Berlition 600 tablets: instructions for use

active substance - thioctic acid 600 mg

Excipients: hard fat, medium chain triglycerides.

shell: 70% sorbitol solution, non-crystallizing (in terms of anhydrous substance), 85% glycerin (in terms of anhydrous substance), gelatin, titanium dioxide (E 171), carmine varnish (E 120).

Pharmacological properties

In humans, thioctic acid is rapidly absorbed after oral administration. Due to the pronounced effect of the first passage through the liver, the absolute bioavailability (in comparison with iv administration) of thioctic acid taken internally is approx. 20 %. Due to the rapid distribution in tissues, the half-life of thioctic acid from plasma in humans is approximately 25 minutes.

The relative bioavailability of thioctic acid when taken orally in solid dosage forms is greater than 60% in relation to oral solutions. The maximum plasma content of approx. 4 mcg / ml, achieved after approx. 0.5 h after oral administration of 600 mg of thioctic acid.

In experiments on animals (rats, dogs) using a radioactive label, it was possible to identify mainly the renal route of excretion (80-90%), namely, in the form of metabolites. In humans, only insignificant amounts of excreted intact substance are also found in urine. Biotransformation occurs mainly by oxidative shortening of the side chain (beta oxidation) and / or by S-methylation of the corresponding thiols.

Thioctic acid reacts in vitro with metal ion complexes (e.g. cisplatin). Thioctic acid with sugar molecules enters into sparingly soluble complex compounds.

Pharmacodynamics

Thioctic acid is a vitamin-like but endogenous substance that acts as a coenzyme in the oxidative decarboxylation of alpha-keto acids. Hyperglycemia caused by diabetes mellitus leads to the deposition of glucose on the matrix proteins of blood vessels and the formation of end products of progressive glycosylation ("Advanced Glycosylation End Products"). This process leads to a decrease in endoneural blood flow and to endoneural hypoxia / ischemia, which is associated with increased production of free oxygen radicals that damage peripheral nerves. In peripheral nerves, depletion of antioxidants, such as glutathione, has also been found. Experimental studies show that thioctic acid is involved in these biochemical processes, reducing the formation of end glycosylation products, improving endoneural blood flow, and increasing physiological levels of glutathione antioxidant. It also acts as an antioxidant against oxygen free radicals in nerves affected by diabetes. These effects observed during the experiment suggest that with the help of thioctic acid, the functionality of peripheral nerves can be improved. This applies to sensitivity disorders in diabetic polyneuropathy, which can manifest as dysesthesia and paresthesia (for example, burning, pain, numbness or crawling). Clinical studies demonstrate the beneficial effects of thioctic acid in the symptomatic treatment of diabetic polyneuropathy, accompanied by well-known symptoms such as burning, paresthesia, numbness and pain.

Pharmacodynamics and pharmacokinetics

Berlition includes as an active ingredient thioctic acid (alpha lipoic acid) in the form of an ethylene diamine salt, which is an endogenous antioxidant that binds free radicals with a coenzyme of alpha-keto acid decarboxylation processes.

Berlition treatment reduces plasma levels. glucose and increase liver glycogenweakens insulin resistance, stimulates cholesterol, regulates lipid and carbohydrate metabolism. Thioctic acidDue to its inherent antioxidant activity, it protects the cells of the human body from damage caused by their decay products.

In patients diabetes thioctic acid reduces the release of end products protein glycation in nerve cells, increases microcirculation and improves endoneural blood flow, increases physiological concentration glutathione antioxidant. Due to its ability to reduce the plasma glucose content, it affects an alternative pathway of its metabolism.

