There is no data on overdose of the drug.
Treatment in case of accidental employment of high-dose: induction of vomiting, gastric lavage, administration of activated charcoal, and, if necessary, symptomatic therapy.
hypersensitivity to the active or any of the excipients,
lactase deficiency, galactosemia, or glucose/galactose malabsorption syndrome (due to the presence of lactose in the drug),
celiac disease (gluten enteropathy) — due to the presence of wheat starch in the preparation,
children under 12 years of age (insufficient clinical data available).
With caution: patients with hormonal disorders (endometriosis, uterine fibroids, breast, ovarian and uterine carcinoma, prostate carcinoma) - possible manifestation of the estrogen-like effect of silymarin.
Pharmacodynamic drug interactions
Silymarin does not significantly affect the pharmacodynamics of other drugs. With the combined use of silymarin with oral contraceptives and drugs that are used in hormone replacement therapy, it is possible to reduce the effects of the latter.
Pharmacokinetic drug interactions
Since silymarin has an inhibitory effect on the cytochrome P450 system, it is possible to increase the concentration in the blood plasma of such drugs as diazepam, alprazolam, ketoconazole, lovastin, vinblastine.
Solid gelatin capsules No. 0 are light brown in color.
The contents of the capsules - powdery mass from light yellow to yellow-brown color with agglomerates.
The drug is well tolerated.
Adverse reactions are very rare, and they are usually mild and transient.
Undesirable adverse reactions are classified by frequency and by system-organ class. Software frequency MedDRA It is defined as follows: very often (>1/10), often (>1/100 - <1/10), infrequently (>1/1000 — <1/100), rarely (>1/10000 — <1/1000), very rarely (<1/10000), with an unknown frequency (based on existing data, it is impossible to make an estimate).
From the immune system: very rarely-skin allergic reactions (itching, rash), with an unknown frequency-anaphylactic shock.
On the part of the organ of hearing and labyrinth disorders: rarely-an increase in existing vestibular disorders.
From the gastrointestinal tract: rarely-diarrhea as a result of increased liver and gallbladder function, with unknown frequency-nausea, vomiting, dyspepsia, decreased appetite, flatulence.
Without a prescription.
Influence on the ability to drive vehicles and work with mechanisms. The use of the drug in monotherapy does not affect the ability to drive vehicles and work with mechanisms.
As part of the complex therapy of the following conditions and diseases:
toxic liver damage,
States with a history of acute hepatitis,
chronic hepatitis of non-viral etiology,
liver steatosis (non-alcoholic and alcoholic),
cirrhosis of the liver,
prevention of liver damage with prolonged use of drugs, alcohol, chronic intoxication (including professional).
Karsil® Forte contains an extract of milk thistle fruit, the main active ingredients of which is a mixture of 6 isomers of flavonolignans (silymarin): silibinin A and B, isosilibinin A and B, silidianin and silicristin. Of these, silibinin is the most active. The mechanism of hepatoprotective action is not fully understood, the existing data prove the presence of several main mechanisms of action
Antioxidant effect. Silymarin interacts with free radicals in the liver and converts them into less toxic compounds, interrupting the process of lipid peroxidation, prevents the destruction of cellular structures, binds to free radicals and regulates the intracellular content of glutathione. Depending on the concentration, it suppresses microsomal peroxidation caused by NADPH-Fe2 - ADF. It affects the enzyme systems associated with glutathione and superoxide dismutase. Silymarin components inhibit linolenic acid peroxidation catalyzed by lipoxygenase and protect hepatic mitochondria and microsomes from the formation of lipid peroxides caused by various agents.
Membrane-stabilizing effect. Silymarin stabilizes cell membranes and regulates their permeability, which prevents the entry of hepatotoxic agents into hepatocytes. It was found that the membrane-stabilizing effect of silymarin is due to its competing interaction with the receptors for the corresponding toxins on the hepatocyte membrane. The effect of silymarin on membrane permeability is associated with qualitative and quantitative changes in membrane lipids — cholesterol and phospholipids.
Silymarin stimulates regeneration processes in the liver (restoration of damaged hepatocytes) as a result of activation of the synthesis of structural and functional proteins (ribosomal synthesis of RNA, protein and DNA) and phospholipids. It has been experimentally established that silymarin also inhibits the transformation of star-shaped liver cells into myofibroblasts, a process responsible for the location of collagen fibers.
Anti-inflammatory effect. According to the results of experimental studies, it is shown that silybin in a certain concentration is able to inhibit the synthesis of LT B4 (leukotriene B4/LTB4) in isolated Kupfer cells of animals. Silymarin, silybin, silydianin and silychristin inhibit the activity of lipoxygenase and prostaglandinas in vitro. In research in vitro In human polymorphonuclear leukocytes, it was shown that one of the mechanisms for the implementation of the anti-inflammatory effect of silybin is the suppression of the formation of hydrogen peroxide.
Clinically, the pharmacodynamic properties of silymarin are expressed in improving the subjective and objective symptoms and normalizing the indicators of the functional state of the liver (transaminase, gamma-globulin, bilirubin).
Suction. After oral administration, silymarin is not completely absorbed from the gastrointestinal tract (up to 23-47%). Plasma Cmax it is achieved in 4-6 hours after oral administration of a single dose.
Distribution. In studies with 14With C-labeled silibinin, the highest concentrations are found in the liver, lungs, stomach, and pancreas, and in small amounts in the kidneys, heart, and other organs.
Metabolism. Undergoes intestinal-hepatic recirculation. It is metabolized in the liver by conjugation with sulfates and glucuronic acid. Glucuronides and sulfates were found as metabolites in bile.
Output. T1/2 it is 1-3 hours for unchanged silymarin and 6-8 hours for its metabolites. It is excreted mainly with bile (about 80%) in the form of glucuronides and sulfates, to a small extent (about 5%) by the kidneys in unchanged form. It does not accumulate.
In a dry place, protected from light, at a temperature not exceeding 25 °C.
Keep out of reach of children.
Shelf life of the drug Karsil® Forte3 года.Do not use after the expiration date indicated on the package.
| Capsules | 1 caps. |
| active substance: | |
| milk thistle spotted fruit extract dry | 163.6-225 mg |
| (equivalent to 90 mg silymarin content) | |
| excipients: lactose monohydrate-38.2–7.5 mg, MCC (type 101) - 38.2–7.5 mg, wheat starch-15.5 mg, povidone K25-3.7 mg, polysorbate 80-3.7 mg, colloidal anhydrous silicon dioxide-3.4 mg, mannitol-80 mg, crospovidone-14 mg, sodium bicarbonate-6 mg, magnesium stearate-3.7 mg | |
| capsule: iron oxide black-0.02%, iron oxide red-0.03%, titanium dioxide-0.6666%, iron oxide yellow-0.35%, gelatin-up to 100% |
Capsules, 90 mg. In blisters made of PVC film and aluminum foil for 6 pcs., in a pack of cardboard 5 bl.
It is not recommended to use the drug during pregnancy and during breastfeeding.
Inside, with a sufficient amount of water.
Adults and children over 12 years of age: treatment of severe liver damage begins with a dose of 1 capsule. 3 times a day.
In more mild and moderate cases, the dosage is 1 capsule. 1-2 times a day.
For the prevention of chemical intoxication — 1-2 caps. per day.
The course of treatment — at least 3 months.
A05BA03 Silymarin
