Neurobion Injections N3 3ml
Ingredients.
1 ampoule (3 ml) contains: thiamine hydrochloride (vitamin B1) 100 mg, pyridoxine hydrochloride (vitamin B6) 100 mg, cyanocobalamin (vitamin B12) 1 mg;
Other ingredients : sodium hydroxide solution 1M, potassium cyanide, water for injection.
Pharmaceutical form :Solution for injection.
Basic physical and chemical properties: red, transparent solution.
Pharmacotherapeutic group
Vitamin B1 preparations in combination with vitamin B6 and/or vitamin B12. ATC code A11D B.
Pharmacological properties
Pharmacodynamics of Neurobion.
The drug in the dosage form of a solution for injection in ampoules contains a combination of neurotropic active substances of a complex of B vitamins. The vitamins included in the drug, namely thiamine (B1), pyridoxine (B6) and cobalamin (B12), play a special role as coenzymes in intermediate metabolism in the central and peripheral nervous system. Like all vitamins, they are essential nutrients that the body cannot synthesize on its own. The therapeutic use of vitamins B1, B6 and B12 compensates for their insufficient intake with food and thus ensures the presence of the required amount of coenzymes in the body.
Thiamine (vitamin B1). Thiamine pyrophosphate (TPP) is the active form of vitamin B1 and acts as a coenzyme for a number of enzymes (e.g. pyruvate dehydrogenase and transketolase). Accordingly, vitamin B1 is primarily involved in carbohydrate metabolism, but it is also involved in the synthesis of lipids and amino acids. Nerve cells cover their energy needs exclusively through the enzymatic oxidation and decarboxylation of glucose, which means that an adequate supply of vitamin B1 is very important. Thiamine is involved in the conduction of nerve impulses.
Pyridoxine (vitamin B6). Pyridoxal phosphate, a biologically active form of pyridoxine, is a crucial coenzyme in amino acid metabolism. It is involved in the formation of physiologically active amines (e.g. serotonin, histamine, epinephrine) through decarboxylation processes, as well as in anabolic and catabolic processes through transamination. Pyridoxal phosphate plays an important role in the central nervous system, especially in enzymatically controlled neurotransmitter metabolism. As a catalyst for the first stages of sphingosine biosynthesis, pyridoxal phosphate also plays a key role in the metabolism of sphingolipids, which are important components of the myelin membranes of nerve cells.
Cobalamin (vitamin B12). Vitamin B12 in its active form (5-deoxyadenosylcobalamin and methylcobalamin) is involved in enzyme-catalyzed intramolecular hydrogen transfer and intramolecular transfer of methyl groups. Vitamin B12 is also involved in the synthesis of methionine (closely related to the synthesis of nucleic acids) and in lipid metabolism by converting propionic acid to succinic acid. Vitamin B12 is involved in methylation of myelin, the main protein of the myelin sheaths of the nervous system. Methylation increases the lipophilic properties of the basic protein, improving its incorporation into the myelin sheath.
A combination of vitamins B1, B6 and B12. Given their biochemical functions, vitamins B1, B6, and B12 are particularly important for the metabolic processes of the nervous system, both individually and in combination. In addition, most vulnerable groups of patients, such as the elderly, diabetics, and others, have a deficiency of all three of these neurotropic vitamins. Animal studies have shown that this combination of neurotropic B vitamins accelerates regenerative processes in damaged nerve fibers, which in turn leads to faster recovery of muscle function and innervation. The use of combinations of B vitamins in rats with diabetes mellitus prevented nerve damage or attenuated damage in such a way that the deterioration of functional properties was reduced (antineuropathic effect).
In animal experiments and in clinical trials, antinociceptive effect of vitamins B1, B6 and B12 has been shown.
Pharmacokinetics of Neurobion.
The combined use of vitamins B1, B6 and B12 does not affect the pharmacokinetics of individual vitamins.
Thiamine (vitamin B1)
The biological half-life in the human body is approximately 9.5-18.5 days with an elimination half-life of approximately 4 hours. The human body can store 20-30 mg of thiamine (mainly in the heart, brain, liver and kidneys). Due to rapid metabolism, reserve reserves are very limited and are used up in 4-10 days.
