Octolipen, 30 mg/ml concentrate 10 ml 10 pcs

Pharmacotherapeutic group: metabolic agent

ATX code: A16AX01

Pharmacological properties

Pharmacodynamics

p>Thioctic acid (alpha-lipoic acid) is an endogenous antioxidant of direct (binds free radicals) and indirect action. As a coenzyme of mitochondrial multienzyme complexes is involved in oxidative decarboxylation of pyruvic acid and alpha-keto acids. It promotes reduction of blood glucose concentration and increase of glycogen content in the liver, as well as overcoming insulin resistance. By the nature of the biochemical action is close to the B vitamins. Participates in the regulation of lipid and carbohydrate metabolism, stimulates cholesterol metabolism. It has hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effect. Improves trophism of neurons.

Thioctic acid in diabetes reduces the formation of glycation end products, improves endoneural blood flow and increases glutathione content to physiological levels that as a result improves the functional state of peripheral nerve fibers in diabetic polyneuropathy. Due to its involvement in fat metabolism, thioctic acid increases the biosynthesis of phospholipids, particularly phosphoinositides, restoring damage to cell membranes; it normalizes energy metabolism and nerve impulse conduction. Thioctic acid eliminates the toxic effects of alcohol metabolites (acetaldehyde, pyruvic acid), reduces endoneural hypoxia and ischemia, weakening manifestations of polyneuropathy in the form of paresthesia, burning sensation, pain and numbness of the extremities.

Thioctic acid thus has antioxidant, neurotrophic effects and improves lipid metabolism.

Pharmacokinetics

Absorption and distribution. When thioctic acid is administered intravenously at a dose of 600 mg, the maximum plasma concentration after 30 minutes is approximately 20 µg/mL. The area under the curve “concentration-time” is about 5 µg/h/ml. Bioavailability is 30%. The volume of distribution is about 450 ml/kg.

Metabolism and excretion. Thioctic acid (alpha-lipoic acid) has a “first pass” effect through the liver. Metabolites are formed by oxidation of the side chain and conjugation. Thioctic acid and its metabolites are excreted by the kidneys mainly as metabolites (80-90%), in small amounts unchanged. The elimination half-life is about 25 min. Total plasma clearance is 10-15 ml/min.

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Indications

Type 2 diabetes, Type 1 diabetes, Alcoholism

• diabetic polyneuropathy;
• alcoholic polyneuropathy.

Active ingredient

Thioctic acid

Composition

Active ingredient: thioctic acid (α-lipoic acid) – 300 mg;

Associates: ethylenediamine, 87.4 mg; diatrium edetate (diatrium salt of ethylenediaminetetraacetic acid), 1 mg; water for injection, up to 10 ml.

How to take, the dosage

The drug is intended for preparation of a solution for intravenous infusion after pre-dilution in 0.9% sodium chloride solution. 1 ampoule of 10 ml of the drug contains 300 mg of thioctic acid. At the beginning of treatment the drug is administered intravenously by drop infusion in a daily dose of 600 mg (2 ampoules of 10 ml).

The solvent for the drug can only be 0.9% sodium chloride solution.

In order to prepare the solution the contents of 2 ampoules of 10 ml are diluted in 250 ml of 0.9% sodium chloride solution and injected intravenously by drip, slowly at a rate of not more than 2 ml/min. The course of therapy is 2-4 weeks. Then it is necessary to switch to maintenance therapy – administration of thioctic acid in oral form in a daily dose of 600 mg.

The drug is photosensitive, therefore, the solution for infusion should be prepared immediately before use. During infusion, protect the bottle with the solution from light (you can use light shielding bags, aluminum foil). The prepared solution should be stored in a light-protected place and used within 6 hours after preparation.

The duration of treatment and the need for its repetition is determined by the doctor.

Interaction

Thioctic acid is capable of forming chelate complexes, therefore coadministration with preparations of iron, magnesium, calcium should be avoided.

Thioctic acid (in the form of infusion solution) leads to decreased effectiveness of cisplatin when used simultaneously.

