Benfotiamine is an active ingredient present in many medicines. It is also available as a separate drug. It has some features that you should definitely familiarize yourself with before using the product.
What vitamin is this
This is a fat-soluble form (analogue) ().
International nonproprietary name
INN: Benfotiamine
Trade names
Benfotiamine.
ATX and registration number
ATC classification: A11DA03.
R No: 012520.01.
Pharmacotherapeutic group
Vitamins (metabolics).
Mechanism of action
The active substance replenishes the deficiency of B vitamins in the body and normalizes metabolism. This allows us to improve the functioning of the body and the condition of patients.
Improved metabolism is due to increased carbohydrate metabolism. Thanks to this, the functioning of the central nervous system is stabilized and reflex processes are optimized.
This synthetic compound has the following features:
- regulates the functioning of the central nervous system;
- improves metabolism and replenishes thiamine deficiency.
Composition and release form of the drug Benfotiamine
1 pill contains the following substances:
- active ingredient – 100 mg;
- pyridoxine hydrochloride – 100 mg;
- cyanocobalamin – 200 mcg;
- additional ingredients: calcium hydrogen phosphate, stearic acid, colloidal silicon dioxide, magnesium stearate, croscarmellose;
- shell: maltodextrin, Opadry II white, titanium dioxide, medium chain triglycerides, polydextrose.
The tablets are placed in contour blisters of 30 pieces or in plastic bottles of 60 pieces. The medicine is sold in a cardboard box.
Indications for use of the drug Benfotiamine
Action active ingredients the drug is effective for the following conditions and pathologies:
- vitamin deficiency/hypervitaminosis B1;
- myocardial dystrophy;
- disruptions in the nervous system (including impaired blood circulation);
- Alzheimer's disease;
- intestinal atony;
- viral form;
- rheumatic heart disease;
- neuritis and;
- paralysis, paresis (peripheral);
- thyrotoxicosis;
- itchy skin And skin diseases of different etiologies (eczema, rashes, dysfunction sebaceous glands etc.).
In addition, Benfotiamine is prescribed for chronic stages as part of complex treatment.
Contraindications
Restrictions on the use of Benfotiamine capsules:
- glucose-galactose malabsorption;
- increased sensitivity to lactose;
- individual intolerance (hypersensitivity);
- lack of isomaltase and/or sucrase.
The drug is used with caution in patients under 18 years of age.
Directions for use and dosage of Benfotiamine
The medication is taken orally 1.5-2 hours after meals. Frequency of administration – 1-4 times a day.
For adult patients average rate– 25-50 mg per day. Maximum dose– 0.2 g.
If Benfotiamine is prescribed to children, then its dosage is 10-30 mg.
For elderly patients, the minimum dosage is selected.
special instructions
You should not take an increased dose of Benfotiamine if you missed a previous dose. If this rule is neglected, the effectiveness of the drug may decrease or increase, which will lead to a violation of the treatment regimen.
In patients with alcoholism and/or menopause (in the pre- and postmenopausal period), using the medicine may develop allergic reaction, accompanied by itching, fever, chills, drowsiness and increased fatigue.
During pregnancy and lactation
Taking Benfotiamine during breastfeeding and pregnancy is contraindicated. In rare cases, the drug can be prescribed during lactation, but breastfeeding must be stopped because the active and auxiliary components of the drug can pass into breast milk.
In childhood
In old age
For elderly patients, Benfotiamine is prescribed in minimal doses. At the same time, they need careful monitoring of clinical indicators.
For liver dysfunction
Benfotiamine should not be used in acute liver failure.
For impaired renal function
If there are malfunctions in the functioning of this organ, dosage adjustment of the drug is not required.
Side effects
When using Benfotiamine, the following negative reactions may occur:
- allergies: urticaria, skin itching, anaphylactic shock, Quincke's edema;
- CNS: headache(rare), sensory peripheral neuropathy may develop with prolonged use;
- digestive system: nausea;
- dermatology: acne, excessive sweating;
- CVS: tachycardia.