Thioctic acid reduces the accumulation of pathological polyol metabolites, thereby contributing to the reduction of swelling of the nervous tissue. Normalizes the conduction of nerve impulses and energy metabolism. Participating in fat metabolism, increases biosynthesis phospholipidsas a result of which the damaged structure of the cell membranes is reformed. Eliminates toxic effects metabolic products of alcohol (pyruvic acid, acetaldehyde), reduces the excess release of oxygen free radical molecules, reduces ischemia and endoneural hypoxiamitigating symptoms polyneuropathyin the form paresthesiaburning sensations, numbness and pain in the limbs.

Based on the foregoing, thioctic acid is characterized by its hypoglycemic, neurotrophic and antioxidant activity, as well as improving lipid metabolism action. Use in the preparation of the active ingredient in the form ethylene diamine salt allows you to reduce the severity of the likely negative side effects of thioctic acid.

When taken orally, thioctic acid is rapidly and completely absorbed from the digestive tract (food taken in parallel decreases absorption somewhat). TCmax in plasma varies between 25-60 minutes (with iv administration of 10-11 minutes). Plasma Cmax is 25-38 mcg / ml. Bioavailability of approximately 30%, Vd of approximately 450 ml / kg, AUC of approximately 5 μg / h / ml.

Thioctic acid is susceptible to a “first pass” effect through the liver. Isolation of metabolic products made possible by processes conjugation and side chain oxidation. Excretion in the form of metabolites is 80-90% carried out by the kidneys. T1 / 2 takes approximately 25 minutes. The total plasma clearance is 10-15 ml / min / kg.

Contraindications

Berlition is contraindicated in patients under 18 years of age, patients with personal hypersensitivity to the active (thioctic acid) or any of the auxiliary ingredients used in the treatment of the medicinal form of the drug, as well as to lactating and pregnant women.

Berlition 300 tablets, due to the presence in this dosage form lactosecontraindicated in patients with any hereditary sugar intolerance.

For all dosage forms of the drug

  • violation / change in taste,
  • decrease in plasma contentglucose (due to the improvement of its absorption),
  • symptomatology hypoglycemiaincluding visual impairment, dizziness, hyperhidrosis, headaches,
  • allergic manifestationsincluding skin rash/itchingurticaria rash (urticaria), anaphylactic shock (in isolated cases).

Additionally for parenteral forms of the drug

  • diplopia,
  • burning in the area of ​​the injection,
  • cramps,
  • thrombocytopathy,
  • purpura,
  • shortness of breath and increased intracranial pressure (noted in cases of rapid iv administration and passed spontaneously).

Berlition, instructions for use (Method and dosage)

The official instructions for use of Berlition 300 are identical to the instructions for use of Berlition 600 for all dosage forms of this drug (injection solution, capsules, tablets).

The medicine Berlition intended for the preparation of infusions is initially prescribed in a daily dosage of 300-600 mg, which is administered intravenously every day for a minimum of 30 minutes, for 2-4 weeks. Immediately before the infusion, a solution of the drug is prepared by mixing the contents of 1 ampoule of 300 mg (12 ml) or 600 mg (24 ml) with 250 ml Sodium Chloride Injection (0,9%).

In connection with the photosensitivity of the prepared infusion solution, it must be protected from exposure to light by wrapping with aluminum foil, for example. In this form, the solution can retain its properties for about 6 hours.

After 2-4 weeks of therapy with the use of infusions, they switch to treatment with the use of oral dosage forms of the drug. Berlition capsules or tablets are prescribed in a daily maintenance dose of 300-600 mg and taken on an empty stomach as a whole about half an hour before meals, drinking 100-200 ml of water.

The duration of the infusion and oral therapeutic course, as well as the possibility of re-conducting them, is determined by the attending physician individually.

Overdose

Negative symptoms of moderate overdose thioctic acid manifests itself nausea rolling in vomit and headaches.

In severe cases, it may be noted blurred consciousness or psychomotor agitationgeneralized cramps, hypoglycemia (before coma), severe acid-base disorders with lactic acidosissharp muscle necrosis skeleton multiple organ failure, hemolysis, DIC, inhibition of bone marrow activity.

