Berlition 300 - instructions for use, dose, side effects, contraindications

Thioktovaya (alpha-lipoic) acid is an endogenous antioxidant of direct (binds free radicals) and indirect action. It is a coenzyme of the reactions of decarboxylation of a-ketoacids. Helps to reduce the concentration of glucose in the blood plasma and increase the concentration of glycogen in the liver, also reduces insulin resistance, participates in the regulation of carbohydrate and lipid metabolism,stimulates the exchange of cholesterol. Due to its antioxidant properties, thioctic acid protects cells from damage by their decay products, reduces the formation of end products of progressive glycosylation of proteins in nerve cells in diabetes mellitus, improves microcirculation and endoneural blood flow, increases the physiological content of glutathione antioxidant. By contributing to a decrease in the concentration of glucose in the blood plasma, it affects the alternative metabolism of glucose in diabetes mellitus, reduces the accumulation of pathological metabolites in the form of polyols, and, thereby, reduces edema of the nervous tissue. Through the participation in the metabolism of fats, thioctic acid increases the biosynthesis of phospholipids, in particular, phosphoinositol, thereby improving the damaged structure of cell membranes; normalizes the energy exchange and the conduct of nerve impulses. Thioctic acid eliminates the toxic effect of alcohol metabolites (acetaldehyde, pyruvic acid), reduces the excessive formation of molecules of free oxygen radicals, reduces endonevralnoy hypoxia and ischemia, weakening manifestations of polyneuropathy in the form of paresthesias,burning sensation, pain and numbness of the extremities.

In this way, thioctic acid has antioxidant, neurotrophic, hypoglycemic action, improves lipid metabolism.

Application in the form of ethylenediamine salt allows to reduce the severity of possible side effects of thioctic acid.

Pharmacokinetics:

With intravenous administration of 600 mg of thioctic acid, the maximum plasma concentration in 30 minutes is about 20 μg / ml.

Has the effect of "first pass" through the liver. The formation of metabolites occurs as a result of side chain oxidation and conjugation. Thioctic acid in the form of metabolites is excreted mainly by the kidneys (80-90%).

Half-life up to 25 min. The total plasma clearance is 10-15 ml / min / kg.

Indications:

Diabetic polyneuropathy;

alcoholic polyneuropathy.

Contraindications:

Hypersensitivity to thioctic (α-lipoic) acid in history, hypersensitivity to other components of the drug;

pregnancy, the period of breastfeeding (there is insufficient experience of the drug).

age to 18 years (efficacy and safety of use of the drug are not established)

Pregnancy and lactation:

The use of Berlition® 300 during pregnancy is possible only if the intended benefit of therapy for the mother exceeds the potential risk to the fetus. In view of the lack of sufficient clinical experience in the use of Berlition® 300 during pregnancy and during breastfeeding, its use in appropriate categories of patients is not recommended.

Dosing and Administration:

For intravenous administration.

At the beginning of treatment, the preparation Berlition® 300 is prescribed intravenously drip in a daily dose of 300-600 mg (1-2 ampoules).

Before use, the contents of 1-2 ampoules (12-24 ml of the preparation) are diluted in 250 ml of 0.9% sodium chloride solution and administered intravenously drip slowly, for at least 30 minutes. Since the active substance is sensitive to light, the infusion solution is prepared immediately prior to use. The prepared solution must be protected from exposure to light, for example, using aluminum foil. The light-shielded solution can be stored for about 6 hours.

The course of treatment is 2-4 weeks. Then they switch to maintenance therapy with Berlition® 300 (film-coated tablets) at a dose of 300-600 mg per day.

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

Side effects:

Possible side effects with the use of the drug Berlition®300 are given below in the descending incidence frequency: often (≥ 1/100, <1/10), infrequently (≥ 1/1000, <1/100), rarely (≥ 1/10000, <1/1000), very rarely (<1/10000), including individual messages. Correlations of the incidence of side effects with the sex or age of patients are not observed.

From the nervous system:

Very rarely: change or violation of taste, diplopia, convulsions.

From the side of the hemostasis system:

Very rarely: purpura, thrombocytopathy.

