Dosage form
No. 1 brown opaque hard gelatin capsules containing a yellowish-brown oily pasty mass.
Compound
1 capsule contains:
active ingredient: soybean phospholipids containing 76% (3-sn-phosphatidyl)-choline (synonyms: EPL, essential phospholipids) - 300 mg;
auxiliary ingredients: solid fat - 57.000 mg, soybean oil - 36.000 mg, hydrogenated castor oil - 1.600 mg, ethanol 96% - 8.100 mg, ethylvanillin - 1.500 mg, 4-methoxyacetophenone - 0.800 mg, α-tocopherol - 0.750 mg.
Capsule composition: gelatin - 67.945 mg, purified water - 11.495 mg, titanium dioxide (E 171) - 0.830 mg, iron dye yellow oxide (E 172) - 2.075 mg, iron dye black oxide (E 172) - 0.332 mg, iron dye red oxide (E 172) - 0.198 mg, sodium lauryl sulfate - 0.125 mg.
Pharmacotherapeutic group
hepatoprotective agent
Pharmacodynamics
Essential phospholipids are the main structural elements of the cell membrane and cell organelles. In liver diseases, there is always damage to the membranes of liver cells and their organelles, which leads to disruption of the activity of enzymes and receptor systems associated with them, a deterioration in the functional activity of liver cells and a decrease in the ability to regenerate.
Phospholipids, which are part of Essentiale® forte N, correspond in their chemical structure to endogenous phospholipids, but surpass endogenous phospholipids in activity due to their higher content of polyunsaturated (essential) fatty acids. The incorporation of these high-energy molecules into damaged areas of hepatocyte cell membranes restores the integrity of liver cells and promotes their regeneration. The cis-double bonds of their polyunsaturated fatty acids prevent the parallel arrangement of hydrocarbon chains in the phospholipids of cell membranes, the phospholipid structure of the cell membranes of hepatocytes is “loosened”, which leads to an increase in their fluidity and elasticity, and 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.
Phospholipids, which are part of Essentiale® Forte, regulate the metabolism of lipoproteins, transferring neutral fats and cholesterol to the sites of oxidation, mainly by increasing the ability of high density lipoproteins to bind to cholesterol.
Thus, there is a normalizing effect on the metabolism of lipids and proteins; on the 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 promotes the natural recovery of liver cells.
With the excretion of phospholipids 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 reduction in the degree of steatosis.
In clinical and observational studies, against the background of the use of Essentiale® Forte N in patients with chronic liver diseases, there was an improvement in the general condition and symptoms, such as increased fatigue / weakness, decreased appetite, pain or discomfort in the abdomen, a feeling of early satiety, a feeling of fullness or heaviness after food, bloating, nausea. Significant improvement in symptoms was seen 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 a regression of psoriatic rashes, a decrease in the psoriasis prevalence and severity index (PASI). The addition of essential phospholipids to PUVA therapy made it possible to achieve faster remission while reducing the total dose of ultraviolet radiation.
Pharmacokinetics
More than 90% of ingested phospholipids 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 into polyunsaturated phosphatidylcholine during the process of absorption in the intestinal mucosa. This polyunsaturated phosphatidylcholine enters the bloodstream with the lymph flow and from there, mainly in the form associated with high-density lipoproteins, enters the liver.
Pharmacokinetic studies in humans have been performed with radioactively labeled dilinoleyl phosphatidylcholine (3H and 14C). The choline moiety was labeled with 3H and the linoleic acid moiety was labeled with 14C.
The maximum concentration of 3H is reached 6-24 hours after administration and is 19.9% ​​of the prescribed dose. The half-life of the choline component is 66 hours.
The maximum concentration of 14C is reached 4-12 hours after administration and is up to 27.9% of the prescribed dose. half-lifethe duration of this component is 32 hours.
In the feces, 2% of the administered dose of 3H and 4.5% of the administered dose of 14C are found, in the urine - 6% of the 3H and only a minimal amount of 14C.
Both isotopes are more than 90% absorbed in the intestine.
Indications
- Chronic hepatitis, cirrhosis of the liver, fatty degeneration of the liver of various etiologies, toxic liver damage, alcoholic hepatitis, liver dysfunction in other somatic diseases.
- Toxicosis of pregnancy.
- Prevention of recurrence of the formation of gallstones.
- Psoriasis (as an adjuvant therapy).
- Radiation syndrome.
Contraindications
- Hypersensitivity to phosphatidylcholine, soy, soybeans or other ingredients of the drug.
- Children under 12 years of age (lack of sufficient evidence base).
Use during pregnancy and during breastfeeding
Pregnancy
The use of Essentiale® forte N during pregnancy is not recommended without medical supervision. Not enough research is available.
breastfeeding period
To date, no risks have been identified when using products containing soy during breastfeeding. However, due to the lack of relevant studies involving women during breastfeeding, the use of Essentiale® forte N during breastfeeding is not recommended.
Dosage and administration
inside.
Capsules should be swallowed whole with plenty of water (about 1 cup).
For adolescents over 12 years old and weighing more than 43 kg, as well as for adults, Essentiale® forte N is recommended to take 2 capsules - 3 times a day with meals.
The recommended course of therapy is 3 months.
The course can be individually determined by the doctor.
Side effects
The drug Essentiale® forte N is usually well tolerated by patients.
According to the World Health Organization (WHO), side effects are classified according to their frequency of development as follows: very often (≥ 1/10), often (≥1/100, <1/10), infrequently (≥1/1000, < 1/100), rare (≥1/10000, <1/1000) and very rare (<1/10000); frequency unknown (frequency cannot be determined from the available data).
From the gastrointestinal tract
Frequency unknown: stomach discomfort, soft stools or diarrhea.
From the skin and subcutaneous tissues
Frequency unknown: allergic reactions (rash, exanthema, urticaria), itching.
Overdose
The use of the drug Essentiale® forte N in doses exceeding the recommended ones may lead to an increase in side effects.
drug interaction
The interaction of the drug Essentiale® forte N with anticoagulants cannot be excluded. It is necessary to adjust the dose of anticoagulants when used together with Essentiale® forte N.
special instructions
The drug Essentiale® forte N can cause severe allergic reactions, as it contains soybean oil.
Patients should be informed that taking Essentiale® forte N does not replace the need to avoid the damaging effects of certain substances on the liver (for example, alcohol).
Maintenance therapy with phospholipids is justified only if the subjective signs of the condition improve during treatment. Patients should be informed of the need to consult a doctor if symptoms worsen or other unclear symptoms appear.
Influence on the ability to drive vehicles and mechanisms
The drug Essentiale® forte N does not affect the ability to drive vehicles or mechanisms.
Storage temperature
2℃ to 21℃
Special storage conditions
At a temperature not higher than +21 °