Effect on driving
Clinical trials have shown that the drug does not have any effect on psychomotor skills and concentration, so driving a vehicle is not prohibited while taking Benfotiamine. However, the instructions for use of the medicine do not provide any information on this matter.
Overdose
Cases severe complications There were no cases of excess Benfotiamine dosage. In rare cases, dose-dependent enhancement may occur side effects. Subsequent treatment is aimed at eliminating symptoms.
Drug interactions
The active substance Benfotiamine reduces the level of effectiveness of depolarizing type muscle relaxants and suxamethonium iodide.
Under the influence of fluorouracil, the intensity of the drug's effect decreases
Alcohol compatibility
It inhibits and changes the effect of the medication, therefore, when treating with the drug, it is undesirable to drink alcohol-containing drinks.
Conditions for dispensing from pharmacies
Benfotiamine is an over-the-counter medication.
Price
The cost of a pack of 30 tablets is from 550 to 700 rubles. A package of 60 pills costs between 610-740 rubles.
Storage conditions
Benfotiamine must be stored out of the reach of children at a temperature of +15...+25°C.
Best before date
Up to 3 years from the date of production.
“Benfotiamine” belongs to the pharmacological group of vitamins, and is an analogue of thiamine (vitamin B1), and in its action and properties is very close to this and its derivatives.
Description
- The main active ingredient of the drug, benfotiamine, is a synthetic compound that is similar in structure and action to thiamine and cocarboxylase.
- It has a metabolic effect on the body, normalizes carbohydrate metabolism and replenishes deficiency.
- Benfotiamine takes an active part in metabolism, regulation nervous system and energy metabolism of tissues.
- The pharmacokinetic properties of the substance are radically different from water-soluble forms of thiamine.
- After benfotiamine is taken orally, it reaches the upper parts of the body. small intestine where it is absorbed.
- When the drug is absorbed in the gastrointestinal tract, the saturation effect does not occur.
- It fully penetrates into epithelial cells, where it is partially transformed into thiamine.
Release form
Active (active) substance – Benfotiamine:
- Benfotiamine is available in the form of tablets (5 and 25 mg) in packages of 50 and 100 pieces, as well as in the form of dragees (150 mg).
- The price is 700 rubles, available without a prescription.
- Store the drug at moderate humidity and room temperature(not higher than 30 o) and keep away from children.
- The shelf life of Benfotiamine is 4 years.
- Drug interactions.
At simultaneous administration"Benfotiamine" and some medicines and substances (for example, reducing and oxidizing compounds, as well as Fluorocil and its analogues), the effect of thiamine can be neutralized. can accelerate the breakdown of benfotiamine, and with increasing pH values, the substance loses its properties. The drug may weaken the effect of using Suxamethonium iodide and other peripherally acting depolarizing muscle relaxants.
Indications for use. Contraindications. Overdose
Benfotiamine is prescribed to patients as part of complex treatment for the following diseases:
- Hypo- or vitamin deficiency B1.
- Heart diseases, including ischemic disease, cardiopathy, rheumatic carditis, extrasystole.
- Chronic tonsillitis.
- Circulatory disorders of various origins.
- Chronic hepatitis in the acute stage.
- Skin diseases and dermatoses.
- Nervous system disorders.
A contraindication to taking the drug is hypersensitivity or individual intolerance to benfotiamine.
Mode of application:
- Benfotiamine is taken orally 1-4 times a day. per day.
- The dosage is prescribed by the doctor in each specific case.
- For adults single dose usually 0.025-0.05 g, for children – 0.03-0.035 g/day. (from 10 years old).
- For children aged 12 months and older – 0.01-0.03 g/day.
- The course of treatment can range from 10 to 30 days.
Overdose
Overdose may increase side effects which sometimes occur when taking the drug. In such cases, the patient is advised symptomatic treatment: gastric lavage, use of absorbents.
