Composition
The solution for intravenous use is pinkish-red to red in color, with a specific smell.
1 ml | |
pyridoxine hydrochloride | 50 mg |
thiamine hydrochloride | 50 mg |
cyanocobalamin | 0.5 mg |
lidocaine hydrochloride | 10 mg |
Auxiliary substances:
benzyl alcohol-20 mg,
sodium tripolyphosphate-10 mg,
potassium hexacyanoferrate-0.1 mg,
sodium hydroxide solution of 10 M-up to pH 4.0-5.0,
water for injection – up to 1 ml
Pharmacological action
Combined multivitamin agent. The effect of the combination is determined by the properties of the vitamins that make up its composition. Neurotropic B vitamins have a beneficial effect on inflammatory and degenerative diseases of the nervous system and musculoskeletal system.
Thiamine (vitaminB1) is involved in conducting a nerve impulse.
Pyridoxine (vitaminB6) has a vital effect on the metabolism of proteins, carbohydrates and fats, is necessary for normal hematopoiesis, the functioning of the central and peripheral nervous system. It 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 (vitaminB12) is involved in the synthesis of nucleotides, is an important factor in the normal growth, hematopoiesis and development of epithelial cells, and is necessary for folic acid metabolism and myelin synthesis.
Lidocaine has an anesthetic effect at the injection site, dilates blood vessels, promoting the absorption of vitamins. The local anesthetic effect of lidocaine is caused by the blockade of potential-dependent Na+channels, which prevents the generation of impulses in the endings of sensitive nerves and the conduction of pain impulses along nerve fibers.
Indications
In the complex therapy of the following neurological diseases: trigeminal neuralgia; facial neuritis; pain syndrome caused by diseases of the spine (intercostal neuralgia, lumboschialgia, lumbar syndrome, cervical syndrome, cervical-brachial syndrome, radicular syndrome caused by degenerative changes of the spine); polyneuropathy of various etiologies (diabetic, alcoholic).
Recommendations for use
If the pain syndrome is severe, it is advisable to start treatment with an intravenous injection (deep) of 2 ml daily for 5-10 days, with a further transition to either oral use of this combination in fixed doses, or to more rare injections (2-3 times/week. within 2-3 weeks) with possible continuation of therapy with an oral dosage form.
Contraindications
Severe and acute forms of decompensated heart failure; pregnancy; lactation (breastfeeding); childhood (due to lack of data); hypersensitivity to the components of the combined agent.
With caution
Cardiac arrhythmias, severe hypotension.
Side effects
Possible: Â allergic reactions in the form of pruritus, urticaria; difficulty breathing, angioedema, anaphylactic shock.
In some cases: Â sweating, tachycardia, acne.
Interaction
VitaminB1 completely breaks down in solutions containing sulfites, is incompatible with oxidizing and reducing substances (mercury chloride, iodide, carbonate, acetate, tannic acid, iron(III)-ammonium citrate), as well as sodium phenobarbital, riboflavin, benzylpenicillin, dextrose and sodium metabisulfite.
Levodopa reduces the effect of therapeutic doses of vitaminB6.
VitaminB12 is incompatible with heavy metal salts, ascorbic acid.
Functional features
After intravenous use, thiamine is rapidly absorbed and enters the bloodstream. The concentration of thiamine is 484 ng / ml 15 minutes after use of the drug at a dose of 50 mg (on the 1st day of use). Thiamine is unevenly distributed in the body. The content of thiamine in white blood cells is 15%, in red blood cells-75% and in plasma-10%. Due to the lack of significant reserves of vitamin in the body, it must be ingested daily. Thiamine passes through the BBB and placental barrier and is found in breast milk. The main metabolites of thiamine are thiamincarboxylic acid, pyramine, and some unknown metabolites. Of all the vitamins, thiamine is stored in the body in the smallest amounts. The adult body contains about 30 mg of thiamine in the form of 80% thiamine pyrophosphate,10% thiamine triphosphate and the remaining amount in the form of thiamine monophosphate. Thiamine is excreted in the urine, T1/2 of the α-phase – 0.15 h, β-phase-1 h and terminal phase-within 2 days.
After intravenous use, pyridoxine is rapidly absorbed into the systemic circulation and distributed in the body, acting as a coenzyme after phosphorylationof the CH2 groupIT is in the 5th position. Pyridoxine is distributed throughout the body, penetrates the placental barrier and is found in breast milk. The body contains 40-150 mg of vitaminB6, its daily elimination rate is about 1.7-3.6 mg with a replenishment rate of 2.2-2.4%. About 80% of pyridoxine binds to plasma proteins. Pyridoxine is deposited in the liver and oxidized to 4-pyridoxic acid, which is excreted in the urine, a maximum of 2-5 hours after absorption.
After parenteral use, cyanocobalamin forms complexes with the transport protein transcobalamin, which are rapidly absorbed by the liver, bone marrow, and other organs. Cyanocobalamin is excreted in the bile and participates in the intestinal-hepatic circulation. Penetrates the placental barrier.
After intravenous use of lidocaine, absorption is almost complete. Distribution is rapid, Vd is about 1 l / kg (lower in patients with heart failure). Binding to proteins depends on the concentration of the Active ingredient in plasma and is 60-80%. It is mainly metabolized in the liver with the formation of active metabolites, which can contribute to the manifestation of therapeutic and toxic effects, especially after infusion for 24 hours or more. T1/2 tends to be two-phase with a distribution phase of 7-9 min. In general, T1/2 depends on the dose, is 1-2 hours and can increase to 3 hours or more during prolonged intravenous infusions (more than 24 hours). It is excreted by the kidneys in the form of metabolites,10% unchanged.
Special instructions
In case of accidental intravenous use, the patient should be under medical supervision or hospitalized, depending on the severity of the symptoms.
In case of overdose, dizziness, nausea, vomiting, itching, urticaria, increased sweating, tachycardia are possible.
Active ingredient
Pyridoxine, Thiamine, Cyanocobalamin, [Lidocaine]
Conditions of release from pharmacies
By prescription
Dosage form
solution for injection
Indications
Sciatica, Neuralgia, Sciatica, Neuritis, Lumbago, Osteochondrosis
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Side effects of Larigama solution for intramuscular injection 2ml, 10pcs.
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