ÜÑÓ½¿Ô¿«¡® 300

General characteristics. Structure:

Contains in 1 ampoule (12 ml):

active ingredient: etilendiaminovy salt of thioctic (α-lipoic)))))))))) acids of 0,388 g (in terms of thioctic (α-lipoic)))))))))) acid - 0,300 g);

excipients: propylene glycol, ethylene diamine, water for an injection.

1 tablet, coated, contains:

active ingredient: thioctic (α-lipoic)))))))))) acid - 300 mg;

excipients: lactoses monohydrate, magnesium stearate, cellulose microcrystallic, sodium of a kroskarmelloz, povidone (value K = 30), silicon dioxide colloid anhydrous; in a cover - Opadry OY-S-22898 "zhelty" consisting from: gipromelloza, dioxide titanium (Е 171), sodium of a dodetsilsulfat, liquid paraffin, dye quinolinic yellow (Е 104), dye yellow-orange (Е 110) and liquid paraffin.

Pharmacological properties:

Pharmacodynamics. Thioctic acid (α-lipoic)))))))))) - endogenous antioxidant (connects free radicals), in an organism is formed at oxidizing decarboxylation of α-ketonic acids.......... As a coenzyme of mitochondrial multifermental complexes participates in oxidizing decarboxylation of pyruvic acid and α-ketonic acids.......... Promotes decrease in content of glucose in blood and to increase in maintenance of a glycogen in a liver, and also to overcoming insulin resistance. On character of a biochemical effect it is close to group B vitamins. Participates in regulation of lipidic and carbohydrate metabolism, stimulates cholesterol exchange, improves function of a liver.

Renders hepatoprotective, hypolipidemic, gipokholesterinemichesky, hypoglycemic action. Use of etilendiaminovy salt of thioctic acid in solutions for in/in introductions (having neutral reaction) allows to reduce expressiveness of side reactions.

 

Pharmacokinetics. Has effect of "the first passing" through a liver. Formation of metabolites results from oxidation of a side chain and a konjyugirovaniye.
Distribution volume - about 450 ml/kg. Thioctic acid and its metabolites are removed by kidneys (80-90%).

Form for injections

At intravenous administration time of achievement of the maximum concentration - 10-11 min., the maximum concentration - 25-38 mkg/ml, the area under a curve concentration time - about 5 mkg of h/ml.

The tableted form

At intake it is quickly and fully soaked up from digestive tract (reception with food reduces absorption). Time of achievement of the maximum concentration - 40-60 min. Bioavailability - 30%.

Elimination half-life - 20-50 min. The general plasma clearance - 10-15 ml/min.

Indications to use:

Diabetic and alcoholic polyneuropathy.

Route of administration and doses:

Form for injections

The daily dose makes 300-600 mg (1-2 ampoules). 1-2 ampoules of drug (12-24 ml of solution) dissolve physiological 0.9% of solution of sodium of chloride in 250 ml and enter intravenously kapelno within about 30 minutes.

At the beginning of a course the drug is administered intravenously within 2-4 weeks. Then it is possible to continue reception of thioctic acid inside in a dose of 300-600 mg a day.

The tableted form

Appoint inside 600 mg (2 tablets) once a day. A pill is taken on an empty stomach, approximately in 30 minutes prior to the first meal, without chewing and washing down with enough liquid. Duration of a course of treatment is determined by the doctor.

Features of use:

The patients accepting the drug Берлитион® 300 should refrain from alcohol intake.

At patients with a diabetes mellitus constant control of concentration of glucose in blood, especially at an initial stage of therapy is necessary. In certain cases it is necessary to reduce a dose of insulin or peroral hypoglycemic drug to avoid development of a hypoglycemia.

Form for injections

Solution needs to be protected from light influence, for example, by means of aluminum foil. The solution protected from light can be stored within about 6 hours.

Side effects:

Form for injections

Usually Берлитион® 300 it is transferred well. Spasms are very seldom possible; diplopia; dot hemorrhages in mucous membranes, skin; trombotsitopatiya; hemorrhagic rash (purpura); thrombophlebitis; at bystry introduction increase in intracranial pressure is possible (emergence of feeling of weight in the head); breath difficulty. The listed side effects pass independently. Local reactions in an injection site are possible (burning); allergic reactions: a small tortoiseshell, system allergic reactions (up to development of an acute anaphylaxis). Development of a hypoglycemia is possible (in connection with improvement of digestion of glucose).

The tableted form

Usually Берлитион® 300 it is transferred well. Dyspepsia is possible, including
 nausea, vomiting, heartburn. Development skin is in some cases possible
 allergic reactions (urticaria). Development of a hypoglycemia is possible (in connection with improvement of digestion of glucose).

Interaction with other medicines:

In vitro thioctic acid reacts with ionic complexes of metals (for example, with Cisplatinum) therefore at simultaneous use of Berlition 300 can reduce effect of Cisplatinum.

At simultaneous use Берлитион® 300 strengthens effect of insulin and peroral hypoglycemic means. Alcohol (ethanol) reduces therapeutic activity of thioctic acid.

Form for injections

With molecules of sugars thioctic acid forms badly soluble complex compounds. Therefore, infusion solution of thioctic acid is incompatible with dextrose solution, Ringer's solution and with solutions which can react with connections by SH groups or having disulfide bridges.

The tableted form

After administration of drug Берлитиона® 300 morning to use iron preparations, magnesium, and also it is recommended to use dairy products (because of content of calcium in them) after a lunch or in the evening.

Contraindications:

• Hypersensitivity to drug components.
• Pregnancy, the breastfeeding period (there is no sufficient experience of use of drug).
• Children's age (efficiency and safety of use are not established).

Overdose:

Symptoms: headache, nausea, vomiting.

Treatment: symptomatic. There is no specific antidote.

Storage conditions:

List B. In the place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity the Form for injections: 3 years. The tableted form: 2 years.

Issue conditions:

According to the recipe

Packaging:

Form for injections

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

On 12 ml of drug in ampoules of dark hydrolytic glass like I (Evr. T.) with a white ring in an upper part of an ampoule.

On 5 ampoules in cardboard planimetric packaging (tray) with the application instruction in a cardboard pack.

The tableted form

Tablets, coated, 300 mg.

On 10 tablets in the blister from an opaque PVC film / PVDH / aluminum foil.

On 3 blisters together with the application instruction place in a cardboard pack.