Side effects and special instructions
After administration, in some cases, various skin conditions may occur, in particular, itching, rash and Quincke's edema.
Special instructions:
- Taking Benfotiamine is possible only in cases of laboratory confirmed thiamine deficiency, when the benefit to the woman exceeds possible risk for a child.
- The drug is prescribed with great caution to women during menopause.
- Patients suffering from alcoholism.
Analogues
Benfotiamine analogues include the following drugs:
- "Benfogamma". This is the main and most affordable analogue drug, active substance which also includes benfotiamine.
- "Milgamma compositum". In addition to benfotiamine, Milgamma compositum contains pyridoxine (vitamin B6), and is therefore considered a drug of combined action.
- "Unigamma". Another complex one vitamin preparation, which contains vitamins B1, B6 and.
- "Kombilipen". Medicine, which is similar in composition and action to Unigamma.
Combilipen® tabs
International nonproprietary name
Dosage form
Film-coated tablets
Compound
One tablet contains
active substances: benfotiamine 100 mg, pyridoxine hydrochloride 100 mg, cyanocobalamin 2 mcg,
Excipients:
core: carmellose sodium, povidone-K30, microcrystalline cellulose, talc, calcium stearate, polysorbate-80, sucrose,
shell: hypromellose, macrogol-4000, low molecular weight povidone, titanium dioxide (E 171), talc.
Description
Round, biconvex, film-coated tablets, white or almost white.
Pharmacotherapeutic group
A combination of vitamin B1 with vitamins B6 and B12.
ATX code A11DB
Pharmacological properties
Pharmacokinetics
Benfotiamine is a fat-soluble form of thiamine (vitamin B1). Absorption - high, throughout small intestine. After absorption, it turns into the biologically active coenzyme form thiamine diphosphate. It accumulates mainly in the myocardium, skeletal muscles, nervous tissue, liver, and kidneys. It is excreted primarily in the urine, approximately 50% unchanged or in the form of sulfate ester.
Vitamin B6 is phosphorylated and oxidized to pyridoxal-5-phosphate. In blood plasma, pyridoxal 5-phosphate binds to albumin. To pass through the cell membrane, pyridoxal 5-phosphate bound to albumin is hydrolyzed alkaline phosphatase in pyridoxal.
Vitamin B12 after parenteral administration forms transport protein complexes that are quickly absorbed by the liver, bone marrow and other proliferative organs. Vitamin B12 enters the bile and takes part in the enterohepatic circulation. Vitamin B12 passes through the placenta.
Pharmacodynamics
Combined multivitamin complex. The effect of the drug is determined by the properties of the vitamins included in its composition.
Benfotiamine is a fat-soluble form of thiamine (vitamin B1). Participates in the conduction of nerve impulses.
Pyridoxine hydrochloride (vitamin B6) - participates in the metabolism of proteins, carbohydrates and fats, is necessary for normal hematopoiesis, the functioning of the central and peripheral nervous system. Provides synaptic transmission, inhibition processes in the central nervous system, participates in the transport of sphingosine, which is part of the nerve sheath, and participates in the synthesis of catecholamines.
Cyanocobalamin (vitamin B12) - participates in the synthesis of nucleotides, is important factor normal growth, hematopoiesis and development of epithelial cells; necessary for metabolism folic acid and myelin synthesis.
Indications for use
Neuralgia, neuritis
Pain syndrome caused by diseases of the spine (intercostal neuralgia, lumboischialgia, lumbar syndrome, cervical syndrome, cervicobrachial syndrome, radicular syndrome caused by degenerative changes spine)
Polyneuropathy of various etiologies(diabetic, alcoholic)
Directions for use and doses
Tablets should be taken after meals, without chewing and drinking sufficient quantity liquids. Adults: 1 tablet 1 time per day. IN severe cases, after preliminary consultation With your doctor, you can increase the number of doses up to 3 times a day.
