GENERAL

• Sulfur-containing fatty acid (with carboxy group) and thioalcohol (with thiol group)
• Present in mitochondria (“power plants” of our cells)
• Soluble in fat and water (can therefore pass the blood-brain barrier)
• Autologous synthesis only possible in small amounts (from octanoic acid and L-cysteine)
• Occurs as (interconvertible)
• Dihydrolipoic acid DHLA (reduced form)
• Lipoic acid LA (oxidized form) and
• Component of the coenzymes lipoamide (oxidized) and dihydrolipoamide (reduced) à lipoamide = lipoic acid + lysine
• S- vs R-alpha lipoic acidR-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 actually harmful to the body, as it can counteract the beneficial effects of RALA and promote insulin resistance.

BENEFITS OF R-ALPHA-LIPOIC ACID AS SODIUM LIPOATE

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

This so-called Na-RALA is significantly more bioavailable (Studies on comparable products have shown 21-fold increased bioavailability (determined) as a simple, unstabilized R-alpha lipoic acid based on the maximum blood plasma concentration (Cmax) and is also 100% free of S-alpha lipoic acid. In contrast to 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 has an antioxidant effect (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:

• 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) in the degradation of branched-chain amino acids leucine, isoleucine and valine
• in the Glycine Cleavage System (GCS) during the degradation of glycine
• in the 2-oxoadipate dehydrogenase complex during the degradation of lysine

INDICATIONS FOR RALA SUPPLEMENTATION

• Radical exposure in general
• Pollutant detoxification (z.B. Heavy metal pollution)
• 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,
• Promoting 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)
• Renal dysfunction
• aging
• oncology
• Obesity

POSSIBLE SIDE EFFECTS & INTERACTIONS

• 200 mg per kg body weight is considered safe for long-term intake
• In isolated cases and especially with rapid parenteral (= infusion) administration: Head pressure, shortness of breath, nausea, stomach discomfort and/or diarrhea may occur
• Influence on thyroid function with lowering of thyroid hormones, v.a. if T4 is given at the same time (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 with iron, magnesium and calcium supplements when taken simultaneously – therefore ensure a time interval of 1-2 hours
• Weakening of the effect by metal ion complex formation (z.B. Cisplatin, isoniazid, cycloserine, D-penicillamine)
• Increased effect of insulin and oral antidiabetics 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

There is insufficient data regarding:

Pregnant and breastfeeding women (only under strict indication!), as well as those with serious liver and kidney diseases. Therefore, in these cases, the use of the medication should always be discussed with the attending physician.

CAUSES & CONSEQUENCES OF LIPOIC ACID DEFICIENCY

Possible causes

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

Possible consequences

• Cell damage
• Diseases of the nervous system
• Disturbance of glucose utilization
• Kidney diseases

DOSAGE

• The exact lipoic acid requirement in addition to diet and self-synthesis is not known and depends on many factors (such as intake, synthesis, individual situation); u.g. Ranges are taken from current studies.
• Intake through food is not sufficient 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