Alpha-lipoic acid: benefits, dosage, contraindications

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Alpha-lipoic acid (ALA) is a powerful antioxidant whose chemical structure is similar to a vitamin. It is synthesized endogenously, mainly in the liver and other tissues, but can also be obtained through the diet. Yeast, liver, red meats, spinach, and broccoli are good sources of alpha-lipoic acid. Alpha-lipoic acid is an enzyme cofactor in metabolic and energetic pathways. It is involved at the mitochondrial level, which, combined with its antioxidant properties, gives it anti-aging qualities. It is primarily used in the management of diabetes, neuropathies, and also in the modulation of immunity and inflammation.

Other name(s) 

Lipoic acid

Scientific name(s)

alpha-lipoic acid

Family or group: 

Pseudovitamins


Indications

Rating methodology

EFSA approval.

Several clinical trials (> 2) randomized controlled with double blind, including a significant number of patients (>100) with consistently positive outcomes for the indication.
Several clinical trials (> 2) randomized controlled with double blind, and including a significant number of patients (>100) with positive outcomes for the indication.
One or more randomized studies or multiple cohorts or epidemiological studies with positive outcomes for the indication.
Clinical studies exist but are uncontrolled, with conclusions that may be positive or contradictory.
Lack of clinical studies to date that can demonstrate the indication.


Oxidative stress
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Exogenous alpha-lipoic acid and its metabolite dihydrolipoic acid (DHLA) have antioxidant activity and can scavenge free radicals both intra and extracellularly. Additionally, alpha-lipoic acid is soluble in water and fats and can regenerate endogenous antioxidants, such as vitamin E, vitamin C, and glutathione, thereby preventing tissue and neuronal damage caused by oxidative stress, such as cerebral ischemia, brain damage caused by excitotoxic amino acids, mitochondrial dysfunction, muscle ischemia associated with peripheral arterial disease, diabetes, and diabetic neuropathy. The antioxidant effects of alpha-lipoic acid may also be beneficial in liver diseases linked to oxidative stress.

Posologie

posologieOral

posologie300 - 600 mg


Wrinkles
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Applying a night cream containing 5% alpha-lipoic acid is reported to reduce the appearance of fine lines and damage caused by sun exposure. Another study highlights the improvement in indicators of skin elasticity and thickness after the oral intake of ALA alongside vitamins, minerals, and a maritime pine bark extract.

Posologie

posologieTopical, Oral

populationAdults


Type 2 diabetes
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A meta-analysis of 16 small clinical studies on patients with type 2 diabetes shows that daily intake of 200 to 1,200 mg of alpha-lipoic acid for up to 52 weeks results in a slight improvement in glycemic figures, which is not clinically significant. Compared to placebo, alpha-lipoic acid reduced fasting blood glucose by 6 mg/dL, glycated hemoglobin (HbA1c) by 0.17%, triglyceride levels were reduced by 19 mg/dL.

Posologie

posologieOral

posologie200 - 1200 mg

duration52 weeks

populationAdults

Efficacy and safety of oral alpha-lipoic acid supplementation for type 2 diabetes management: a systematic review and dose-response meta-analysis of randomized trials
Enhancement of glucose disposal in patients with type 2 diabetes by alpha-lipoic acid.
Scientific Opinion on the substantiation of health claims related to alpha-lipoic acid and protection of body lipids from oxidative damage (ID 1434, 3134), maintenance of normal blood cholesterol concentrations (ID 3134), increased beta-oxidation of fatty acids (ID 3134), maintenance of normal blood glucose concentrations (ID 1435, 3162), and “regeneration of genes, regeneration of gene transcription and the influence to activity NF-kappa B” (ID 3133) pursuant to Article 13(1) of Regulation (EC) No 1924/2006
Oral administration of RAC-alpha-lipoic acid modulates insulin sensitivity in patients with type-2 diabetes mellitus: a placebo-controlled, pilot trial.
Glycemic and oxidative status of patients with type 2 diabetes mellitus following oral administration of alpha-lipoic acid: a randomized double-blinded placebo-controlled study.
Alpha-lipoic acid (ALA) supplementation effect on glycemic and inflammatory biomarkers: A Systematic Review and meta-analysis.
Effect of alpha-lipoic acid on blood glucose, insulin resistance and glutathione peroxidase of type 2 diabetic patients.
Improvement of insulin-stimulated glucose-disposal in type 2 diabetes after repeated parenteral administration of thioctic acid.
Alpha-lipoic acid treatment decreases serum lactate and pyruvate concentrations and improves glucose effectiveness in lean and obese patients with Type 2 diabetes.
The effects of lipoic acid and a-tocopherol supplementation on the lipid profile and insulin sensitivity of patients with type 2 diabetes mellitus: a randomized, double-blind, placebo-controlled trial.