Side effects
Allergic reactions (skin reactions in the form of itching, urticaria)
Increased sweating
Nausea
Tachycardia
Anaphylactic shock
Acne
Difficulty breathing, Quincke's edema
Contraindications
Hereditary fructose intolerance, glucose-galactose malabsorption, sucrase-isomaltase deficiency
Hypersensitivity to the components of the drug
Heavy and sharp forms decompensated heart failure
Thromboembolism
Erythremia
Erythrocytosis
Pregnancy and lactation
Children's and adolescence up to 18 years old
Drug interactions
Levodopa reduces the effect of therapeutic doses of vitamin B6. Vitamin B12 is incompatible with salts heavy metals. Ethanol reduces the absorption of thiamine. While taking the drug, it is not recommended to take multivitamin complexes containing B vitamins.
Antacids slow down the absorption of vitamin B1. Possible interactions with D-penylamine, cycloserine.
special instructions
The drug contains sucrose, so it should be administered with caution to patients with diabetes mellitus.
In rare cases, excessive daily doses of vitamin B6 (500 mg or more over more than 5 months) lead to peripheral sensory neuropathy, which usually disappears when the drug is stopped.
Taking vitamin B12 is contraindicated in patients with psoriasis due to the possible worsening of symptoms of the disease.
Pyridoxine hydrochloride may cause acne.
Other vitamins can be inactivated in the presence of vitamin B1 breakdown products.
In 1954, Japanese scientists from the Sankyo company synthesized the substance benfotiamine. The created compound is similar to thiamine in its activity. Thus, benfotiamine is a fat-soluble synthetic analogue of vitamin B1.
Pyridoxine - water soluble vitamin B6, which enters the body with various foods. Thus, the substances benfotiamine and pyridoxine are independent medicinal products and in combination are included in other medications.
Pharmacological action of B1 and B6
Benfotiamine has enhanced penetration into peripheral nerves, the highest concentration of the substance in plasma, liver, cerebrospinal fluid, red blood cells and ability long time persist in the human body. Has higher bioavailability compared to water-soluble B1.
Metabolic effect on the body:
- normalizing carbohydrate metabolism, replenishes thiamine deficiency;
- actively participates in metabolic processes;
- regulates the activity of the nervous system, improves the conduction of impulses of nerve endings;
- normalizes carbohydrate-energy metabolism in tissues;
- protects blood vessels and nerve fibers from damage by glycotoxins.
Pyridoxine is a water-soluble form of vitamin B6, necessary for the full functioning of the central nervous system. Stimulates metabolic processes, participates as a coenzyme in the metabolism of proteins and amino acids, and affects lipid and fat metabolism in the body.
The therapeutic use of active neurotropic substances is justified by the insufficient intake of B vitamins in the body. Benfotiamine and peridoxine in combination have a pronounced effect and have the most positive therapeutic effect. Use of B1, B6 for diseases of various origins aimed at replenishing their deficiency and stimulating natural mechanisms recovery.
For the compounds benfotiamine and pyridoxine tradename depends on the patent pharmaceutical company for the production of medicines in which they are present as basic or additional. In our country the most common combination drugs containing these substances are Polynervin, Benevron, Benfogamma and Milgama Compositum.
Combined multivitamin preparation
Benfotiamine and peridoxine have a beneficial effect on the effectiveness of treatment in their complex combination. Such a drug is "Milgamma Compositum". Therapeutic effect aimed at enhancing metabolic processes in tissues and organs, regulation of cell energy resources, restoration of nerve impulse conduction.
Widely used for inflammatory processes, degenerative diseases musculoskeletal system, pathologies of the central nervous system, for relief pain syndrome. Provides a moderate analgesic effect.
The drug is available in two dosage forms: injection (solution) and tablets (dragees). The composition of the solution for injection additionally includes cyanocobalamin - vitamin B12. The price for the drug "Milgamma Compositum" varies depending on dosage form. So, 10 ampoules of 2 milliliters each cost about 500 rubles, and a package of 100 mg tablets of 60 pieces costs 1,180 rubles.