Pyridoxine (vitamin B6)
Vitamin B6 is predominantly phosphorylated in the liver, forming the biologically active form pyridoxal phosphate. In order to pass through the cell membrane, phosphorylated vitamin B6 must be hydrolyzed by alkaline phosphatase to release vitamin B6. Transportation within the cell occurs by diffusion followed by re-phosphorylation. The biological half-life of pyridoxal phosphate is 15-25 days, and the elimination half-life is approximately 3 hours. Approximately 40-150 mg can be retained in the human body, with cumulation occurring within 14-42 days, and excretion
Cobalamin (vitamin B12)
Orally administered vitamin B12 has a low absorption rate, which may be further reduced after bariatric surgery, in elderly patients, in patients on dialysis, and in patients with other forms of malabsorption. In addition to the saturated active absorption of orally ingested vitamin B12 with a maximum daily absorption level of approximately 1.5 mcg, vitamin B12 can also be absorbed by passive diffusion. The proportion that is absorbed by passive diffusion is only about 1-2% of the amount taken. It can be further reduced in patients who have undergone bariatric surgery or who have impaired gastrointestinal absorption due to other diseases. For such patients, parenteral administration may be appropriate.
Approximately 90% of cobalamin in the blood plasma is bound to proteins (transcobalamins). Vitamin B12 does not circulate in the blood plasma, it accumulates mainly in the liver, and its daily requirement is approximately 1 mcg. The metabolic rate is 2.5 mcg/day, or 0.05% of the amount stored.
Vitamin B12 is secreted primarily into bile and reabsorbed in large quantities through the intestinal and hepatic circulation. If the body's storage capacity is exceeded due to high doses, especially parenterally, the excess is excreted in the urine.
Indications.
Neurological diseases accompanied by severe deficiency of vitamins B1, B6 and B12, which cannot be eliminated by oral means.
Contraindications.
Hypersensitivity to the active substances or to any of the excipients.
Vitamin B1 is contraindicated in case of allergic diseases.
Vitamin B6 is contraindicated in case of gastric and duodenal ulcers in the acute stage (as it may increase the acidity of gastric juice).
Vitamin B12 is contraindicated in case of erythremia, erythrocytosis, thromboembolism.
It is contraindicated in children (under 18 years of age).
Special safety precautions
Use syringes and needles (not included in the package of Neurobion) only once. Dispose of syringes and needles immediately after use. Unused medicine or waste should be disposed of in accordance with applicable laws.
It is not recommended to mix Neurobion, solution for injection, with other medicinal products in the same syringe.
Interaction with other medicinal products and other types of interaction
Cobalamin (vitamin B12). Vitamin B12 in its active form (5-deoxyadenosylcobalamin and methylcobalamin) is involved in enzyme-catalyzed intramolecular hydrogen transfer and intramolecular transfer of methyl groups.
Vitamin B12 is also involved in the synthesis of methionine (closely related to the synthesis of nucleic acids) and in lipid metabolism by converting propionic acid to succinic acid. Vitamin B12 is involved in methylation of myelin, the main protein of the myelin sheaths of the nervous system.
Methylation increases the lipophilic properties of the basic protein, improving its incorporation into the myelin sheath. A combination of vitamins B1, B6 and B12.
Given their biochemical functions, vitamins B1, B6, and B12 are particularly important for the metabolic processes of the nervous system, both individually and in combination. In addition, most vulnerable groups of patients, such as the elderly, diabetics, and others, have a deficiency of all three of these neurotropic vitamins.
Animal studies have shown that this combination of neurotropic B vitamins accelerates regenerative processes in damaged nerve fibers, which in turn leads to faster recovery of muscle function and innervation.
The use of combinations of B vitamins in rats with diabetes mellitus prevented nerve damage or attenuated damage in such a way that the deterioration of functional properties was reduced (antineuropathic effect).
In animal experiments and in clinical trials, antinociceptive effect of vitamins B1, B6 and B12 has been shown.