If you suspect the toxic effect of thioctic acid (for example, when taking more than 80 mg of the therapeutic agent per 1 kg of weight), it is recommended that the patient be hospitalized immediately and immediately begin to implement generally accepted measures to counter accidental poisoning (gastrointestinal tract cleaningreception sorbents etc.). In the future, symptomatic therapy is indicated.

Treatment lactic acidosis, generalized seizures and other potentially life-threatening illnesses of the patient should occur in the ward intensive care. Specific antidote not identified. Hemoperfusion, hemodialysis and other forced filtering methods are ineffective.

Release form and composition

The dosage form of Berlition 600 is a concentrate for the preparation of an infusion solution: a clear liquid, greenish-yellow in 24 ml in glass ampoules (25 ml) of dark color with a break line (white label) and green-yellow-green stripes, per 5 pieces. in a plastic pallet, in a cardboard bundle 1 pallet.

1 ampoule contains:

  • active substance: thioctic acid - 0.6 g,
  • auxiliary components: ethylenediamine, water for injection.

Pharmacokinetics

With intravenous administration of the drug, the maximum concentration of thioctic acid in plasma is reached after 30 minutes. C valuemax approximately 20 μg / ml. Metabolized by oxidation of the side chain, as well as conjugation. Vd (distribution volume) is 450 ml / kg. Thioctic acid and its metabolites are excreted by the kidneys (the main route of excretion). The elimination half-life is about 25 minutes.

Berlition 600: instructions for use (dosage and method)

Berlition 600 is administered intravenously in the form of an infusion solution.

At the beginning of therapy, the drug is prescribed at a dose of 600 mg per day (1 ampoule of concentrate). As a rule, the course of treatment is 2–4 weeks, after which maintenance therapy with thioctic acid in the form of tablets at a dose of 300–600 mg per day is carried out. The general duration of therapy, as well as the need for repeated courses, is determined by the doctor.

To prepare a solution for infusion, the contents of one ampoule are diluted in 250 ml of physiological saline. The finished solution is administered intravenously, slowly (at least 30 minutes). Thioctic acid is photosensitive, so the drug should not be diluted in advance. The prepared solution must be protected from exposure to light.

Side effects

  • metabolism: very rarely - a decrease in plasma glucose, sometimes up to hypoglycemia (manifested by symptoms such as dizziness, headache, blurred vision and severe sweating),
  • central and peripheral nervous system: very rarely - a change in taste, binocular vision disorder, convulsions,
  • hematopoietic system: very rarely - thrombophlebitis, hemorrhagic rash, increased bleeding due to impaired platelet function,
  • allergic reactions: very rarely - urticaria, itching, rash on the skin, isolated cases - anaphylactic shock,
  • local reactions: very rarely - a burning sensation at the injection site of the infusion solution,
  • Other: difficulty breathing and a feeling of heaviness in the head (appear with the rapid administration of the drug and pass on their own).

Special instructions

Patients with diabetes taking special hypoglycemic agents should regularly check their blood sugar levels (especially at the beginning of therapy with Berlition 600). This is necessary for the timely prevention of a hypoglycemic state. In some cases, dose adjustment of insulin or hypoglycemic drugs for oral administration may be required.

With intravenous administration, hypersensitivity reactions may occur. The appearance of skin itching, nausea, malaise or other signs of hypersensitivity is an indication for the immediate abolition of thioctic acid.

Alcohol reduces the effectiveness of Berlition 600, so during the treatment period you should abandon the use of alcohol-containing drinks.

Only 0.9% sodium chloride solution can be used as a solvent for the concentrate. The prepared solution must be stored in a dark place, additionally protected from light by aluminum foil. The shelf life of the solution is no more than 6 hours.

Influence on the ability to drive vehicles and complex mechanisms

There is no data on the effect of Berlition 600 on the patient’s ability to concentrate or quickly respond to a situation, since no special studies have been conducted. During treatment with the drug, caution should be exercised when performing any work associated with an increased danger to life and health.

