Benfogamma® [Benfotiamine]

Pharmacological properties

Vitamin B1 is the main active substance. the fat-soluble precursor of benfotiamine in the body is converted into biologically active thiamine pyrophosphate (TPP). TPF plays an active role in important hydrocarbon metabolism functions. during the conversion of pyruvate to acetyl coa and transketolases in the pentose phosphate cycle, thiamine pyrophosphate acts as a coenzyme. in addition, he takes part in the conversion of α-ketoglutarate to succinyl koa in the citric acid cycle. in the process of metabolism, there is an interaction with other vitamins of complex b. in addition, cocarboxylase is a coenzyme of pyruvate dehydrogenase, which plays a key role in the oxidation of glucose. since energy in nerve cells is generated primarily through the oxidation of glucose, an adequate amount of thiamine is necessary for the functioning of nerve cells. if glucose levels increase, the need for thiamine also increases. insufficient amount of cocarboxylase leads to the accumulation of intermediate decomposition products in the blood and tissues, such as pyruvate, lactate and ketoglutarate, to the presence of which muscle tissue, myocardium and central nervous system are very sensitive. benfotiamine reduces the accumulation of these toxic substances.

Determination in erythrocytes of the activity of enzymes dependent on thiamine diphosphate, for example erythrocyte transketolase (ETK), and their level of ability to activate (activation coefficient - α-ETK) are suitable for determining the status of vitamin B₁. The concentration of ETK in blood plasma is 2–4 μg / 100 ml.

Pharmacokinetics Following oral administration of benfotiamine, dephosphorylation occurs to S-benzoyl thiamine (SBT) using intestinal phosphatases. SBT is fat soluble, therefore it has a high degree of permeability. SBT is absorbed without any significant transformation of thiamine.

In contrast to thiamine, saturation kinetics is not characteristic of benfotiamine. Benfotiamine has a significantly higher bioavailability than water-soluble thiamine derivatives. In addition, benfotiamine lingers in tissues for a longer period.

Indications

• Treatment of polyneuropathy and cardiovascular disorders (caused by vitamin B1 deficiency); clinically confirmed vitamin B1 deficiency or an unbalanced diet (for example, take it), parenteral nutrition for a long time, “zero” diet, hemodialysis, malabsorption of nutrients, increased need for vitamin B1 (for example, during pregnancy and lactation); chronic alcoholism (alcoholic cardiomyopathy, Wernicke encephalopathy, Korsakoff syndrome).

Application

Applied inside, the tablet is taken whole, washed down with a sufficient amount of liquid. to treat vitamin B1 deficiency, take 1 tablet per day.

In the treatment of polyneuropathy, the recommended dose is 1 tablet per day for 3 weeks. Further treatment is determined depending on the therapeutic effect obtained.

Contraindications

Hypersensitivity to the components of the drug; allergic reactions to vitamin b1.

Side effects

Distributed by frequency: very often (1/10); (often (1/100, 1/10); infrequently (1/1000, 1/100); rarely (1/10 000, 1/1000); very rarely (1/10 000), including individual messages.

On the part of the immune system: very rarely - hypersensitivity reactions, including anaphylactic shock, angioedema, allergic reactions (urticaria, exanthema); itching, hyperemia.

From the digestive tract: nausea, vomiting, abdominal pain, diarrhea.

Others: dizziness, headache, tachycardia.

special instructions

Patients with a very rare hereditary galactose intolerance, lactase deficiency or impaired glucose and galactose absorption should not take this medicine.

Use during pregnancy and lactation. Due to the lack of sufficient experience in the use of the drug during pregnancy, it should be used only in the case of laboratory-confirmed thiamine deficiency.

Children. The effectiveness and safety of the drug in children have not been established, so it is not used in pediatric practice.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. There are no warnings regarding the use of the drug for vehicle drivers and persons working with complex mechanisms. But it should be borne in mind that adverse reactions may appear, such as dizziness, headache, and others (see ADVERSE EFFECTS), which reduce the reaction rate.

Interactions

Benfotiamine is incompatible with oxidizing and reducing compounds: mercury chloride, iodide, carbonate, acetate, tannic acid, iron-ammonium citrate, as well as sodium phenobarbital, riboflavin, benzylpenicillin, fluorouracil, glucose, and is metabolically inactive in them. copper accelerates the breakdown of benfotiamine; in addition, thiamine loses its effect with increasing pH values ​​(3). antacids reduce the absorption of thiamine. loop diuretics (such as furosemide), inhibiting tubular reabsorption, with prolonged therapy can cause an increase in the excretion of thiamine and thus reduce its level.

Overdose

With an overdose, the severity of symptoms of side effects of the drug increases.

When using vitamin B₁ in high doses, a curariform effect is manifested. With prolonged use of vitamin B₁ at a dose of 2 g / day, neuropathies with ataxia and sensitivity disorders, cerebral seizures with changes in the EEG, and in some cases hypochromic anemia and seborrheic dermatitis were recorded.

Treatment: gastric lavage, intake of activated carbon, symptomatic therapy.

Storage conditions

In the original packaging at a temperature not exceeding 25 ° C.