Composition
1 capsule contains:
Active ingredient: phospholipids from soy beans (synonyms: EPL, essential phospholipids) - 300 mg, containing 80% of phosphatidylcholine - 240 mg;
Ingredients: solid fat - 57,000 mg, soybean oil - 36,000 mg, hydrogenated castor oil - 1,600 mg, ethanol 96% - 8,100 mg, ethylvaniline - 1,500 mg, 4-methoxyacetophenone - 0,800 mg, α-tocopherol - 0,750 mg.
Capsule contents: gelatin - 67.945 mg, purified water - 11.495 mg, titanium dioxide (E 171) - 0.830 mg, iron oxide yellow dye (E 172) - 2.075 mg, iron oxide black dye (E 172) - 0.332 mg, iron oxide red dye (E 172) - 0.198 mg, sodium lauryl sulfate
- 0.125 mg.
Pharmacological action
Pharmacotherapeutic group: hepatoprotective agent.
ATH code: A05C.
Pharmacological properties
Pharmacodynamics .
Essential phospholipids are basic elements of cell membrane structure and cell organelles. In liver diseases there is always damage of liver cell envelopes and their organelles that leads to disturbances in activity of associated enzymes and receptor systems, worsens functional activity of liver cells and decreases ability for regeneration.
Phospholipids, contained in the preparation Essenciale® forte H, correspond in their chemical structure to endogenous phospholipids, but exceed the activity of endogenous phospholipids due to their higher polyunsaturated (essential) fatty acids content. The incorporation of these high-energy molecules into damaged portions of hepatocyte cell membranes restores the integrity of hepatic cells and promotes their regeneration. Cis-double bonds of their polyunsaturated fatty acids prevent parallel arrangement of hydrocarbon chains in phospholipids of cell membranes, phospholipid structure of hepatocyte cell membranes
"loosens up", that results in increase of their fluidity and elasticity, improves a metabolism. The formed functional blocks increase activity of enzymes fixed on membranes and promote normal physiological way of most important metabolic processes.
Phospholipids contained in Essenciale® forte regulate lipoprotein metabolism, transferring neutral fats and cholesterol to the oxidation sites, mainly by increasing the ability of high-density lipoproteins to bind to cholesterol.
Thus, there is a normalizing effect on lipid and protein metabolism; on detoxifying liver function; on restoration and preservation of liver cellular structure and phospholipid-dependent enzyme systems, which ultimately prevents formation of connective tissue in the liver and promotes natural regeneration of liver cells. When phospholipids are excreted into the bile, the lithogenic index decreases and the bile stabilizes.
In patients with non-alcoholic fatty liver disease the use of essential phospholipids in controlled randomised clinical trials resulted in a significant reduction of steatosis.
In clinical and observational studies on the background of Essenciale® Forte H administration in patients with chronic liver disease, a relief of general condition and symptoms, such as increased fatigability/weakness, decreased appetite, pain or discomfort in the stomach, feeling of rapid satiety, feeling of fullness or heaviness after eating, bloating, nausea were observed. Meaningful improvement of symptoms has been observed in studies already after 4 weeks (30 days) of therapy.
The use of essential phospholipids in controlled and observational studies in patients with psoriasis resulted in regression of psoriatic rashes, reduction of the psoriasis prevalence and severity index (PASI). The addition of essential phospholipids to PUVA therapy resulted in faster remission while reducing the total dose of ultraviolet irradiation.
Pharmacokinetics
More than 90% of ingested phospholipids are absorbed in small intestine. Most of them are broken down by phospholipase A to 1-acyl-lysophosphatidylcholine, 50% of which are immediately reverse-acetylated to polyunsaturated phosphatidylcholine during the intestinal mucosal absorption process. This polyunsaturated phosphatidylcholine enters the bloodstream with the lymph and from there, mainly bound to the high-density lipoproteins, it enters the liver.
Pharmacokinetic studies in humans were carried out using radioactively labelled dilinoleoyl phosphatidylcholine (3H and 14C). The choline part was 3H-labelled and the linoleic acid residue had 14C as the tag.