Indications for use
Benfotiamine (B1) and peridoxine (B6) are used in case of deficiency of one of the vitamins and in combination as a means for symptomatic therapy a number of diseases:
- CNS pathologies of various origins: myalgia, neuritis, neuralgia, radicular syndrome, paresis, paralysis, diabetic or alcoholic polyneuropathy;
- atherosclerosis;
- anemia;
- Alzheimer's disease;
- spicy, chronic intoxication;
- diseases associated with circulatory disorders;
- inflammatory and degenerative diseases of the musculoskeletal system;
- viral hepatitis;
- cirrhosis of the liver;
- seasickness;
- Meniere's disease;
- shingles;
- neurodermatitis;
- dermatitis
- herpes and others.
In addition, in combination with other drugs they can be used as an analgesic.
Included in the preparations
ATX:N.07.X.X Other drugs for the treatment of diseases of the nervous system
Pharmacodynamics:The drug is a combination of vitamins
B.Benfotiamine , a fat-soluble derivative of thiamine (vitamin B1), is phosphorylated in the body to the biologically active coenzymes thiamine diphosphate and thiamine triphosphate. Thiamine diphosphate is a coenzyme of pyruvate decarboxylase, 2-oxyglutarate dehydrogenase and transketolase, thus participating in the pentose phosphate cycle of glucose oxidation (aldehyde group transfer).
Phosphorylated formopyridoxine (vitamin B 6) - is a coenzyme of a number of enzymes that influence all stages of non-oxidative metabolism of amino acids. participates in the process of decarboxylation of amino acids, and, consequently, in the formation of physiologically active amines (for example, adrenaline, serotonin, dopamine, tyramine). Participating in the transamination of amino acids, it is involved in anabolic and catabolic processes (for example, being a coenzyme of such transaminases as glutamate-oxaloacetate transaminase, glutamate-pyruvate transaminase, gamma-aminobutyric acid (GABA), α-ketoglutarate transaminase), as well as in various reactions breakdown and synthesis of amino acids. Vitamin B 6 is involved in 4 different stages tryptophan metabolism.
Pharmacokinetics:Suction and distribution
When taken orally most of benfotiamine is absorbed into duodenum, smaller - in the upper and middle parts of the small intestine. absorbed due to active resorption and due to passive diffusion (in different concentrations). Being a fat-soluble derivative of thiamine (vitamin B1), it is absorbed faster and more completely than water-soluble thiamine hydrochloride. In the intestine it is converted to S-benzoylthiamine as a result of dephosphorylation by phosphatases. S-benzoylthiamine is fat-soluble, has a high penetrating ability and is absorbed, basically, without being converted into. Due to enzymatic debenzoylation after absorption, the biologically active coenzymes thiamine diphosphate and thiamine triphosphate are formed. Especially high levels These coenzymes are observed in the blood, liver, kidneys, muscles and brain.
Pyridoxine (vitamin B 6) and its derivatives are absorbed primarily into upper sections Gastrointestinal tract during passive diffusion. In blood serum, pyridoxal is bound to albumin. Before penetration through the cell membrane, bound to albumin, it is hydrolyzed by alkaline phosphatase to form pyridoxal.
Metabolism and excretion
Both vitamins are excreted primarily in the urine. Approximately 50% of thiamine is excreted unchanged or as sulfate. The remainder consists of several metabolites, among which are thiamine acid, methylthiazoacetic acid and pyramine. The average half-life of benfotiamine in the blood is 3.6 hours.
Half-life
pyridoxine when taken orally is approximately 2-5 hours. The biological half-life of thiamine and pyridoxine is approximately 2 weeks. Indications:Neurological diseases with confirmed deficiency of vitamins B 1 and B 6.
