Thioctacid^® HR (Tablets) Instructions for Use

Marketing Authorization Holder

Meda Pharma, GmbH & Co. KG (Germany)

Manufactured By

Rottapharm, Ltd. (Ireland)

ATC Code

A16AX01 (Thioctic acid)

Active Substance

Thioctic acid (BAN)

Dosage Form

Thioctacid® BV

Film-coated tablets, 600 mg: 30, 60 or 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets light green in color, oblong, biconvex.

Excipients: low-substituted hypromellose – 157 mg, hypromellose – 20 mg, magnesium stearate – 24 mg.

Film coating composition: hypromellose – 15.8 mg, macrogol 6000 – 4.7 mg, titanium dioxide – 4 mg, talc – 2.02 mg, aluminum lake based on quinoline yellow dye – 1.32 mg, aluminum lake based on indigo carmine – 0.16 mg.

30 pcs. – dark glass bottles (1) – cardboard packs.
60 pcs. – dark glass bottles (1) – cardboard packs.
100 pcs. – dark glass bottles (1) – cardboard packs.

Clinical-Pharmacological Group

Drug with antioxidant action, regulating carbohydrate and lipid metabolism

Pharmacotherapeutic Group

Metabolic agent

Pharmacological Action

It is an endogenous antioxidant that binds free radicals.

Thioctic (α-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 respect to 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 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 mainly in the form of 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

Administer orally or intravenously via slow bolus or drip infusion.

The recommended daily dose is 600 mg.

For severe diabetic polyneuropathy, initiate therapy with parenteral administration for 2-4 weeks.

Follow the initial intravenous course with oral tablet administration.

Take tablets on an empty stomach, at least 30 minutes before breakfast.

Do not take with food, as this can significantly reduce bioavailability.

Avoid concomitant intake with dairy products or mineral supplements containing calcium, magnesium, or iron.

Adjust the final treatment regimen, method of administration, and duration individually based on disease severity and patient response.

Monitor blood glucose levels closely in diabetic patients, especially at therapy initiation.

Reduce the dose of insulin or oral hypoglycemic agents if necessary to prevent hypoglycemia.

Discontinue use immediately if symptoms of hypoglycemia occur.

Administer intravenous formulations with caution in patients over 75 years of age.

Refrain from alcohol consumption throughout the entire treatment course.

Adverse Reactions

From the immune system: 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.

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

From the nervous system: often – dizziness; very rarely – change or disturbance of taste sensations, “flushes”, seizures.

From the digestive system often – nausea, vomiting; very rarely – abdominal pain, diarrhea.

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

From the liver and biliary tract: after intravenous administration very rarely – increased activity of liver enzymes.

From the cardiovascular system: with rapid intravenous administration very rarely – thrombophlebitis, pain in the heart area, tachycardia.

From the organ of vision: 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).

Other: 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 period (breastfeeding); childhood and adolescence under 18 years.

Use in Pregnancy and Lactation

Use is contraindicated during pregnancy and during the lactation period (breastfeeding).

If use is necessary during lactation, the issue of discontinuing breastfeeding should be decided.

Pediatric Use

Use is contraindicated 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

For 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 intake reduces the effectiveness of treatment with thioctic acid.

During therapy, patients should refrain from consuming alcohol throughout the entire course of treatment, and also, 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 development in patients with diabetes mellitus during treatment with thioctic acid have been described, 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 mechanisms

During the use of thioctic acid, patients should exercise caution when driving vehicles and mechanisms, 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 thioctic acid therapy.

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 action 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.