The maximum concentration of 3H is reached 6-24 hours after administration and amounts to 19.9% of the administered dose. The elimination half-life of the choline component is 66 hours.
Maximal concentration of 14C is reached 4-12 hours after administration and makes up 27.9 % of prescribed dose. Half-life of this component is 32 hours. In the faeces, 2% of the administered dose of 3H and 4.5% of the administered dose of 14C are found, while in the urine, 6% of 3H and only minimal amounts of 14C are found.
Both isotopes are more than 90% absorbed in the intestine.
Indications
Chronic hepatitis, cirrhosis, fatty liver dystrophy of various etiologies, toxic liver damage, alcoholic hepatitis, liver dysfunction in other somatic diseases.
Toxicosis of pregnancy.
Prevention of recurrence of gallstones.
Psoriasis (as an adjuvant therapy).
Radiation syndrome.
Using during pregnancy and lactation
Pregnancy
It is not recommended to apply Essenciale® forte N during pregnancy without medical supervision. A sufficient number of trials are lacking.
Period of breast feeding
Up to now, no risks of usage of products containing soy during breastfeeding have been identified. Nevertheless, because of lack of adequate trials involving women during the breastfeeding period, it is not recommended to use Essenciale® Forte H during breastfeeding period.
Contraindications
Hypersensitivity to phosphatidylcholine, soybeans, soybeans or other ingredients of the preparation.
Children under 12 years of age (insufficient evidence).
Side effects
Essenciale® forte N is usually well tolerated by patients.
According to the data of World Health Organization (WHO) side effects are classified according to their frequency of development in the following way: very frequently (≥ 1/10), frequently (≥ 1/100, < 1/10), infrequently (≥ 1/1000, < 1/100), rarely (≥ 1/10000, < 1/1000) and very rarely (< 1/10000); frequency is unknown (frequency cannot be determined based on available data).
Gastrointestinal tract disorders
Frequency unknown: gastrointestinal discomfort, mild stools or diarrhoea.
Skin and subcutaneous tissue
Frequency unknown: allergic reactions (rash, exanthema, urticaria), itching.
Interaction .
Interaction of Essenciale® forte N with anticoagulants cannot be excluded. It is necessary to correct the dose of anticoagulants in co-administration with Essenciale® forte N.
How to take, course of treatment and dosage
Orally. The capsules should be swallowed in whole with enough water (about 1 cup). For teenagers older than 12 years of age and those weighing more than 43 kg, and for adults - 2 capsules 3 times a day with meal. The recommended course of therapy is 3 months. The course of treatment may be determined by the physician individually.
Overdose
Essenciale® forte N usage in doses exceeding the recommended ones can cause intensification of side effects.
Special directions
Because of its content of soybean oil, Essenciale® forte N may cause serious allergic reactions.
Patients should be informed that Essenciale® forte N administration is not a substitute for the necessity of avoiding the damaging effects of some substances on liver (e.g., alcohol).
Supportive therapy with phospholipids is only justified if subjective signs improve during treatment. Patients should be informed about the necessity of consulting a physician in case of worsening of symptoms or appearance of other unclear symptoms.
Effect on driving and operating ability
Essenciale® forte N does not influence on the ability to drive vehicles and mechanisms.
Form of production
Capsules 300 mg.
In 10 capsules in blister of PVC and aluminium foil, PVC/PTFE and aluminium foil or PVC/PE/PVC and aluminium foil.
Blister 3, 9 or 18 blisters together with instructions for use in a carton pack.
Pack 9 blisters with instructions for use in a carton box, 2 cartons in a carton box.
Storage conditions
Store at a temperature not exceeding 21 °C. Keep out of reach of children.
Shelf life
For capsules in blister of PVC and aluminum foil - 3 years.
For capsules in blister of PVC/PTFE and aluminium foil or PVC/PE/PVC and aluminium foil - 30 months.
Do not use after expiry date stated on the package.
Active substance
Phospholipids
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