly decreased in Alzheimer’s. Many of the drugs that are currently used to treat this disease work to increase Ach levels. In rats, it was shown that lipoic acid raises the level of acetylcholine (ACh) and choline acetyltransferase (ChAT, an enzyme that increases available acetylcholine levels) and decreased the activity of acetycholinesterase (AchE) in the brain (R).

13) Lipoic Acid May Help with Parkinson’s Disease

Parkinson’s disease is described as a disease with reduced dopamine function and loss neurons in the brain due to misfolded proteins, poor autophagy, increased oxidative stress and inflammation, and mitochondria dysfunction (R).

In a mouse model of Parkinson’s disease, lipoic acid improves motor dysfunction, protects against dopaminergic neurons loss, and decreases α-synuclein accumulation in the substantia nigra area of the brain. Further, lipoic acid inhibits the activation of nuclear factor-κB (NF-κB) and decreases pro-inflammatory molecules (R).

Lipoic acid reduces neuronal death in laboratory models of Parkinson’s disease (R).

14) Lipoic Acid Can Help Reduce Side Effects of Antipsychotics

Weight gain and other metabolic disturbances are major side effects of atypical antipsychotic drugs (AAPDs). In schizophrenia patients using AAPDs, lipoic acid reduced BMI (weight to height ratio) and total cholesterol levels (R).

Lipoic acid also promoted weight loss and reduced abdominal fat in overweight and clinically stable schizophrenia patients. Moreover, lipoic acid was well tolerated throughout the 12-week study (R).

Lipoic acid also improved metabolic risk factors in Schizophrenia patients. A study showed that lipoic acid increased adiponectin and decreased fasting glucose and aspartate aminotransferase (AST, a liver enzyme) (R).

15) Lipoic Acid is Beneficial in Multiple Sclerosis

Lipoic acid was shown to have anti-inflammatory effect in subjects with multiple sclerosis (MS) (R), and to improve their total antioxidant capacity (R).

Lipoic acid may prove useful in treating MS by inhibiting MMP-9 activity, interfering with T-cell migration into the brain/spinal cord (R), and reducing both Th1 and Th2 cytokines (R).

In a Russian study, lipoic acid reduced relapse frequency in multiple sclerosis patients and decreased corticosteroid use (R). Effects were further magnified by adding other antioxidants to the treatment.

Lipoic acid is highly effective at suppressing and treating MS in a mouse model (R).

16) Lipoic Acid Can Protect Your Eyes and Vision

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Oxidative stress increases with aging and conditions such as diabetes, and it can have detrimental effects on vision. Lipoic acid can help by counteracting oxidative stress in the eyes.

A study has shown that lipoic acid improves vision and other symptoms in patients with glaucoma (R).

Lipoic acid also improves the vision-related quality of life in patients with age-related macular degeneration (AMD) (R).

Lipoic acid inhibits cataract formation in animals, especially diabetes-related cataracts (R, R).

Lipoic acid reduces retinal cell death in mice with retinis pigmentosa – an inherited, degenerative eye disease (R).

17) Lipoic Acid Can Prevent Migraines

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Migraines have been linked to mitochondrial disorders (R) and oxidative stress (R). Lipoic acid helps with both.

In patients with migraine, lipoic acid has the ability to reduce the frequency, duration, and intensity of migraines (R).

Lipoic acid improved the effectiveness of the migraine drug topiramate. The combination of lipoic acid and topiramate was significantly more effective at decreasing the frequency and duration of migraines than the drug alone. In addition, lipoic acid helped reduced topiramate-related side effects (R).

18) Lipoic Acid Alleviates Pain

Lipoic acid improves the quality of life in patients with neuropathies. Significant reduction was observed in a number of pain parameters, such as intensity, burning, unpleasantness and superficial pain (R).

Lipoic acid reduced the postoperative incidence of pain in patients with carpal tunnel syndrome (R).

Lipoic acid decreased sciatic pain caused by a herniated disc. Patients on lipoic acid reported a decreased need for analgesia (R).

In patients with chronic neck pain, a combination of lipoic acid and superoxide dismutase (SOD) improved pain control and the efficacy of physiotherapy (R).

Lipoic acid administered together with gamma-linolenic acid (GLA) reduced symptoms and functional impairment in patients with carpal tunnel syndrome (R).

19) Lipoic Acid May Help with Ulcers and IBD

In rats, lipoic acid protects against alcohol-induced stomach ulcers (R).

In mouse models of IBD, lipoic acid suppresses diarrhea, inflammation, and reduced colon lining injuries (R).

Other studies also showed that lipoic acid effectively attenuates ulcerative colitis in mice (R, R). However, in one study in mice with mild ulcerative colitis, lipoic acid actually increased oxidative damage to the colon and liver (R).