Breastfeeding
Vitamins B1, B6 and B12 are excreted in human breast milk. High concentrations of vitamin B6 (600 mg per day) may inhibit breast milk production. There are no animal studies on the extent of secretion into breast milk. Therefore, the medicine is not recommended for use during breastfeeding. The decision to stop breastfeeding or discontinue the drug should be made taking into account the benefits of breastfeeding for the child and the benefits of treatment for the mother.
The ability to influence the reaction rate when driving vehicles or other mechanisms.
If dizziness is observed during treatment with the drug, you should refrain from driving vehicles and operating other machinery. This medicine does not affect or has a negligible effect on the ability to drive vehicles and work with other machinery.
Dosage and administration route
The drug is intended for intramuscular administration.
Dosage.
In severe (acute) cases: one ampoule per day until the intensity of acute symptoms decreases.
After symptoms subside: one ampoule 1-3 times a week.
To maintain or prolong the initial therapeutic course of injections and to prevent relapse, it is recommended to use the drug in the form of coated tablets.
Children.
The experience of using the drug in children is limited. Therefore, the drug should not be prescribed to patients in this group.
Method of administration
The drug should be administered intramuscularly (deep injection into the gluteal muscle).
Children. Do not use in children under 18 years of age.
Overdose.
In case of prolonged use in high doses, liver enzymes activity disorders, pain in the heart area, hypercoagulability may occur.
Vitamin B1
Thiamine has a wide therapeutic range. Very high doses (more than 10 g) have a ganglion-blocking effect and inhibit the conduction of nerve impulses in a curar-like manner.
Vitamin B6
The toxicity of vitamin B6 can be considered very low.
However, long-term (> 6-12 months) use of vitamin B6 in daily doses of more than 50 mg may cause peripheral sensory neuropathy. Symptoms gradually disappear after discontinuation of the drug.
Continuous use of vitamin B6 in daily doses of more than 1 g for more than two months may lead to neurotoxic adverse reactions.
When used in excess of 2 g per day, cases of neuropathy with ataxia and sensory disturbances, cerebral convulsions with EEG changes, and in some cases hypochromic anemia and seborrheic dermatitis have been described.
In animal studies, high doses of vitamin B6 disrupted spermatogenesis.
Vitamin B12
After parenteral administration in high doses, eczematous skin lesions and acne-like rashes were observed.
Side effects
The following are adverse reactions classified by organ system and frequency. The evaluation of adverse reactions is based on the following frequency classification:
very often (≥ 1/10); often (≥ 1/100, < 1/10); infrequently (≥ 1/1000, < 1/100); rarely (≥ 1/10000, < 1/1000); very rarely (< 1/10000); frequency unknown (cannot be estimated from available data).
Immune system: rash, skin flushing.
Very rarely: hypersensitivity reactions, such as sweating, tachycardia and skin reactions, in particular acne, eczema, pruritus and urticaria, as well as anaphylaxis.
Nervous system: nervous excitement, malaise, dizziness, headache.
Frequency is unknown: long-term use (more than 6-12 months) of vitamin B6 in doses of more than 50 mg per day may lead to peripheral sensory neuropathy. Symptoms gradually decrease after discontinuation of the vitamin.
Digestive system: increased acidity of gastric juice.
The frequency is unknown: gastrointestinal complaints such as nausea, vomiting, diarrhea, abdominal pain.
From the skin and subcutaneous tissue.
The frequency is unknown: eczematous skin lesions, acne and acne-like rashes have been observed after high doses of vitamin B12.
Kidney and urinary tract disorders.
The frequency is unknown: chromaturia (red urine coloration observed during the first hours after drug administration; normalization usually occurs shortly after drug discontinuation).
Systemic disorders and complications at the injection site.
Frequency unknown: injection site reactions.
Shelf life.
3 years.
Storage conditions.
Store at a temperature of 2-8 °C in a dark place. Keep out of the reach of children.
Other vitamins, especially cyanocobalamin (vitamin B12), may be deactivated in the presence of drugs that have a destructive effect on vitamin B1.
Packaging.
3 ml in an ampoule; 3 ampoules in a cardboard box.
Manufacturer
Senexi HSC, France.