From the side of metabolism:

Very rarely: a decrease in the level of glucose in the blood plasma (due to improved absorption of glucose). There have been reports of complaints of a hypoglycemic condition, such as dizziness, sweating, headache and visual impairment.

From the immune system:

Very rarely: allergic reactions, such as a skin rash, urticaria (urticaria rash), itching, in isolated cases - anaphylactic shock.

Local reactions:

Very rarely: burning sensation at the injection site

Other: with rapid intravenous injection, spontaneous increases in intracranial pressure (a feeling of heaviness in the head) and difficulty in breathing were observed.

Overdose:

Symptoms: nausea, vomiting, headache.

In severe cases: psychomotor agitation or confusion, generalized convulsions, severe acid-base balance disorders with lactic acidosis, hypoglycemia (up to the development of coma), acute necrosis of skeletal muscles, DIC-syndrome, hemolysis, suppression of bone marrow activity, multi-organ failure.

Treatment: If suspected of intoxication with thioctic acid (eg taking more than 80 mg of the drug per 1 kg of body weight), urgent hospitalization is recommended and immediate application of the measures in accordance with the general principles adopted for accidental poisoning. Therapy is symptomatic. Treatment of generalized seizures, lactic acidosis and other life-threatening consequences of intoxication should be conducted in accordance with the principles of modern intensive care. There is no specific antidote. Hemodialysis, hemoperfusion and filtration methods with forced excretion of thioctic acid are not effective.

Interaction:

Due to thioctic acid is capable of forming chelate complexes with metals, joint use with iron preparations should be avoided.

Simultaneous application of the drug Berlition® 300 with cisplatin reduces the effectiveness of the latter.

With sugar molecules thioctic acid forms poorly soluble complex compounds. The preparation Berlition® 300 is incompatible with solutions of glucose, dextrose, fructose, Ringer, and also with solutions reacting with SH-groups or disulfide bonds.

The preparation Berlition® 300 enhances the hypoglycemic action of insulin and hypoglycemic drugs for oral administration when combined.

Ethanol reduces the therapeutic effectiveness of the drug Berlition® 300.

Special instructions:

In patients with diabetes mellitus, who take insulin or hypoglycemic preparations for oral administration, a constant control of the concentration of glucose in the blood plasma, especially at the initial stage of therapy with the preparation Berlition®300, is necessary. In some cases, it may be necessary to reduce the dose of insulin or hypoglycemic drugs for oral use in order to avoid the development of hypoglycemia.

With parenteral application, hypersensitivity reactions may occur.If symptoms such as itching, nausea, malaise occur, treatment with Berlition® 300 should be discontinued immediately.

Drinking alcohol reduces the effectiveness of treatment with Berlition® 300, therefore patients should be refrained from drinking alcohol during the course of treatment, and, if possible, during breaks between courses, during the treatment with Berlition® 300.

The prepared solution of the preparation Berlition® 300 should be protected from exposure to light.

Effect on the ability to drive transp. cf. and fur:

The effect of the preparation Berlition® 300 on the ability to drive vehicles and control mechanisms has not been specifically studied, therefore, during the treatment with Berlition® 300, caution should be exercised when driving vehicles and engaging in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Concentrate for the preparation of a solution for infusions of 25 mg / ml.

Packaging:

For 12 ml of the drug in a dark glass ampoule with a white ring (line of break) in the upper part of the ampoule.

For 5, 10 or 20 ampoules are placed in a cardboard package (tray) and together with instructions for use in a cardboard box.

Storage conditions:

Store at a temperature of no higher than 25 ° C, in a place protected from light. Do not freeze! Keep the medicine out of the reach of children!

Shelf life:

3 years

Shelf life after dilution with saline solution of sodium chloride is 6 hours when stored under conditions of protection from light.

Do not use after the expiration date stated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011434 / 01

Date of registration:02.09.2011

Expiration Date:Unlimited

The owner of the registration certificate:Berlin-Chemie / Menarini Pharma, GmbH Berlin-Chemie / Menarini Pharma, GmbH Germany

Manufacturer: & nbsp

JENAHEXAL PHARMA, GmbH Germany

BERLIN-CHEMIE, AG Germany

Information update date: & nbsp23.01.2017

Illustrated instructions

Instructions

Berlition® 300 (Berlithion® 300)