Levocarnitine (Solution) Instructions for Use

ATC Code

A16AA01 (Levocarnitine)

Active Substance

Levocarnitine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

A drug that improves tissue metabolism and energy supply

Pharmacotherapeutic Group

Other agents for the treatment of gastrointestinal diseases and metabolic disorders; amino acids and their derivatives

Pharmacological Action

Levocarnitine is an agent for the correction of metabolic processes; it has metabolic, anabolic, antihypoxic, and antithyroid action, activates fat metabolism, stimulates regeneration, and increases appetite.

Levocarnitine is a natural substance related to B vitamins. It is a cofactor of metabolic processes that maintain the activity of coenzyme A (CoA). It reduces the basal metabolic rate and slows down the breakdown of protein and carbohydrate molecules.

It promotes the penetration through mitochondrial membranes and the breakdown of long-chain fatty acids (palmitic acid, etc.) with the formation of acetyl-CoA (necessary for ensuring the activity of pyruvate carboxylase in the process of gluconeogenesis, the formation of ketone bodies, the synthesis of choline and its esters, oxidative phosphorylation, and the formation of ATP).

It mobilizes fat (due to the presence of 3 labile methyl groups) from fat depots. By competitively displacing glucose, it activates the fatty acid metabolic shunt, the activity of which is not limited by oxygen (unlike aerobic glycolysis), which is why Levocarnitine is effective in conditions of acute hypoxia (including cerebral hypoxia) and other critical conditions.

It causes slight depression of the central nervous system, increases the secretion and enzymatic activity of digestive juices (gastric and intestinal), and improves food absorption.

It reduces excess body weight and decreases the fat content in skeletal muscles.

It increases the threshold of resistance to physical exertion, reduces the degree of lactate acidosis, and restores working capacity after prolonged physical exertion. At the same time, it promotes economical consumption of glycogen and increases its reserves in the liver and muscles.

It has a neurotrophic effect, inhibits apoptosis, limits the area of damage, and restores the structure of nervous tissue. It normalizes protein and fat metabolism, the increased basal metabolic rate in thyrotoxicosis (being a partial antagonist of thyroxine); and restores the alkaline reserve of the blood.

Pharmacokinetics

After oral administration, it is well absorbed. C_max is reached after 3 hours, and the therapeutic concentration is maintained for 9 hours. After intramuscular administration, it is detected in plasma for 4 hours. After intravenous administration, it disappears from the blood as early as 3 hours later. It easily penetrates the liver and myocardium, and more slowly into the muscles. It is excreted by the kidneys mainly in the form of acyl esters.

Indications

For oral administration: as part of complex therapy in adults during intense and prolonged physical exertion, psychoemotional stress: to increase working capacity, endurance, reduce fatigue, including in the elderly; during the rehabilitation period after past illnesses and surgical interventions, injuries, including to accelerate tissue regeneration; in nervous anorexia; in diseases accompanied by carnitine deficiency or its increased loss (myopathies, cardiomyopathies, mitochondrial diseases, hereditary diseases with concomitant mitochondrial insufficiency): to replenish its deficiency as part of complex therapy; in sports medicine and during intensive training (during the training process when working on aerobic performance): to improve speed-strength indicators and movement coordination, to increase muscle mass and reduce body fat mass, to prevent post-training syndrome (accelerating recovery processes after physical exertion), in traumatic injuries to accelerate muscle regeneration.

For intramuscular and intravenous administration: as part of complex therapy for acute hypoxic conditions (acute cerebral hypoxia, ischemic stroke, transient ischemic attack); in the acute, subacute, and recovery periods of cerebrovascular accidents; in dyscirculatory encephalopathy and various traumatic and toxic brain lesions, in the recovery period after surgical interventions; in primary and secondary carnitine deficiency, including in patients with chronic renal failure on hemodialysis; in cardiomyopathy, coronary artery disease (angina pectoris, acute myocardial infarction, post-infarction conditions), hypoperfusion due to cardiogenic shock and other myocardial metabolism disorders.

ICD codes

Dosage Regimen

Determine the dose, route of administration, and duration of therapy individually based on the indication and clinical situation.

For oral administration in adults, use a typical daily dose of 500 mg to 2 g, divided into 2-3 doses. The maximum daily dose is 3 g.

For intramuscular administration, inject slowly. For intravenous administration, administer as a slow bolus over 2-3 minutes or as an infusion.

For acute myocardial infarction and cardiogenic shock, administer 2-6 g/day intravenously, divided into 3-4 doses.

For primary and secondary carnitine deficiency, including in hemodialysis patients, administer 10-30 mg/kg/day intravenously or 0.5-1 g/day orally after dialysis sessions.

For acute cerebral hypoxia and ischemic stroke, administer 1 g/day intravenously for 3-5 days, then switch to 0.5-1 g/day orally for 3-7 days.

For dyscirculatory encephalopathy and brain injury sequelae, administer 0.5-1 g/day intravenously for 3-5 days, then switch to oral therapy for 2-4 months.

To increase physical endurance and reduce fatigue, administer 0.5-1.5 g/day orally for 2-4 weeks. For sports medicine, use 1-2 g 30-60 minutes before training.

For nervous anorexia, administer 1-2 g/day orally for 1-2 months.

Adjust the dose for patients with severe renal impairment to avoid accumulation of toxic metabolites. Monitor blood glucose levels in diabetic patients due to risk of hypoglycemia.

Adverse Reactions

Nervous system disorders: very rarely – myasthenic disorders (in patients with uremia).

Gastrointestinal disorders: very rarely – gastralgia, dyspepsia.

Skin and subcutaneous tissue disorders: very rarely – rash, allergic dermatitis.

Local reactions: with rapid intravenous administration (80 drops/min or more), pain along the vein may occur, which disappears when the injection rate is reduced.

Contraindications

Hypersensitivity to levocarnitine; pregnancy, breastfeeding period.

With caution in diabetes mellitus.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding). If it is necessary to use during lactation, the issue of discontinuing breastfeeding should be decided.

Use in Renal Impairment

Long-term use of levocarnitine in high doses in patients with severe renal impairment may cause an increase in the concentration of potentially toxic metabolites, trimethylamine and trimethylamine-N-oxide.

Pediatric Use

In children and adolescents under 18 years of age, Levocarnitine is used in appropriate dosage forms.

Geriatric Use

It can be used in elderly patients according to indications, in recommended doses and dosage forms.

Special Precautions

Increased glucose absorption with the use of levocarnitine in patients with diabetes mellitus receiving insulin or oral hypoglycemic drugs may cause hypoglycemia. For this reason, in this category of patients, blood glucose levels should be constantly monitored during treatment with levocarnitine for immediate correction of the dosage regimen of hypoglycemic drugs.

Long-term use of levocarnitine in high doses in patients with severe renal impairment may cause an increase in the concentration of potentially toxic metabolites, trimethylamine and trimethylamine-N-oxide, because these metabolites are usually excreted in the urine. In this case, urine, breath, and sweat have an unpleasant odor.

In children and adolescents under 18 years of age, Levocarnitine is used in appropriate dosage forms.

Drug Interactions

With simultaneous use, anabolic agents enhance the effect of levocarnitine.

With simultaneous use, corticosteroids promote the accumulation of levocarnitine in tissues (except the liver).

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.