Instructions Lekarnit solution for injection 1 g/5 ml ampoule 5 ml No. 5
Composition
active ingredient: levocarnitine;
1 ml of solution contains 200 mg of levocarnitine;
Excipients: diluted hydrochloric acid, water for injections.
Dosage form
Solution for injection.
Main physicochemical properties: clear solution from colorless to yellowish.
Pharmacotherapeutic group
Amino acids and their derivatives. ATX code A16A A01.
Pharmacological properties
Pharmacodynamics
Levocarnitine is present as a natural component in animal tissues, microorganisms and plants. In humans, physiological needs for carnitine are met through the consumption of foods containing carnitine (primarily meat products) and through endogenous synthesis in the liver from trimethyllysine. Only the L-isomer is biologically active. Levocarnitine plays an important role in lipid metabolism, as well as in the metabolism of ketone bodies. Levocarnitine is necessary for the transport of long-chain fatty acids into mitochondria for their subsequent beta-oxidation. By releasing coenzyme-A from complex thioesters, levocarnitine also enhances the oxidation of carbohydrates in the Krebs tricarboxylic acid cycle, and also stimulates the activity of the key enzyme of glycolysis - pyruvate dehydrogenase, and in skeletal muscles - the oxidation of branched-chain amino acids. Thus, levocarnitine directly or indirectly participates in most energy processes, its presence is required for the oxidation of fatty acids, amino acids, carbohydrates and ketone bodies. The highest concentration of levocarnitine is determined in muscle tissue, in the myocardium and liver. Levocarnitine plays an important role in cardiac metabolism, since the oxidation of fatty acids depends on the presence of a sufficient amount of this substance. Experimental studies have shown that under certain conditions, such as stress, acute ischemia, myocarditis, etc., a decrease in the level of levocarnitine in myocardial tissue is possible. A large number of studies have been conducted on animals, which have confirmed the positive effect of levocarnitine in the case of various induced cardiac disorders: acute and chronic ischemia, decompensation of cardiac activity, heart failure as a result of myocarditis, drug cardiotoxicity (taxanes, adriamycin, etc.).
Pharmacokinetics
Absorption
Levocarnitine is absorbed by the cells of the small intestinal mucosa and enters the bloodstream relatively slowly; absorption is probably due to an active transluminal mechanism. Absorption after oral administration is limited (<0%) and variable.
Distribution
Absorbed levocarnitine is transported to various organs via the blood; the erythrocyte transport system is thought to be involved in the transport process.
Breeding
Levocarnitine is excreted mainly in the urine. The rate of excretion is directly proportional to the concentration of carnitine in the blood.
Metabolism
Levocarnitine is practically not metabolized in the body.
Indication
Primary and secondary carnitine deficiency in adults and children, including newborns and infants.
Secondary carnitine deficiency in patients undergoing hemodialysis.
Suspect secondary carnitine deficiency in patients undergoing hemodialysis in the following cases:
severe and persistent muscle spasms and/or hypotensive episodes during dialysis; energy deficit leading to a significant negative impact on quality of life; muscle weakness and/or myopathy; cardiopathy; anemia unresponsive to erythropoietin treatment or requiring high doses of erythropoietin; loss of muscle mass.
Contraindication
Hypersensitivity to the components of the drug.
Interaction with other medicinal products and other types of interactions
Simultaneous use of glucocorticoids leads to the accumulation of levocarnitine in body tissues (except the liver). Other anabolic agents enhance the effect of the drug.
Application features
Levocarnitine improves glucose absorption, so the use of Lecarnitine in patients with diabetes mellitus who are treated with hypoglycemic drugs may lead to hypoglycemia. The level of glucose in the blood plasma in such cases must be regularly monitored for timely correction of therapy.
Use during pregnancy or breastfeeding
In preclinical studies, no teratogenic effects of the drug were detected. When using the highest dose tested, 600 mg/kg body weight, a statistically insignificant increase in the frequency of post-implantation fetal death in early pregnancy was observed in animals. The significance of these results for humans is unknown.
Considering the serious consequences of carnitine deficiency for a pregnant woman, the risk to the mother of interrupting treatment is considered greater than the theoretical risk to the fetus if treatment is continued.
Levocarnitine is a normal component of breast milk.
The ability to influence the reaction speed when driving or working with other mechanisms
Unknown.
Method of administration and doses
The solution for injection is administered by slow intravenous injection (2-3 minutes) or infusion.
Use in congenital metabolic disorders.
During therapy, it is advisable to monitor carnitine and acyl-carnitine levels in both blood plasma and urine.
The required dose depends on the specifics of the inborn error of metabolism and the severity of the disease.
In case of acute decompensation, the recommended dose may be up to 100 mg/kg per day in 3-4 doses. Higher doses may be used if necessary, although side effects, including diarrhea, may be increased.
Secondary carnitine deficiency in patients undergoing hemodialysis.
Before starting therapy with Lecarnit, it is advisable to monitor the level of carnitine in the blood plasma. Secondary carnitine deficiency is diagnosed when the ratio of acylcarnitine to free carnitine in the blood plasma is more than 0.4 and/or when the concentration of free carnitine is less than 20 μmol/l.
A dose of 2 g should be administered intravenously by bolus injection at the end of each dialysis session. The overall response should be determined by monitoring plasma acylcarnitine and free carnitine levels and by assessing the patient's condition. Normalization of carnitine content in muscle tissue and cardiomyocytes occurs approximately 3 months after reaching normal plasma carnitine concentrations. If carnitine administration is discontinued, its levels will inevitably begin to decline again. The need for a repeated saturating course of treatment is determined by quantitative determination of plasma carnitine at regular intervals and by monitoring the patient's condition.
Hemodialysis is a supportive therapy.
After a loading course of intravenous levocarnitine, a maintenance dose of 1 g of levocarnitine per day is administered orally. On the day of dialysis, Lecarnitine is administered intravenously at a dose of 1 g immediately after the end of the next session.
Children
The drug is used in children from the first day of life, including premature babies.
Overdose
There have been no reports of toxicity of levocarnitine in overdose. Large doses of the drug may cause diarrhea. Levocarnitine is easily removed from blood plasma by dialysis. Treatment: take measures to remove the drug from the digestive tract in case of ingestion, carry out symptomatic and supportive therapy. No cases of life-threatening overdose have been reported.
Adverse reactions
Various mild gastrointestinal disturbances have been observed with long-term oral levocarnitine administration, including transient nausea and vomiting, abdominal pain, and diarrhea. Dose reduction often reduces or eliminates gastrointestinal symptoms. Tolerability should be closely monitored during the first week of administration and after any dose increase. Intravenous administration of Lecarnitine is generally well tolerated.
Expiration date
3 years.
Storage conditions
Store in the original packaging, at a temperature not exceeding 25 °C, out of the reach of children.
Incompatibility
Do not mix with other medicines.
Packaging
5 ml in dark glass ampoules, 5 ampoules in a cardboard box.
Vacation category
According to the recipe.
Producer
HELP S.A. for Perreri Farmaceutici SRL, Corso San Lorenzo 1, 37026, Pescantina, Verona, Italy
Location of the manufacturer and address of its place of business
Pedini Ioanninon, Ioannina, 45500, Greece.
