Thiolepta® (Tablets, Solution, Concentrate) Instructions for Use
ATC Code
A16AX01 (Thioctic acid)
Active Substance
Thioctic acid (BAN)
Clinical-Pharmacological Group
Drug regulating lipid and carbohydrate metabolism
Pharmacotherapeutic Group
Other drugs for the treatment of gastrointestinal diseases and metabolic disorders; other drugs 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. Cmax is reached within 30 minutes after administration and is 4 µg/ml.
After intravenous administration of thioctic acid at a dose of 600 mg, Cmax 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. Vd 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. 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 total daily dose of 600 mg orally or intravenously.
For intravenous administration, inject slowly as a bolus or by infusion to minimize adverse reactions.
Initiate treatment of severe diabetic polyneuropathy with a 2 to 4-week course of intravenous therapy.
Transition to oral forms for maintenance therapy following the initial intravenous course.
Adjust the method of administration, treatment schedule, and duration individually based on disease severity and patient response.
Administer oral doses on an empty stomach, at least 30 minutes before a meal, for optimal absorption.
Avoid concomitant intake with dairy products, calcium, magnesium, or iron supplements, as they can form insoluble complexes.
Monitor blood glucose levels closely in diabetic patients, especially during the initial phase of treatment.
Reduce the dose of insulin or oral hypoglycemic agents if necessary to prevent symptomatic hypoglycemia.
Exercise caution with intravenous administration in elderly patients over 75 years of age.
Discontinue use immediately if symptoms of hypoglycemia or other severe adverse reactions occur.
Advise patients to completely abstain from 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 absorption), 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, “flushes”, 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
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 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 discontinued 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, 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; 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 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.
Medical DisclaimerBrand (or Active Substance), Marketing Authorisation Holder, Dosage Form
Concentrate for solution for infusion 30 mg/1 ml: amp. 10 ml 5 or 10 pcs.
Marketing Authorization Holder
Canonpharma Production, CJS (Russia)
Manufactured By
Grotex, LLC (Russia)
Dosage Form
 |
Thiolepta® | Concentrate for solution for infusion 30 mg/1 ml: amp. 10 ml 5 or 10 pcs. |
Dosage Form, Packaging, and Composition
Concentrate for solution for infusion in the form of a transparent, yellow or greenish-yellow solution.
| 1 ml | |
| Meglumine thioctate* | 58.4 mg, |
| Equivalent to thioctic acid content | 30 mg |
* formed as a result of the interaction of thioctic acid 30 mg and meglumine 28.4 mg.
Excipients : macrogol 400 – 200 mg, meglumine – to pH 8.2-8.5 from 1.1 mg to 2.9 mg, water for injections – up to 1 ml.
10 ml – dark glass ampoules (5) – contour cell packs (1) – cardboard packs.
10 ml – dark glass ampoules (5) – contour cell packs (2) – cardboard packs.
Film-coated tablets, 300 mg: 10, 30, 50, 60, 90, 100, or 120 pcs.
Marketing Authorization Holder
Canonpharma Production, CJS (Russia)
Dosage Form
|
Thiolepta® | Film-coated tablets, 300 mg: 10, 30, 50, 60, 90, 100, or 120 pcs. |
Dosage Form, Packaging, and Composition
Film-coated tablets light yellow in color, round, biconvex.
| 1 tab. | |
| Thioctic acid | 300 mg |
Excipients : potato starch, Aerosil A-300 (colloidal silicon dioxide), primellose (sodium croscarmellose), calcium stearate, lactose, microcrystalline cellulose, castor oil, selecoat AQ-01812, hydroxypropyl methylcellulose (hypromellose), polyethylene glycol 400 (macrogol 400), polyethylene glycol 6000 (macrogol 6000), titanium dioxide, yellow iron oxide, quinoline yellow.
10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (5) – cardboard packs.
10 pcs. – contour cell packs (6) – cardboard packs.
10 pcs. – contour cell packs (9) – cardboard packs.
10 pcs. – contour cell packs (10) – cardboard packs.
15 pcs. – contour cell packs (2) – cardboard packs.
15 pcs. – contour cell packs (4) – cardboard packs.
15 pcs. – contour cell packs (6) – cardboard packs.
15 pcs. – contour cell packs (8) – cardboard packs.
30 pcs. – jars (1) – cardboard packs.
Film-coated tablets, 600 mg: 30 or 60 pcs.
Marketing Authorization Holder
Canonpharma Production, CJS (Russia)
Dosage Form
|
Thiolepta® | Film-coated tablets, 600 mg: 30 or 60 pcs. |
Dosage Form, Packaging, and Composition
Film-coated tablets brownish-yellow in color, oval, biconvex; on the cross-section – light yellow in color.
| 1 tab. | |
| Thioctic acid (alpha-lipoic) | 600 mg |
Excipients : calcium stearate – 31 mg, potato starch – 27.4 mg, colloidal silicon dioxide – 27.6 mg, sodium croscarmellose – 49.6 mg, lactose monohydrate – 232 mg, povidone K-30 – 65.2 mg, microcrystalline cellulose (type 101) – 167.2 mg.
Film coating composition: Opadry 20A220053 yellow – 40 mg, including hypromellose (hydroxypropyl methylcellulose) – 11.6 mg, hypromellose (hydroxypropyl methylcellulose) – 11.6 mg, yellow iron oxide dye – 1.652 mg, sunset yellow FCF dye – 0.008 mg, talc – 4 mg, titanium dioxide – 10.74 mg.
10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (6) – cardboard packs.
15 pcs. – contour cell packs (2) – cardboard packs.
15 pcs. – contour cell packs (4) – cardboard packs.
30 pcs. – jars (1) – cardboard packs.
60 pcs. – jars (1) – cardboard packs.
Solution for infusion 12 mg/ml: 50 ml fl. 1 or 10 pcs.
Marketing Authorization Holder
Canonpharma Production, CJS (Russia)
Labeled By
FIRMA FERMENT, LLC (Russia)
Dosage Form
|
Thiolepta® | Solution for infusion 12 mg/ml: 50 ml fl. 1 or 10 pcs. |
Dosage Form, Packaging, and Composition
| Solution for infusion | 1 ml |
| Thioctic acid | 12 mg |
50 ml – bottles (1) – cardboard packs.
50 ml – bottles (10) – cardboard packs.
![Thiolepta® [Tablets, Solution, Concentrate] 1](https://www.medixlife.com/wp-content/uploads/Medixlife_favi_512.png "Thiolepta® [Tablets, Solution, Concentrate] 2")