Glutargin tablets 0.25 g 30 pcs.

Pharmacodynamics. Glutargin is a compound of arginine and glutamic acid, which play an important role in ensuring the biochemical processes of neutralization and excretion from the body of a highly toxic metabolite of the metabolism of nitrogen-containing substances – ammonia. The hypoammonemic effect of the drug is realized as a result of the activation of the processes of ammonia neutralization in the ornithine cycle of urea synthesis, the binding of ammonia to non-toxic glutamine, as well as the enhancement of the removal of ammonia from the central nervous system and its excretion from the body. Due to these properties, Glutargin reduces the general toxic and neurotoxic effects of ammonia.

Glutargin also exhibits hepatoprotective effects, has antioxidant, antihypoxic and membrane-stabilizing activities, positively affecting the energy supply of hepatocytes.

In case of alcohol intoxication, Glutargin stimulates the utilization of alcohol in the monooxygenase system of the liver, prevents the inhibition of the key enzyme for ethanol utilization – alcohol dehydrogenase; accelerates the inactivation and excretion of toxic products of ethanol metabolism as a result of increased formation and oxidation of succinic acid; reduces the inhibitory effect of alcohol on the CNS due to the neurotransmitter properties of glutamic acid. Due to these properties, Glutargin exhibits antitoxic and sobering effects.

In pregnancy pathology, due to its endothelium-protective action, Glutargin normalizes impaired vascular permeability and thromboresistance, prevents hypercoagulation, reduces the sensitivity of vessels to vasoconstrictor agents (endothelin, angiotensin, thromboxane), which causes generalized vasospasm. Arginine, after preliminary biotransformation into nitric oxide, has a vasodilator effect, positively affects blood clotting and the functional properties of circulating blood elements. As a result of the vasodilator and antihypoxic effects of Glutargin, maternal-fetal hemodynamics improves, intrauterine hypoxia of the fetus decreases. In pregnancy pathology, the drug also exhibits antitoxic and hepatoprotective activity, acts as a nonspecific metabolic regulator of metabolic processes. Due to these properties of Glutargin, during pregnancy, the level of circulating immune complexes in the blood decreases, the severity of metabolic intoxication syndrome and immunotoxicosis decreases, and the body’s compensatory and adaptive reactions increase.

Glutargin does not exhibit embryotoxic, gonadotoxic, mutagenic and teratogenic effects, and does not cause allergic and immunotoxic reactions.

Pharmacokinetics have not been studied.

As part of the complex therapy of acute and chronic hepatitis of various etiologies, poisoning with hepatotropic poisons (poison of the pale toadstool, chemicals and drugs), with cirrhosis of the liver, liver damage in leptospirosis. hepatic encephalopathy, precoma and coma, accompanied by hyperammonemia.

Acute alcohol intoxication of mild and moderate severity, as well as as part of complex therapy of post-intoxication disorders after acute severe alcohol poisoning, including alcoholic encephalopathy and coma. Prevention of intoxication and hepatotoxic effects of alcohol.

Post-intoxication disorders, hangover syndrome caused by alcohol consumption.

Complications in the third trimester of pregnancy: late gestosis, including its severe forms – preeclampsia and eclampsia, fetoplacental insufficiency, chronic pathologies of the hepatobiliary system in pregnant women.

Hepatitis, hyperammonemia.

Tablets. Adults are prescribed orally 3 tablets of 0.25 g (0.75) or 1 tablet of 0.75 3 times a day for 15 days, regardless of meals. If necessary, the dose of the drug and the course of treatment can be extended to 20 days. The maximum single dose is 2 g, the maximum daily dose is 8 g.

Solution for injection (4%). The drug is prescribed to adults i / v. It is administered i / v drip 2 times a day, 50 ml (2 g) in 150-250 ml of isotonic sodium chloride solution at a rate of 60-70 drops per 1 min. In severe cases, the daily dose of the drug is increased to 150-200 ml (6-8 g). The course of treatment is 5-10 days. The maximum daily dose is 200 ml (8 g).

