Karsil Forte - instructions for use, doses, side effects, contraindications

Capsule contents: 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); Silica colloidal anhydrous dioxide (3.4 mg), mannitol (80.0 mg), crospovidone (14.0 mg), sodium pyrocarbonate (6.0 mg), magnesium stearate (3.7 mg).

excipients shell capsule: iron oxide the black (0.02%), iron oxide red (0.03%), titanium dioxide (0.6666%), iron oxide yellow (0.35%), gelatin (up to 100%).

Description:

Hard gelatin capsules № 0 light brown color.

The contents of the capsule are pulverulent masses from light yellow to yellow-brown in color with agglomerates.

Pharmacotherapeutic group:Hepatoprotective agent

ATX: & nbsp

A.05.B.A Preparations for the treatment of liver diseases

Pharmacodynamics:

Karsil Forte contains an extract of the milk thistle fruit, the main active ingredients of which is a mixture of 6 isomers of flavonolignanes (silymarin): silybinin A and B. iso-silibinin A and B. silidianin and silicristin. Of these, silibinin is the most active. The mechanism of hepatoprotective action has been thoroughly studied until the end, existing data prove the presence 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-Fe²⁺-AAD. 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, in as a result, the entry of hepatotoxic agents into gayatocytes. It is established, that the membrane-stabilizing action of silymarin is due to its competing interaction with receptors to the corresponding toxins on the membrane of hepatocytes. The effect of silymarin on membrane permeability is related to qualitative and quantitative changes in 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 silybin at a certain concentration is able to inhibit the synthesis of leukotriene B.t (leukotriene B4 / LTB₄ in isolated Kupfer cells of animals. Silymarin. silibin, 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 action of silybin is suppression of the formation of hydrogen peroxide. Clinically, the pharmacodynamic properties of silymarin are expressed in the improvement of subjective and objective symptoms and normalization of indicators of the functional state of the liver (traisinamases, gamma globulin, bilirubin).

Pharmacokinetics:

Suction

After application, silymarin is not completely absorbed from the gastrointestinal tract (GIT) (up to 23-47%). The maximum plasma concentration is achieved 4-6 hours after oral administration of a single dose.

Distribution

In studies with C¹⁴ labeled silibininom highest concentrations are established 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

The elimination half-life 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;
states 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).

Contraindications:

Hypersensitivity to the active or any of the excipients;
Children under 12 years of age;
Lactase insufficiency,galactosemia or malabsorbicin glucose / galactose syndrome (due to the presence of lactose).
Celiac disease (gluten enteropathy) (due to the presence of wheat starch).

Carefully:

Patients with hormonal disorders (endometriosis, uterine myoma, carcinoma of the breast, ovaries and uterus, prostate carcinoma) 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.

Dosing and Administration:

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 a day.

In more light and moderate cases, the dosage is 1 capsule 1-2 times a day.

For the prevention of chemical intoxication - 1-2 capsules a 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 effects:

The drug is well tolerated.

Adverse reactions are very rare and tend to be mild and transient.

Undesirable adverse reactions are classified by frequency and by system-organ class. The frequency but MedDRA is defined as follows: very often (> 1/10), often (> 1/100 to <1/10), infrequently (> 1/1 000 to <1/100). rarely (> 1/10 000 to <1/1 000). very rarely (<1/10 000). with an unknown frequency (based on existing data can not make an estimate).

Immune system disorders:

Very rarely: skin allergic reactions - itching. rash;

With unknown frequency: anaphylactic shock.

Hearing disorders and labyrinthine disorders:

Rarely: an increase in existing vestibular disorders.

Disorders from the digestive tract:

Rarely: diarrhea as a result of increased liver and gallbladder function.

With unknown frequency: nausea, vomiting, dyspepsia, decreased appetite, flatulence.

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.

Interaction:

Pharmacodynamic drug interactions

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 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, lovastine, vinblastine.

Effect on the ability to drive transp. cf. and fur:

The use of the drug in monotherapy does not affect the ability to drive vehicles and work with mechanisms.

Form release / dosage:

Capsules 90 mg.

Packaging:

6 capsules per blister of PVC film and aluminum foil.

For 5 blisters together with instructions for use in a cardboard box.

Storage conditions:

In dry the dark place at a temperature of no higher than 25 C.

Keep out of the reach of children!

Shelf life:

3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-000128

Date of registration:11.01.2011 / 12.01.2016

Expiration Date:Unlimited

The owner of the registration certificate:Sopharma, AOSopharma, AO Bulgaria

Manufacturer: & nbsp

SOPHARMA, AD Bulgaria

Representation: & nbspSOFARMA SA SOFARMA SA Bulgaria

Information update date: & nbsp14.12.2017

Illustrated instructions

Instructions

Karsil® Forte (Carsil® Forte)