Legalon^® 140 (Capsules) Instructions for Use

Marketing Authorization Holder

Meda Pharma, GmbH & Co. KG (Germany)

Manufactured By

Madaus GmbH (Germany)

ATC Code

A05BA03 (Silymarin)

Active Substance

Cardui mariae fructus (German DAB Pharmacopoeia)

Dosage Form

Legalon® 140

Capsules 140 mg: 20, 30, or 60 pcs.

Dosage Form, Packaging, and Composition

Capsules hard gelatin, size “1”, brown body and cap; the appearance of the capsule contents is a yellow powder.

Excipients: polysorbate 80, povidone, mannitol, sodium carboxymethyl starch (type A), magnesium stearate.

Capsule shell composition: gelatin, iron oxide red dye (E172), titanium dioxide (E171), sodium lauryl sulfate, iron oxide black dye (E172).

10 pcs. – blisters (2) – cardboard packs.
10 pcs. – blisters (3) – cardboard packs.
10 pcs. – blisters (6) – cardboard packs.

Clinical-Pharmacological Group

Hepatoprotective agent

Pharmacotherapeutic Group

Hepatoprotective agent

Pharmacological Action

Silybum marianum fruit dry extract is standardized by silymarin content.

Therapeutic action of silymarin

Detoxifying action. The antitoxic action of silymarin was identified during studies on various models of liver damage, for example, by the toxins phalloidin and alpha-amanitin from the death cap mushroom, lanthanides, carbon tetrachloride, galactosamine, thioacetamide, and the hepatotoxic virus FV3.

Cytoprotective action. Silymarin inhibits the penetration of some hepatotoxic substances (death cap poison) into the cell.

Antioxidant action. Due to its ability to bind free radicals, silymarin possesses antioxidant activity. The pathophysiological process of lipid peroxidation, responsible for the destruction of cell membranes, is interrupted or prevented. Silymarin acts not only as an antioxidant, reducing the degree of free radical generation, but also as an agent stimulating the regeneration of the glutathione system, one of the most important protective systems of the liver.

Regenerative action. Membrane-stabilizing action. Silymarin stimulates the synthesis of proteins and phospholipids. Cell membranes are stabilized. The body’s own proteins and phospholipids restore the damaged structures of the hepatocyte. Restorative capacity improves and liver cell regeneration accelerates. This effect is not observed in undamaged cells.

Hypocholesterolemic action. Silymarin normalizes hyperlipidemia, reduces the level of cholesterol and LDL in blood plasma.

Antifibrotic action. Silymarin inhibits collagenase and elastase in the liver, contributing to a reduction in the degree of fibrosis.

Anti-inflammatory action. A key feature of silymarin/silybinin is its ability to block the 5-lipoxygenase pathway and exert a suppressive effect on leukotriene formation.

Pharmacokinetics

The main component of silymarin is silybinin. When taken orally, silybinin dissolves quickly and enters the intestine, then 85% of it enters the liver via the portal vein system and is selectively distributed in hepatocytes, where it is metabolized by conjugation. Up to 80% of the active substance is excreted with bile during the “first pass” through the liver in conjugation with glucuronides and sulfates. Due to deconjugation in the intestine, up to 40% of the silybinin excreted with bile is reabsorbed and enters enterohepatic circulation, T_1/2 is 6.3 h. Bioavailability is 85%.

When taking Silybum marianum fruit extract in therapeutic doses (140 mg of silymarin 3 times/day), the level of silybinin in bile is the same after repeated doses and after a single dose. The results showed that silybinin does not accumulate in the body.

After multiple oral administrations of silymarin at 140 mg 3 times/day, a stable level of biliary excretion is achieved.

Indications

As part of complex therapy

• Chronic inflammatory liver diseases;
• Liver cirrhosis;
• Toxic liver damage (caused by substances toxic to the liver).

ICD codes

Dosage Regimen

Take the capsules orally, after meals, with a small amount of water.

The standard therapeutic dosage is one 140 mg capsule three times daily.

For long-term maintenance therapy, reduce the dosage to one capsule twice daily.

Swallow the capsules whole; do not chew or crush them.

Adhere strictly to the prescribed dosing schedule to maintain consistent therapeutic levels.

The duration of treatment is determined by the physician based on the specific liver condition and clinical response.

Do not exceed the recommended daily dose of three capsules.

For chronic inflammatory liver diseases, cirrhosis, and toxic liver damage, use only as part of a comprehensive therapeutic regimen.

If a dose is missed, take it as soon as remembered unless it is almost time for the next dose; in that case, continue with the regular schedule.

Adverse Reactions

The frequency of adverse effects is defined as follows: very common: (>1/10), common (<1/10 >1/100), uncommon (<1/100 >1/1000), rare (<1/1000 >1/10000), very rare (<1/10000).

Immune system disorders very rare – hypersensitivity reactions, rash.

Respiratory disorders very rare – dyspnea.

Gastrointestinal disorders rare – gastrointestinal disorders, soft stools.

Contraindications

• Hypersensitivity to the components of the drug (Silybum marianum fruits and/or other plants of the Asteraceae family, or to any of the excipients);
• Children under 12 years of age.

Use in Pregnancy and Lactation

Studies have not revealed any direct or indirect toxic effects on reproductive function.

As a precautionary measure, it is recommended to avoid use during pregnancy and breastfeeding.

Use in Hepatic Impairment

Used for liver diseases according to indications.

Pediatric Use

The drug in this dosage form is contraindicated in children under 12 years of age.

Geriatric Use

There are no specific restrictions for use in elderly patients.

Special Precautions

Effect on ability to drive vehicles and operate machinery

Does not affect the ability to drive vehicles or engage in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

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.