Combilipen
Combilipen is a Russian-made complex multivitamin preparation used in combination therapy for neurological diseases, including the elimination of pain in diseases of the spine. The pharmacological effect of the drug consists of the individual properties of the vitamins included in its composition: thiamine (B1), pyridoxine (B6) and cyanocobalamin (B12), as well as the anesthetic lidocaine. As is known, B vitamins have a positive effect on inflammatory and degenerative diseases of the musculoskeletal system and nervous system. Thiamine takes part in conducting impulses along nerve fibers. Pyridoxine plays a key role in the metabolism of proteins, fats and carbohydrates. In addition, it is vital for ensuring normal hematopoiesis and the functioning of the central and peripheral nervous systems. This vitamin ensures interneuronal transmission, regulates inhibition processes, takes part in the transport of sphingosine (one of the components that form the nerve sheath), as well as in the formation of catecholamines. Cyanocobalamin is involved in protein synthesis, growth processes, hematopoiesis and proliferation of epithelial cells. It is necessary for the metabolism of folic acid and the formation of myelin (the latter forms the electrically insulating membrane of neurons). Lidocaine numbs the injection site.
Another useful function is the local expansion of blood vessels, which ensures more complete absorption of vitamins from the injection site. The local analgesic effect of lidocaine is associated with the blockade of sodium channels, which suppresses the generation of nerve impulses in the endings of afferent neurons and their propagation along nerve fibers. It should be noted that the analgesic effect is also characteristic of B vitamins, to a greater extent this applies to cyanocobalamin. In addition, the B complex of vitamins can enhance the analgesic effect of non-steroidal anti-inflammatory drugs. And if earlier, in order to achieve the required effect, it was necessary to administer each of these three vitamins separately, with daily alternation, which undoubtedly increased the pharmacotherapeutic course, today, having combilipen in their arsenal, neurologists and their patients are in a clearly advantageous position .
Kombilipen is available in the form of a solution for intramuscular administration (there is also a tablet form - Kombilipen tabs - but its composition is not identical to the injection Kombilipen). For severe pain, the initial dose of the drug is 2 ml once a day for 5-10 days, after which either the frequency of injections is reduced (2-3 times a week for 2-3 weeks) or the patient is transferred to Combilipen Tabs.
Buy Combilipen injection solution 2ml No. 10 in pharmacies
Trade name of the drug:
Combilipen®
International nonproprietary or generic name:
Pyridoxine + Thiamine + Cyanocobalamin + [Lidocaine]
Dosage form:
solution for intramuscular administration
Compound
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 drugs
Pharmacological properties
Pharmacodynamics
Combined multivitamin preparation. The effect of the drug is determined by the properties of the vitamins included in 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 crucial in the metabolic processes of nervous tissue (participates in the conduction of nerve impulses), as well as in the Krebs cycle with subsequent 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, 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 each other’s action, manifested in a positive effect on the nervous, neuromuscular and cardiovascular systems.
Cyanocobalamin (vitamin B12) - is involved in the synthesis of nucleotides and is an important factor in normal growth, hematopoiesis and development of epithelial cells; 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 due to the blockade of voltage-gated sodium channels, which prevents the generation of impulses at the endings of sensory nerves and the conduction of pain impulses along nerve fibers.
Pharmacokinetics
Thiamine
After intramuscular administration, thiamine is quickly absorbed from the injection site and enters the blood (484 ng/ml after 15 minutes on the first day of administration of a 50 mg dose) and is unevenly distributed in the body with its content in leukocytes 15%, erythrocytes 75% and blood plasma 10 %. Due to the lack of significant reserves of the vitamin in the body, it must be supplied to the body daily. Thiamine penetrates 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, and in the final (terminal) phase within 2 days. The main metabolites are: thiaminecarboxylic acid, pyramine and some unknown metabolites. Of all the vitamins, thiamine is stored in the body in the smallest quantities. The adult human body contains about 30 mg of thiamine: 80% in the form of thiamine pyrophosphate, 10% in the form of thiamine triphosphate and the rest in the form of thiamine monophosphate.
Pyridoxine
After intramuscular injection, pyridoxine is rapidly absorbed from the injection site and distributed throughout the body, acting as a coenzyme after phosphorylation of the CH2OH group at the 5th position. About 80% of the vitamin binds to blood plasma proteins. Pyridoxine is distributed throughout the body, penetrates the placenta, and is found in breast milk. It accumulates in the liver and is oxidized to 4-pyridoxic acid, which is excreted by the kidneys within 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 with a replacement rate of 2.2-2.4%.
Cyanocobalamin
Cyanocobalamin, after intramuscular administration, binds to transcobalamins I and II and is transported to various tissues of the body. The maximum concentration after intramuscular administration is achieved after 1 hour. Communication with blood plasma proteins - 90%. Penetrates the placental barrier and is found in breast milk. Metabolized primarily in the liver to form 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 renal function, 0-7% is excreted by the kidneys and 70-100% through the intestines.
