Pharmacological properties

Pharmacodynamics. the left carnitine is present as a natural component at tissues of animals, microorganisms and plants. at the person the physiological needs for a carnitine are replenished due to consumption of the food containing a carnitine (first of all meat products), and by endogenous synthesis in a liver from a trimetillizin. only l-isomer is biologically active. the left carnitine plays an important role in lipidic metabolism and also in metabolism of ketone ph. the left carnitine is necessary for transportation of long-chain fatty acids in a mitochondrion for their further beta oxidation. releasing coenzyme from complex monothioesters, the left carnitine also strengthens oxidation of carbohydrates in a cycle of tricarboxylic acids of Krebs, stimulates activity of key enzyme of glycolysis — pyruvatedehydrogenase, and in skeletal muscles — oxidation of amino acids with a branched chain. thus, the left carnitine directly or indirectly participates in the majority of power processes, its existence is obligatory for oxidation of fatty acids, amino acids, carbohydrates and ketone ph.

Highest concentration of a left carnitine is defined in muscle tissue, in a myocardium and a liver. The left carnitine plays an important role in warm metabolism as oxidation of fatty acids depends on enough this substance. Results of pilot studies demonstrated that under some conditions, such as stress, acute ischemia, myocarditis and other, decrease in level of a left carnitine in myocardial fabric is possible. Many researches on animals confirmed positive impact of a left carnitine at the induced cardiac disorders, such as acute and chronic ischemia, decompensation of warm activity, heart failure as a result of myocarditis, medicamentous cardiotoxicity (taxons, adriamycin, etc.).

Pharmacokinetics

Absorption. Levokarnitin is soaked up by cells of a mucous membrane of a small intestine and rather slowly enters the blood channel; possibly, absorption is connected with the active transluminal mechanism. Absorption after oral administration is limited (10%) and is changeable.

Distribution. The absorbed left carnitine is transported in various bodies through blood; it is considered that in the course of transportation the transport system of erythrocytes is involved.

Removal. Levokarnitin is brought mainly with urine. Clearance rate is directly proportional to concentration of a carnitine in blood.

Metabolism. The left carnitine is practically not metabolized in an organism.

Indication

Primary and secondary karnitinovy insufficiency at adults and children, including at newborns and babies.

Secondary karnitinovy insufficiency at the patients who are on a hemodialysis.

Secondary karnitinovy insufficiency should be suspected at the patients who are on a hemodialysis of the following cases:

• strong persistent spasms in muscles and/or hypotensive episodes during dialysis;
• power deficit having considerable negative impact on quality of life;
• muscle weakness and/or myopathy;
• cardiopathy;
• anemia which does not respond to treatment with erythropoietin or demands high doses of erythropoietin;
• loss of muscle bulk.

Use

Drug is administered in/in slowly within 2–3 min.

Use at congenital disturbance of metabolism. During therapy it is reasonable to control levels of a carnitine and acylcarnitine both in blood plasma, and in urine.

Necessary dose depends on specifics of congenital disturbance of metabolism and weight of manifestations of a disease. In case of a sharp decompensation the recommended dose can make up to 100 mg/kg of body weight a day for 3–4 introductions. In case of need it is possible to apply also higher doses though at the same time side effects, in particular diarrhea can amplify.

Secondary deficit of a carnitine at the patients who are on a hemodialysis. Before therapy by Metakartin it is desirable to carry out an inspection of level of a carnitine in blood plasma.

at an acylcarnitine ratio to a free carnitine in blood plasma 0.4 and/or when concentration of a free carnitine makes 20 µmol/l.

Dose of 2 g should be entered in/in struyno at the end of each session of dialysis. The general reaction should be estimated by monitoring of levels of an acylcarnitine and a free carnitine in blood plasma and on a condition of the patient. Normalization of maintenance of a carnitine in muscle tissue and cardiomyocytes occurs approximately in 3 months after achievement of normal concentration of a carnitine in blood plasma. If to stop introduction of a carnitine, its levels by all means will begin to decrease again. Need of the repeated saturating course of treatment is determined by quantitative definition of a carnitine in blood plasma through equal intervals of time and by a condition of the patient.

Hemodialysis — maintenance therapy. After the saturating course of introduction of a left carnitine apply a maintenance dose — 1 g of medicament a day orally. In day of dialysis Metakartin apply in/in in a dose of 1 g right after completion of another session.

Children. Drug is used to children from the first day of life, including premature.

Contraindication

Hypersensitivity to medicament components.

Moderate gastrointestinal disorders were observed by

at long reception of an oral left carnitine, including fleeting nausea and vomiting, an abdominal pain and diarrhea. the dose decline often reduces expressiveness or eliminates gastrointestinal symptoms. it is necessary to control carefully shipping within 1 week of reception and after any increase in a dose. the metapicture is usually transferred in to use well.

Special instructions

Levokarnitin improves digestion of glucose therefore the metapicture at the patsiyen with diabetes receiving treatment by glucose-lowering medicaments can lead use to a hypoglycemia. glucose level in blood plasma in such cases needs to be controlled regularly for timely correction of therapy.

Use during pregnancy or feeding by a breast. Teratogenic action in preclinical trials of medicament is not revealed. At use of the most studied dose of 600 mg/kg of body weight for animals statistically insignificant increase in frequency of post-implantation death of a fruit in the early stages of pregnancy was noted. The importance of these results for the person is unknown.

Despite consequences of karnitinovy insufficiency for pregnant women, treatment interruption by a left carnitine for mother seems big risk, than theoretical risk for a fruit in case of treatment continuation.

Levokarnitin — a usual component of breast milk of the person.

Ability to influence speed of response at control of vehicles or work with other mechanisms. It is unknown.

Simultaneous use gks leads

Interaction

Incompatibility. Not to mix with other medicines.

Overdose

Messages about toxicity of a left carnitine at overdose was not. use of medicament in high doses can cause diarrhea. the left carnitine easily is removed from blood plasma dialysis.

Treatment: to take measures for removal of medicament from a digestive tract at intake, to carry out symptomatic and maintenance therapy. It was not reported about cases of overdose, life-threatening.

Storage conditions

At a temperature not above 25 °C.