Solution for injection (20%). The drug is prescribed to adults i / v and i / m. It is administered i / v drip 1-2 times a day, 10 ml (2 g) per 150-250 ml of physiological sodium chloride solution or 5% glucose solution at a rate of 60-70 drops per 1 min. In severe cases, the daily dose of the drug is increased to 30-40 ml (6-8 g), divided into 2 doses. The course of treatment is 5-10 days. The maximum daily dose with i / v administration is 40 ml (8 g).

The drug is administered intramuscularly slowly deep into the gluteal muscle 1-2 times a day, 5 ml (1 g). If necessary, the dose of the drug is increased to 10 ml (2 g) 1-2 times a day. The course of treatment is 5-10 days. The maximum daily dose for intramuscular administration is 20 ml of the drug (4 g).

Concentrate for preparation of solution for infusions

The drug is prescribed to adults in / in the form of infusions. It is administered in / in drip 2 times a day, 5 ml (2 g) in 150-250 ml of isotonic sodium chloride solution at a rate of 60-70 drops per 1 min. In severe cases, the daily dose of the drug is increased to 15-20 ml (6-8 g). The course of treatment is 5-10 days. The maximum daily dose is 20 ml (8 g).

Alcohol poisoning.

Tablets. Prescribe 4 tablets of 0.25 g (1.0 g) or 1 g 4 times a day with an interval of 1-2.5 hours, in the next 2-3 days – 2 tablets of 0.25 g (0.5 g) or ½ 1 g 3 times a day. In case of severe alcohol intoxication after a course of treatment with Glutargin injections, Glutargin tablets are prescribed 3 tablets of 0.25 g (0.75 g) or 1 tablet of 0.75 g 2 times a day, or 1 ^_1/2 tablets of 1 g 1 time a day for 20 days. For the prevention of alcohol intoxication – 2 g 60-120 minutes before drinking alcohol.

Powder for oral solution

The drug is prescribed to adults orally, after dissolving the packet in ¼-½ cup of water.

For the prevention of intoxication and hepatotoxic effects of alcohol, 2 g (2 packets) are prescribed 1-2 hours before drinking alcohol or 1 g (1 packet) 1 hour before drinking alcohol and 1 g (1 packet) within 0.5 hours after drinking alcohol. For the treatment of acute alcohol intoxication of mild and moderate severity, 1 g (1 packet) is prescribed 4 times a day with intervals of 1-2.5 hours, in the next 2-3 days – 1 g (1 packet) 2 times a day. For severe alcohol intoxication, Glutargin Alkoklin powder is prescribed 1 g (1 packet) 2 times a day for 20 days as part of complex therapy after a course of treatment with injectable forms of the drug Glutargin.

Solution for injection (4%). For the treatment of alcohol intoxication, 20 ml (0.8 g) is prescribed, administered dropwise in 150-250 ml of isotonic sodium chloride solution at a rate of 60-70 drops per minute 2 times a day for 2-3 days, then the dose is reduced to 10 ml (0.4 g) 2 times a day for 10 days. In severe cases (alcoholic coma), the daily dose is increased to 50 ml (2 g) 2 times a day.

After a course of treatment with Glutargin injection/infusion solution, if necessary, you should switch to taking Glutargin tablets.

Solution for injection (20%). The drug is prescribed to adults in / in and in / m. It is administered in / in drip 2 times a day, 4 ml (0.8 g) per 150-250 ml of physiological sodium chloride solution or 5% glucose solution at a rate of 60-70 drops per 1 min. After 2-3 days, the dose is reduced to 2 ml (0.4 g).

The drug is injected slowly deep into the gluteal muscle in a dose of 4 ml (0.8 g) 2 times a day for 2-3 days, then the dose is reduced to 2 ml (0.4 g) 2 times a day for 5-10 days. In severe cases (alcoholic coma), the daily dose of intravenous or intramuscular administration is increased to 10 ml (2 g) 2 times a day.

Concentrate for preparation of solution for infusions

For the treatment of alcohol poisoning, 2 ml (0.8 g) is prescribed intravenously, administered dropwise in 150-250 ml of isotonic sodium chloride solution at a rate of 60-70 drops per minute 2 times a day for 2-3 days, then the dose is reduced to 1 ml (0.4 g) 2 times a day for 10 days. In severe cases (alcoholic coma), the daily dose is increased to 5 ml (2 g) 2 times a day.

