Octolipen^® (Tablets, Capsules, Concentrate) Instructions for Use

ATC Code

A16AX01 (Thioctic acid)

Active Substance

Thioctic acid

Clinical-Pharmacological Group

Drug with antioxidant action, regulating carbohydrate and lipid metabolism

Pharmacotherapeutic Group

Other agents for the treatment of gastrointestinal diseases and metabolic disorders

Pharmacological Action

It is an endogenous antioxidant that binds free radicals. Thioctic (alpha-lipoic) acid is involved in the mitochondrial metabolism of the cell; it functions as a coenzyme in the complex transformation of substances with a pronounced antitoxic effect.

They protect the cell from reactive radicals arising during intermediate metabolism or during the breakdown of exogenous foreign substances, and from heavy metals. Thioctic acid exhibits synergism with insulin, which is associated with increased glucose utilization.

In patients with diabetes mellitus, Thioctic acid leads to a change in the concentration of pyruvic acid in the blood.

Pharmacokinetics

When taken orally, it is rapidly and completely absorbed from the gastrointestinal tract. C_max is reached within 30 minutes after administration and is 4 µg/ml.

With intravenous administration of thioctic acid at a dose of 600 mg, C_max in blood plasma after 30 minutes is about 20 µg/ml.

Thioctic acid has a “first-pass” effect through the liver. Metabolite formation occurs as a result of side chain oxidation and conjugation. V_d is about 450 ml/kg.

Thioctic acid and its metabolites are excreted by the kidneys, predominantly as metabolites (80-90%), and a small amount is excreted unchanged. T_1/2 is 25 minutes. Total plasma clearance is 10-15 ml/min/kg.

Indications

Diabetic polyneuropathy. Alcoholic polyneuropathy.

ICD codes

Dosage Regimen

Capsules, Concentrate

Used orally and intravenously (by slow bolus or drip). The recommended dose is 600 mg/day. The method of application, treatment regimen, and duration of the treatment course are established individually, depending on the severity of the disease.

Tablets

Orally at a dose of 600 mg once a day.

The type and duration of the therapy course are determined by the doctor.

Adverse Reactions

Immune system disorders: very rarely – allergic reactions (skin rash, eczema, urticaria, skin itching); frequency unknown – anaphylactic shock, autoimmune insulin syndrome in patients with diabetes mellitus, which is characterized by frequent hypoglycemia in the presence of autoantibodies to insulin.

Metabolism and nutrition disorders: very rarely – hypoglycemia (due to improved glucose absorption), the symptoms of which include dizziness, increased sweating, headache, and visual impairment.

Nervous system disorders: often – dizziness; very rarely – change or impairment of taste sensations, “flushes”, convulsions.

Gastrointestinal disorders: often – nausea, vomiting; very rarely – abdominal pain, diarrhea.

Blood and lymphatic system disorders: after intravenous administration very rarely – petechial hemorrhages in the mucous membranes, skin; hemorrhagic rash (purpura), thrombocytopathy, hypocoagulation.

Hepatobiliary disorders: after intravenous administration very rarely – increased activity of liver enzymes.

Cardiac and vascular disorders: with rapid intravenous administration very rarely – thrombophlebitis, pain in the heart area, tachycardia.

Eye disorders: after intravenous administration very rarely – diplopia, blurred vision.

Local reactions: after intravenous administration very rarely – burning sensation at the injection site, frequency unknown – allergic reactions at the injection site (irritation, redness, or swelling).

General disorders and administration site conditions: with rapid intravenous administration very rarely – self-limiting increased intracranial pressure (feeling of heaviness in the head) and difficulty breathing, weakness.

Contraindications

Hypersensitivity to thioctic acid; pregnancy, lactation (breastfeeding); children and adolescents under 18 years of age.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding). If use during lactation is necessary, the issue of discontinuing breastfeeding should be considered.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

Intravenous administration of thioctic acid should be carried out with caution in elderly patients (over 75 years of age).

Special Precautions

In severe diabetic polyneuropathy, it is recommended to start treatment with parenteral administration of thioctic acid for 2-4 weeks, followed by the use of oral forms of thioctic acid.

During the use of thioctic acid in patients with diabetes mellitus, constant monitoring of blood plasma glucose concentration is necessary, especially at the initial stage of therapy. In some cases, it may be necessary to reduce the dose of insulin or oral hypoglycemic drugs to avoid the development of hypoglycemia. If symptoms of hypoglycemia occur (dizziness, increased sweating, headache, visual impairment, nausea), the use of thioctic acid should be stopped immediately.

Alcohol consumption reduces the effectiveness of treatment with thioctic acid. During therapy, patients should refrain from consuming alcohol throughout the entire course of treatment, and, if possible, during breaks between courses. Alcohol consumption during treatment with thioctic acid is also a risk factor for the development and progression of neuropathy.

Several cases of autoimmune insulin syndrome have been described in patients with diabetes mellitus during treatment with thioctic acid, which was characterized by frequent hypoglycemia in the presence of autoantibodies to insulin. The possibility of developing autoimmune insulin syndrome is determined by the presence of HLA-DRB1*0406 and HLA-DRB1*0403 haplotypes in patients.

Effect on ability to drive vehicles and operate machinery

During the use of thioctic acid, patients should exercise caution when driving vehicles and operating machinery, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

With simultaneous use of thioctic acid and cisplatin, a decrease in the effectiveness of cisplatin is noted.

Thioctic acid is capable of forming chelate complexes with metals; simultaneous administration with iron, magnesium, and calcium preparations should be avoided. It should be borne in mind that dairy products contain calcium. Therefore, it is also necessary to avoid the use of thioctic acid simultaneously with dairy products (due to their calcium content).

With simultaneous use of thioctic acid and insulin or oral hypoglycemic drugs, their action may be enhanced, so regular monitoring of blood glucose levels is recommended, especially at the beginning of therapy with thioctic acid. In some cases, a reduction in the dose of hypoglycemic drugs may be acceptable to avoid the development of hypoglycemia symptoms.

Thioctic acid enhances the anti-inflammatory effect of corticosteroids.

Ethanol and its metabolites weaken the effect of thioctic acid.

With sugar molecules, Thioctic acid forms poorly soluble complex compounds. Thioctic acid is incompatible with dextrose (glucose), fructose, Ringer’s solutions, as well as with solutions that react with disulfide or SH-groups.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.