Indications for use of Essentiale Forte are:

• chronic hepatitis; cirrhosis of the liver; fatty degeneration of the liver of various etiologies; toxic liver damage; alcoholic hepatitis; dysfunction of the liver in other somatic diseases;
• toxicosis of pregnancy;
• prevention of recurrence of gallstone formation;
• psoriasis (as an adjuvant therapy);
• radiation syndrome.

Pharmacodynamics:

Essential phospholipids are the main elements of the structure of the cell membrane and cell organelles. In liver diseases, there is always damage to the membranes of the liver cells and their organelles, which leads to disruptions in the activity of enzymes and receptor systems associated with them, impairment of the functional activity of liver cells and a decrease in the ability to regenerate.

The phospholipids that make up Essentiale® forte N correspond in their chemical structure to endogenous phospholipids, but surpass endogenous phospholipids in activity due to their higher content of PUFA (essential). The incorporation of these high-energy molecules into the damaged areas of the cell membranes of hepatocytes restores the integrity of the liver cells and promotes their regeneration. Cis-double bonds of PUFA prevent the parallel arrangement of hydrocarbon chains in the phospholipids of cell membranes, the phospholipid structure of the cell membranes of hepatocytes "loosens", which causes an increase in their fluidity and elasticity, improves metabolism. The resulting functional blocks increase the activity of enzymes fixed on the membranes and contribute to the normal physiological pathway of the most important metabolic processes.

The phospholipids that make up Essentiale® forte N regulate the metabolism of lipoproteins, transferring neutral fats and cholesterol to the sites of oxidation, mainly due to an increase in the ability of HDL to bind with cholesterol.

Thus, there is a normalizing effect on the metabolism of lipids and proteins; detoxification function of the liver; to restore and preserve the cellular structure of the liver and phospholipid-dependent enzyme systems, which ultimately prevents the formation of connective tissue in the liver and contributes to the natural restoration of liver cells.

When phospholipids are excreted into bile, the lithogenic index decreases and bile stabilizes.

In patients with non-alcoholic fatty liver disease, the use of essential phospholipids in controlled randomized clinical trials led to a significant decrease in the degree of steatosis. In clinical and observational studies on the background of the use of Essentiale® forte N in patients with chronic liver diseases, relief of the general condition and symptoms was observed, such as increased fatigue / weakness, decreased appetite, pain or discomfort in the abdomen, a feeling of fast satiety, a feeling of fullness or heaviness after eating, bloating, nausea. Significant improvement in symptoms was noted in studies as early as 4 weeks (30 days) of therapy.

The use of essential phospholipids in controlled and observational studies in patients with psoriasis led to regression of psoriatic eruptions, a decrease in the prevalence index and severity of psoriasis (PASI). The addition of essential phospholipids to PUVA therapy made it possible to achieve remission faster with a decrease in the total dose of UV radiation.

Pharmacokinetics:

More than 90% of the phospholipids taken orally are absorbed in the small intestine. Most of them are cleaved by phospholipase A to 1-acyl-lysophosphatidylcholine, 50% of which immediately undergoes reverse acetylation to polyunsaturated phosphatidylcholine during the absorption process in the intestinal mucosa. This polyunsaturated phosphatidylcholine enters the bloodstream with the lymph flow and from there, mainly in the form associated with HDL, enters the liver.

Pharmacokinetic studies in humans were performed using radioactively labeled dilinoleyl phosphatidylcholine (3H and 14C). The choline part was labeled with 3H, and the linoleic acid residue was labeled with 14C.

Cmax 3H is achieved 6-24 hours after administration and is 19.9% ​​of the prescribed dose. The T1 / 2 of the choline component is 66 hours.

Cmax 14C is achieved 4-12 hours after administration and is up to 27.9% of the prescribed dose. T1 / 2 of this component is 32 hours.

In feces, 2% of the administered dose of 3H and 4.5% of the administered dose of 14C are found, in urine - 6% of 3H and only a minimal amount of 14C.

Both isotopes are absorbed by more than 90% in the intestine.