Drug interaction

Berlition 600 is able to form chelate complexes with iron, magnesium, calcium and other metals, so their simultaneous use should be avoided.

Thioctic acid enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs, and also reduces the therapeutic effect of cisplatin.

Ethanol significantly reduces the effect of Berlition 600.

To prepare a solution for infusion, you can not use solutions of fructose, dextrose, glucose, Ringer, as well as solutions that interact with disulfide bridges and SH-groups.

The analogues of Berlition 600 are: Tiolepta, Thioctic acid-Vial, Thiogamma, Thioctacid 600 T, Lipoic acid, Alpha-lipoic acid, Thioctic acid, Lipothioxin, Berlition 300, Thioctacid BV, Espa-Lipon, Octolipen, Lipolion, Tolipion, Tolipion, Tolipion, Tolipion, Politon, .

Berlition 600 reviews

The drug has earned many positive reviews, as it is not only effective, but also well tolerated by patients. Due to its antitoxic effect, Berlition 600 is often used in the treatment of alcoholism. It also helps well in the prevention and treatment of complications of diabetes, being more effective than some analogues.

According to reviews, Berlition 600 has almost no flaws, with the exception of a rather high cost.

Dosage and administration

The daily dose is 1 capsule of the drug Berlition® 600 capsules (corresponding to 600 mg of thioctic acid), which is taken once, approximately 30 minutes before the first meal.

With severe paresthesia, you can first carry out infusion therapy with thioctic acid.

Children and teens

Berlition® 600 capsules should not be taken by children and adolescents

Berlition® 600 capsules should be taken on an empty stomach, swallowing whole and drinking plenty of fluids. Simultaneous eating can make absorption difficult. Therefore, for patients who are characterized by a long time of gastric emptying, it is especially important that the medicine be taken half an hour before breakfast.

Since it is a chronic disease in the case of diabetic polyneuropathy, prolonged therapy may be necessary.

The basis of treatment for diabetic polyneuropathy is the optimal control over the course of diabetes.

Release form and packaging

15 capsules are placed in a blister strip packaging of PVC film (lined PVDH) and aluminum foil.

1 or 2 contour packs together with instructions for medical use in the state and Russian languages ​​are put in a pack of cardboard.

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children!

Do not use after expiration date!

Interaction

For thioctic acid characteristic is its interaction with therapeutic agents, including ionic metal complexes (e.g. with platinum Cisplatin) In this regard, the combined use of Berlition and metal preparations can lead to a decrease in the effectiveness of the latter.

Concurrent administration of ethanol-containing drugs leads to a decrease in the therapeutic effect of Berlition.

Thioctic acid enhances hypoglycemic activity oral hypoglycemic drugs and insulinthat may require adjustment of their dosage regimen.

Berlition for injection is incompatible with medicinal solutions used as the basis for the preparation of infusion mixtures, including ringer's solution and Dextroseas well as solutions that react with disulfide bridges or SH-groups.

Thioctic acid is capable of creating sparingly soluble complexes with sugar molecules.

Pharmacy Vacation Terms

Manufacturer / Owner of Registration Certificate

BERLIN-HEMI AG (MENARINI GROUP)

Gliniker Veg 125

12489 Berlin, Germany

Packer

Catalent Germany Schorndorf GmbH, Germany

The address of the organization accepting complaints from consumers on the quality of products (goods) in the territory of the Republic of Kazakhstan:

Representation of JSC "Berlin-Chemie AG" in the Republic of Kazakhstan

Phone number: +7 727 2446183, 2446184, 2446185

Berlition or Heptral

In connection with the hepatoprotective properties of Berlition, a group of drugs with a restorative effect on liver cells, one of the prominent representatives of which is Heptral. Of course, to draw parallels regarding the effects of these two therapeutic agents is quite difficult, because they still belong to different medicinal groups, include different active ingredients and are characterized by different mechanisms of action, however, in the treatment of liver pathologies, they rarely replace or complement each other.

