Milgamma, 2 ml 5 pcs.

Pharmacotherapeutic group: B vitamins + other

ATX code: A11DB/N07X

Pharmacological properties

Pharmacodynamics:

The B-group neurotropic vitamins have beneficial effects on inflammatory and degenerative diseases of the nerves and the motor system. They increase blood flow and improve the function of the nervous system. Thiamine plays a key role in metabolism of carbohydrates, as well as in the Krebs cycle, with subsequent participation in the synthesis of TPP (thiamine pyrophosphate) and ATP (adenosine triphosphate). Pyridoxine is involved in protein metabolism and, in part, in carbohydrate and fat metabolism. The physiological function of both vitamins is to potentiate each other’s action, manifesting itself in positive effects on the nervous, neuromuscular and cardiovascular systems. In vitamin B₆ deficiency, widespread deficiency states are quickly counteracted after administration of these vitamins. Cyanocobalamin is involved in the synthesis of myelin sheath, stimulates hematopoiesis, reduces pain associated with lesions of the peripheral nervous system, stimulates nucleic metabolism through activation of folic acid. Lidocaine is a local anesthetic agent, causing all types of local anesthesia: terminal, infiltration, conductive.

Pharmacokinetics:

After intramuscular administration, thiamine is rapidly absorbed from the injection site and enters the blood (484 ng/mL after 15 minutes on the first day of the 50 mg dose) and is unevenly distributed in the body with its content in leukocytes 15%, red blood cells 75% and plasma 10%. Because of the lack of significant stores of the vitamin in the body, it must be supplied daily. Thiamine penetrates the blood-brain and placental barriers and is found in 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% thiamine pyrophosphate, 10% thiamine triphosphate and the rest as thiamine monophosphate.

After intramuscular injection, pyridoxine is rapidly absorbed into the bloodstream and distributed in the body, acting as a coenzyme after phosphorylation of the CH₂ON group at the 5th position. About 80% of the vitamin is bound to plasma proteins. Pyridoxine is distributed throughout the body and crosses the placenta and is found in the mother’s milk, deposited in the liver and oxidized to 4-pyridoxylic acid, which is excreted in the urine, maximum 2 to 5 hours after absorption. The human body contains 40 to 150 mg of vitamin B₆ and its daily elimination rate is about 1.7 to 3.6 mg with a replenishment rate of 2.2 to 2.4%.

Indications

Myalgia (muscle pain), Lumbago, Pain, Neuritis, Osteochondrosis, Sciatica, trigeminal neuralgia

As a pathogenetic and symptomatic agent in the complex treatment of diseases and syndromes of the nervous system of different origin: neuralgia, neuritis, facial nerve paresis, retrobulbar neuritis, ganglionitis (including shingles), plexopathy, neuropathy, polyneuropathy (diabetic, alcoholic, etc.), night-time muscle cramps, especially in older age groups, neurological manifestations of spinal osteochondrosis: radiculopathy, lumboishalgia, muscle-tonic syndromes.

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Composition

2 ml of solution for intramuscular injection contains:

active ingredients: thiamine hydrochloride 100.0 mg, pyridoxine hydrochloride 100.0 mg, cyanocobalamin 1.0 mg, lidocaine hydrochloride 20.0 mg;

excipients: benzyl alcohol 40.0 mg, sodium polyphosphate 20 mg, potassium hexacyanoferrate 0.20 mg, sodium hydroxide 12.0 mg, water for injection to 2 ml.

How to take, the dosage

Injections are performed deeply intramuscularly.

In cases of severe pain syndrome in order to quickly achieve high levels of the drug in the blood it is advisable to start treatment with 2.0 ml daily for 5-10 days. Later on, after the pain syndrome has subsided and in case of light forms of the disease, the therapy should be continued either with oral dosage form (e.g., Milgamma^® Compositum) or less frequent injections (2-3 times per week for 2-3 weeks) with possible continuation of oral dosage form therapy (e.g., Milgamm^® Compositum).

A weekly monitoring of therapy by a physician is recommended.

The transition to therapy with an oral dosage form (e.g., Milgamma^® Compositum) is recommended as soon as possible.

Interaction

Thiamine breaks down completely in solutions containing sulfites. And as a consequence, the breakdown products of thiamine inactivate the actions of other vitamins.

Thiamine is incompatible with oxidizing and reducing compounds, including: iodides, carbonates, acetates, tannic acid, ammonium iron citrate, phenobarbital, riboflavin, benzylpenicillin, dextrose, disulfites, etc.

Copper accelerates the degradation of thiamine; in addition, thiamine loses its effectiveness when pH values (greater than 3) are increased.

Therapeutic doses of pyridoxine weaken the effect of levodopa (the anti-Parkinsonian effect of levodopa is reduced) when taken simultaneously. Interaction with cycloserine, penicillamine and isoniazid is also observed.

In parenteral use of lidocaine with additional use of norepinephrine and epinephrine an increased side effect on the heart is possible. Interaction with sulfonamides is also observed.

Cyanocobalamin is incompatible with salts of heavy metals. Riboflavin also has a destructive effect, especially when simultaneously exposed to light; nicotinamide accelerates photolysis, while antioxidants have an inhibitory effect.

Special Instructions

In case of accidental intravenous injection, the patient should be monitored by a doctor or hospitalized depending on the severity of symptoms.

The ability to affect reaction rate when driving motor vehicles or operating other mechanisms. There is no information about a caution regarding the use of the drug by drivers of vehicles and persons working with potentially dangerous mechanisms.

Contraindications

Pregnancy and breastfeeding period (see section “Administration during pregnancy and breastfeeding”).

Children’s age.

Decompensated heart failure.

High individual sensitivity to the components of the drug.

Overdose

The treatment of an overdose consists of withdrawal of the drug and symptomatic therapy.