Berlithion^® 300 (Tablets, Concentrate) Instructions for Use

ATC Code

A16AX01 (Thioctic acid)

Active Substance

Thioctic acid (BAN)

Clinical-Pharmacological Group

Drug with antioxidant action, regulating carbohydrate and lipid metabolism

Pharmacotherapeutic Group

Metabolic agent

Pharmacological Action

Thioctic (alpha-lipoic) acid is an endogenous antioxidant (binds free radicals) that is formed in the body during the oxidative decarboxylation of alpha-keto acids. As a coenzyme of mitochondrial multienzyme complexes, it participates in the oxidative carboxylation of pyruvic acid and alpha-keto acids.

It helps reduce blood glucose levels and increase liver glycogen content, as well as overcome insulin resistance. In terms of the nature of its biochemical action, it is similar to B vitamins. It participates in the regulation of lipid and carbohydrate metabolism, stimulates cholesterol metabolism, and improves liver function.

It has hepatoprotective, hypolipidemic, hypocholesterolemic, and hypoglycemic effects.

The use of the ethylenediamine salt of thioctic acid in solutions for intravenous administration (which has a neutral reaction) helps reduce the severity of adverse reactions.

Pharmacokinetics

Absorption and Distribution

After intravenous administration, the C_max is 25-38 µg/ml and is reached within 10-11 minutes, AUC is about 5 µg x h/ml.

V_d is about 450 ml/kg.

Metabolism and Excretion

It has a first-pass effect through the liver. Metabolites are formed as a result of side chain oxidation and conjugation. Thioctic acid and its metabolites are excreted in the urine (80-90%).

Indications

• Diabetic polyneuropathy;
• Alcoholic polyneuropathy.

ICD codes

Dosage Regimen

Concentrate

The daily dose is 300-600 mg (1-2 ampoules). 1-2 ampoules of the drug (12-24 ml of solution) are diluted in 250 ml of 0.9% sodium chloride solution and administered intravenously by drip over approximately 30 minutes.

At the beginning of the treatment course, the drug is administered intravenously for 2-4 weeks. Then, thioctic acid can be continued orally at a dose of 300-600 mg/day.

Tablets

Take orally 600 mg once a day, on an empty stomach, approximately 30 minutes before the first meal. The duration of the treatment course is determined individually by the doctor.

Adverse Reactions

From the central nervous system very rarely – seizures, diplopia; with rapid intravenous administration, sensations of heaviness in the head (increased intracranial pressure) and difficulty breathing are possible, which resolve on their own.

From the blood coagulation system very rarely – petechiae on the skin and mucous membranes, thrombocytopathy, hemorrhagic rash (purpura), thrombophlebitis.

From metabolism possible – hypoglycemia (due to improved glucose utilization).

Allergic reactions possible – urticaria, systemic allergic reactions up to anaphylactic shock.

Local reactions possible – burning at the injection site.

Contraindications

• Childhood (efficacy and safety have not been established);
• Pregnancy (insufficient experience with the use of the drug);
• Breastfeeding (insufficient experience with the use of the drug);
• Hypersensitivity to the components of the drug.

Use in Pregnancy and Lactation

The use of Berlithion^® 300 during pregnancy and lactation is contraindicated due to the lack of sufficient clinical data confirming the safety and efficacy of the drug in this category of patients.

Special Precautions

In patients with diabetes mellitus, constant monitoring of blood glucose concentration is necessary, especially at the initial stage of therapy. In some cases, it is necessary to reduce the dose of insulin or oral hypoglycemic drug to avoid the development of hypoglycemia.

Patients receiving Berlithion^® 300 should refrain from consuming alcohol.

Overdose

Symptoms headache, nausea, vomiting.

Treatment symptomatic. There is no specific antidote.

Drug Interactions

In vitro, thioctic (alpha-lipoic) acid interacts with ionic metal complexes (for example, with cisplatin). Therefore, with simultaneous use, a reduction in the effect of cisplatin is possible.

Berlithion^® 300 enhances the hypoglycemic effect of insulin and oral hypoglycemic agents.

With simultaneous use, ethanol and its metabolites may reduce the therapeutic activity of Berlithion^® 300.

Pharmaceutical interaction

Thioctic (alpha-lipoic) acid forms poorly soluble complex compounds with sugar molecules.

Berlithion^® 300 is incompatible with dextrose solutions, Ringer’s solution, as well as with solutions known to react with SH-groups or disulfide bridges.

Storage Conditions

List B. The drug should be stored out of the reach of children, protected from light, at a temperature not exceeding 25°C (77°F).

Shelf Life

The shelf life is 3 years.

Dispensing Status

The drug is dispensed by prescription.

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.