Thiogamma® turbo

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT THIOGAMMA® Turbo (THIOGAMMA® Turbo)

Composition:

Active substance: α-lipoic acid;

50 ml of solution contain 1.2% meglumine salt of α-lipoic acid 1167.7 mg (equivalent to 600 mg of α-lipoic acid);

Excipients: meglumine, macrogol 300, water for injections.

Pharmaceutical form. Infusion solution.

Main physicochemical properties: yellowish or greenish-yellow solution.

Pharmacotherapeutic group.
Agents affecting the digestive system and metabolic processes. ATC code A16AX01.

Pharmacological properties.

Pharmacodynamics.

Alpha-lipoic acid is a substance synthesized in the body and acts as a coenzyme in the oxidative decarboxylation of α-keto acids; it plays an important role in cellular energy production. It promotes reduction of blood glucose levels and increases hepatic glycogen content. Deficiency or impaired metabolism of alpha-lipoic acid (thioctic acid) due to intoxications or excessive accumulation of certain breakdown products (e.g., ketone bodies) leads to impaired aerobic glycolysis. Alpha-lipoic acid can exist in two physiologically active forms (oxidized and reduced), both of which possess antitoxic and antioxidant properties. Alpha-lipoic acid affects cholesterol metabolism, participates in the regulation of lipid and carbohydrate metabolism, and improves liver function (due to hepatoprotective, antioxidant, and detoxifying effects). Pharmacologically, alpha-lipoic acid is similar to the B-complex vitamins.

Pharmacokinetics.

Alpha-lipoic acid undergoes significant changes during first-pass metabolism in the liver. Considerable interindividual variability in systemic availability of alpha-lipoic acid is observed. It is excreted primarily by the kidneys, mainly as metabolites. Metabolite formation occurs through side-chain oxidation and conjugation. The elimination half-life of the medicinal product ThioGama® Turbo from blood serum is 10–20 minutes.

Clinical characteristics.

Indications.

Impaired sensation in diabetic polyneuropathy.

Contraindications.

Hypersensitivity to α-lipoic acid or to other components of the drug.

Interaction with other medicinal products and other forms of interaction.

Thioctic acid may enhance the glucose-lowering effect of insulin and/or other antidiabetic agents; therefore, regular monitoring of blood glucose levels is recommended, especially at the beginning of thioctic acid (α-lipoic acid) therapy. In individual cases, to prevent symptoms of hypoglycemia, a reduction in the dose of insulin or oral antidiabetic agent may be required.

Ethanol reduces the therapeutic efficacy of α-lipoic acid.

Warning: regular alcohol consumption is a significant risk factor for the development and progression of neuropathy symptoms and thus may negatively affect the treatment process. Therefore, patients with diabetic neuropathy are generally advised, if possible, to abstain from alcohol consumption. Restrictions on alcohol consumption also apply during treatment-free intervals.

Special precautions for use.

When administering Thioctacid® Turbo, light-protective black bags must be used (see cardboard packaging), which are placed over the vial during intravenous administration of the drug.

The main factor in effective treatment of diabetic polyneuropathy is optimal control of the patient's blood glucose level.

When Thioctacid® Turbo is administered parenterally, there is a risk of allergic reactions, including anaphylactic shock; therefore, patients should be monitored for such reactions. If symptoms such as itching, nausea, or malaise occur, administration of the drug must be immediately discontinued and appropriate therapeutic measures initiated.

In some patients with poorly controlled or uncontrolled diabetes mellitus and worsening general health, severe anaphylactic reactions associated with the use of Thioctacid® Turbo may develop.

During treatment of polyneuropathy, due to regenerative processes, transient increased sensitivity may occur, accompanied by paresthesia with sensations of "crawling ants."

Certain limitations for intravenous administration of α-lipoic acid preparations exist in elderly patients (over 75 years of age).

Autoimmune insulin syndrome has been reported during treatment with α-lipoic acid. Patients with certain human leukocyte antigen (HLA) genotypes, such as HLA-DRB1*04:06 and HLA-DRB1*04:03, are more susceptible to developing autoimmune insulin syndrome (a hormonal disorder affecting blood glucose regulation, characterized by pronounced hypoglycemia) during treatment with α-lipoic acid. The HLA-DRB1*04:03 allele (odds ratio for susceptibility to autoimmune insulin syndrome 1.6) is primarily found in Caucasians and is more prevalent in Southern Europe than in Northern Europe; the HLA-DRB1*04:06 allele (odds ratio for susceptibility to autoimmune insulin syndrome 56.6) is predominantly found in patients from Japan and Korea.

