Polition^® (Concentrate) Instructions for Use

Marketing Authorization Holder

Valenta Pharm, JSC (Russia)

Manufactured By

Novosibkhimpharm, JSC (Russia)

ATC Code

A16AX01 (Thioctic acid)

Active Substance

Thioctic acid (BAN)

Dosage Form

Polition®

Concentrate for solution for infusion 25 mg/1 ml: amp. 12 ml or 24 ml 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Concentrate for solution for infusion greenish-yellow in color, transparent, with a specific odor.

Excipients : 0.5 M trometamol (tromethamine**) solution – to pH 8.2-8.5, water for injections – to 1 ml.

* formed as a result of the interaction of thioctic (α-lipoic) acid – 25 mg and trometamol (tromethamine) – 28.5 mg.
** 0.5 M trometamol (tromethamine) solution is prepared from trometamol (tromethamine) and water for injections.

12 ml – dark glass ampoules (5) – contour cell packaging (1) – cardboard boxes.
12 ml – dark glass ampoules (5) – contour cell packaging (2) – cardboard boxes.
24 ml – dark glass ampoules (5) – contour cell packaging (1) – cardboard boxes.
24 ml – dark glass ampoules (5) – contour cell packaging (2) – cardboard boxes.

Clinical-Pharmacological Group

Drug regulating lipid and carbohydrate 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 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.

After 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 to a small extent 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 intravenously or orally. The recommended daily dose is 600 mg.

For intravenous infusion, administer the concentrate slowly as an intravenous bolus or by drip infusion.

For initial treatment of severe diabetic polyneuropathy, begin with a 2 to 4-week course of parenteral administration.

Following the initial intravenous course, transition to an oral formulation for maintenance therapy.

Determine the specific method of administration, treatment regimen, and duration of therapy individually based on disease severity.

Prepare the infusion solution by diluting the concentrate with 0.9% Sodium Chloride solution.

Use the prepared infusion solution immediately; do not store it.

Avoid mixing with other medications or infusion solutions except 0.9% Sodium Chloride.

Do not administer with dextrose (glucose), fructose, Ringer’s solution, or solutions that react with SH-groups.

In patients with diabetes mellitus, closely monitor blood glucose levels, especially during therapy initiation.

Adjust the dose of insulin or oral hypoglycemic agents as necessary to prevent hypoglycemia.

If symptoms of hypoglycemia occur, discontinue treatment immediately.

Administer intravenous doses with caution to elderly patients over 75 years of age.

Instruct patients to completely avoid alcohol consumption during the entire treatment course.

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 uptake), the symptoms of which include dizziness, increased sweating, headache, and visual impairment.

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

Gastrointestinal disorders frequently – 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 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

Use is contraindicated during pregnancy and lactation (breastfeeding). If use during lactation is necessary, 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 performed 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 consumption 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 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; concurrent 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.