Lidocaine
When administered intramuscularly, the maximum plasma concentration of lidocaine is observed 5-15 minutes after injection. Depending on the dose, about 60-80% of lidocaine is bound to plasma proteins. 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 the blood-brain and placental barriers and is found in breast milk (up to 40% of the concentration in the mother's blood plasma). Metabolized in the liver with the participation of microsomal enzymes with the formation of active metabolites - monoethylglycine xylide and glycine xylide, which have a half-life of 2 and 10 hours, respectively. Metabolic intensity decreases in liver diseases. 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; - plexopathies; - 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.
Use during pregnancy and breastfeeding
The use of the drug is contraindicated during pregnancy and breastfeeding.
Directions for use and doses
Injections are performed deep intramuscularly (see section “Special instructions”).
In cases of severe pain, it is advisable to begin treatment with intramuscular injection (deep) of 2 ml daily for 5-10 days, with subsequent transition either to oral administration or to more rare injections (2-3 times a week for 2-3 weeks) with possible continuation of therapy with the oral dosage form.
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.
It is recommended to switch to therapy with an oral dosage form as soon as possible.
Side effect
The frequency of adverse reactions is given in accordance with the WHO classification:
Very often - 1/10 prescriptions, often - 1/100 prescriptions, infrequently - 1/1000 prescriptions, rarely - 1/10000 prescriptions, very rarely - less than 1/10000 prescriptions, frequency unknown (cannot be determined based on available data).
From the immune system:
rarely: allergic reactions (skin rash, difficulty breathing, anaphylactic shock, Quincke's edema).
From the nervous system:
frequency unknown: dizziness, confusion.
From the cardiovascular system:
very rarely: tachycardia; frequency unknown: bradycardia, arrhythmia.
From the gastrointestinal tract:
frequency unknown: vomiting.
For the skin and subcutaneous tissues:
very rare: increased sweating, acne, itching, urticaria.
From the musculoskeletal and connective tissue side:
frequency unknown: convulsions.
General disorders and disorders at the injection site:
frequency unknown: irritation may occur at the injection site; systemic reactions are possible with rapid administration or overdose.
If administered rapidly (eg, due to inadvertent intravascular injection or administration into tissues with a rich blood supply) or if the dose is exceeded, systemic reactions may occur, including confusion, vomiting, bradycardia, arrhythmia, dizziness and convulsions.
If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.
Overdose
Symptoms: vomiting, bradycardia, arrhythmia, possible systemic reactions including dizziness, confusion, convulsions.
Treatment: if symptoms of overdose appear, treatment with the drug should be discontinued and, if necessary, symptomatic therapy should be prescribed.
Interaction with other drugs
B vitamins
Vitamin B1 (thiamine) completely disintegrates in solutions containing sulfites. And as a result, thiamine breakdown products inactivate the actions of other vitamins. Thiamine is incompatible with oxidizing and reducing compounds, including: mercuric chloride, iodide, carbonate, acetate, tannic acid, ferric ammonium citrate, as well as phenobarbital, riboflavin, benzylpenicillin, dextrose and metabisulfite. Copper accelerates the breakdown of thiamine; in addition, thiamine loses its effectiveness when pH values increase (more than 3).
Therapeutic doses of vitamin B6 (pyridoxine) weaken the effect of levodopa (the antiparkinsonian effect of levodopa decreases) when used simultaneously. Interactions with cycloserine, penicillamine, and isoniazid are also observed.
Vitamin B12 (cyanocobalamin) is incompatible with ascorbic acid and heavy metal salts.
Lidocaine
With parenteral use of lidocaine, in the case of additional use of norepinephrine and epinephrine, adverse reactions on the heart may increase. Interaction with sulfonamides is also observed. In case of overdose of local anesthetics, additional epinephrine and norepinephrine should not be used.
special instructions
The drug must be administered only intramuscularly, preventing it from entering the vascular bed. If accidental intravenous administration occurs, the patient should be monitored by a physician or hospitalized depending on the severity of symptoms.
The drug can cause neuropathies when used for more than 6 months.
Impact on the ability to drive vehicles and machinery
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 and speed of psychomotor reactions. However, caution is recommended, given the possibility of developing adverse drug reactions.
Release form
Solution for intramuscular administration.
2 ml in light-protective glass ampoules.
5 ampoules are placed in a blister pack made of polyvinyl chloride film.
1 or 2 blister packs along with instructions for use are placed in a cardboard pack.
Storage conditions
In a place protected from light at a temperature of 2 to 8 °C. Keep out of the reach of children.
Best before date
2 years. Do not use after the expiration date stated on the package.
Vacation conditions
Dispensed by prescription.