Carnitine
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Clinical Pharmacology
Carnitine chloride is an anabolic means of non-steroid nature. The drug stimulates metabolic processes, participating in various links of energy metabolism, has anabolic, antihypoxic and antithyroid action, activates lipid metabolism, stimulates regeneration, increases appetite. Carnitine is a natural substance related to vitamins of group B. It is a cofactor of metabolic processes that maintain the activity of CoA. Reduces basal metabolism, slows the breakdown of protein and carbohydrate molecules. It promotes the penetration of mitochondria through the membranes and the cleavage of long-chain fatty acids (palmitic and others) with the formation of acetyl-CoA, which is necessary to ensure the activity of pyruvate carboxylase during gluconeogenesis, the formation of ketone bodies, the synthesis of choline and its esters, oxidative phosphorylation and the formation of ATP. Mobilizes fat (the presence of three labile methyl groups) from the fat depot. Competitively displacing glucose, includes fatty acid metabolic shunt, the activity of which is not limited by oxygen (unlike aerobic glycolysis), and therefore the drug is effective in conditions of acute hypoxia (including the brain) and other critical conditions. It has a neurotrophic effect, inhibits apoptosis, limits the affected area and restores the structure of the nervous tissue. Normalizes protein and fat metabolism, increased basal metabolic rate in hyperthyroidism (being a partial thyroxin antagonist). The drug restores the alkaline reserve of blood, does not affect the blood coagulation system, reduces the formation of keto acids, increases the resistance of tissues to the effects of toxic decomposition products, activates aerobic processes and inhibits anaerobic glycolysis, has antihypoxic properties, stimulates and accelerates reparative processes.
Indications
- Acute disorders of cerebral circulation - ischemic stroke, transient ischemic attack - in acute, subacute and recovery periods.
- Encephalopathy.
- Traumatic and toxic brain damage. As monotherapy or as part of complex therapy.
Composition
1 ml of solution contains: 100 mg of carnitine chloride and up to 1 ml of water for injection.
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Dosage and Administration
The drug is administered intravenously slowly (no more than 60 drops per minute!). Before introducing the contents of one or two vials, 5-10 ml of 10% solution of carnitine chloride (0.5-1 g) - diluted in 200 ml of 0.9% sodium chloride solution for injection. In acute disorders of cerebral blood circulation, it is prescribed in the first three days 1 g once a day, and then within 7 days 0.5 g per day. After 10-12 days, repeated courses are recommended - 0.5 g once a day for 3-5 days.
When prescribing the drug in the subacute and recovery periods, with dyscirculatory encephalopathy and various brain lesions, patients are given 0.5-1 g (1-2 ampoules) of the drug once a day for 3-5 days. If necessary, after 12-14 days appoint a second course.
Adverse reactions
Allergic reactions are possible.
Muscular weakness is possible in patients with uremia.
With the rapid introduction (80 drops per minute or more), pain may occur along the veins, passing at a decrease in the rate of administration.
Contraindications
Hypersensitivity to carnitine chloride.
Drug interactions
When combined with carnitine chloride, glucocorticoids contribute to its accumulation in tissues (except the liver).
Other anabolic agents enhance the effect.
Pregnancy and Lactation
Special studies on the possibility of using during pregnancy and during breastfeeding have not been conducted. The decision on use should be made by evaluating the ratio of the possible risk to the child and the benefit to the mother.
- First prenatal diagnosis of the carnitine transporter defect
- Quantitation of L-carnitine, acetyl-L-carnitine, propionyl-L-carnitine and their deuterated analogues by high-performance liquid chromotography tandem mass spectrometry
- Dietary carnitine supplements slow disease progression in a putative mouse model for hereditary ceroid-lipofuscinosis
- Changes in skeletal muscle histology and metabolism in patients undergoing exercise deconditioning: Effect of propionyl-L-carnitine
- Analysis of organic acids, amino acids, and carnitine in dogs with lipid storage myopathy
- Effects of a low-dose L-carnitine supplement on an adult patient with mitochondrial trifunctional protein deficiency
- Molecular analysis in spanish patients with muscle carnitine palmitoyltransferase deficiency
- Biochemical and molecular correlations in carnitine palmitoyltransferase II deficiency
- Cancer and anticancer therapy-induced modifications on metabolism mediated by carnitine system
- Two CPT2 mutations in three Japanese patients with carnitine palmitoyltransferase II deficiency: Functional analysis and association with polymorphic haplotypes and two clinical phenotypes
- Novel mutations associated with carnitine palmitoyltransferase II deficiency
- Two novel missense mutations of the OCTN2 gene (W283R and V446F) in a patient with primary systemic carnitine deficiency
- A missense mutation in the OCTN2 gene associated with residual carnitine transport activity
- Carnitine levels in patients with skeletal myopathy due to anorexia nervosa before and after refeeding
- Physiological mechanism-based analysis of dose-dependent gastrointestinal absorption of L-carnitine in rats
- Investigation of the effect of theophylline administration on total, free, short-chain acyl and long-chain acyl carnitine distributions in rat renal tissues
- Synthesis of [methyl-14C]crotonobetaine from DL-[methyl-14C]carnitine
- Nuclear magnetic resonance studies of boar seminal plasma. Problems encountered in the identification of small molecules: hypotaurine and carnitine
- Transport of carnitine in RBE4 cells - an in vitro model of blood-brain barrier
- Carnitine: An osmolyte that plays a metabolic role
- Identification of novel mutations in Spanish patients with muscle carnitine palmitoyltransferase II deficiency
- Functional analysis of mutations in the OCTN2 transporter causing primary carnitine deficiency: Lack of genotype–phenotype correlation
- Abnormal plasma carnitine derivatives reflecting an altered metabolic state in anorexic women at rest and following maximal effort treadmill exercise
- Synthesis of Poly-β-hydroxybutyrate by Agrobacterium radiobacter after Growth on D-Carnitine