20) Lipoic Acid Improves Sperm Quality

In infertile men, lipoic acid significantly increases total sperm count, sperm concentration, and motility levels (R).

21) Lipoic Acid May Help with High-Risk Pregnancies

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In high risk pregnancies, lipoic acid can speed up the return to normal pregnancy conditions and improve the conditions of both the mother and the fetus (R). Additionally, smaller number of miscarriages was recorded with lipoic acid supplementation (R).

Lipoic acid decreases inflammation in women with gestational diabetes (R).

Lipoic acid reduced cervical inflammation after a preterm labor episode (R).

22) Lipoic Acid Prevents Bone Loss

In postmenopausal women with osteopenia (low bone density), lipoic acid slightly increased bone mineral density (BMD) (R).

Several laboratory studies showed that lipoic acid inhibits inflammation induced bone loss (R, R, R).

In female rats with osteopenia, lipoic acid not only stopped the bone resorption, but stimulated its formation (R).

23) Lipoic Acid May Improve Osteoarthritis

Lipoic acid decreased inflammation and ameliorated cartilage degeneration in rats with osteoarthritis (R).

24) Lipoic Acid Removes Toxic Metals from the Body

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Lipoic acid can chelate (bind to) toxic metals and neutralize them (R, R). This can protect the liver, the kidneys, and the nervous system.

Lipoic acid protects cells from cadmium (Cd)-induced toxicity by activating Nrf2 and regenerating GSH (R).

Lipoic acid protects against Cd-induced oxidative stress and kidney cell death in rats (R).

Lipoic acid attenuates liver damage caused by copper nanoparticles in rats(R).

In rats, administration of lipoic acid together with zinc and calcium ameliorated lead (Pb) toxicity, and decreased lead body burden to near-normal. Lipoic acid does this by preventing the accumulation of lead within the blood and tissues (R).

25) Lipoic Acid Counters Other Toxic Compounds

Dimethylnitrosamine (DMN) is a waste product of several industrial processes. Lipoic acid reduces kidney damage caused by this chemical in male mice (R).

Lipoic acid protects against polychlorinated biphenyl (PCB)-induced testicular toxicity in male rats (R).

Lipoic acid reduced methylmercury-induced brain injury in rats (R).

Lipoic acid reduces nicotine-induced lung and liver damage in rats (R).

Lipoic acid attenuates antimycin A-induced cell toxicity (R).

26) Lipoic Acid Promotes Wound Healing

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Hyperbaric oxygen therapy is used as a treatment for wounds that won’t heal as a result of diabetes or radiation injury. Lipoic acid accelerates wound repair in patients affected by chronic wounds undergoing hyperbaric oxygen (HBO) therapy (R, R, R).

27) Lipoic Acid is Beneficial for the Skin

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Lipoic acid increased the thickness (R) and decreased the roughness and photoaging of skin in older women (R).

Lipoic acid reverses skin damage caused by cigarette smoke (R).

28) Lipoic Acid Fights Cancer

Cell-based and animal model studies have shown that lipoic acid inhibits the initiation and promotion stages of cancer (R).

Lipoic acid-treated lung cancer cells had a decreased ability to survive (R).

Lipoic acid inhibits breast cancer cell proliferation (R).

Lipoic acid also increased the susceptibility of lung cancer cells to cisplatin, etoposide and paclitaxel-induced cell death (R).

29) Lipoic Acid May Increase Lifespan

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Lipoic acid extends the life span of adult flies (R) and worms (R).

The situation in mice is more complex, as the conclusions from the literatures are mixed. Lipoic acid may decrease (R), increase (R), or have no impact on the lifespan (R).

A study showed that while lower doses of lipoic acid increased the total life span in mice, high doses decreased it (R).

It is well known that dietary restriction extends lifespan. When mice were first exposed to dietary restriction, and then allowed to feed as desired, the beneficial effect of dietary restriction was abolished. However, when mice were supplemented with lipoic acid in the second phase, the beneficial effect of dietary restriction on longevity was maintained (R).

Lipoic acid may improve longevity by:

  • Fighting free radicals. Aging and reduced longevity are due in part to the action of free radicals. Lipoic acid is effective in protecting against the damage caused by the free radicals (R).
  • Rejuvenating mitochondria. Feeding old rats with acetyl carnitine and lipoic acid for a few weeks restored mitochondrial function and lowered oxidants to the level of young rats (R).
  • Increasing telomerase. Lipoic acid may increase telomerase (R), thereby increasing telomere length and reversing the aging process.

30) Other Conditions in Which Lipoic Acid is Beneficial:

Because of its antioxidant and anti-inflammatory effects, lipoic acid is beneficial in many diverse conditions, whether it improves the disease directly, or metabolic and oxidative stress indices. Some of the conditions are listed below.

