Thiolipon® concentrate for solution for intravenous administration 30 mg/ml

Thiolipon® concentrate for solution for intravenous administration 30 mg/ml

International nonproprietary name

Thioctic acid

Pharmacological group

Метаболические средства

Composition

1 ml of the drug contains:
Active substance:
thioctic acid (lipoic acid) - 30 mg,
excipients: ethylenediamine, propylene glycol, water for injection.

Pharmacological action

Thioctic acid (alpha lipoic acid) is an endogenous antioxidant (binding free radicals), it forms in the body during oxidative decarboxylation of alpha-keto acids.
The drug as a coenzyme of mitochondrial multienzyme complexes is involved in oxidative decarboxylation of pyruvic acid and alpha-keto acids. The drug promotes reducing blood glucose and glycogen in the liver, as well as elliminates insulin resistance. The nature of biochemical effect is close to the vitamins of group B.
It participates in regulation of lipid and carbohydrate metabolism, stimulates exchange of cholesterol, improves liver function.
Thioliponhas hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effects. Thiolipon improves trophic neurons.

Pharmacokinetics

Time to maximum concentration after intravenous administration is 10-11 min, the maximum concentration is 25-38 μg/ml, the area under the concentration-time curve is about 5 μg h/ml. Bioavailability is 30%.
Thioctic acid has the effect of "first passage" through the liver. Metabolite formation occurs as a result of the side chainoxidation and conjugation. The volume of distribution is about 450 ml / kg. Thioctic acid and its metabolites are excreted by the kidneys (80-90%). Half-life is 20-50 minutes. The total plasma clearance is 10-15 ml/min.

Indications for Use

Diabetic polyneuropathy; alcoholic polyneuropathy.

Contraindications

Increased sensation to the drug components; pediatric use at the age less than 18 years old (safety and efficacy are not determined); pregnancy and lactation period.

Cautions

Patients with diabetes mellitus require frequent monitoring of glucose concentration in the blood especially at the beginning of treatment. In some cases dose of hypoglycemic agents shall be reduced. During treatment drinking alcohol is strictly prohibited, because the effect of alcohol reduces the therapeutic effect of thioctic acid.
The drug photosensitive, therefore the ampoules shall be taken from the pack just before administration. The bottle with solution is recommended to be protected from light during infusion (light-protective bags, aluminum foil can be used). The prepared solution shall be stored in a dark place and administered not later than within 6 hours after preparation.

Dosing and Administration

The drug is intended for preparation of solution for intravenous administration after preliminary dilution in an isotonic sodium chloride solution.
For severe forms of diabetic or alcoholic polyneuropathy the drug shall be administered at dose 300-600 mg once per day in the form of intravenous drip infusion. Intravenous infusion duration shall be 50 minutes. The drug is recommended for administration during 2-4 weeks.
Then the therapy my be continued with oral administration at dose 300-600 mg per day. The minimum duration of treatment with oral administration is 3 months.

Side effect

After intravenous administration convulsions are rarely; diplopia; point bleeding in mucous membranes, skin; thrombocytopathy; hemorrhagic rash (purpura), thrombophlebitis.
After rapid administration possible increase in intracranial pressure (heavy head feeling); difficult breathing. The mentioned adverse effects disappear without treatment.
Possible allergic reactions: urticaria fever, systemic allergic reactions up to anaphylactic shock.
Possible hypoglycemia (associated with improved absorption of glucose).
Overdose
Symptoms: headache, nausea, vomiting.
Treatment: expectant. No specific antidote.

Interaction with other medicines

Alpha-lipoic acid (in the form of solution for intravenous administration) decreases the effect of cisplatin.
Simultaneous administration with insulin and other oral hypoglycemic agents increases the hypoglycemic effect.
Alpha-lipoic acid forms hardly soluble complex compounds with sugar molecules (for example, a levulose solution), therefore, it is incompatible with glucose solution, Ringer's solution and also with compounds (including their solutions) reacting with disulfide and SH-groups.

Form release

Storage conditions

In a dark place at temperature maximum 25 °С.

Expiration date

3 years