Composition, form of production and packaging
? Capsules hard gelatinous, size в„–0, light brown color, contents of capsules - powdery mass from light yellow to yellow-brown color with agglomerates.
1 caps.
dry extract of the milk thistle fruit spotted 163.6-225 mg,
equivalent to 90 mg of silymarin
Auxiliary substances: lactose monohydrate - 38.2-7.5 mg, microcrystalline cellulose (type 101) - 38.2-7.5 mg, wheat starch - 15.5 mg, povidone K25 - 3.7 mg, polysorbate 80 - 3.7 mg, silicon dioxide colloidal anhydrous - 3.4 mg, mannitol - 80 mg, crospovidone - 14 mg, sodium hydrogen carbonate - 6 mg, magnesium stearate - 3.7 mg.
The composition of the capsule shell: iron oxide black - 0.02%, iron oxide red - 0.03%, titanium dioxide - 0.6666%, iron oxide yellow - 0.35%, gelatin - up to 100%.
6 pcs. - blisters (5) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
Hepatoprotective agent. Karsil В® Forte contains an extract of thistle fruit spotted, the main active ingredients of which is a mixture of 6 isomers of flavonolignanes (silymarin): silibinin A and B, iso-silibinin A and B, silidianin and silicristin. Of these, silibinin is the most active. The mechanism of hepatoprotective action is not fully understood, existing data prove the existence of several basic mechanisms of action.
Antioxidant action. Silymarin interacts with free radicals in the liver and converts them to less toxic compounds, interrupting the process of lipid peroxidation, prevents the destruction of cellular structures, binding to free radicals and regulating the intracellular content of glutathione. Depending on the concentration, it suppresses microsomal peroxidation caused by NADPH-Fe 2+ -ADP. Affects the enzyme systems associated with glutathione and superoxide dismutase. The components of silymarin suppress the peroxidation of linoleic acid catalyzed by lipoxygenase and protect the hepatic mitochondria and microsomes from the formation of lipid peroxides caused by various agents.
Membrano-stabilizing action. Silymarin stabilizes cell membranes and regulates their permeability, which prevents the entry of hepatotoxic agents into hepatocytes. It has been established that the membrane-stabilizing effect of silymarin is due to its competing interaction with receptors to corresponding toxins on the membrane of hepatocytes. The effect of silymarin on membrane permeability is associated with qualitative and quantitative changes in membrane lipids - cholesterol and phospholipids.
Silymarin stimulates regenerative 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 suppresses the transformation of star-shaped liver cells into myofibroblasts, the process responsible for the arrangement of collagen fibers.
Anti - inflammatory effect. Based on the results of experimental studies, it has been shown that silybinin at a certain concentration is able to inhibit the synthesis of leukotriene B4 (leukotriene B4 / LTB 4 ) in isolated Kupfer cells of animals. Silymarin, silibinin, silidianin and silicystrin inhibit the activity of lipoxygenase and prostaglandin synthase in vitro. In in vitro studies on human polymorphonuclear leukocytes, it has been shown that one of the mechanisms for realizing the anti-inflammatory effect of silybinin 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 (transaminases, gamma globulin, bilirubin).
PHARMACOKINETICS
Suction
After oral administration, silymarin is not completely absorbed from the digestive tract (up to 23-47%). C max in plasma is achieved 4-6 hours after oral administration of a single dose.
Distribution
In studies with 14 S 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. Metabolised in the liver by conjugation with sulfates and glucuronic acid. As metabolites in the bile, glucuronides and sulfates were detected.
Excretion
T 1/2 is 1-3 hours for unchanged silymarin and 6-8 hours for its metabolites. It is mainly derived from bile (about 80%) in the form of glucuronides and sulfates, to an insignificant extent (about 5%) by the kidneys in unchanged form. Do not cumulate.
INDICATIONS
As part of complex therapy:
- toxic liver damage;
- conditions after acute hepatitis;
- chronic hepatitis of non-viral etiology;
- steatosis of the liver (not alcoholic and alcoholic);
- cirrhosis of the liver;
- prevention of liver damage with prolonged use of drugs, alcohol, with chronic intoxication (including professional).
DOSING MODE
Capsules are taken orally by washing with plenty of water.
Adults and children over 12 years of age
Treatment of severe liver damage begins with a dose of 1 capsule 3 times / day. For more mild and moderate cases, the dose is 1 capsule 1-2 times per day.
For the prevention of chemical intoxication - 1-2 capsules per day. The course of treatment lasts not less than 3 months.
Children under 12 years of age
There is insufficient clinical data on the use in children.
SIDE EFFECT
The drug is well tolerated. Adverse reactions are very rare and tend to be mild and transient.
Undesirable adverse reactions are classified according to frequency and system-organ classes. The frequency according to MedDRA is determined as follows: very often (> 1/10), often (> 1/100 to <1/10), infrequently (> 1/1000 to <1/100), rarely (> 1/10 000 to <1/1000), very rarely (<1/10 000), 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.
From the side of the hearing organ and labyrinthine disturbances: rarely - strengthening of existing vestibular disorders.
From the digestive tract: rarely - diarrhea as a result of increased liver and gallbladder function; with an unknown frequency - nausea, vomiting, indigestion, decreased appetite, flatulence.
CONTRAINDICATIONS
- hypersensitivity to the active or any of the excipients;
- children under 12 years;
- lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome (due to the presence of lactose in the composition).
- celiac disease (gluten enteropathy) (due to the presence of wheat starch).
With caution: appoint patients with hormonal disorders (endometriosis, uterine fibroids, breast carcinoma, ovaries and uterus, carcinoma of the prostate gland) because of the possible manifestation of the estrogen-like effect of silymarin.
PREGNANCY AND LACTATION
It is not recommended to use the drug during pregnancy and during breastfeeding.
APPLICATION FOR CHILDREN
Contraindicated in children younger than 12 years.
SPECIAL INSTRUCTIONS
Impact on the ability to drive vehicles and mechanisms
The use of the drug as a monotherapy does not affect the ability to drive vehicles and work with mechanisms.
OVERDOSE
There is no evidence of an overdose of the drug.
Treatment for accidental high-dose: induction of vomiting, gastric lavage, the use of activated carbon, if necessary, symptomatic therapy.
DRUG INTERACTION
Pharmacodynamic drug interaction
Silymarin has no significant effect on the pharmacodynamics of other drugs.
With the joint use of silymarin with oral contraceptives and drugs that are used for hormone replacement therapy, it is possible to reduce the effects of the latter.
Pharmacokinetic drug interaction
Because 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, lovastatin, vinblastine.
TERMS OF RELEASE FROM PHARMACY
Without recipe.
TERMS AND CONDITIONS OF STORAGE
Keep in dry the dark place at a temperature of no higher than 25 В° C. Shelf life - 3 years.
Keep out of the reach of children!
Do not use after the expiration date printed on the package.