  • Hypothyroidism: In patients with subclinical hypothyroidism, lipoic acid improves endothelial function, by decreasing oxygen-derived free radicals (R).
  • HIV infection: In human immunodeficiency virus (HIV)-infected subjects with a history of unresponsiveness to highly active antiretroviral treatment, lipoic acid increased glutathione levels and enhanced or stabilized lymphocyte proliferation (R).
  • Cystinuria: Lipoic acid inhibits cystine stone formation in mice (R).
  • Liver Surgery: Lipoic acid reduced ischemia/reperfusion injury of the liver in humans undergoing liver surgery (R).
  • Heart Surgery: In patients with coronary heart disease and those planned for coronary artery bypass graft operation, lipoic acid significantly decreased inflammation when blood is removed from the body (extracorporeal circulation) (R).
  • High-fructose corn syrup- caused pancreatic damage: Lipoic acid ameliorated metabolic changes and pancreatic lesions (R).
  • Peripheral Artery Disease: 3 months of lipoic acid supplementation improved walking tolerance and delayed pain onset in peripheral arterial disease (R).
  • Acute Coronary Syndrome: Lipoic acid ameliorates oxidative stress in patients with confirmed acute coronary syndrome (ACS) (R).
  • Takotsubo syndrome: Takotsubo syndrome is a form of stress-induced heart muscle damage. Lipoic acid treatment improves the innervation of adrenergic nerve cells in the hearts of patients with Takotsubo syndrome (R).
  • Heart Failure: Lipoic acid effectively decreases heart cell death (R, R), can prevent progressive heart remodeling and even improve heart function (R).
  • Olfactory Loss: Infections of the upper respiratory tract sometimes result in the loss of the sense of smell. Lipoic acid improves olfactory function (R).
  • Burning Mouth Syndrome: A single study indicates significant improvement upon treatment with lipoic acid (R), while other studies found no significant effect (R, R, R).
  • Idiopathic dysgeusia: In patients with idiopathic dysgeusia, an altered perception of taste, lipoic acid caused significant symptomatic improvements (R).
  • Sickle Cell Disease: In patients with sickle cell disease, lipoic acid treatment protected a subset of patients from oxidative damage to fat and proteins (R).
  • Polycystic ovary syndrome: Lipoic acid together with d-chiro-inositol (DCI) improved clinical and metabolic health in women with polycystic ovary syndrome (R). Supplementation of myoinositol and lipoic acid improved reproductive outcome and metabolic profiles in PCOS women undergoing in vitro fertilization (R).
  • Chronic Spinal Cord Injury: In men with chronic spinal cord injury, lipoic acid reduced fasting blood sugar, body weight, BMI, waist circumference and blood pressure. Lipoic acid also decreased food intake (R).

Natural Sources

  • Vegetables (spinach, broccoli, tomato) (R).
  • Meat (kidney, liver, heart) (R).

Dosage

Recommended oral therapeutic dosages of lipoic acid range from 600-1800 mg daily (R). Studies show that increased dosage is also followed by increased side effects.

Oral lipoic acid has a limited bioavailability of about 30% (R). Studies show that there is significant inter-subject variability in peak blood lipoic acid concentrations, due to individual differences in gut absorption (R).

Supplements

Life Extension Super R-Lipoic Acid

AOR High dose lipoic acid

Potential Risks and Side Effects

Urticaria and itching are the most common adverse events, but they are generally mild and transient (R).

Lipoic acid is also associated with a dose-dependent increase in nausea, vomiting, and vertigo (R). Higher doses of 1200 mg and 1800 mg have more frequent adverse effects (R). An oral dose of 600 mg once daily appears to provide the optimum risk-to-benefit ratio (R).

This is particularly the case in the elderly population, where 600 mg dose was well tolerated, but higher doses caused intolerable flushing and intolerable upper gastrointestinal side effects. However, subjects taking gastrointestinal prophylaxis medications had no upper gastrointestinal side effects (R).

Lipoic acid (possible overdose) can cause refractory convulsions in children (R).

One study in mice suggests that prophylactic and abundant intake of lipoic acid causes fatty liver and liver injury (R). There is one recorded case of lipoic acid causing acute cholestatic hepatitis in humans (R). It may be prudent to monitor cholesterol and liver enzymes with long-term lipoic acid supplementation.

Finally, in rats, it was shown that lipoic acid reduces the absorption of iron. Lipoic acid supplementation could potentially trigger iron deficiency anemia (R). No such events have been reported in humans though.

