2010/12/17

Berlithion 300

Release form, composition and packing Berlithion 300 

Film-coated tablets pale yellow, round, with risk on one side. 1 tab. thioctic (α-lipoic) acid 300 mg Excipients: lactose monohydrate, magnesium stearate, microcrystalline cellulose, croscarmellose sodium, povidone (K-30), colloidal silicon dioxide, anhydrous. The composition of the shell: Opadry OY-S-22898 yellow (hypromellose, titanium dioxide (E171), sodium dodecyl sulphate, liquid paraffin, quinoline yellow (E104), yellow-orange dye (E110), liquid paraffin).

Concentrate for solution for infusion is transparent, greenish-yellow. 1 ml 1 amp. ethylenediamine salt of thioctic (α-lipoic acid) 32.33 mg 388 mg, which resp. content of thioctic (α-lipoic acid) 25 mg 300 mg Excipients: Propylene glycol, ethylene diamine, water, d / and.

Clinico-pharmacological group: drug with antioxidant action, regulating carbohydrate and lipid metabolism. Hepatoprotector.

Pharmacological action

The drug, which regulates metabolism. Thioctic (α-lipoic) acid - an endogenous antioxidant, is formed in the body in the oxidative decarboxylation of α-keto acid and pyruvic acid. Helps reduce blood glucose and increased glycogen content in the liver, as well as to overcome insulin resistance.

By the nature of the biochemical actions similar to vitamin B. Participates in the regulation of lipid and carbohydrate metabolism, stimulates cholesterol metabolism, improves liver function. Exerts hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effect.

The use of ethylenediamine salt of thioctic acid in solution for iv administration (which has a neutral reaction) can reduce the severity of adverse reactions.

Pharmacokinetics

Absorption and distribution

After oral thioctic (α-lipoic) acid is rapidly and completely absorbed from the gastrointestinal tract. Reception with food reduces the absorption.

Time to reach Cmax - 40-60 min. Bioavailability - 30%. At iv administration Cmax is 25-38 ug / ml and is reached through 10.11 min, AUC - about 5 ug x hr / ml. Vd - about 450 ml / kg.

Metabolism and Elimination

Has the effect of "first passage" through the liver. The formation of metabolites occurs as a result of oxidation of the side chain and conjugation. Thioctic acid and its metabolites are excreted in the urine (80-90%). T1 / 2 - 20-50 min. The total plasma clearance - 10-15 ml / min.

Statement
diabetic polyneuropathy;
alcoholic polyneuropathy.

Dosing regimen

Inside the adult prescribe 600 mg 1 time per day. Tablets are taken on an empty stomach, approximately 30 minutes before the first meal, without chewing and drinking plenty of fluids. Duration of treatment is determined by the physician individually. In severe forms of polyneuropathy in the beginning of the treatment drug is prescribed IV to 300-600 mg (12-24 ml, respectively) per day for 2-4 weeks. Later moving to supportive therapy and prescribe Valium 300 in the form of tablets of 300-600 mg / day.

Rules for preparation and storage solution infuzionnnogo

To prepare the infusion solution 1-2 ampoules Valium 300 diluted with 250 ml 0.9% sodium chloride solution and injected iv infusion over 30 min. Because of the sensitivity of the active substance infusion solution should be prepared immediately before use. Solution of the drug must be protected from exposure to light, for example, using aluminum foil. Protected from light, the solution can be stored for approximately 6 hours

Side effect
From the digestive system: it is possible (after ingestion) - dyspepsia, including nausea, vomiting, heartburn.
CNS: in some cases (after iv administration) - seizures, diplopia, with the rapid IV administration may be the feeling of heaviness in the head and breathing difficulties, which are alone.
From the hemopoietic system: in some cases (after iv injection) - petechiae on the skin and mucous membranes, thrombocytopathies, hemorrhagic rash (purpura).
From the metabolic: hypoglycemia (due to improved glucose uptake).

Allergic reactions: in some cases - urticaria, systemic allergic reactions up to anaphylactic shock.

Local reactions: sometimes - a burning sensation at the injection site.

Contraindications
children's age (efficacy and safety have not been established);
pregnancy;
Lactation (breastfeeding);
hypersensitivity to the drug.

Pregnancy and lactation

Application Valium 300 during pregnancy and lactation is contraindicated because of the lack of sufficient clinical data supporting the safety and efficacy of its application in this category of patients.

Cautions

In patients with diabetes requires constant monitoring of blood glucose levels, especially at the initial stage of therapy.

In some cases it is necessary to reduce the dose of insulin or oral hypoglycemic agents to avoid hypoglycemia. After taking the drug Valium 300 in the morning, apply the product of iron, magnesium, and also consume dairy products (due to their content of calcium) is recommended in the afternoon or evening.

Patients taking the drug Valium 300 should abstain from alcohol.

Use in pediatrics

Valium 300 should not be prescribed for children and adolescents due to lack of clinical experience with the drug in these patients.

Overdose

Symptoms: headache, nausea, and vomiting.

Treatment: symptomatic. No specific antidote.

Drug Interactions

In vitro thioctic (α-lipoic) acid reacts with complexes containing metal ions (eg, cisplatin). Therefore, for simultaneous administration may weaken the effect of cisplatin.

With the simultaneous application of ethanol and its metabolites may reduce the therapeutic activity of Valium 300. Valium 300 enhances the hypoglycemic action of insulin and oral hypoglycemic agents.

Pharmaceutical interactions

Thioctic (α-lipoic) acid forms with the molecules of dextrose (including with solutions levulozy) soluble complex compounds. Valium 300 IU is incompatible with dextrose solution, Ringer's solution, as well as with solutions, which are known to react with SH-groups or disulfide bridges.

Conditions and terms of

List B. The drug should be kept in the dark, place inaccessible to children at or above 25 ° C. Shelf Life tablets - 2 year shelf life of concentrate for solution for infusion - 3 years.