Тригамма®

General characteristics. Structure:

Active ingredients:
thiamin a hydrochloride (in terms of anhydrous substance) - 50 mg, a pyridoxine a hydrochloride (in terms of anhydrous substance) - 50 mg, cyanocobalamine (in terms of anhydrous substance) - 0,5 mg, lidocaine a hydrochloride (in terms of anhydrous substance) - 10 mg.

Excipients: a benzetoniya chloride, dinatrium эдетат (Trilonum of B), sodium hydroxide, water for injections.

Description: Transparent liquid of red color.

Pharmacological properties:

Neurotropic vitamins of group B have favorable effect on inflammatory and degenerative diseases of nerves and the motive device.

Thiamin (B1) plays a key role in the processes of carbohydrate metabolism having crucial importance in exchange processes of nervous tissue and also in a tricarbonic acid cycle with the subsequent participation in synthesis of TPF (thiamine pyrophosphate) and ATP (adenosinetriphosphate). The pyridoxine (B6) participates in metabolism of proteins, and partially, in metabolism of carbohydrates and fats. Physiological function of both vitamins (B1 and B6) is the potentiation of action of each other which is shown in positive influence on nervous, neuromuscular and cardiovascular systems.

Cyanocobalamine (B12) participates in synthesis of a myelin cover, stimulates a hemogenesis, reduces the pain connected with defeat of a peripheral nervous system, stimulates nucleinic exchange through activation of folic acid.

Lidocaine - has mestnoanesteziruyushchy effect.

Pharmacokinetics. Thiamin.
After intramuscular introduction thiamin is quickly absorbed from the place of an injection and comes to blood (484 ng/ml in 15 min. in the first day of introduction of a dose of 50 mg) and is distributed unevenly in an organism at contents it in leukocytes of 15%, erythrocytes of 75% and in a blood plasma of 10%. Due to the lack of considerable reserves of vitamin B an organism it has to come to an organism daily. Thiamin gets through hematoencephalic and placental barriers, it is found in maternal milk. Thiamin is removed by kidneys in an alpha phase in 0,15 hours, in a beta phase - in 1 hour and in a terminal phase - within 2 days. The main metabolites are: tiaminkarbonovy acid, pyramine and some unknown metabolites. From all vitamins thiamin remains in an organism in the smallest quantities. The organism of the adult contains about 30 mg of thiamin in a look: 80% in the form of thiamin of a pyrophosphate, 10% of thiamin of triphosphate and other quantity in the form of monophosphate thiamin.
 
Pyridoxine.
After an intramuscular injection the pyridoxine is quickly absorbed in a blood channel and distributed in an organism, carrying out a coenzyme role after phosphorylation of the CH2OH group in the 5th situation. About 80% of vitamin contact proteins of a blood plasma. The pyridoxine is distributed on all organism, gets through a placenta, it is found in maternal milk. It is deposited in a liver and is oxidized to 4-pyridoxynew acid which is excreted by kidneys, at most in 2-5 hours after absorption. The human body contains 40-150 mg of B6 vitamin, its daily speed of elimination makes about 1,7-3,6 mg at a speed of completion of 2,2-2,4%. Cyanocobalamine.

In blood cyanocobalamine (B12) contacts transcobalamines I and II which transport it in fabric. It is deposited preferential in a liver. Communication with proteins of plasma - 90%. The maximum concentration after hypodermic and intramuscular introduction is reached in 1 hour.

Out of a liver it is brought with bile in intestines and again soaked up in blood. An elimination half-life - 500 days. It is removed at normal function of kidneys of 7-10% by kidneys, about 50% - through intestines; at depression of function of kidneys of 0-7% kidneys, 70-100% - through intestines. Gets through a placental barrier, into breast milk.

Lidocaine
Time of achievement of the maximum concentration in a blood plasma at intramuscular introduction - 5-15 minutes. Proteins of a blood plasma connect 50-80% of drug. It is quickly distributed (within 6-9 minutes) in bodies and fabrics with good perfusion, including in heart, lungs, a liver, kidneys, then in muscular and fatty tissue. Gets through hematoencephalic and placental barriers, cosecretes with maternal milk (to 40% of concentration in mother's plasma). It is metabolized mainly in a liver (90-95% of a dose) with the participation of microsomal enzymes with formation of active metabolites - a monoetilglitsinksilidida and the glitsinksilidida having an elimination half-life of 2 h and 10 h respectively. Intensity of metabolism decreases at liver diseases (can make from 50 to 10% of a normal amount). It is removed with bile and kidneys (to 10% in an invariable look).

Indications to use:

In complex therapy of the following neurologic diseases: neuritis (including retrobulbar neuritis), neuralgia, polyneuropathy (diabetic, alcoholic, etc.); mialgiya, radicular syndromes, the surrounding herpes, paresis of a facial nerve.

Route of administration and doses:

At the expressed pain syndrome treatment is reasonable to begin with intramuscular introduction (deeply) 2 ml of drug daily within 5-10 days with transition further or on reception of peroral dosage forms, or on more rare injections (2-3 times a week within 2-3 weeks).

Features of use:

Use at pregnancy and in the period of a lactation: It is not recommended to apply.

Side effects:

Allergic reactions. In some cases the increased sweating, tachycardia can be noted, acne rash develops. Skin reactions in the form of an itch, a small tortoiseshell are described.

In rare instances the hypersensitivity phenomena to drug, for example, rash, the complicated breath, a Quincke's disease, an acute anaphylaxis can be observed.

Interaction with other medicines:

Thiamin completely breaks up in the solutions containing sulfites. Other vitamins are inactivated in the presence of B1 vitamin decomposition products.

Copper accelerates thiamin destruction; besides, thiamin loses the action at increase in values рН (more than 3).

The pyridoxine accelerates decarboxylation of a levodopa in fabrics, reducing that its efficiency at Parkinson's disease. At parenteral use of lidocaine, in case of additional use of Epinephrinum and Norepinephrinum, strengthening of side effect on heart is possible.

B12 vitamin pharmaceutical is incompatible with ascorbic acid, salts of heavy metals.

Contraindications:

- hypersensitivity to any of drug components;

- dekompensirovanny heart failure;

- children's age (due to the lack of researches).

Overdose:

Symptoms: in cases of very bystry administration of drug there can be system reactions (dizziness, arrhythmia, spasms), they can be also result of overdose.

Treatment: symptomatic therapy.

Storage conditions:

In the place protected from light at a temperature from 0 to 8 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Solution for intramuscular introduction.

On 2 ml in ampoules of brown glass or an ampoule from light-protective glass.

On 5 ampoules place in a blister strip packaging from a film polyvinyl chloride.

1 or 2 blister strip packagings with the scarificator ampoule ceramic or the scarificator ampoule abrasive and the application instruction place in a pack from a cardboard.

When using ampoules with a point or a ring of a break scarificators ampoule do not invest.