Kombilipen solution for injection, 2ml # 10

In complex therapy:

• mono- and polyneuropathies of various origins;

• dorsalgia;

• plexopathy;

• lumboischialgia;

• radicular syndrome caused by degenerative changes in the spine.

V / m (deep).

In cases of severe pain syndrome, in order to quickly achieve a high level of the drug in the blood, it is advisable to start treatment with 2 ml daily for 5-10 days. Later, after the pain syndrome subsides and in milder forms of the disease, they switch either to therapy with a dosage form for oral administration (for example, MilgammaЃ compositum), or to more rare injections (2-3 times a week for 2-3 weeks) with a possible continuation therapy with a dosage form for oral administration.

A weekly monitoring of therapy by a physician is recommended.

The transition to therapy with a dosage form for oral administration is recommended to be carried out as soon as possible.

active substances:

thiamine hydrochloride - 100 mg

pyridoxine hydrochloride - 100 mg

cyanocobalamin - 1 mg

lidocaine hydrochloride - 20 mg

excipients: benzyl alcohol - 40 mg; sodium polyphosphate - 20 mg; potassium hexacyanoferrate - 0.2 mg; sodium hydroxide - 12 mg; water for injection - up to 2 ml.

• Hypersensitivity to the components of the drug.

• Acute heart failure, chronic heart failure in the stage of decompensation.

• Children under 18 years of age (efficacy and safety have not been established).

Trade name of the drug:

CombilipenЃ

International non-proprietary or group name:

Pyridoxine + Thiamine + Cyanocobalamin + [Lidocaine]

Dosage form:

solution for intramuscular injection

Composition

Active ingredients:

Thiamine hydrochloride - 100 mg
Pyridoxine hydrochloride - 100 mg
Cyanocobalamin - 1 mg
Lidocaine hydrochloride - 20 mg

Excipients: benzyl alcohol - 40.0 mg, sodium tripolyphosphate - 20.0 mg, potassium hexacyanoferrate - 0.20 mg, sodium hydroxide - up to pH 4.5 ± 0.2, water for injection - up to 2 ml.

Description:

transparent pinkish-red liquid with a specific odor.

Pharmacotherapeutic group:

B vitamins + other preparations

ATX code: A11DB / N07X

Pharmacological properties

Pharmacodynamics

Combined multivitamin preparation. The effect of the drug 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 (vitamin B1 ) - plays a key role in the processes of carbohydrate metabolism, which are of decisive importance in the metabolic processes of the nervous tissue (it participates in the conduction of a nerve impulse), as well as in the Krebs cycle, followed by participation in the synthesis of thiamine pyrophosphate (TPP) and adenosine triphosphate (ATP).

Pyridoxine (vitamin B6) - has a vital effect on the metabolism of proteins, carbohydrates and fats, it is necessary for normal hematopoiesis, the functioning of the central and peripheral nervous system. Provides synaptic transmission, inhibition processes in the central nervous system (CNS), participates in the transport of sphingosine, which is part of the nerve sheath, and participates in the synthesis of catecholamines. The physiological function of both vitamins (B1 and B6) is to potentiate the action of each other, which manifests itself in a positive effect on the nervous, neuromuscular and cardiovascular systems.

Cyanocobalamin (vitamin B12) - participates in the synthesis of nucleotides, is an important factor in the normal growth, hematopoiesis and development of epithelial cells; essential for the metabolism of folic acid 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 due to the blockade of voltage-gated sodium channels, which prevents the generation of impulses at the endings of the sensory nerves and the conduction of pain impulses along the nerve fibers.

Pharmacokinetics

Thiamine

After intramuscular administration, thiamine is rapidly absorbed from the injection site and enters the bloodstream (484 ng / ml after 15 minutes on the first day of a 50 mg dose) and is unevenly distributed in the body when its content in leukocytes is 15%. erythrocytes 75% and in blood plasma 10 %.Due to the lack of significant reserves of vitamin in the body, it must be ingested daily. Thiamine crosses the blood-brain and placental barriers and is found in breast milk. Thiamine is excreted by the kidneys in the alpha phase after 0.15 hours, in the beta phase - after 1 hour, in the final (terminal) phase - within 2 days. The main metabolites are thiamincarboxylic acid, pyramine and some unknown metabolites. Of all the vitamins, thiamine is stored in the body in the smallest amount. The body of an adult contains about 30 mg of thiamine: 80% in the form of thiamine pyrophosphate. 10% as thiamine triphosphate and the rest as thiamine monophosphate.

Pyridoxine

After intramuscular injection, pyridoxine is rapidly absorbed from the injection site and distributed in the body, acting as a coenzyme after phosphorylation of the CH2OH group in the 5th position. About 80% of the vitamin binds to blood plasma proteins. Pyridoxine is distributed throughout the body, crosses the placenta, and is found in breast milk. It accumulates in the liver and is oxidized to 4-pyridoxinic acid, which is excreted by the kidneys a maximum of 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 at a replenishment rate of 2.2-2.4%.

Cyanocobalamin

After intramuscular administration, cyanocobalamin binds to transcobalamins I and II and is transferred to various tissues of the body. The maximum concentration after intramuscular administration is reached after 1 hour. Communication with blood plasma proteins - 90%. Penetrates through the placental barrier, is found in breast milk. It is metabolized mainly in the liver with the formation of adenosylcobalamin, which is the active form of cyanocobalamin. It is deposited in the liver, enters the intestines with bile and is reabsorbed into the blood (the phenomenon of enterohepatic recirculation). The half-life is long, excreted mainly by the kidneys (7-10%) and through the intestines (50%). With a decrease in kidney function, it is excreted by the kidneys - 0-7% and through the intestines - 70-100%.

