Combilipen Neo, 2 ml 10 pcs

Pharmacotherapeutic group: B vitamins

ATX code: A11DB

Pharmacological properties

Pharmacodynamics

Pharmacological action is determined by the properties of the vitamins that make up the drug. The drug contains vitamins B1 (thiamin), B6 (pyridoxine) and B12 (cyanocobalamin), deficiency of which may lead to neurological disorders, mainly in the peripheral nervous system.
Neurotropic B vitamins have beneficial effects on inflammatory and degenerative diseases of the nerves and musculoskeletal system.

A special role in the metabolic processes of the nervous system plays a combined effect of vitamins B1, B6, B12, proven that the effectiveness of the combination is superior to the individual component. The combined use of B vitamins accelerates the regeneration of damaged nerve fibers, also proven analgesic effect of the complex.

Thiamine plays a key role in the processes of carbohydrate metabolism, which are critical in the metabolic processes of nervous tissue (involved in the conduction of the nerve impulse), and the Krebs cycle, with subsequent participation in the synthesis of thiamine pyrophosphate (TPP) and adenosine triphosphate (ATP).

Pyridoxine has a vital influence on the metabolism of proteins, carbohydrates and fats and is necessary for normal hematopoiesis and the functioning of the central and peripheral nervous system. It provides synaptic transmission, the processes of inhibition in the central nervous system (CNS), participates in the transport of sphingosine, which is part of the nerve sheath, participates in the synthesis of catecholamines.

The physiological function of both vitamins is to potentiate each other’s action, manifesting itself in a positive effect on the nervous, neuromuscular and cardiovascular systems. It is a cofactor in the reactions of the transfer of single-carbon groups, is involved in the synthesis of myelin sheath, stimulates hematopoiesis, reduces pain associated with lesions of the peripheral nervous system, stimulates nucleic metabolism through the activation of folic acid.

Pharmacokinetics

. After intramuscular administration, thiamine is rapidly absorbed from the injection site and enters the blood (484 ng/mL after 15 min on the first day of the 50 mg dose) and is unevenly distributed in the body, with its content in white blood cells 15%, red blood cells 75% and in plasma 10%.

Thiamine penetrates the blood-brain and placental barriers and is found in the mother’s milk. Thiamine is excreted in the urine in the alpha phase after 0.15 hours, in the beta phase after 1 hour and in the terminal phase within 2 days. The main metabolites are thiamine carboxylic acid, pyramine and some unknown metabolites. Of all vitamins, thiamine is retained in the body in the smallest amounts. The adult body contains about 30 mg of thiamine as 80% thiaminpyrophosphate, 10% thiaminotriphosphate, and the rest as thiaminmonophosphate.

After intramuscular administration, pyridoxine is rapidly absorbed into the bloodstream and distributed in the body, acting as a coenzyme after phosphorylation of the CH2ON group in the 5th position to form metabolically active pyridoxalphosphate. About 80% of the vitamin is bound to plasma proteins.

Pyridoxine is distributed throughout the body and crosses the placenta and is found in mother’s milk, deposited in the liver and oxidized to 4-pyridoxylic acid, which is excreted in the urine, maximum 2-5 hours after absorption. The human body contains 40-150 mg of vitamin B6 and its daily elimination rate is about 1.7-3.6 mg with a replenishment rate of 2.2-2.4%.

After parenteral administration, cyanocobalamin forms complexes with the transcobalamin transport protein, which are rapidly absorbed by the liver, bone marrow and other organs. Cyanocobalamin is excreted into the bile and takes part in the intestinal-hepatic circulation. It passes through the placenta.

Indications

In the treatment of: mono- and polyneuropathies of different genesis; dorsalgia; plexopathies; lumboichialgia radicular syndrome caused by degenerative changes in the spine.

Composition

Active ingredients:

Thiamine hydrochloride – 100.0 mg

Pyridoxine hydrochloride – 100.0 mg

Cyanocobalamin – 1.0 mg

Excipients: diethanolamine – 5.0 mg, water for injection – up to 2.0 ml.

How to take, the dosage

The drug is injected intramuscularly (deep injections into the gluteal muscle).

Treatment is recommended to start with intramuscular injection of 1 ampoule (2 ml) per day until acute symptoms are relieved.

After symptoms improve or in cases of moderate disease severity: one ampoule 2-3 times a week for 2-3 weeks.

For maintenance therapy, for relapse prevention or continuation of the current course of treatment it is recommended to switch to oral administration of the drug

Kombilipen® tablets in the form of film-coated tablets.

Treatment duration is determined by the doctor individually depending on the severity of the symptoms.

Interaction

When used concomitantly with levodopa, vitamin B6 may decrease the antiparkinsonian effect of levodopa.

Concurrent use of pyridoxine antagonists (e.g., isoniazid, hydralazine, penicillamine or cycloserine) may increase the need for pyridoxine.

“Loop” diuretics, such as furosemide, can block tubular reabsorption, thus increasing thiamine excretion with long-term use, resulting in lower blood thiamine levels.

Vitamin B1 is destroyed in interaction with solutions containing sulfites.

It is not recommended to mix the drug with other drugs in the same syringe.

Cyanocobalamin is incompatible with ascorbic acid, salts of heavy metals.

Special Instructions

The drug should only be administered intramuscularly, avoiding vascular ingestion. If accidentally administered intravenously, the patient should be monitored by a physician or hospitalized depending on the severity of the resulting symptoms. Other vitamins, especially cyanocobalamin, may be inactivated in the presence of vitamin B1 degradation products.

The clinical picture as well as laboratory tests for funicular myelosis or pernicious anemia may lose their specificity with vitamin B12 administration.

The drug may cause neuropathies with prolonged use over 6 months.

Influence on the ability to drive and operate vehicles

There is no information about caution regarding the use of the drug Kombilipen® NEO by drivers of vehicles and persons working with potentially dangerous mechanisms. However, caution is recommended, taking into account the possibility of developing adverse reactions of the drug.

Synopsis

Transparent pinkish-red liquid with a characteristic odor.

Contraindications

Hypersensitivity to the drug components.

Childhood.

Pregnancy and breastfeeding.

Overdose

Vitamins B1, B6 and B12 have a wide therapeutic range. Symptoms of overdose are not observed when using the drug in the recommended doses and regimen.

Vitamin B1: report the following symptoms after administration of a dose greater than 100 times the recommended (>10 g): curare-like ganglioblocking effects, causing disruption of nerve impulse conduction.

Vitamin B6: prolonged use (>6-12 months) of vitamin B6 at a daily dose of >50 mg may cause peripheral sensory neuropathy. Prolonged use of vitamin B6 at a daily dose greater than 1 g for more than 2 months may cause neurotoxic effects. After administering more than 2 g per day there have been described cases of hypochromic anemia and seborrheic dermatitis, neuropathy with ataxia, sensory disorders, epileptiform seizures with EEG changes.

Vitamin B12: after parenteral administration of a high dose allergic reactions, eczematous skin disorders and benign form of acne were observed.

Treatment: In case of overdose symptoms the drug shall be discontinued. If necessary, symptomatic therapy, including desensitizing therapy, is prescribed.