After a course of treatment with a 40% solution of Glutargin, if necessary, you should switch to taking Glutargin tablets.

pregnancy pathologies

Tablets. Prescribe 0.25-0.5 g (1-2 tablets of 0.25 g) 2-3 times a day for 10-15 days. If necessary, a single dose of the drug can be increased to 0.75 g (3 tablets of 0.25 g or 1 tablet of 0.75 g), the course of treatment – up to 20 days. The highest single dose is 0.75 g, the highest daily dose – 2.25 g.

Solution for injection (4%). Administer 1-2 times a day, 50 ml (2 g). Course of treatment – 5-7 days. Highest daily dose – 100 ml (4 g).

Concentrate for preparation of solution for infusions. Administered dropwise 1-2 times a day, 5 ml (2 g) per 150-250 ml of physiological sodium chloride solution at a rate of 60-70 drops per minute. The course of treatment is 5-7 days. The maximum daily dose is 10 ml (4 g).

Relative contraindications are feverish conditions, increased excitability, and severe disorders of the filtration (nitrogen excretion) function of the kidneys.

Tablets: rarely – a feeling of mild discomfort in the stomach and intestines, nausea immediately after taking the drug, self-resolving.

Solution for injection/infusion: rarely possible – severe weakness, shortness of breath, chest pain, chills, heart rhythm disturbances in the form of atrial fibrillation, hypotension, Quincke’s edema. In isolated cases – mild allergic reactions (urticaria, hyperemia, itching).

When prescribing to patients with endocrine gland dysfunction, it should be taken into account that the drug is able to stimulate the secretion of insulin and growth hormone.

Children: Experience with the use of the drug in children is insufficient.

Impact on the ability to drive vehicles and work with complex mechanisms.

Tablets: no effect.

R-r: since adverse reactions from the central nervous system (headache, dizziness, tremor) may occur during treatment, caution should be exercised when driving or working with other mechanisms.

When used simultaneously with aminophylline, an increase in the concentration of endogenous insulin in the blood is possible. Glutargin can enhance the effect of antiplatelet agents (dipyridamole, etc.). Prevents and reduces the severity of neurotoxic phenomena that may occur when using isoniazid. Reduces the effect of vinblastine.

Symptoms: chest pain, AV block.

Treatment: in this case, intravenous administration of corticosteroids is indicated. Symptomatic therapy.

Tablets in original packaging at a temperature not exceeding 25 °C, solution for injection in original packaging at a temperature of 25 °C, concentrated solution for injection in a place protected from light at a temperature of 25 °C.

Glutargin is a drug that is a nonspecific regulator of metabolism with a predominant hepatoprotective and evaluate the effectiveness. The active substance of this drug is necessary for many chemical and biological processes in the body, which makes it necessary to prescribe it for damage to the central nervous system and liver cells by various poisons and toxins, for capillary blood flow disorders, and severe cases of multiple organ failure.

Composition. Release formThe therapeutic effect of Glutargin is realized due to the active substance – arginine glutamate. For various purposes, it is available in injectable and tablet form. For parenteral administration, a concentrate for solution for infusions 400 mg/ml ampoule 5 ml, solution for injection 40 mg/ml ampoule 5 ml, solution for injection 200 mg/ml ampoule 5 ml is available. Tablets are available in two convenient dosage options: 250 or 750 mg (instructions of the Ministry of Health of Ukraine).

Pharmacological propertiesThe pharmacodynamic characteristics of the drug are determined by the combination of the therapeutic effect of glutamic acid and arginine. Glutamic acid is one of the most common essential amino acids (synthesized in the body and supplied from the outside with food). Therefore, it is involved in many different biological processes. Glutamic acid is one of the important factors in the transmission of nerve impulses in synapses, has an excitatory effect on the central nervous system, which is widely used in neurotoxicosis of various genesis. Glutamic acid is also a starting material for the formation of endogenous folic acid. These characteristics of glutamic acid are especially often used in the treatment of poisoning with low-quality alcohol. In addition to the function of a neurotransmitter, glutamic acid affects the monooxygenase system of hepatocytes (metabolism of ethyl alcohol, excretion of toxic metabolites), prevents the blocking of alcohol dehydrogenase.