Thioctic acid forms insoluble complex compounds with sugar molecules, therefore, it is incompatible with dextrose (glucose) solution, fructose, Ringer’s solution, as well as with solutions that interact with disulfide and SH-groups.

In concomitant use with insulin and oral hypoglycemic agents an increase in hypoglycemic effect is observed.

Thioctic acid increases the anti-inflammatory effect of glucocorticosteroids.

Ethanol and its metabolites reduce the therapeutic effectiveness of thioctic acid.

Special Instructions

In patients with diabetes mellitus, especially at the beginning of treatment, continuous monitoring of plasma glucose concentration is necessary. In some cases, it may be necessary to reduce the dose of hypoglycemic agents. In case of symptoms of hypoglycemia (dizziness, increased sweating, headache, visual disturbances, nausea) the drug administration should be stopped immediately.

Parenteral administration may cause hypersensitivity reactions. If symptoms such as itching, malaise occur, the drug administration should be stopped immediately.

At the time of treatment, and, if possible, during the breaks between courses, it is necessary to refrain from drinking alcohol, because therapeutic effect of thioctic acid is reduced by exposure to alcohol, and it is also a risk factor for the development and progression of neuropathy.

The drug is photosensitive, therefore the prepared solution of the drug should be protected from exposure to light.

There have been several cases of thioctic acid-induced autoimmune insulin syndrome, characterized by frequent hypoglycemia in patients with diabetes in the presence of autoantibodies to insulin. The possibility of autoimmune insulin syndrome was determined by the presence of HLA-DRB1*0406 and HLA-DRB1*0403 haplotypes in patients.

Influence on the ability to drive and operate vehicles

The effect on the ability to operate vehicles and other mechanisms has not been specifically studied, so during the treatment with Octolipen^® treatment is recommended to be cautious when driving vehicles and operating other mechanisms and engaging in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Synopsis

a clear greenish-yellow liquid.

Contraindications

• high sensitivity to thioctic acid and/or any excipient of the drug
• age under 18 years (efficacy and safety of use have not been established)
• pregnancy and breastfeeding (there is not enough experience of using the drug).

Cautions

Intravenous administration of the drug should be used with caution in elderly patients (>75 years).

Side effects

According to the World Health Organization (WHO) adverse reactions are classified according to their frequency of development as follows: frequently (≥ 1/100, < 1/10), infrequently (≥ 1/1000, < 1/100), rarely (≥ 1/10000, < 1/1000) and very rarely (< 1/10000); frequency is unknown (frequency of events cannot be determined based on available data). There is no correlation of the incidence of adverse reactions with the gender or age of patients.

Blood and lymphatic system disorders:

very rarely: petechial hemorrhages in mucous membranes, skin; hemorrhagic rash (purpura), thrombocytopathy, hypocoagulation.

immune system disorders:

very rarely: allergic reactions (skin rash, eczema, urticaria, pruritus);

frequency unknown – anaphylactic shock; autoimmune insulin syndrome in patients with diabetes, characterized by frequent hypoglycemia in the presence of autoantibodies to insulin.

Metabolic and nutritional disorders:

very rarely: hypoglycemia (due to improved glucose utilization), symptoms of which include dizziness, increased sweating, headache, visual disturbances.

Nervous system disorders:

very rarely:change or disturbance in taste sensation, “flushes,” seizures.

Gastrointestinal tract disorders:

often: nausea, vomiting;

very rarely: abdominal pain, diarrhea.

Liver and biliary tract disorders:

very rarely:increased activity of “liver” enzymes.

Cardiac disorders:

frequency unknown:pain in the heart region, tachycardia may occur when the drug is rapidly administered.

vascular disorders:

very rarely thrombophlebitis.

Visual disorders:

very rare:diplopia, blurred vision.

General disorders and disorders at the site of administration:

very rarely: weakness, burning sensation at the site of administration;

frequency unknown: allergic reactions at the site of administration – irritation, hyperemia, or swelling.

Others:

very rarely: with rapid intravenous administration, spontaneous increase in intracranial pressure (occurrence of a feeling of heaviness in the head), difficulty in breathing, and weakness may occur.