Due to the insufficiently studied effect of Berlition on the children's body, its use in pediatrics is contraindicated.

Instructions for use

Berlition refers to metabolic agents that regulate the metabolism of fats and carbohydrates. The active substance of the drug is thioctic acid. The medicine is produced in tablets and in the form of a concentrate for the preparation of a solution for infusion.

Berlition is prescribed to patients suffering from the following pathologies:

  • polyneuropathy, developed against the background of diabetes mellitus and chronic alcoholism,
  • steatohepatitis of various origins,
  • liver steatosis
  • fatty hepatosis
  • chronic intoxication.

Side effects

The following undesirable effects may be observed during treatment with Berlition:

Hives

For all dosage forms:

  • allergy, which can manifest itself in urticaria (when using injection forms, systemic allergic reactions can occur up to anaphylaxis),
  • a decrease in blood sugar, as glucose is better absorbed.

For injection forms:

  • cramps
  • double vision
  • intracranial hyperplasia and shortness of breath (observed with the rapid administration of a medication, these undesirable effects pass independently),
  • thrombophlebitis
  • spot hemorrhages in the skin and mucous membranes,
  • platelet lowering,
  • hemorrhagic rash,
  • taste perversion
  • burning at the injection site.

1 tablet contains 300 mg of thioctic acid.

As additional components it includes:

  • MCC
  • twin
  • milk sugar,
  • fumed silica,
  • E 572,
  • croscarmellose sodium.

The shell consists of the following substances:

  • titanium white
  • liquid paraffin
  • hypromellose,
  • sodium dodecyl sulfate,
  • dye E104 and E110.

In 1 ampoule of the concentrate for the preparation of a solution for infusion, 300 or 600 mg of active substance may be contained.

As auxiliary substances, the concentrate contains water, ethylenediamine, and Berlition 300 also has a macrogol.

Pharmacology and pharmacokinetics

Thioctic acid is an antioxidant. As a coenzyme of mitochondrial multienzyme complexes, it takes part in the oxidative carboxylation of propanonic acid and alpha-keto acids.

It reduces the level of glucose in the blood and increases the concentration of glycogen in the liver, helps to overcome insulin resistance. Regulates the metabolism of lipids and carbohydrates, improves liver function. Lowers the level of glucose, lipids and cholesterol in the blood, has a hepatoprotective effect.

When taken orally, it is well absorbed from the gastrointestinal tract, while at the same time with food, the degree of adsorption decreases. With intravenous administration, the maximum concentration is observed after 10 minutes, when taken orally after 40-60 minutes.

Passing through the liver, the active substance is metabolized, it is excreted through the kidneys.

Terms of purchase and storage

You can buy a medication according to a doctor’s prescription.

It is necessary to store the concentrate at a temperature of no more than 25 degrees in a dark place where children can not get it.

The medicine should not be frozen.

The shelf life of the concentrate is 36 months.

Tablets should be stored in a place inaccessible to children, at a temperature not exceeding 25 degrees. Shelf life is 24 months.

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* - The average value among several sellers at the time of monitoring is not a public offer

Berlition price, where to buy

In Russia, the average price of Berlition 600 in ampoules No. 5 is 900 rubles, and Berlition 300 in ampoules No. 5 is 600 rubles. The price of Berlition 600 in capsules No. 30 is about 1000 rubles. The price of Berlition 300 in tablets No. 30 is approximately 800 rubles.

In Ukraine (including Kiev, Kharkov, Odessa, etc.) Berlition on average can be purchased: ampoules 300 No. 5 - 280 hryvnia, ampoules 600 No. 5 - 540 hryvnia, capsules 300 No. 30 - 400 hryvnia, capsules 600 No. 30 - 580 hryvnia , tablets 300 No. 30 - 380 hryvnias.

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