GENERAL

• Sulfur-containing fatty acid (with carboxyl group) and thioalcohol (with thiol group)
• Present in mitochondria (“powerhouses” of our cells).
• Soluble in fat and water (therefore it can cross the blood-brain barrier)
• Endogenous synthesis is only possible in small quantities (from octanoic acid and L-cysteine)
• Occurs as (interchangeable)
• Dihydrolipoic acid DHLA (reduced form)
• Lipoic acid LA (oxidized form) as well as
• Component of the coenzymes lipoamide (oxidized) and dihydrolipoamide (reduced) à lipoamide = lipoic acid + lysine
• S- vs. R-alpha lipoic acid: R-alpha lipoic acid (RALA) is the natural, endogenous form, while S-alpha lipoic acid is the synthetic variant. However, only R-alpha lipoic acid has health-promoting effects, whereas S-alpha lipoic acid has no function or is rather detrimental to the body, as it counteracts the positive effects of RALA and can promote insulin resistance.

BENEFITS OF R-ALPHA-LIPOIC ACID AS SODIUM LIPOATE

Ordinary R-alpha lipoic acid is very unstable and often begins to decompose into an insoluble polymer during the processing. Therefore, we use a highly purified, stabilized R-alpha lipoic acid in the form of sodium R-lipoate.

This so-called Na-RALA is significantly more bioavailable (Studies on comparable products have shown a 21-fold increased bioavailability (determined) as a simple, unstabilized R-alpha lipoic acid, as measured by the maximum blood plasma concentration (Cmax), and is also 100% free of S-alpha lipoic acid. Furthermore, unlike the potassium salt (K-RALA), the sodium salt is completely water-soluble and therefore requires no excipients.

In contrast to the production of racemic alpha-lipoic acid, the additional processing steps required for the production of Na-RALA also ensure particularly thorough purification, so that the active ingredient is ultimately free of residues.

EFFECTS

a)    Lipoic acid acts as an antioxidant (non-enzymatic antioxidant) and synergistically supports other antioxidants:

b)    Lipoic acid regenerates other antioxidants:

c)    Lipoic acid plays a central role in the body's own detoxification process:

• Detoxification Phase I: Lipoic acid is involved in the disposal of radicals and reactive metabolites.
• Detoxification Phase II and III (chelation): Lipoic acid complexes metals such as iron, copper, mercury, and cadmium and is involved in their elimination.

d)    Lipoic acid and cofactor effects:

• Energy generation: Lipoic acid is a component of the coenzyme lipoamide.
• in the pyruvate dehydrogenase complex and (PDH)
• in the 2-oxoglutarate or α-ketoglutarate dehydrogenase complex (OGDC)
• Amino acid metabolism: Lipoic acid is a component of the coenzyme lipoamide.
• in the branched-chain α-ketoglutarate dehydrogenase complex (BCKDC) during the breakdown of branched-chain amino acids leucine, isoleucine and valine
• in the glycine cleavage system (GCS) during the breakdown of glycine
• in the 2-oxoadipate dehydrogenase complex during the degradation of lysine

INDICATIONS FOR RALA SUPPLEMENTATION

• Radical stress in general
• Pollutant detoxification (z.B. Heavy metal contamination
• nervous system (z.B. Dysfunction of peripheral nerves
• Polyneuropathy (including chemotherapy-induced CIPN)
• Alzheimer's disease, multiple sclerosis, Down syndrome
• Psychological stress (z.B. Stress, schizophrenia)
• Diabetes mellitus
• Promoting the conversion of carbohydrates into energy,
• Promotes glucose uptake into muscle tissue,
• Increased sensitivity of glucose to insulin
• Cardiovascular diseases (z.B. Arteriosclerosis)
• Eye diseases (z.B. Cataract)
• Liver diseases (z.B. Hepatitis C)
• Kidney dysfunction
• aging
• oncology
• Obesity

POSSIBLE SIDE END & INTERACTIONS

• 200 mg per kg of body weight is considered safe for long-term intake.
• In isolated cases, and especially with rapid parenteral (= infusion) administration: headache, shortness of breath, nausea, stomach upset and/or diarrhea are possible.
• Influence on thyroid function with a reduction in thyroid hormones, v.a. when T4 is administered concurrently (Source: Study Segermann J 1991: ALA reduces T4-induced T3 formation by 56%; University of Maryland: “Alpha-lipoic acid may lower levels of thyroid hormone.Blood hormone levels and thyroid function tests should be monitored closely in people taking thyroid hormones who are also taking alpha-lipoic acid")

The following interactions could appear:

• Chelation occurs with iron, magnesium, and calcium supplements when taken simultaneously – therefore, ensure a time interval of 1-2 hours.
• Weakening of the effect due to metal ion complex formation (z.B. Cisplatin, isoniazid, cycloserine, D-penicillamine)
• Increased effect of insulin and oral antidiabetic drugs at very high doses (leads to a drop in blood sugar)
• Sugar molecule complexes (z.B. Fructose, glucose and Ringer's solution)
• Solutions that react with SH groups or disulfide bridges

Insufficient data is available regarding:

Pregnant and breastfeeding women (only under strict indication!) as well as those with serious liver and kidney diseases. Therefore, its use should always be discussed with the treating physician.

CAUSES & CONSEQUENCES OF LIPOIC ACID DEFICIENCY

Possible causes

• Reduced intake (z.B. Nutritional deficiencies, absorption disorders)
• Increased consumption (z.B. (in case of illness)
• Synthesis disorder

Possible consequences

• Cell damage
• Diseases of the nervous system
• Impaired glucose utilization
• Kidney disease

DOSAGE

• The exact lipoic acid requirement in addition to diet and endogenous synthesis is unknown and depends on many factors (such as intake, synthesis, individual situation); the u.g. Ranges are taken from the current state of research.
• Dietary intake is insufficient for medical-therapeutic effects.
• Bioavailability is approximately 70% when taken orally; this can be significantly increased by adding bioenhancers such as pipern.
• Preventive dosage: 100-300 mg
• Therapeutic dosage: 600-1200 mg