Lidocaine

With intramuscular administration, the maximum plasma concentration of lidocaine is observed 5-15 minutes after injection. Depending on the dose, about 60-80% of lidocaine binds to plasma proteins. It is quickly distributed (within 6-9 minutes) in organs and tissues with good perfusion, incl. heart, lungs, liver, kidneys, then in muscle and adipose tissue. Penetrates through the blood-brain and placental barriers, is found in breast milk (up to 40% of the concentration in the mother's blood plasma).

It is metabolized in the liver with the participation of microsomal enzymes with the formation of active metabolites - monoethylglycinexylide and glycinexylide, with a half-life of 2 and 10 hours, respectively. Metabolic intensity decreases in liver disease. It is excreted mainly in the form of metabolites by the kidneys and up to 10% unchanged.

Indications for use

In complex therapy:

• mono- and polyneuropathies of various origins;

• dorsalgia;

• plexopathy;

• lumboischialgia;

• radicular syndrome caused by degenerative changes in the spine.

Contraindications

• Hypersensitivity to the components of the drug.

• Acute heart failure, chronic heart failure in the stage of decompensation.

• Children under 18 years of age (efficacy and safety have not been established).

The period of pregnancy and breastfeeding.

The use of the drug is contraindicated during pregnancy and breastfeeding.

Method of administration and dosage

Injections are performed deeply intramuscularly (see section 'Special instructions').

In cases of severe pain syndrome, it is advisable to start treatment with intramuscular injection (deep), 2 ml daily for 5-10 days, with the transition in the future either to oral administration or to more rare injections (2-3 times a week for 2-3 weeks) with the possible continuation of therapy with the oral dosage form.

A weekly monitoring of therapy by a physician is required. The duration of treatment is determined by the doctor individually, depending on the severity of the symptoms of the disease.

The transition to therapy with a dosage form for oral administration is recommended to be carried out as soon as possible.

Side effect

The incidence of adverse adverse reactions is given in accordance with the WHO classification:

Very often - 1/10 appointments, often - 1/100 appointments, infrequently - 1/1000 appointments, rarely - 1/10000 appointments, very rarely - less than 1/10000 appointments, the frequency is unknown (cannot be determined from the available data).

From the immune system:

rarely: allergic reactions (skin rash, shortness of breath, anaphylactic shock, Quincke's edema).

From the nervous system:

frequency unknown: dizziness, confusion.

On the part of the cardiovascular system:

very rare: tachycardia;

frequency unknown: bradycardia, arrhythmia.

From the gastrointestinal tract:

frequency unknown: vomiting.

On the part of the skin and subcutaneous tissues:

very rare: increased sweating, acne, itching, urticaria.

Musculoskeletal and connective tissue disorders: frequency unknown: convulsions.

General disorders and disorders at the injection site:

the frequency is unknown: irritation may occur at the injection site; systemic reactions are possible with rapid administration or overdose.

With rapid administration (for example, due to inadvertent intravascular administration or injection into tissues with a rich blood supply) or when the dose is exceeded, systemic reactions may develop, including confusion, vomiting, bradycardia, arrhythmia, dizziness and convulsions.

If any of the side effects indicated in the instructions are aggravated, or you notice any other side effects not listed in the instructions, inform your doctor.

Overdose

Symptoms: vomiting, bradycardia, arrhythmia, systemic reactions are possible, including dizziness, confusion, convulsions.

Treatment: if symptoms of an overdose appear, treatment with the drug should be canceled, if necessary, symptomatic therapy should be prescribed.

Interaction with other medicinal products

B vitamins

Vitamin B1 (thiamine) is completely degraded in solutions containing sulfites. And as a consequence, the decay products of thiamine inactivate the actions of other vitamins. Thiamine is incompatible with oxidizing and reducing compounds, including: mercury chloride, iodide, carbonate, acetate, tannin acid, ammonium-iron citrate, as well as phenobarbital, riboflavin, benzylpenicillin, dextrose and metabisulfite. Copper accelerates the breakdown of thiamine; in addition, thiamine loses its effectiveness with increasing pH values ??(more than 3).

Therapeutic doses of vitamin B6 (pyridoxine) weaken the effect of levodopa (the antiparkinsonian effect of levodopa decreases) with simultaneous use. Interaction with cycloserine, penicillamine, isoniazid is also observed.

Vitamin B12 (cyanocobalamin) is incompatible with ascorbic acid, heavy metal salts.

Lidocaine

With parenteral use of lidocaine, in the case of additional use of norepinephrine and epinephrine, an increase in adverse reactions to the heart is possible.

Interaction with sulfonamides is also observed. In case of an overdose of local anesthetics, epinephrine and norepinephrine should not be used additionally.

special instructions

The drug must be administered only intramuscularly, preventing it from entering the vascular bed. In case of accidental intravenous administration, the patient should be under medical supervision or hospitalized depending on the severity of the symptoms. The drug can cause neuropathy if used for more than 6 months.

Influence on the ability to drive vehicles, mechanisms

There is no information on the effect of the drug on the ability to drive vehicles, as well as on the performance of potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions. However, caution is advised, given the potential for adverse drug reactions.

Release form

Solution for intramuscular injection.
2 ml in light-protective glass ampoules.
5 ampoules are placed in a blister made of polyvinyl chloride film.
1 or 2 blister packs together with instructions for use are placed in a cardboard box.

Storage conditions

In a dark place at a temperature of 2 to 8 ? C. Keep out of the reach of children.

Shelf life

2 years.

Do not use after the expiration date printed on the package.

Vacation conditions

Dispensed by prescription.

Manufacturer / organization accepting customer claims

OJSC 'Pharmstandard-UfaVITA'

450077. Russia, Republic of Bashkortostan, Ufa, st. Khudayberdin, 28,