Itilokt® (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. Hepatoprotector
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 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. Cmax is reached within 30 minutes after administration and is 4 µg/ml.
With intravenous administration of thioctic acid at a dose of 600 mg, the Cmax in blood plasma after 30 minutes is about 20 µg/ml.
Thioctic acid has a “first-pass” effect through the liver. The formation of metabolites occurs as a result of oxidation of the side chain and conjugation. Vd is about 450 ml/kg.
Thioctic acid and its metabolites are excreted by the kidneys, mainly in the form of metabolites (80-90%), and in small amounts – unchanged. T1/2 is 25 minutes. Total plasma clearance is 10-15 ml/min/kg.
Indications
Diabetic polyneuropathy. Alcoholic polyneuropathy.
ICD codes
| ICD-10 code | Indication |
| G62.1 | Alcoholic polyneuropathy |
| G63.2 | Diabetic polyneuropathy |
| ICD-11 code | Indication |
| 8C03.0 | Diabetic polyneuropathy |
| 8D44.0 | Alcoholic polyneuropathy |
Dosage Regimen
| The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen. |
Administer a recommended dose of 600 mg once daily.
For severe diabetic polyneuropathy, initiate therapy with parenteral administration for 2-4 weeks.
Follow parenteral administration with a transition to oral forms for maintenance therapy.
Administer intravenous formulations by slow intravenous injection or as an intravenous infusion.
Avoid rapid intravenous injection to minimize the risk of local reactions and systemic adverse effects.
For intravenous infusion, dilute the concentrate only with 0.9% Sodium Chloride solution.
Do not mix or dilute with dextrose (glucose) solutions, Ringer’s solution, or other incompatible solutions.
Administer oral tablets on an empty stomach, at least 30 minutes before breakfast.
Do not take oral tablets simultaneously with dairy products or preparations containing calcium, magnesium, or iron.
Establish the exact treatment duration and regimen individually, based on disease severity and patient response.
In patients with diabetes mellitus, monitor blood glucose levels closely, especially during initial therapy.
Adjust the dose of insulin or oral hypoglycemic agents as necessary to prevent hypoglycemia.
Discontinue use immediately if symptoms of hypoglycemia occur.
Advise patients to completely abstain from alcohol consumption during the entire treatment course.
Exercise caution with intravenous administration in elderly patients over 75 years of age.
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 the 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 : frequently – dizziness; very rarely – change or impairment of taste sensations, “flushes”, convulsions.
From the digestive system frequently – 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, hyperemia, 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 (breastfeeding); children and adolescents under 18 years of age.
Use in Pregnancy and Lactation
Contraindicated for use during pregnancy and lactation (breastfeeding). If it is necessary to use during lactation, the issue of discontinuing breastfeeding should be decided.
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 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 drinking 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 the development of autoimmune insulin syndrome 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 preparations of iron, magnesium, and calcium 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 symptoms of hypoglycemia.
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) solutions, fructose, Ringer’s solution, 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.
Medical DisclaimerBrand (or Active Substance), Marketing Authorisation Holder, Dosage Form
Concentrate for solution for infusion 25 mg/1 ml: vial 12 ml or 24 ml 5 or 10 pcs.
Concentrate for solution for infusion 30 mg/1 ml: amp. 10 ml or 20 ml 5 or 10 pcs.
Marketing Authorization Holder
Grotex, LLC (Russia)
Dosage Forms
 |
Itilokt® | Concentrate for solution for infusion 25 mg/1 ml: vial 12 ml or 24 ml 5 or 10 pcs. |
| Concentrate for solution for infusion 30 mg/1 ml: amp. 10 ml or 20 ml 5 or 10 pcs. |
Dosage Form, Packaging, and Composition
Concentrate for solution for infusion in the form of a transparent or slightly opalescent solution, yellow or greenish-yellow in color.
| 1 ml | |
| Trometamol salt of thioctic acid | 39.7 mg, |
| Equivalent to thioctic acid content | 25 mg |
Excipients : trometamol – to pH 8.2-8.5, water for injections – up to 1 ml.
Theoretical osmolarity: 356 mOsm/l.
12 ml – dark glass vials (10) – cardboard packs.
12 ml – dark glass vials (5) – cardboard packs.
24 ml – dark glass vials (10) – cardboard packs.
24 ml – dark glass vials (5) – cardboard packs.
Concentrate for solution for infusion in the form of a transparent or slightly opalescent solution, yellow or greenish-yellow in color.
| 1 ml | |
| Trometamol salt of thioctic acid | 47.6 mg, |
| Equivalent to thioctic acid content | 30 mg |
Excipients : trometamol – to pH 8.2-8.5, water for injections – up to 1 ml.
Theoretical osmolarity: 427 mOsm/l.
