Esslial forte (Capsules) Instructions for Use

Marketing Authorization Holder

Atoll LLC (Russia)

Manufactured By

Ozon, LLC (Russia)

Contact Information

OZON LLC (Russia)

ATC Code

A05BA10 (Phospholipids)

Active Substance

Phospholipids (Grouping Name)

Dosage Form

Esslial forte

Capsules 300 mg: 5, 6, 10, 12, 15, 18, 20, 24, 25, 30, 36, 40, 45, 50, 54, 60, 90, or 100 pcs.

Dosage Form, Packaging, and Composition

Capsules hard gelatin, size No. 0, body and cap dark brown, opaque. The capsule contents are a yellow-brown or brown homogeneous mass of ointment-like to denser consistency with a characteristic odor.

* with an average L-α-phosphatidylcholine content of 76% – 228 mg.

Excipients: ethyl alcohol 95% – 4 mg.

Capsule body composition: iron oxide black – 0.53%, iron oxide red – 0.93%, iron oxide yellow – 0.2%, titanium dioxide – 0.3333%, gelatin – up to 100%.
Capsule cap composition: iron oxide black – 0.53%, iron oxide red – 0.93%, iron oxide yellow – 0.2%, titanium dioxide – 0.3333%, gelatin – up to 100%.

5 pcs. – contour cell packs (1) – cardboard packs.
5 pcs. – contour cell packs (2) – cardboard packs.
5 pcs. – contour cell packs (3) – cardboard packs.
5 pcs. – contour cell packs (4) – cardboard packs.
5 pcs. – contour cell packs (5) – cardboard packs.
5 pcs. – contour cell packs (6) – cardboard packs.
5 pcs. – contour cell packs (9) – cardboard packs.
5 pcs. – contour cell packs (10) – cardboard packs.
6 pcs. – contour cell packs (1) – cardboard packs.
6 pcs. – contour cell packs (2) – cardboard packs.
6 pcs. – contour cell packs (3) – cardboard packs.
6 pcs. – contour cell packs (4) – cardboard packs.
6 pcs. – contour cell packs (5) – cardboard packs.
6 pcs. – contour cell packs (6) – cardboard packs.
6 pcs. – contour cell packs (9) – cardboard packs.
6 pcs. – contour cell packs (10) – cardboard packs.
10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (2) – cardboard packs.
10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (4) – cardboard packs.
10 pcs. – contour cell packs (5) – cardboard packs.
10 pcs. – contour cell packs (6) – cardboard packs.
10 pcs. – contour cell packs (9) – cardboard packs.
10 pcs. – contour cell packs (10) – cardboard packs.

Clinical-Pharmacological Group

Hepatoprotective agent with immunomodulatory and antiviral action

Pharmacotherapeutic Group

Means for the treatment of diseases of the liver and biliary tract; agents for the treatment of liver diseases, lipotropic agents

Pharmacological Action

Essential phospholipids are the main elements of the structure of cell membranes and cellular organelles of the liver. In liver diseases, there is always damage to the membranes of liver cells and their organelles, which leads to disturbances in the activity of associated enzymes and receptor systems, deterioration of the functional activity of liver cells, and reduced ability to regenerate.

The phospholipids that are part of the drug Esslial forte 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 density of the phospholipid structure of hepatocyte cell membranes decreases, which leads to an increase in their fluidity and elasticity, and improves metabolism. The resulting functional blocks increase the activity of membrane-bound enzymes and promote the normal physiological pathway of the most important metabolic processes.

The phospholipids that are part of the drug Esslial forte regulate lipoprotein metabolism by transporting neutral fats and cholesterol to the sites of oxidation, mainly by increasing the ability of HDL to bind to cholesterol.

Thus, a normalizing effect on the metabolism of lipids and proteins is exerted; on the detoxification function of the liver and phospholipid-dependent enzyme systems; which ultimately prevents the formation of connective tissue in the liver and promotes the natural restoration of liver cells.

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

Pharmacokinetics

More than 90% of orally administered 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 reacetylated into polyunsaturated phosphatidylcholine during the absorption process in the intestinal mucosa.

This polyunsaturated phosphatidylcholine enters the bloodstream via the lymph flow, and from there, mainly bound to HDL, enters the liver.

Pharmacokinetic studies in humans were conducted using dilinoleoyl-phosphatidylcholine with a radioactive label (³H and ¹⁴C). The choline part was labeled with ³H, and the linoleic acid residue had ¹⁴C as a label. C_max of ³H is reached after 6-24 hours and is 19.9% of the administered dose. T_1/2 of the choline component is 66 hours. C_max of ¹⁴C is reached after 4-12 hours and is up to 27.9% of the administered dose. T_1/2 of this component is 32 hours.

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

Indications

• Chronic hepatitis;
• Liver cirrhosis;
• Fatty liver dystrophy of various etiologies;
• Toxic liver damage;
• Alcoholic hepatitis;
• Liver function disorders in other somatic diseases;
• Pregnancy toxemia;
• Prevention of recurrence of gallstone formation;
• Psoriasis (as an auxiliary therapy);
• Radiation syndrome.

ICD codes

Dosage Regimen

Administer orally.

Swallow capsules whole with a full glass of water.

For adults and adolescents over 12 years of age weighing more than 43 kg, the standard dosage is 2 capsules three times daily.

Take doses with meals to improve absorption.

Initiate therapy based on the diagnosed liver condition, including chronic hepatitis, cirrhosis, fatty liver dystrophy, and toxic liver damage.

For psoriasis, use as an adjuvant therapy.

For prevention of gallstone recurrence, use as directed.

Continue treatment for the duration prescribed; therapy duration is often not limited and may be long-term.

Do not administer to children under 12 years of age due to insufficient clinical data.

Do not exceed the recommended daily dose of 6 capsules.

If a dose is missed, take it as soon as remembered unless it is nearly time for the next dose; do not double the dose.

Discontinue use and consult a physician if severe gastrointestinal discomfort or allergic reactions occur.

Adverse Reactions

The drug Esslial forte is usually well tolerated by patients. To assess the frequency of side effects, the following definitions are used: very common (> 1/10), common (>1/100-<1/10), uncommon (>1/1000 – <1/100), rare (>1/10 000-<1/1000), very rare (<1/10 000), unknown frequency (cannot be estimated from the available data).

Gastrointestinal rare – discomfort in the epigastric region, loose stools, nausea, gastralgia.

Allergic reactions very rare – rash, exanthema, urticaria; unknown frequency – itching.

Contraindications

• Individual intolerance to phosphatidylcholine or auxiliary components of the drug;
• Soy intolerance;
• Children under 12 years of age (lack of sufficient evidence base).

Use in Pregnancy and Lactation

Use during pregnancy is possible if indicated.

Special Precautions

Effect on ability to drive vehicles and mechanisms

No effect.

Overdose

No information.

Drug Interactions

No information.

Storage Conditions

The drug should be stored out of the reach of children, protected from light, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years.

Dispensing Status

The drug is available without a prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.