I.B00-B09.B02.2 Herpes zoster with other nervous system complications
VI.G50-G59.G50.0 Trigeminal neuralgia
VI.G50-G59.G51 Facial nerve lesions
VI.G50-G59.G54 Lesions of nerve roots and plexuses
VI.G60-G64.G60 Hereditary and idiopathic neuropathy
VI.G60-G64.G61 Inflammatory polyneuropathy
VI.G60-G64.G62.1 Alcoholic polyneuropathy
VI.G60-G64.G63.2* Diabetic polyneuropathy (E10-E14+ with a common fourth sign.4)
VII.H46-H48.H46 Optic neuritis
XIII.M40-M43.M42 Osteocondritis of the spine
XIII.M50-M54.M54.1 Radiculopathy
XIII.M50-M54.M54.3 Sciatica
XIII.M50-M54.M54.4 Lumbago with sciatica
XIII.M70-M79.M79.2 Neuralgia and neuritis, unspecified
XVIII.R25-R29.R25.2 Cramp and spasm
Contraindications:Decompensated heart failure; childhood(due to lack of data); pregnancy; period breastfeeding; hypersensitivity to thiamine, benfotiamine, pyridoxine or other components of the drug.
Carefully:Should be used with caution in congenital fructose intolerance, glucose/galactose malabsorption syndrome or glucose-isomaltase deficiency.
Pregnancy and lactation:The use of the drug is contraindicated during pregnancy and lactation (breastfeeding).
Directions for use and dosage:The pills should be taken orally and washed down with plenty of liquid.
Adults are prescribed 1 tablet per day.
In acute cases, after consulting a doctor, the dose can be increased to 1 tablet 3 times a day.
After 4 weeks of treatment, the doctor must decide on the need to continue taking the drug at an increased dose and consider reducing the dose of vitamins B 6 and B 1 to 1 tablet per day. If possible, the dose should be reduced to 1 tablet per day in order to reduce the risk of developing neuropathy associated with the use of vitamin B6.
Side effects:Allergic reactions:
very rarely - skin reactions, itching, urticaria, skin rash, difficulty breathing, Quincke's edema, anaphylactic shock.From the nervous system:
in some cases - headache; frequency unknown (single spontaneous reports) - peripheral sensory neuropathy with long-term use of the drug (more than 6 months).From the digestive system:
very rarely - nausea.For the skin and subcutaneous fat:
frequency unknown (single spontaneous reports) - acne, increased sweating.From the cardiovascular system:
frequency unknown (single spontaneous messages) - tachycardia. Overdose:Given the wide therapeutic range, overdose of benfotiamine when taken orally is unlikely.
Taking high doses of pyridoxine (vitamin B6) over a short period of time (at a dose of more than 1 g per day) can lead to short-term neurotoxic effects. When using the drug at a dose of 100 mg per day for more than 6 months, the development of neuropathies is also possible. Overdose, as a rule, manifests itself in the development of sensory polyneuropathy, which may be accompanied by ataxia. Taking the drug in extremely high doses can lead to seizures. In newborns and infants, the drug can have a strong sedative effect, cause hypotension and breathing disorders (dyspnea, apnea).
Treatment of overdose
When taking pyridoxine in a dose exceeding 150 mg/kg body weight, it is recommended to induce vomiting and take. Provocation of vomiting is most effective during the first 30 minutes after taking the drug. Emergency symptomatic therapy may be required.
Interaction:In therapeutic doses (vitamin B 6) may reduce the effect of levodopa.
Concomitant use of pyridoxine antagonists (for example, hydralazine, isoniazid, penicillamine, cycloserine), alcohol consumption and long-term use Estrogen-containing oral contraceptives can lead to vitamin B6 deficiency in the body.
When taken simultaneously with fluorouracil, deactivation of thiamine (vitamin B1) is observed, since it competitively inhibits the phosphorylation of thiamine to thiamine diphosphate.
Special instructions:Impact on the ability to drive vehicles and operate machinery
There are no warnings regarding the use of the drug by vehicle drivers and persons working with potentially dangerous mechanisms.
Instructions
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