ESSENTIAL® N

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ESSENTIALE® N (ESSENTIALE® N)

Composition:

Active substance: "Essential phospholipids"® = EPL®-substance (soybean phospholipids (93% (3-sn-phosphatidyl)choline), containing α-tocopherol, 96% ethanol);

1 ml of solution contains "Essential phospholipids"® = EPL®-substance (soybean phospholipids (93% (3-sn-phosphatidyl)choline), containing α-tocopherol, 96% ethanol) – 50 mg;

Excipients: benzyl alcohol, deoxycholic acid, sodium chloride, sodium hydroxide, riboflavin (E 101), water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: clear yellow solution, practically free from visible suspended particles.

Pharmacotherapeutic group. Drugs used in liver diseases, lipotropic agents. ATC code A05BA.

Pharmacological Properties.

Pharmacodynamics. In liver diseases, hepatocyte membranes and their organelles are always damaged, which may lead to changes in the activity of membrane-bound enzymes and receptor systems, disruption of the cell's metabolic function, and reduced intensity of liver regeneration.

The phospholipids contained in the drug Essentiale® N are chemically similar to endogenous phospholipids but have a much higher content of polyunsaturated (essential) fatty acids. These high-energy molecules are primarily incorporated into cellular membrane structures and facilitate the restoration of damaged liver tissue. Due to the presence of cis-double bonds in these polyene fatty acids, which prevent parallel alignment of hydrocarbon chains in membrane phospholipids, the packing density of phospholipid structures decreases, thereby increasing the rate of substance influx and efflux. Membrane-bound enzymes form functional units that may enhance their activity and ensure physiological progression of key metabolic processes. Phospholipids influence impaired lipid metabolism by regulating lipoprotein metabolism, resulting in the conversion of neutral fats and cholesterol into transportable forms, particularly due to increased ability of high-density lipoproteins (HDL) to bind cholesterol, directing them toward further oxidation. During excretion of phospholipids through the biliary tract, the lithogenic index decreases and bile stabilization occurs.

Pharmacokinetics. After oral administration, more than 90% of the drug is absorbed in the small intestine. The majority is cleaved by phospholipase A into 1-acyl-lysophosphatidylcholine, 50% of which is immediately reacylated into polyunsaturated phosphatidylcholine during absorption in the small intestine. Polyunsaturated phosphatidylcholine enters the bloodstream via lymphatic pathways and is subsequently transported predominantly in complex with HDL to the liver. The maximum concentration of phosphatidylcholine in blood 6–24 hours after oral administration averages 20%.

The elimination half-life is 66 hours for the choline component and 32 hours for saturated fatty acids.

In human kinetic studies, less than 5% of each administered isotope of 3H and 14C was excreted in feces.

Clinical characteristics.

Indications.

Non-alcoholic steatohepatitis, alcoholic steatohepatitis, acute and chronic hepatitis of various etiologies, liver cirrhosis, pre- and postoperative treatment in surgical interventions on the liver and biliary tract, psoriasis, radiation syndrome.

Contraindications.

Hypersensitivity to any component of the drug.

Essentiale® N should not be administered to newborns and premature infants, as the formulation contains benzyl alcohol.

Special precautions.

Use only a clear solution.

The drug is incompatible with electrolyte solutions (e.g., sodium chloride physiological solution, Ringer's solution, etc.).

Do not mix with other medicinal products in the same syringe.

The drug should be administered slowly intravenously.

Essentiale® N injection solution for intravenous use must not be administered intramuscularly, as it may cause local irritation.

Warning: Essentiale® N intravenous solution contains 0.6% alcohol by volume.

Interaction with other medicinal products and other forms of interaction.

Electrolyte solutions must not be used for dilution of the drug.

Instructions for use.

When diluting Essentiale® N to prepare an infusion solution (in cases where the patient's own blood cannot be used), electrolyte-free solutions should be used, namely: 5% or 10% glucose solution (in a 1:1 ratio), 5% xylitol solution.

The drug must not be administered intramuscularly due to the possibility of local irritation.

Use during pregnancy or breastfeeding.

Due to limited clinical data on use in pregnant women and because the formulation contains benzyl alcohol, which may cross the placental barrier, the use of Essentiale® N is not recommended during pregnancy and breastfeeding.

Ability to influence reaction rate when driving or operating machinery.
Not observed.

Method of Administration and Dosage

For adults and children aged 12 years and older, the recommended dose is 5–10 mL daily administered slowly intravenously; in severe cases, the dose may be increased to 10–20 mL per day. A volume of 10 mL of the drug may be administered at once. If dilution is required, it is recommended to use the patient's own blood to dilute the drug in a 1:1 ratio. Intravenous infusions are generally administered for up to 10 days.

Parenteral therapy should be supplemented (supported) as early as possible with oral administration of Essentiale® Forte N capsules.

The total treatment duration is 3–6 months.

For psoriasis treatment, start with 2 capsules of Essentiale® Forte N taken 3 times daily for 2 weeks. After this period, administer 10 intravenous injections of 5 mL each, concurrently with PUVA therapy.

After completion of the injection course, resume oral capsule intake and continue treatment for an additional 2 months.

Children

The drug is indicated for use in children aged 12 years and older with a body weight of 43 kg or more (see section "Method of Administration and Dosage").

Overdose

No cases of overdose have been reported.

Adverse reactions.

In individual cases, when using higher doses of Essentiale® N, gastrointestinal disorders (diarrhea) are possible.

In rare cases, hypersensitivity reactions, skin rash, itching, urticaria, and reactions at the injection site may occur.

Shelf life. 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 must not be used for dilution of the preparation.

Packaging. No. 5: 5 ml in an ampoule; 5 ampoules in a blister pack in a cardboard box.

Prescription status. Prescription only.

Manufacturer.

JSC "Galichfarm", Ukraine.

FAMAR HEALTH CARE SERVICES MADRID, S.A.U., Spain.

Manufacturer's address and location of its business activities.

6/8 Opryshkivska St., Lviv, 79024, Ukraine.

Avenida Leganes, 62, Alcorcon 28923, Madrid, Spain.

Marketing Authorization Holder. Opella HealthCare Ukraine LLC, Ukraine.

Address of the Marketing Authorization Holder.

48-50A Zhylianska St., Kyiv, 01033, Ukraine.