Instructions for use L'Esfal solution for injection 50 mg/ml ampoule 5 ml No. 5
Composition
active ingredient: 1 ml of solution contains phosphatidylcholine from soybeans 50 mg;
Excipients: benzyl alcohol, deoxycholic acid, sodium chloride, sodium hydroxide, riboflavin (E 101), water for injections.
Dosage form
Solution for injection.
Main physicochemical properties: clear yellow solution.
Pharmacotherapeutic group
Hepatotropic drugs. ATX code A05B A.
Pharmacological properties
Pharmacodynamics.
In liver diseases, hepatocyte membranes and their organelles are always damaged, which can lead to changes in the activity of membrane-bound enzymes and receptor systems, disruption of the metabolic function of the cell, and a decrease in the intensity of liver regeneration.
Phospholipids contained in the drug Lesfal are similar in chemical structure to endogenous phospholipids, but far outweigh them due to the high content of polyunsaturated (essential) fatty acids. These high-energy molecules are mainly incorporated into the structures of cell membranes and facilitate the restoration of damaged liver tissues. Since the cis-double bonds of these polyenoic acids prevent the parallel arrangement of the hydrocarbon chains of membrane phospholipids, the density of the arrangement of phospholipid structures decreases, as a result of which the rate of entry and excretion of substances increases. Membrane-bound enzymes form functional units that can enhance their activity and ensure the physiological course of the main metabolic processes. Phospholipids affect impaired lipid metabolism by regulating lipoprotein metabolism, as a result of which neutral fats and cholesterol are converted into forms suitable for transport, especially by increasing the ability of high-density lipoproteins (HDL) to bind cholesterol, and are directed for further oxidation. During the excretion of phospholipids through the biliary tract, the lithogenic index decreases and bile is stabilized.
Pharmacokinetics.
When taken orally, more than 90% of the drug is absorbed in the small intestine. The main amount is broken down by phospholipase-A to 1-acyl-lyso-phosphatidylcholine, 50% of which is immediately reacylated into polyunsaturated phosphatidylcholine during absorption in the small intestine. Polyunsaturated phosphatidylcholine enters the blood through the lymphatic system and is then transported to the liver, mainly in a complex with HDL. The maximum content of phosphatidylcholine in the blood 6-24 hours after oral administration is on average 20%.
The half-life for the choline component is 66 hours, for saturated fatty acids – 32 hours.
In human kinetic studies, less than 5% of each of the administered 3H and 14C isotopes was excreted in the feces.
Indication
Non-alcoholic steatohepatitis, alcoholic steatohepatitis, acute and chronic hepatitis of various etiologies, liver cirrhosis, pre- and postoperative treatment for surgical intervention on the liver and biliary tract, toxicosis of pregnant women, psoriasis, radiation syndrome.
Contraindication
Hypersensitivity to any of the components of the drug.
Lesfal should not be prescribed to newborns and premature infants, as the drug contains benzyl alcohol.
Interaction with other medicinal products and other types of interactions
Electrolyte solutions should not be used to dilute the drug.
Application features
When diluting Lesfal for the preparation of an infusion solution (if it is impossible to use the patient's own blood), solutions free of electrolytes should be used, namely: 5% or 10% glucose solution (in a ratio of 1: 1), 5% xylitol solution.
Use only clear solution.
The drug is incompatible with electrolyte solutions (saline sodium chloride solution, Ringer's solution, etc.).
Do not mix with other medications in the same syringe.
Caution: the solution contains 5.02 mg/ml of alcohol.
1 ml of Lesfal contains 0.1 mmol sodium. When taking the drug in a dose of 10 ml, the sodium content is 1.0 mmol (25.8 mg), which should be taken into account by patients on a controlled sodium diet.
For intravenous use only. The drug should be administered slowly.
Lesfal solution should not be administered into the muscle (intramuscularly) as this may cause local irritation.
Use during pregnancy or breastfeeding
Due to the limited amount of clinical trial data on use in pregnant women and due to the presence of benzyl alcohol, which can pass through the placental barrier, the use of Lesfal is not recommended during pregnancy or breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
Not detected.
Method of administration and doses
Adults and children over 12 years of age should be administered intravenously slowly 5-10 ml per day, and in severe cases - from 10 to 20 ml per day. 10 ml of the drug can be administered at a time. If the drug is administered diluted, it is recommended to use the patient's own blood and dilute the drug in a 1:1 ratio. Intravenous infusion is usually used for up to 10 days.
It is recommended to support (supplement) parenteral therapy with oral administration of drugs containing phosphatidylcholine as early as possible.
The total course of treatment is 3 – 6 months.
Treatment of psoriasis should begin with oral administration of phosphatidylcholine for 2 weeks. After that, 10 intravenous injections of 5 ml are recommended with simultaneous administration of PUVA therapy.
After completing the course of injections, resume oral intake of phosphatidylcholine and continue using the drug for 2 months.
Children. Lesfal solution for intravenous injection should not be administered to newborns and premature infants, as the preparation contains benzyl alcohol. Administration of preparations containing benzyl alcohol to infants and premature infants has been associated with the development of a fatal dyspnea syndrome ("gasping syndrome", symptoms of which include sudden onset of dyspnea, hypotension, bradycardia and cardiovascular collapse).
The drug is intended for use in children aged 12 years and over and weighing approximately 43 kg (see section “Method of administration and dosage”).
Overdose
No reports of overdose have been recorded.
Side effects
In some cases, when using increased doses of Lesfal, gastrointestinal disorders (diarrhea) are possible.
In rare cases, hypersensitivity reactions, rash, itching, urticaria and reactions at the injection site may occur.
Expiration date
3 years.
Do not use the drug after the expiration date indicated on the package.
Storage conditions
Store in a place protected from light at a temperature of 2 ºС to 8 ºС.
Keep out of reach of children.
Packaging
5 ml in an ampoule. 5 or 10 ampoules in a pack.
5 ampoules in a blister. 1 or 2 blisters in a pack.
Vacation category
According to the recipe.
Producer
JSC "Farmak".
Address
Ukraine, 04080, Kyiv, Kyrylivska St., 74.
