Essenciale forte N, 300 mg capsules 30 pcs

Pharmacotherapeutic group: hepatoprotective agent.

ATX code: A05C.

Pharmacological properties

Pharmacodynamics

Essential phospholipids are the basic elements of the structure of cell membrane and cell organelles. In liver diseases there is always damage of liver cell envelopes and their organelles which leads to disorders of activity of associated enzymes and receptor systems, deterioration of functional activity of liver cells and decreased ability to regenerate.

Phospholipids contained in the preparation Essenciale ^® forte H correspond in their chemical structure to endogenous phospholipids, but exceed endogenous phospholipids in activity, due to the higher content of polyunsaturated (essential) fatty acids in them. The incorporation of these high-energy molecules into the damaged parts 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”, which causes increase of their fluidity and elasticity, improves metabolism. Formed functional blocks increase activity of enzymes fixed on membranes and promote normal, physiological course of the most important metabolic processes.

The phospholipids in Essenciale^® forte regulate lipoprotein metabolism by transporting neutral fats and cholesterol to the oxidation sites, mainly by increasing the ability of high-density lipoproteins to bind to cholesterol.

Thereby, there is a normalizing effect on lipid and protein metabolism; on the detoxifying function of the liver; on restoration and preservation of the liver cell structure and phospholipid-dependent enzyme systems; that eventually 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 nonalcoholic 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 on the background of Essenciale^® Forte H administration in patients with chronic liver disease, relief of general condition and symptoms such as increased fatigue/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 was noted in the studies 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 and reduction of the psoriasis prevalence and severity index (PASI). Adding essential phospholipids to PUVA therapy allowed faster remission while reducing the total dose of ultraviolet irradiation.

Pharmacokinetics

More than 90% of ingested phospholipids are absorbed in the small intestine. Most of them are broken down by phospholipase A to 1-acyl-lysophosphatidylcholine, 50% of which is immediately reverse-acetylated to polyunsaturated phosphatidylcholine during the absorption process in the intestinal mucosa. This polyunsaturated phosphatidylcholine enters the bloodstream with the lymph and from there, mainly in the form bound to high-density lipoproteins, reaches the liver.

Pharmacokinetics studies in humans were performed using radioactively labeled dilinoleoyl phosphatidylcholine (³H and ¹⁴C). The choline portion was ³H-labeled and the linoleic acid residue had ¹⁴C as a tag.

The maximum concentration of ³H is reached 6-24 hours after administration and is 19.9% of the administered 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. The half-life 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 detected; in the urine, 6% of ³H and only minimal amounts of ¹⁴C.

Both isotopes are more than 90% absorbed in the gut.

Indications

Active ingredient

Composition

1 capsule contains:

The active ingredient: phospholipids from soybeans (synonyms: EPL, essential phospholipids) – 300 mg, containing 80% phosphatidylcholine – 240 mg;

Additives: solid fat – 57,000 mg, soybean oil – 36,000 mg, hydrogenated castor oil – 1,600 mg, 96% ethanol – 8,100 mg, ethylvaniline – 1,500 mg, 4-methoxyacetophenone – 0,800 mg, α-tocopherol – 0,750 mg.

Composition of the capsule: 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.

How to take, the dosage

Interaction

Special Instructions

The drug Essenciale® fort H may cause severe allergic reactions because it contains soybean oil.

Patients should be informed that taking Essenciale® Forte H is not a substitute for avoiding the damaging effects of certain substances on the liver (e.g., alcohol).

Maintenance therapy with phospholipids is justified only if subjective signs of the condition improve during treatment. Patients should be advised to consult a physician if symptoms worsen or other unclear symptoms occur.

Influence on ability to drive and operate vehicles

The drug Essenciale ® forte N has no effect on the ability to drive vehicles or operate machinery.

Contraindications

Side effects

The drug Essenciale® forte H 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 common (≥1/10), common (≥1/100, < 1/10), infrequent (≥1/1000, < 1/100), rare (≥1/10000, < 1/1000), and very rare (< 1/10000); frequency unknown (frequency cannot be determined from available data).

Gastrointestinal tract side

Frequency unknown: gastric discomfort, mild stools, or diarrhea.

Skin and subcutaneous tissue

Frequency unknown: allergic reactions (rash, exanthema, urticaria), itching.

Overdose

Pregnancy use

Pregnancy

The use of the drug Essenciale® forte N during pregnancy is not recommended without medical supervision. There are not enough studies available.

Breastfeeding

Today, no risks have been identified with the use of products containing soy during breastfeeding. Nevertheless, due to absence of relevant trials with participation of women during the period of breastfeeding, the use of Essenciale® fort H is not recommended during breastfeeding.

Similarities