Instructions for use Metakartin solution for injection 1 g/5 ml ampoule 5 ml No. 5
Composition
active ingredient: levocarnitine;
1 ampoule (5 ml) of solution for injection contains 1 g of levocarnitine;
1 ml of solution for injection contains 200 mg of levocarnitine;
Excipients: diluted hydrochloric acid, water for injections.
Dosage form
Solution for injection.
Main physicochemical properties: transparent colorless solution.
Pharmacotherapeutic group
Amino acids and their derivatives. Levocarnitine.
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, 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 essential 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 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. Many animal studies have confirmed the positive effect of levocarnitine in induced cardiac disorders, such as 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 (< 10%) 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.
Secondary carnitine deficiency should be suspected in patients undergoing hemodialysis in the following cases:
severe persistent muscle spasms and/or hypotensive episodes during dialysis; energy deficit that has a significant negative impact on quality of life; muscle weakness and/or myopathy; cardiopathy; anemia that does not respond to erythropoietin treatment or requires 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 Metacarnitine in patients with diabetes mellitus receiving treatment 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
Teratogenic effects were not observed in preclinical studies of the drug. When using the highest tested dose of 600 mg/kg body weight in animals, a statistically insignificant increase in the frequency of post-implantation fetal death in early pregnancy was noted. The significance of these results for humans is unknown.
Considering the consequences of carnitine deficiency for a pregnant woman, interrupting treatment with Metacartin seems to pose a greater risk to the mother than the theoretical risk to the fetus if treatment is continued.
Levocarnitine is a common component of human breast milk.
The ability to influence the reaction speed when driving or working with other mechanisms
Unknown.
Method of administration and doses
The drug is administered intravenously slowly over 2-3 minutes.
Use in congenital metabolic disorders.
During therapy, it is advisable to monitor carnitine and acylcarnitine 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 Metacartin, it is advisable to check the level of carnitine in the blood plasma.
Secondary carnitine deficiency is diagnosed when the ratio of acylcarnitine to free carnitine in blood plasma is greater 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 assessed by monitoring plasma acylcarnitine and free carnitine levels and by 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 the patient's condition.
Hemodialysis is a supportive therapy.
After a loading course of intravenous levocarnitine, a maintenance dose of 1 g of the drug per day is used orally. On the day of dialysis, Metacartin is used 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 from overdose of levocarnitine. Large doses of the drug may cause diarrhea. Levocarnitine is readily 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 life-threatening cases of overdose have been reported.
Adverse reactions
Mild gastrointestinal disturbances have been observed with long-term oral administration of levocarnitine, 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 Methacarnitine is generally well tolerated.
Expiration date
4 years.
Storage conditions
Store at a temperature not exceeding 25 °C out of the reach of children.
Incompatibility
Do not mix with other medicines.
Packaging
5 ml in a brown glass ampoule; 5 ampoules in a contour blister pack; 1 or 2 contour blister packs in a cardboard box.
Vacation category
According to the recipe.
Producer
Mefar Ilach San. A.Sh. / Mefar Ilac San. AS
Location of the manufacturer and address of its place of business
Ramazanoglu Mach. Ansar Jad. No. 20, 34906 Kurtkoy – Pendik/Istanbul, Turkey / Ramazanoglu Mah. Ensar Cad. No. 20, 34906 Kurtkoy – Pendik/Istanbul, Turkey.
Applicant
WORLD MEDICINE ILAС SAN. VE TIC. AS, Turkey.