10 ml – dark glass ampoules (5) – contour cell packs (1) – cardboard packs.
10 ml – dark glass ampoules (5) – contour cell packs (2) – cardboard packs.
10 ml – dark glass ampoules (10) – contour cell packs (1) – cardboard packs.
20 ml – dark glass ampoules (5) – contour cell packs (1) – cardboard packs.
20 ml – dark glass ampoules (5) – contour cell packs (2) – cardboard packs.
20 ml – dark glass ampoules (10) – contour cell packs (1) – cardboard packs.
Film-coated tablets, 600 mg
Marketing Authorization Holder
Grotex, LLC (Russia)
Dosage Form
|
Itilokt® BV | Film-coated tablets, 600 mg |
Dosage Form, Packaging, and Composition
Film-coated tablets
| 1 tab. | |
| Thioctic acid | 600 mg |
10 pcs. – contour cell packs – cardboard packs (10 pcs.) – Prescription only
10 pcs. – contour cell packs (10 pcs.) – cardboard packs (100 pcs.) – Prescription only
10 pcs. – contour cell packs (2 pcs.) – cardboard packs (20 pcs.) – Prescription only
10 pcs. – contour cell packs (3 pcs.) – cardboard packs (30 pcs.) – Prescription only
10 pcs. – contour cell packs (4 pcs.) – cardboard packs (40 pcs.) – Prescription only
10 pcs. – contour cell packs (5 pcs.) – cardboard packs (50 pcs.) – Prescription only
10 pcs. – contour cell packs (6 pcs.) – cardboard packs (60 pcs.) – Prescription only
10 pcs. – contour cell packs (7 pcs.) – cardboard packs (70 pcs.) – Prescription only
10 pcs. – contour cell packs (8 pcs.) – cardboard packs (80 pcs.) – Prescription only
10 pcs. – contour cell packs (9 pcs.) – cardboard packs (90 pcs.) – Prescription only
10 pcs. – vials – cardboard packs (10 pcs.) – Prescription only
100 pcs. – vials – cardboard packs (100 pcs.) – Prescription only
14 pcs. – contour cell packs – cardboard packs (14 pcs.) – Prescription only
14 pcs. – contour cell packs (10 pcs.) – cardboard packs (140 pcs.) – Prescription only
14 pcs. – contour cell packs (2 pcs.) – cardboard packs (28 pcs.) – Prescription only
14 pcs. – contour cell packs (3 pcs.) – cardboard packs (42 pcs.) – Prescription only
14 pcs. – contour cell packs (4 pcs.) – cardboard packs (56 pcs.) – Prescription only
14 pcs. – contour cell packs (5 pcs.) – cardboard packs (70 pcs.) – Prescription only
14 pcs. – contour cell packs (6 pcs.) – cardboard packs (84 pcs.) – Prescription only
14 pcs. – contour cell packs (7 pcs.) – cardboard packs (98 pcs.) – Prescription only
14 pcs. – contour cell packs (8 pcs.) – cardboard packs (112 pcs.) – Prescription only
14 pcs. – contour cell packs (9 pcs.) – cardboard packs (126 pcs.) – Prescription only
20 pcs. – vials – cardboard packs (20 pcs.) – Prescription only
30 pcs. – vials – cardboard packs (30 pcs.) – Prescription only
40 pcs. – vials – cardboard packs (40 pcs.) – Prescription only
50 pcs. – vials – cardboard packs (50 pcs.) – Prescription only
60 pcs. – vials – cardboard packs (60 pcs.) – Prescription only
7 pcs. – contour cell packs – cardboard packs (7 pcs.) – Prescription only
7 pcs. – contour cell packs (10 pcs.) – cardboard packs (70 pcs.) – Prescription only
7 pcs. – contour cell packs (2 pcs.) – cardboard packs (14 pcs.) – Prescription only
7 pcs. – contour cell packs (3 pcs.) – cardboard packs (21 pcs.) – Prescription only
7 pcs. – contour cell packs (4 pcs.) – cardboard packs (28 pcs.) – Prescription only
7 pcs. – contour cell packs (5 pcs.) – cardboard packs (35 pcs.) – Prescription only
7 pcs. – contour cell packs (6 pcs.) – cardboard packs (42 pcs.) – Prescription only
7 pcs. – contour cell packs (7 pcs.) – cardboard packs (49 pcs.) – Prescription only
7 pcs. – contour cell packs (8 pcs.) – cardboard packs (56 pcs.) – Prescription only
7 pcs. – contour cell packs (9 pcs.) – cardboard packs (63 pcs.) – Prescription only
70 pcs. – vials – cardboard packs (70 pcs.) – Prescription only
80 pcs. – vials – cardboard packs (80 pcs.) – Prescription only
90 pcs. – vials – cardboard packs (90 pcs.) – Prescription only
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