In addition, glutamine is associated with the synthesis of complex protein components of connective tissue, nitrogen transport, gluconeogenesis and acid-base homeostasis. The cytoprotective effect of the amino acid is realized through the mechanisms of activation of the nuclear factor NF-kB, the balance between pro- and anti-inflammatory cytokines, reduction of neutrophil accumulation, protection against oxidative stress (Yuan Wang, 2019). The latter mechanism is especially important at the risk of developing septicemia and multiple organ failure. In addition, multiple studies have proven the necessity of the presence of this amino acid in hepatocytes for the formation of antioxidants; its importance in the regulation of the formation and secretion of bile acids, liver cell trophism; in the regulation of the formation and release of glycogen, lipids and insulin (Emanuele Therezinha Schueda STONOGA, 2019).

The amino acid arginine is converted into NO 2 in biochemical reactions _, improves blood circulation by eliminating capillary spasm, and together with glutamate is a neurotransmitter. Due to the effect of vasodilation, the overall endurance of the body improves and especially the blood supply to the myocardium improves. Arginine helps reduce insulin resistance during pregnancy, stimulates metabolic processes in the placenta (Morgane Robles, 2019). The effects of arginine also include participation in:

• urea cycle;

• collagen synthesis;

• synthesis of a reserve carrier of cellular energy – arginine phosphate;

• as well as stimulating the production of hormones (somatotropin, insulin), neurotransmitters (serotonin, adrenaline);

• potentiation of the effect of antihypertensive drugs by eliminating capillary spasm;

• acceleration of tissue regeneration by improving their oxygen supply.

Glutargin is effective in pathological processes in late pregnancy. It helps stabilize vascular permeability and thromboresistance, prevents hypercoagulation and generalized vasospasm. Glutargin improves fetoplacental hemodynamics (vasodilator and antihypoxic mechanisms), prevents the development of fetal distress syndrome. In addition, the drug allows you to increase compensatory and adaptive mechanisms in the woman’s body during the period of bearing a child.

No published studies describing the pharmacokinetics of the drug were found in open sources.

Indications for useGlutargin can be included in complex therapy for:

• liver damage by exogenous poisons, especially in the acute period – for example, if a person accidentally ate a poisonous mushroom or was treated with hepatotoxic drugs for a long time. Of the drugs, hepatotoxic effects are most often observed with an overdose of paracetamol or metamizole sodium, long-term use of isoniazid, antiviral drugs. Of the plants, when accidentally or intentionally ingested, toxic hepatitis is usually caused by pale toadstool and male fern;

• cirrhosis of the liver of various genesis – from alcoholic to biliary. Systematic use of low-quality alcoholic beverages leads to premature death (necrosis) of hepatocytes and replacement of liver lobules with fatty and fibrous tissue. With a significant decrease in the number of active hepatocytes, all metabolic functions of the liver are disrupted (inactivation of toxins by the cytochrome system, synthesis of protein, blood clotting factors, etc.). In the pathogenesis of biliary hepatitis, the leading role is played by damage to hepatocytes by bile acids in violation of their adequate outflow through the interlobular ducts;

• acute infectious hepatitis. Particularly severe liver damage is observed in leptospirosis. Leptospires cause severe damage to the liver parenchyma with the development of serous edema and multiple hemorrhages;

• hepatomegaly (severe liver failure), which is accompanied by hyperammonemia;

• severe burn disease (if it is accompanied by multiple organ failure);

• complicated course of late pregnancy. The key link in the pathogenesis of late gestosis is capillary spasm. Due to it, various pathological processes develop in the body of both the mother and the fetus. Due to the spasm of the spiral arterioles of the uterus, placental gas exchange processes are disrupted and fetal hypoxia develops, up to the distress syndrome. In addition, capillary spasm can cause cerebral circulation disorders of varying severity, which forms the pathogenetic basis of preeclampsia and eclampsia. And impaired capillary blood flow in the liver causes the development of acute fatty hepatosis of pregnant women. The pathogenetic substrate of this pathology is massive necrosis of hepatocytes (unprogrammed cell death), which is accompanied by liver failure.

In addition, intensive care protocols recommend the administration of glutamine-containing drugs to critically ill patients (Marie Smedberg, 2016). The dose should be adjusted depending on the level of hyperammonemia.