Technical

Lipoic acid increases antioxidants and antioxidant enzymes:

Lipoic acid decreases markers of oxidative stress:

Lipoic acid decreases inflammation:

Lipoic acid improves fat metabolism:

  • Lipoic acid activates AMPK (R, R).
  • Lipoic acid modestly reduced nonesterified fatty acids (NEFA) (R).
  • Lipoic acid increases LDL receptor (LDL-R) (R).
  • Lipoic acid decreases PPARγ (R), C/EBPα, and C/EBPβ (R).
  • Lipoic acid increases SIRT1 (R)

Lipoic acid is beneficial in exercise:

  • Lipoic acid increases PDK4 (R).
  • Lipoic acid increases PPARβ (PPARD) (R).

Lipoic acid is beneficial for the cardiovascular system:

Lipoic acid improves brain function:

Lipoic acid protects cells and mitochondria:

Buying Lipoic Acid

FDA Compliance

The information on this website has not been evaluated by the Food & Drug Administration or any other medical body. We do not aim to diagnose, treat, cure or prevent any illness or disease. Information is shared for educational purposes only. You must consult your doctor before acting on any content on this website, especially if you are pregnant, nursing, taking medication, or have a medical condition.

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12 COMMENTS

  • Gustavo Fernando Lourenço

    Hello Joe. I need your help . Can my 6-year-old autistic child take a single dose of R-ALA that you recommended (the R-ALA of life extension) per day? is it 240mg in a single dose per day?

  • Mike C

    Berkson, B.M., MD, PhD is a pioneer in the use of Intravenous ALA in his Las Cruces, NM clinic to successfully treat a variety of conditions (see drberkson.com). He recommends the Alpha Lipoic Acid sold by Bio-Tech (simply called “Lipoic”) which is European Sourced. He makes no distinction between R-Lipoic and ALA. He does stress taking the ALA on an empty stomach and with a Mega B Complex vitamin. The metabolism of oral ALA is different when taken with food and less effective, he says. Google Berkson, BM for his peer reviewed articles on the effective use of ALA.

  • Mark shebuski

    Where is best place to get R lipoic acid

  • Matt

    I think no one is really answering this, because there are so many variables to the above comments/questions. I too am in this position, after having amalgam fillings removed and seeing a functional medicine doc.

    If I understand correctly, the biggest problem for most people is supplement regimens without actually looking at the heavy metal load/levels first. I’ve done this, and from what I can tell my levels aren’t really all that high, but I’m still hesitating on the doc’s recommendation to take ALA right away.

    Is there a certain Mercury/aluminum level you would consider safe to begin daily ALA regimine without worrying about the half life/cycling on and off?

  • Michelle

    Thanks Kathy!

  • Kathy Riener

    I have arthritis in my knee and without lipoic acid I needed a cane, it saved my life. My blood pressure is lower too. No longer take blood pressure medication

  • Michelle Chapman

    I’m very interested as well from the above concerns, I’m taking it for kidney health. Along with QoQ10

  • Larry Rotenberg

    Causes my blood glucose to spike 25% from 6 to 7.5

  • Alan

    Hi, what do you think about the therory of Andy Cutler? He says, that ALA in single doses is dangerous and leads to further poisoning.

    After I’ve read Cutler, I’m afraid to Alpha Lipoic Acid.

    1. Jerry

      Redistribution of mercury from single doses of ALA is a very real thing. I learned this the hard way using it two to three times per day close to fifteen years ago while in graduate school. It caused great exacerbation of MS and other autoimmune problems. This is generally ignored or missed by many people, including practitioners and scientists. The effects can be quite insidious and deeply damaging. Hopefully people like Joseph will take a look to consider this perspective.

      1. George

        I have doctor’s best Stabilized R-Lipoic acid. My intention is to use it as an antioxidant for my stimulant stack. How dangerous would it be to take a single dosage of it to test its effects on my body?

        If the main concern about ALA is heavy metal redistribution, what should I do to prevent it?

        I read somewhere that in order to avoid toxicity from heavy metal redistribution, you need to take ALA 3-4 times a day for 3 days, and then take a 3 days break.

        I am confused, and mostly because regular ALA has a 3 hours half-life, allegedly, while R-Lipoic acid (which is what I got) supposedly just 14 minutes? Does that mean I have to take even more frequent dosages with R-Lipoic Acid in order to avoid toxicity? And if yes, why does everyone keep recommending R-Lipoic Acid over ALA?

        Thanks for the help in advance.

    2. Shalom S Fisher

      I, too, am concerned due to Cutler’s warnings and listings on his site of cautionary tales of disasters associated with use of ALA by folks with mercury toxicity in particular finding that the mercury in their bodies is redistributed to their brains! I struggle with a number of heavy metals in excessive levels in my body, including mercury, cadmium, aluminum and lead, sadly. Would love to receive the many benefits listed in this post, if I could be certain that Cutler is not correct in his perception of ALA’s dangers.

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