Berlithione 300, concentrate 25 mg/ml 12 ml 5 pcs

Berlition 300 is hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic.

As a coenzyme of mitochondrial multienzyme complexes it participates in oxidative decarboxylation of pyruvic acid and alpha-keto acids. It promotes reduction of blood glucose content and increase of glycogen content in the liver as well as overcoming insulin resistance.

In terms of biochemical action, it is close to the B vitamins. It participates in the regulation of lipid and carbohydrate metabolism, stimulates cholesterol metabolism and improves liver function. Use of trometamol salt of thioctic acid (which is neutral in reaction) in solutions for I/V administration allows to decrease side reactions.

Pharmacokinetics

In oral administration it is quickly and completely absorbed from the gastrointestinal tract (absorption with food reduces absorption). Time to reach Cmax – 40-60 min. Bioavailability – 30%. It has the effect of “first passage” through the liver.

The formation of metabolites occurs as a result of side chain oxidation and conjugation. The volume of distribution is about 450 ml/kg. The main ways of metabolism are oxidation and conjugation. Thioctic acid and its metabolites are excreted by the kidneys (80-90%). T1/2 is 20-50 min. Total plasma Cl is 10-15 ml/min.

Indications

Diabetic and alcoholic polyneuropathy, steatohepatitis of various etiologies, fatty liver dystrophy, chronic intoxication.

Active ingredient

Composition

Active Effective ingredient:

Ethylenediamine salt of thioctic (α-lipoic) acid 32.33 mg (388 mg), corresponding to the thioctic (α-lipoic) acid content of 25 mg (300 mg).

Auxiliary Ingredients:

Propylene glycol,

Ethylenediamine,

Water d/i.

How to take, the dosage

The daily dose is 300-600 mg (1-2 ampoules). 1-2 ampoules of the drug (12-24 ml of solution) are diluted in 250 ml of 0.9% sodium chloride solution and administered by IV drip for about 30 minutes.

In the beginning of treatment, the drug is administered by IV for 2-4 weeks. Then thioctic acid may be continued orally at a dose of 300-600 mg/day.

Interaction

In vitro thioctic acid (α-lipoic acid) interacts with metal ionic complexes (e.g., with cisplatin). Therefore, concomitant use may reduce the effect of cisplatin.

Berlition® 300 potentiates the hypoglycemic effect of insulin and oral hypoglycemic agents.

When used concomitantly, ethanol and its metabolites may decrease the therapeutic activity of Berlithion® 300.

Pharmaceutical interaction

Thioctic acid (α-lipoic acid) forms insoluble complex compounds with molecules of sugars.

Berlition® 300 is incompatible with dextrose solutions, Ringer’s solution, and solutions known to react with SH groups or disulfide bridges.

Special Instructions

In diabetic patients, continuous monitoring of blood glucose concentrations is necessary, especially during the initial phase of therapy.

In some cases, it is necessary to reduce the dose of insulin or oral hypoglycemic drug to avoid the development of hypoglycemia.

Patients receiving Berlithione® 300 should refrain from drinking alcohol.

Contraindications

Hypersensitivity; childhood (effectiveness and safety not established)

Side effects

CNS disorders: very rarely – seizures, diplopia; with rapid IV infusion there may be a feeling of heaviness in the head (increased intracranial pressure) and difficulty in breathing, which pass on their own.

With the blood coagulation system: very rarely – petechiae on the skin and mucous membranes, thrombocytopathy, hemorrhagic rash (purpura), thrombophlebitis.

Metabolic disorders: possibly hypoglycemia (due to improved glucose absorption).

Allergic reactions: possible urticaria, systemic allergic reactions up to anaphylactic shock.

Local reactions: possible – burning at the injection site.

Overdose

Symptoms:headache, nausea, vomiting.

Treatment: symptomatic. There is no specific antidote.

Pregnancy use

The use of Berlithione® 300 during pregnancy and lactation is contraindicated because there is insufficient clinical data to support the safety and effectiveness of the drug in this patient population.

Similarities