Instructions for use Essentiale H solution for injection 250 mg/5 ml ampoule 5 ml No. 5
Composition
active ingredient: “Essential Phospholipids”®= EPL®-substance (phospholipids from soybeans (93% (3-sn-phosphatidyl)choline), which contain a-tocopherol, ethanol 96%);
1 ml of solution contains “Essential Phospholipids”®= EPL® - substance (phospholipids from soybeans (93% (3-sn-phosphatidyl)choline), which contain a-tocopherol, ethanol 96%) - 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, practically free from visible suspended particles.
Pharmacotherapeutic group
Drugs used in liver diseases, lipotropic substances. 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 preparation Essentiale® H are similar in chemical structure to endogenous phospholipids, but have a much higher 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 basic 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 to 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, psoriasis, radiation syndrome.
Contraindication
Hypersensitivity to any of the components of the drug.
Essentiale® H should not be administered to newborns and premature infants, as the drug contains benzyl alcohol.
Special safety precautions
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.
The drug should be administered slowly into a vein (intravenously).
Essentiale® H solution for intravenous injection should not be administered into the muscle (intramuscularly) as this may cause local irritation.
Caution: Essentiale® H solution for intravenous administration contains 0.6% alcohol (by volume).
Interaction with other medicinal products and other types of interactions
Electrolyte solutions should not be used to dilute the drug.
Application features
When diluting Essentiale® H to prepare an infusion solution (if it is impossible to use the patient's own blood), electrolyte-free solutions should be used, namely: 5% or 10% glucose solution (in a 1:1 ratio), 5% xylitol solution.
The drug should not be administered intramuscularly due to the possible occurrence of 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 Essentiale® H is not recommended during pregnancy and breastfeeding.
The ability to influence the reaction speed when driving or working with other mechanisms
Not detected.
Method of administration and doses
Adults and children over 12 years of age are prescribed 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 Essentiale® forte N capsules as early as possible.
The total course of treatment is 3–6 months.
Treatment of psoriasis begins with taking 2 capsules of Essentiale® forte H 3 times a day for 2 weeks. After that, 10 intravenous injections of 5 ml are recommended with simultaneous administration of PUVA therapy.
After the end of the course of injections, resume taking the capsules and continue using the drug for 2 months.
Children
The drug is intended for use in children aged 12 years and older, whose body weight is 43 kg or more (see the section “Method of administration and dosage”).
Overdose
No reports of overdose have been recorded.
Side effects
In some cases, when using increased doses of Essentiale® H, 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.
Storage conditions
Keep out of reach of children. Store in the original packaging at a temperature of 2 to 8 °C.
Incompatibility
Electrolyte solutions should not be used to dilute the drug.
Packaging
No. 5: 5 ml in an ampoule; 5 ampoules in a contour blister pack in a cardboard box.
Vacation category
According to the recipe.
Producer
JSC "Galychpharm", Ukraine.
FAMAR HEALTHCARE SERVICES MADRID, S.A.U., Spain.
Address
Ukraine, 79024, Lviv, Opryshkivska St., 6/8.
Avenida Leganes, 62, Alcorcón 28923 Madrid, Spain
Applicant
Opela Healthcare Ukraine LLC, Ukraine.