Autoimmune insulin syndrome should be considered in the differential diagnosis of spontaneous hypoglycemia in patients receiving α-lipoic acid.

Use during pregnancy or breastfeeding.

There is insufficient experience with the use of the drug during pregnancy or breastfeeding; therefore, it should not be administered during these periods.

Ability to influence reaction rate while driving or operating machinery.

Caution is required while using the drug when driving vehicles or engaging in other potentially hazardous activities requiring increased attention and rapid psychomotor reactions.

Dosage and Administration

The drug is administered directly from the vial (i.e., without diluent) as an intravenous infusion in adults at a dose of 600 mg per day (contents of 1 vial) over at least 30 minutes.

Since α-lipoic acid is light-sensitive, vials should be stored in the cardboard packaging until immediately before use.

At the beginning of treatment, the drug ThioGama® Turbo is administered intravenously. The treatment course lasts 2–4 weeks.

For subsequent therapy, oral formulations of α-lipoic acid are used at a daily dose of 300–600 mg.

Children

The efficacy and safety of the drug in children have not been established; therefore, it should not be prescribed to this age group of patients.

Overdose

Symptoms: Possible nausea, vomiting, and headache. When very high doses of 10 to 40 g of α-lipoic acid are taken in combination with alcohol, severe intoxication may occur, potentially leading to a fatal outcome. The clinical picture of poisoning initially manifests as psychomotor agitation or impaired consciousness, and subsequently progresses to generalized seizures and the development of lactic acidosis. Consequences of intoxication may include hypoglycemia, shock, rhabdomyolysis, hemolysis, acute necrosis of skeletal muscles, disseminated intravascular coagulation, bone marrow suppression, and multiorgan failure.

Treatment: In case of suspected overdose or intoxication (ingestion of 6000 mg in adults or >50 mg/kg body weight in children), immediate hospitalization is indicated, along with standard supportive measures (e.g., induced emesis, gastric lavage, activated charcoal). Management of life-threatening complications such as generalized seizures and lactic acidosis, as well as other intoxication effects, should follow modern principles of intensive care and be conducted symptomatically. To date, there is no data on the usefulness of hemodialysis, hemoperfusion, or hemofiltration for enhanced elimination of α-lipoic acid.

Adverse Reactions

Very common (≥ 10%), common (≥ 1% to < 10%), uncommon (≥ 0.1% to < 1%), rare (≥ 0.01% to 0.1%), very rare (< 0.01%) or frequency not known.

Injection site reactions: Very rare cases of reactions at the injection site have been reported.

Immune system disorders: Frequency not known: insulin autoimmune syndrome.

Hypersensitivity reactions: Allergic skin reactions, skin rashes, urticaria, pruritus, eczema, as well as systemic reactions up to the development of anaphylactic shock.

Nervous system disorders: Very rare: altered or impaired taste sensations.

Following intravenous administration of α-lipoic acid, very rare cases of seizures and double vision (diplopia) have been observed.

Blood and lymphatic system disorders: Following intravenous administration of α-lipoic acid, very rare cases of hemorrhagic rashes (purpura) and thrombopathies have been observed.

General adverse reactions: When administered intravenously too rapidly, increased intracranial pressure and respiratory distress syndrome may very commonly occur; these symptoms resolve spontaneously.

Due to improved glucose uptake, blood glucose levels may decrease in some cases, very rarely leading to symptoms resembling hypoglycemia such as dizziness, increased sweating, headache, and visual disturbances.

Shelf life: 4 years.

Storage conditions

Store in a light-protected place at a temperature not exceeding 25°C.

Keep out of reach of children.

Store vials in the original packaging until the time of use.

Incompatibilities

α-Lipoic acid reacts in vitro with ionic metal complexes (e.g., cisplatin). With sugar molecules, α-lipoic acid forms poorly soluble complex compounds (e.g., levulose solution).

The solution of α-lipoic acid is incompatible with glucose solution, Ringer's solution, and solutions that may react with SH-groups or disulfide bonds.

Do not administer concomitantly with preparations containing metals (e.g., iron, magnesium preparations).

If necessary, only saline solution may be used as a solvent for the administration of Thioctacid® Turbo solution.

Packaging

1 vial or 10 vials of 50 ml each, together with protective black bag(s), in a cardboard box.

Prescription status: Prescription only.

Manufacturer

SoluPharm Pharmazeutische Erzeugnisse GmbH, Germany.

Manufacturer's address and location of business operations

Industriestraße 3, 34212 Melsungen, Germany.