Metabolic Syndrome
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The increase in inflammatory markers, particularly TNF-α, could promote insulin resistance and alter cytokine expression in adipose tissues, which is considered a major link between metabolic syndrome and insulin resistance. ALA supplementation may reduce inflammatory markers by trapping free radicals. Results from a meta-analysis indicate that ALA supplementation significantly decreased levels of C-reactive protein, interleukin-6 (IL-6), and tumor necrosis factor alpha (TNF-α) (markers of inflammation) in patients diagnosed with metabolic diseases.

Posologie

posologieOral route

posologie300 - 600 mg


Properties


Antioxidant

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The antioxidant properties of alpha-lipoic acid (ALA) lie in its ability to capture free radicals and regenerate endogenous antioxidants: glutathione and vitamins C and E. ALA can protect lipids from oxidative damage and can also help maintain normal blood cholesterol levels.

Usages associés

Wrinkles, Diabetic neuropathy, Oxidative stress, Cardiovascular diseases, Dyslipidemia

Bioenergetic

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Alpha-lipoic acid plays an important role in burning fats to produce energy and in transporting fatty acids across the mitochondrial membranes (cellular organelle) where they are oxidized and transformed into energy.

Usages associés

Obesity

Anti-inflammatory

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Alpha-lipoic acid modulates the inflammatory response and can inhibit vascular inflammation. The anti-inflammatory effect has also been correlated in several studies with a decrease in pro-inflammatory cytokines (small proteins secreted by inflammatory cells) such as TNF alpha and IL6.

Usages associés

Diabetic neuropathy, Metabolic syndrome, Cardiovascular diseases

Hypoglycemic

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Alpha-lipoic acid helps lower blood glucose levels and regulate insulin resistance. Additionally, it has proven effective in protecting against protein glycation (a natural reaction caused by high sugar concentrations in the blood as seen in diabetes) and helps regulate the damage caused by end-glycation products. These glycation products, highly dangerous for the body, accumulate with age and thus contribute to the development of several diseases such as arteriosclerosis, nephropathy, and diabetic retinopathy.

Usages associés

Type 2 diabetes

Anti-aging

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ALA has shown positive effects in fighting certain forms of oxidation and inflammation, helping protect against age-related neurological declines. ALA is also a powerful antioxidant and, from this perspective, is considered an anti-aging ally.

Usages associés

Wrinkles

Chelator

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It has been demonstrated that alpha-lipoic acid chelates heavy metals. In animal research, it has been shown that alpha-lipoic acid increases hepatobiliary excretion of inorganic mercury by forming a stable complex.


Anticancer

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It has been demonstrated that alpha-lipoic acid induces apoptosis (programmed cell death) in human colon cancer cells in vitro. Additionally, ALA has shown antimutagenic activities in animal and human tumorigenic cell models, including breast cancer, melanoma, ovarian epithelium, and colon cancer by inhibiting inflammatory mediators, DNA fragmentation, and inhibiting metastasis.

Usages associés

Cancer


Safety dosage

Adult from 18 years: 200 mg - 1200 mg

Orally, alpha-lipoic acid is very well tolerated in humans up to a dose of 1200 mg/day with treatment durations of up to 4 weeks. It can also be applied topically for up to 12 weeks.


Interactions

Médicaments

Anticancer drugs: moderate interaction

The use of alpha-lipoic acid during chemotherapy is controversial. Antioxidants might reduce chemotherapy activity (including cyclophosphamide, chlorambucil, carmustine, busulfan, and thiotepa) by generating free radicals. However, some researchers hypothesize that antioxidants could make chemotherapy more effective by reducing oxidative stress that may interfere with the apoptosis (cell death) of cancer cells.

Antidiabetics: weak interaction

Theoretically, the use of alkylating agents can produce hypoglycemic effects in diabetic individuals.

Hormones: moderate interaction

Theoretically, administration of alpha-lipoic acid with thyroid hormone-based medications reduces their therapeutic effects.

Plantes ou autres actifs

Hypoglycemic: weak interaction

Theoretically, alpha-lipoic acid could have additive effects with plants that lower blood glucose levels. Herbs with hypoglycemic effects include devil's claw, fenugreek, garlic, horse chestnut, Panax ginseng, psyllium, and Siberian ginseng.


Precautions

Type 2 Diabetes: use with caution

Alpha-lipoic acid should be used with caution in diabetic individuals due to its hypoglycemic action.

Surgical Intervention: avoid

Theoretically, alpha-lipoic acid could cause excessive bleeding or interfere with blood glucose control if used perioperatively.


Contraindications

Child up to 12 years: prohibited

Alpha-lipoic acid is not recommended for children under 12 years of age.

Pregnant woman: prohibited

Alpha-lipoic acid is not recommended during pregnancy.

Breastfeeding woman: prohibited

Due to a lack of studies, avoid the use of lipoic acid during breastfeeding.

Vitamin B1 deficiency: prohibited

Alpha-lipoic acid should not be used in cases of thiamine deficiency (vitamin B1 deficiency in alcoholics, for example), unless this deficiency is treated.