Alpha Lipoic Acid

Pharmacological properties

alpha lipoic acid is synthesized in the body and acts as a coenzyme in the oxidative decarboxylation of α-keto acids; plays an important role in cell energy metabolism. in the amide form (lipoamide) is an essential cofactor of multi-enzyme complexes that catalyze the decarboxylation of alpha-keto acids of the Krebs cycle. Alpha-lipoic acid has inherent antitoxic and antioxidant properties, it is also able to restore other antioxidants, for example in diabetes mellitus. in patients with diabetes, alpha-lipoic acid reduces insulin resistance and inhibits the development of peripheral neuropathy. helps to reduce blood glucose and the accumulation of glycogen in the liver. alpha lipoic acid affects the metabolism of cholesterol, is involved in the regulation of lipid and carbohydrate metabolism, improves liver function (due to hepatoprotective, antioxidant, detoxification effects).

Pharmacokinetics When taken orally, alpha-lipoic acid is rapidly and almost completely absorbed in the digestive tract, metabolized mainly in the liver by oxidation of the side chains and conjugation. The drug is excreted by the kidneys (93–97%), mainly in the form of metabolites. T_½ - 10–20 minutes

Indications

As part of complex therapy for diabetic polyneuropathy, liver disease (hepatitis, cirrhosis), for chronic intoxications (for example, salts of heavy metals, mushrooms).

Application

The drug is administered orally in doses of 600 mg 1 time per day. the drug is taken without chewing, washed down with a small amount of liquid, in the morning 30–45 minutes before eating.

In cases of severe sensitivity disorders associated with diabetic polyneuropathy, treatment should preferably be started with parenteral administration of alpha-lipoic acid (Dialipon^® injection solution) for 2–4 weeks. Subsequently, oral administration of the drug in a dose of 600 mg 1 time per day should be continued.

The duration of treatment depends on the nature and course of the disease and is determined by the doctor.

Contraindications

• Hypersensitivity to alpha lipoic acid and other components of the drug; hereditary galactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome; During pregnancy and breastfeeding; childrens age (up to 18 years).

Side effects

General reactions of the body: hot flushes, sweating, shortness of breath.

From the side of the central nervous system: headache, dizziness, change or violation of taste perception, visual impairment.

From the digestive system: in some cases, dyspepsia (heartburn, nausea, vomiting, moderate abdominal pain, diarrhea) may develop, which disappears if you take the drug during or after a meal.

Metabolic disorders: hypoglycemia (due to improved glucose utilization).

Allergic reactions: pruritus, erythema, urticaria, petechial rash, dermatitis, eczema, rarely - systemic allergic reactions, up to anaphylactic shock.

special instructions

When treating patients with diabetes, frequent monitoring of blood glucose levels is necessary. in some cases, a dose adjustment of hypoglycemic agents is required to prevent hypoglycemia.

During treatment for polyneuropathy, due to regenerative processes, a short-term increase in sensitivity is possible, which is accompanied by paresthesia with a sensation of "crawling creeps."

Continuous alcohol consumption is a risk factor for the development of polyneuropathy and may reduce the effectiveness of Dialipon. Therefore, it is recommended to refrain from drinking alcohol during treatment with the drug. Thioctic acid binds metal ions, therefore, Dialipon should not be prescribed simultaneously with preparations containing metals (preparations of iron, magnesium, calcium), as well as with dairy products.

Use during pregnancy and lactation. There is no sufficient clinical experience with the use of the drug during pregnancy and lactation, therefore it is not recommended to prescribe it during these periods.

Children. Dialipon is not recommended for children under 18 years of age due to the lack of clinical experience with the drug in this category of patients.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. The drug does not affect the reaction rate when driving vehicles or working with other mechanisms, but in case of signs of side effects of the drug (see ADVERSE EFFECTS), it is necessary to refrain from driving vehicles and working with other mechanisms.

Interactions

It is possible to increase the hypoglycemic effect when using insulin or oral hypoglycemic agents. reacts with ionic metal complexes, for example cisplatin, can reduce its effectiveness and lead to a loss of cisplatin activity. forms sugar-soluble complexes with sugar molecules. is a metal chelator, therefore it can not be used with iron preparations.

Overdose

Cases of specific intoxication with alpha-lipoic acid were not reported, in addition, given the pharmacological effect of the substance, it should not be expected. with an overdose, nausea, vomiting, headache are possible.

When using alpha-lipoic acid in very high doses (from 10 to 40 g) in combination with alcohol, severe intoxication is observed, which can lead to death. Clinical signs of intoxication were manifested in the form of a psychomotor disorder or fainting followed by generalized seizures and the development of lactic acidosis. Alpha-lipoic acid intoxication results in hypoglycemia, shock, rhabdomyolysis, hemolysis, disseminated intravascular coagulation, bone marrow suppression and organ failure.

In acute poisoning with alpha-lipoic acid, immediate hospitalization with general therapeutic measures of detoxification of the body (artificial respiration, vomiting, gastric lavage, activated charcoal, etc.) is indicated. To eliminate generalized seizures, lactic acidosis and other consequences of intoxication, one should be guided by the means of modern intensive care and a symptomatic approach to accelerate the excretion of alpha-lipoic acid. Further treatment is symptomatic.

Storage conditions

In the dark place at a temperature of no higher than 25 ° c.