Glutargin

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT GLUTARGIN (GLUTARGIN)

Composition:

Active substance: arginine glutamate;

1 tablet contains arginine glutamate 250 mg (0.25 g) or 750 mg (0.75 g);

Excipients:
250 mg dosage – microcrystalline cellulose, crospovidone, sodium croscarmellose, calcium stearate;
750 mg dosage – microcrystalline cellulose, crospovidone, calcium stearate.

Pharmaceutical form. Tablets.

Main physicochemical properties:
250 mg dosage – white tablets with flat surface, with a score line and bevel;
750 mg dosage – white, elongated tablets with convex surfaces and a score line.

Pharmacotherapeutic group. Drugs used in liver diseases, lipotropic agents. Hepatotropic agents. Arginine glutamate. ATC code A05B A01.

Pharmacological properties.

Pharmacodynamics. Glutargin is a salt of arginine and glutamic acid, both of which play an important role in supporting biochemical processes involved in neutralization and elimination from the body of highly toxic metabolite of nitrogenous compounds – ammonia. The hypoammonaemic effects of the drug are achieved through activation of ammonia detoxification in the ornithine cycle of urea synthesis, binding of ammonia into non-toxic glutamine, as well as enhanced removal of ammonia from the central nervous system and its excretion from the body. Due to these properties, Glutargin reduces general toxic, including neurotoxic, effects of ammonia.

Glutargin also exerts hepatoprotective action, due to its antioxidant, anti-hypoxic, and membrane-stabilizing properties, and positively influences energy supply processes in hepatocytes.

In alcohol intoxication, Glutargin stimulates alcohol utilization in the hepatic monooxygenase system, prevents inhibition of the key enzyme in ethanol metabolism – alcohol dehydrogenase; accelerates inactivation and elimination of toxic ethanol metabolites by increasing the formation and oxidation of succinic acid; reduces the depressant effect of alcohol on the central nervous system through the excitatory neurotransmitter properties of glutamic acid. Due to these properties, Glutargin exhibits antidotal and sobering effects.

In pregnancy-related disorders, due to its endothelioprotective action, Glutargin reduces impaired vascular permeability and thromboresistance, prevents hypercoagulation, and decreases vascular sensitivity to vasoconstrictive agents (endothelin, angiotensin, thromboxane) that cause generalized vasospasm. After prior biotransformation, arginine exerts vasodilatory effects via nitric oxide formation, positively influences blood coagulation and functional properties of circulating blood elements. As a result of vasodilatory and anti-hypoxic effects of Glutargin, maternal-fetal hemodynamics improves and intrauterine fetal hypoxia decreases. In pregnancy-related disorders, the drug also exhibits antidotal and hepatoprotective activity and acts as a non-specific metabolic regulator of metabolic processes. Due to these properties, during pregnancy Glutargin reduces levels of circulating immune complexes, decreases severity of the "metabolic" intoxication and immunotoxicosis syndromes, and enhances the body's compensatory and adaptive responses.

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

Pharmacokinetics. Not studied.

Clinical characteristics.

Indications. As part of complex therapy for acute and chronic hepatitis of various etiologies, including poisoning with hepatotropic toxins (e.g., death cap mushroom, chemical and medicinal substances), and in liver cirrhosis.

Hepatic encephalopathy associated with hyperammonemia.

Mild to moderate acute alcohol intoxication, hangover syndrome, post-intoxication disorders 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.

Contraindications. Hypersensitivity to the components of the drug. Jaundice, increased excitability, severe impairment of renal filtration (nitrogen-excreting) function.

Interaction with other medicinal products and other types of interactions. The effect of Glutargin on insulin secretion is enhanced when used concomitantly with aminophylline. Glutargin may potentiate the effect of antiplatelet agents (dipyridamole). It prevents and reduces neurotoxic symptoms that may occur during isoniazid administration. It diminishes the effect of vinblastine.

Special precautions for use.

When prescribing to patients with endocrine gland function disorders, it should be taken into account that the drug stimulates insulin and growth hormone secretion. The drug activates ammonia binding into urea, which may predictably be accompanied by a transient increase in its blood levels.

Use during pregnancy or breastfeeding. The safety of clinical use of the drug during the first and second trimesters of pregnancy and during breastfeeding has not been studied. If it is necessary to use the drug, breastfeeding should be discontinued.

Ability to affect reaction rate when driving or operating machinery. Does not affect.

Dosage and Administration

The medication should be administered orally to adults.

Hepatitis, hyperammonemia. Administer 750 mg (3 tablets of 250 mg or 1 tablet of 750 mg) three times daily for 15 days, regardless of food intake. If necessary, the dose and duration of treatment may be increased up to 20 days. The maximum single dose is 2 g; the maximum daily dose is 8 g.

Alcohol intoxication. Administer 1 g (4 tablets of 250 mg) four times daily at intervals of 1–2.5 hours; during the following 2–3 days, administer 500 mg (2 tablets of 250 mg) three times daily. In severe alcohol intoxication, after completing treatment with injectable Glutargin, administer Glutargin tablets at a dose of 750 mg (3 tablets of 250 mg or 1 tablet of 750 mg) twice daily for 20 days. For prevention of alcohol intoxication: 2 g taken 60–120 minutes before alcohol consumption.

Pregnancy pathologies (third trimester). Administer 250–500 mg (1–2 tablets of 250 mg) 2–3 times daily for 10–15 days. If necessary, the single dose may be increased to 750 mg (3 tablets of 250 mg or 1 tablet of 750 mg), and the treatment duration may be extended up to 20 days. The maximum single dose is 750 mg; the maximum daily dose is 2.25 g.

Children. The efficacy and safety of the medication in children have not been studied; therefore, the medication should not be used in this age group.

Overdose.

Symptoms: intensification of adverse reactions; possible characteristic effects of glutamic acid: chest pain, atrioventricular block.

Treatment: intravenous administration of corticosteroids.

Side effects.

Rarely possible:

Gastrointestinal tract: nausea, epigastric pain occurring immediately after administration of the drug, which resolve spontaneously.

Immune system: hypersensitivity reactions, including skin rashes, itching, hyperemia, urticaria, angioneurotic edema.

Shelf life. 5 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging. Tablets 250 mg, № 10×3, № 10×6 in blisters in a box or 750 mg, № 10×3, № 10×5 in blisters in a box.

Dispensing category. Over-the-counter.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA".

Limited Liability Company "FARMEKS GROUP".

Manufacturer's address and place of business. Ukraine, 61013, Kharkiv region, city of Kharkiv, Shevchenka Street, 22.

*(LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA")

Ukraine, 08301, Kyiv region, city of Boryspil, Shevchenka Street, 100.

(Limited Liability Company "FARMEKS GROUP")