Glutargin has a sobering effect by stimulating the utilization of ethyl alcohol metabolites. Therefore, it is widely used to treat hangovers (if a person has been poisoned by low-quality alcohol or simply drank too much) at home or in a hospital.

Glutargin is a drug, but its components – arginine and glutamic acid – are widely used in professional sports as biologically active supplements. Due to its role in collagen synthesis and muscle growth, Glutargin can also be used by bodybuilders during periods of muscle gain.

Method of administration and dose selectionIf the general condition of a person is characterized by an average degree of severity (the person is conscious, there are no complaints of vomiting, can swallow freely), then he is prescribed Glutargin orally in tablets three times a day without connection with meals. It is recommended to choose a single dose of 750 mg. The duration of treatment is usually 2 weeks. If necessary (severe course, long recovery period), the course of treatment can be extended to 3 weeks. In this case, the single dose can be increased to 2 g, and the total amount of the drug administered per day can be 8 g. If with hepatitis or late gestosis of pregnant women the general condition is assessed as severe (impaired consciousness, vomiting, etc.), Glutargin is administered intravenously drip. The maximum daily dose for infusion is 8 g. The daily dose is administered in small doses at intervals of 8-12 hours in 150-250 ml of 5% glucose solution or 0.9% NaCl. In addition to the intravenous route of administration, it can also be used intramuscularly (in the buttock). The standard single dose is 5 ml with the possibility of increasing to 10 ml, the frequency of injections is twice a day.

ContraindicationSince Glutargin Tablet is based on two replaceable amino acids, it is usually well tolerated. If, after its administration, the patient shows signs of individual intolerance, increased excitability, signs of fever or impaired renal filtration function (severe) (creatinine clearance (CC) decreases to 30 ml/min), the drug should be discontinued.

FeaturesIn the study (there is literature data) Glutargin Tablet did not reveal any negative effects on germ cells or the embryo (namely, mutagenic, teratogenic effect). The drug usually does not cause allergies, immunotoxic reactions. However, no studies have been conducted on the safety of the drug in the first half of pregnancy and during breastfeeding in humans. The safety of the drug in children has also not been studied (there is no data in the literature). Therefore, when making a decision to prescribe Glutargin tablet, the expected benefits and possible risks of its use should be weighed.

The drug should be prescribed with caution to people with cancer, as exogenous glutamate may reduce the effectiveness of anticancer drugs (Maria T. Grinde, 2019), especially vinblastine.

When prescribing the drug to patients with pathology of the pancreas and adrenal glands, it is necessary to remember that the drug stimulates the secretion of somatotropin and insulin due to the presence of arginine in the composition. The latter effect is further enhanced when combining Glutargin with aminophylline. This drug also promotes faster transformation of ammonia into urea. Which manifests itself in laboratory blood tests in the form of transient hyperuricemia. Glutargin Tablet can enhance the effect of antiplatelet agents. Due to the presence of neurotransmitters in the composition, Glutargin Tablet prevents and reduces neurotoxic side effects of isoniazid.

The drug affects the reaction rate, therefore it is not contraindicated for people who drive or operate complex mechanisms.

Side effects of Glutargin include nausea and pain or heaviness in the stomach area immediately after taking the tablets orally. These phenomena do not require treatment, they disappear on their own.

Various allergic reactions are possible – from skin rash to angioedema. Glutamic acid has a specific side effect – chest pain, heart rhythm and conduction disturbances such as atrioventricular block. To eliminate these phenomena, intravenous administration of corticosteroids is recommended.

conclusion Glutargin, as a nonspecific mediator of many biological and chemical processes in the human body, is suitable for the complex treatment of damage to liver cells and the nervous system by various toxins (infections, drugs, poisonous plants and mushrooms), as well as severe pregnancy pathology or systemic inflammatory response syndrome (sepsis, toxic shock). It is applicable both in a hospital setting and at home for the treatment and prevention of alcohol poisoning.

In addition to therapy, Glutargin can be used by professional athletes to improve the quality of muscle tissue. In addition, it is recommended to prescribe Glutargin to people weakened after serious illnesses for the fastest possible recovery.