Berlition 600 - 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 alpha-keto acids. 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, phosphoinositides, 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,sensations of burning, pain and numbness of the limbs. In this way, thioctic acid has an antioxidant, neurotrophic effect, improves lipid metabolism.

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

Pharmacokinetics:

With intravenous administration of thioctic acid, the maximum plasma concentration in 30 minutes is about 20 μg / ml, the area under the concentration-time curve is about 5 μg / h / ml. Has the effect of "first pass" through the liver. The formation of metabolites occurs as a result of oxidation of the side chain and conjugation. The volume of distribution is about 450 ml / kg. The total plasma clearance is 10-15 ml / min / kg. It is excreted by the kidneys (80-90%), mainly in the form of metabolites. Half-life is about 25 minutes.

Indications:

Diabetic polyneuropathy;

alcoholic polyneuropathy.

Contraindications:

Hypersensitivity to thiectic acid or other components of the drug in the anamnesis;

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

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

Pregnancy and lactation:

Due to the lack of sufficient clinical experience with the use of Berlition® 600 during pregnancy and during breastfeeding, its use in the appropriate category of patients is not recommended.

Dosing and Administration:

The drug is intended for infusion.

At the beginning of treatment, the preparation Berlition® 600 is administered intravenously drip in a daily dose of 600 mg (1 ampoule).

Before use, the contents of 1 ampoule (24 ml) are diluted in 250 ml of 0.9% sodium chloride solution and administered intravenously drip, slowly, for at least 30 minutes. Because of the photosensitivity of the active substance, the infusion solution is prepared immediately before use. The prepared solution must be protected from exposure to light, for example, using aluminum foil.

The course of treatment with Berlition® 600 is 2-4 weeks. As a follow-up maintenance therapy, thiectic acid is used in oral form in a daily dose of 300-600 mg. 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 Berlition® 600 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.

On the part of the hematopoiesis system:

Very rarely: thrombocytopathy, hemorrhagic rash (purpura), thrombophlebitis.

From the side of metabolism:

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

From the immune system:

Very rarely: allergic reactions, such as a skin rash, hives, 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 seizures, expressed disorders of acid-base equilibrium, lactic acidosis, hypoglycemia (up to the development of coma), rhabdomyolysis, disseminated intravascular coagulation, hemolysis, bone marrow suppression, multiple organ failure.

Treatment: In case of suspected toxicity thioctic acid (e.g., administering more than 80 mg thioctic acid per 1 kg of body weight) is recommended emergency hospitalization and immediate application of the measures in accordance with the general principles adopted accidental poisoning. Therapy is symptomatic. Treatment of generalized seizures, lactic acidosis, and other life-threatening effects of intoxication should be in accordance with the principles of modern intensive care. There is no specific antidote. Hemodialysis, hemoperfusion or filtering techniques with positive derivation of thioctic acid are not effective.

Interaction:

Due to thioctic acid capable of forming chelate complexes with the metals should be avoided since the simultaneous administration of iron preparations. Simultaneous application 600 Berlition® drug cisplatin reduces the effectiveness of the latter.

With sugar molecules thioctic acid forms poorly soluble complex compounds. The preparation Berlition® 600 is incompatible with solutions of glucose, fructose and dextrose, Ringer's solution, and also with solutions reacting with disulfide and SH-groups.

The drug Berlition® 600 enhances the hypoglycemic action of insulin and hypoglycemic agents for oral administration with simultaneous application.

Ethanol significantly reduces the therapeutic efficacy of thioctic acid.

Special instructions:

Patients with diabetes require constant monitoring of the plasma glucose concentration, especially at the initial stage of treatment with the preparation of Berlition® 600. In some cases, it may be necessary to reduce the dose of insulin or hypoglycemic agents for oral administration in order to avoid the development of hypoglycemia. Drinking alcohol reduces the effectiveness of treatment with Berlition® 600, 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® 600.

With parenteral application, hypersensitivity reactions may occur.When symptoms of hypersensitivity (itching, malaise) appear, the drug should be discontinued immediately.

Only 0.9% sodium chloride solution can serve as a solvent for the preparation of Berlition® 600. Freshly prepared infusion solution must be protected from exposure to light, for example, using aluminum foil.

The light-shielded solution can be stored for about 6 hours.

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

The influence of the preparation of Berlion® 600 on the speed of psychomotor reactions and the ability to perceive or assess the situation has not been specifically studied, therefore, during the treatment with Berlition® 600, care should be taken when driving vehicles and engaging in potentially dangerous 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 24 ml of the drug in dark glass ampoules with a nominal capacity of 25 ml with a white label-indicator of the fracture line and three strips (green - yellow - green) in the upper part of the ampoule. 5 ampoules in plastic pallets.

1 pallet together with instructions for use in a cardboard bundle.

Storage conditions:

Store in a dark place at a temperature of no higher than 25 ° C.

Do not freeze!

Keep the medicine out of the reach of children!

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001615

Date of registration:28.03.2012

Expiration Date:28.03.2017

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

Manufacturer: & nbsp

HAMELN PHARMACEUTICALS, GmbH Germany

Representation: & nbspBERLIN-CHEMI / MENARINI PHARMA GmbH BERLIN-CHEMI / MENARINI PHARMA GmbH Germany

Information update date: & nbsp23.01.2017

Illustrated instructions

Instructions

Berlition® 600 (Berlithion® 600)