Carsil® forte

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT KARSIl® FORTE (CARSIL® FORTE)

Composition:

Active substance: dry extract of fruits of milk thistle;

1 capsule contains 163.6–225.0 mg of dry extract of milk thistle fruits (Silybi mariani fructus extractum siccum) (35–50:1), equivalent to 90 mg of silymarin, determined as silybin (HPLC);

Excipients: lactose monohydrate, microcrystalline cellulose, wheat starch, povidone, polysorbate 80, colloidal anhydrous silicon dioxide, mannite (E 421), crospovidone, sodium bicarbonate, magnesium stearate, hard gelatin capsule (gelatin, titanium dioxide (E 171), iron oxide (E 172)).

Pharmaceutical form. Hard capsules.

Main physicochemical properties: hard cylindrical gelatin capsules of light brown color. Contents of the capsule: powdered mass with agglomerates, from pale yellow to yellow-brown in color, with a weak specific odor.

Pharmacotherapeutic group.

Agents used in liver disorders, lipotropic agents. Hepatoprotective agents.

ATC code A05B A03.

Pharmacological properties.

Pharmacodynamics.

Silymarin is the active plant component of the medicinal product Carsil® Forte, obtained from the extract of fruits of milk thistle (Silybum marianum).

The drug has hepatoprotective and antitoxic effects. Carsil® Forte inhibits penetration of toxins into liver cells (demonstrated with toxins of the death cap mushroom) and induces physicochemical stabilization of hepatocyte cell membranes.

The antioxidant effect of Carsil® Forte is due to interaction of silibinin with free radicals in the liver, converting them into less toxic compounds. Thus, the process of lipid peroxidation is interrupted, preventing further destruction of cellular structures; toxins are neutralized via physiological pathways.

Carsil® Forte stimulates biosynthesis of structural and functional proteins and phospholipids (due to specific stimulation of RNA polymerase A) and accelerates regeneration of liver cells.

Clinical effects of Carsil® Forte are manifested as improvement in the general condition of patients with liver diseases and reduction of subjective complaints (such as weakness, feeling of heaviness in the right hypochondrium, loss of appetite, skin itching, vomiting). Laboratory parameters improve: decreased activity of transaminases, gamma-glutamyl transferase, alkaline phosphatase, and reduced plasma bilirubin levels. Long-term use of Carsil® Forte significantly increases survival rate in patients with liver cirrhosis.

Pharmacokinetics.

Absorption. After oral administration, silymarin is slowly and incompletely absorbed from the gastrointestinal tract. It undergoes enterohepatic circulation. Does not accumulate in the body.

Elimination. The elimination half-life of silymarin is 6.3 hours. It is excreted predominantly via bile in the form of glucuronides and sulfates.

Clinical characteristics.

Indications.

Hepatic toxicity: for supportive treatment of patients with chronic inflammatory liver diseases and liver cirrhosis.

Contraindications.

Hypersensitivity to the active substance or to any of the excipients. Acute poisoning of any etiology.

Interaction with other medicinal products and other forms of interaction.

When silimarins are used concomitantly with oral contraceptives and drugs used in estrogen replacement therapy, a reduction in the effectiveness of the latter may occur.

Silimarins may enhance the effects of medicinal products such as diazepam, alprazolam, lorazepam, ketoconazole, lovastatin, atorvastatin, and vinblastine due to its inhibitory effect on the cytochrome P450 system.

Due to inhibition of the cytochrome P450 system, silimarins enhance the action of antiallergic drugs (fexofenadine), anticoagulants (clopidogrel, warfarin).

Herbal products containing silimarins are widely used as hepatoprotectors in oncology practice concomitantly with cytostatics. Clinical studies indicate a low risk of potential pharmacokinetic interactions between silimarin, as an inhibitor of the CYP3A4 and UGT1A1 isoenzymes, and cytostatics which are substrates of these enzymes.

Special precautions for use.

Treatment with Karsil® Forte for liver diseases will be more effective if a proper diet is followed and alcohol consumption is avoided.

Due to the possible estrogen-like effect of silymarin, it should be used with caution in patients with hormonal disorders (endometriosis, uterine fibroids, breast, ovarian or uterine carcinoma, prostate carcinoma). In such cases, medical consultation is required.

The medicinal product contains wheat starch as an excipient. Wheat starch may contain gluten, but only in insignificant amounts, and is therefore considered safe for patients with celiac disease. Patients with wheat allergy (distinct from celiac disease) should not use this medicinal product.

The medicinal product contains lactose monohydrate. Patients with rare hereditary galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption should not take this product. Patients with sugar intolerance should consult their physician.

If signs of jaundice develop (skin color changing from light yellow to dark yellow, yellowing of the eye whites), medical consultation is necessary to adjust therapy.

Use during pregnancy or breastfeeding.

There are no data available on the safety and efficacy of using this medicinal product during pregnancy or breastfeeding; therefore, it should not be administered during these periods.

Ability to influence reaction speed when driving or operating machinery.

Karsil® Forte does not affect the ability to drive or operate machinery.

Patients with vestibular disorders should exercise caution when driving or working with machinery while using this medicinal product.

Method of Administration and Dosage.

Take capsules orally, swallowing with sufficient amount of liquid.

Adults and children aged 12 years and older

Treatment of severe liver damage begins with a dose of 1 capsule three times daily.

In cases of mild to moderate liver damage, take 1 capsule 1–2 times daily.

The treatment course should last at least 3 months.

Children

Do not use the drug in children under 12 years of age.

Overdose.

There are no reports of overdose. In case of accidental ingestion of a high dose, induce vomiting, perform gastric lavage, take activated charcoal, and if necessary, apply symptomatic treatment as prescribed by a physician.

Side effects

Rarely, in individuals with increased individual sensitivity, the following adverse reactions may occur.

Gastrointestinal tract: diarrhea due to enhanced liver and gallbladder function, nausea, dyspepsia, vomiting, decreased appetite, flatulence, heartburn.

Immune system: hypersensitivity reactions, including skin rash, pruritus, anaphylactic shock.

Auditory system: worsening of pre-existing vestibular disorders.

Respiratory system: dyspnea.

Urinary system: increased diuresis.

Skin and subcutaneous tissue: exacerbation of alopecia.

Adverse effects are transient and disappear after discontinuation of the drug without the need for special interventions.

Shelf life. 3 years.

Storage conditions.

Keep out of reach of children.

Store in the original packaging at a temperature not exceeding 25 °C.

Packaging.

6 capsules in a blister, 5 blisters in a cardboard box.

Availability. Over-the-counter (without prescription).

Manufacturer.

JSC "Sofarma".

Manufacturer's address and place of business.

16 Iliensko Shose Str., Sofia, 1220, Bulgaria.