Karsil - instructions for use, dose, side effects, contraindications

Auxiliary substances of the core: lactose monohydrate (55.380 mg), wheat starch (55.380 mg), povidone (Colidon 25) (1.650 mg), microcrystalline cellulose (67,000 mg), magnesium stearate (2,500 mg) talc (7,000 mg), dextrose monohydrate (20,600 mg), sorbitol (4,130 mg), sodium hydrogen carbonate (1,360 mg).

Excipients shell: (0.840 mg), diethylphthalate (0.600 mg), sucrose (162.190 mg), acacia gum (1.562 mg), gelatin (0.860 mg), talc (26.718 mg), titanium dioxide (4.820 mg), macrogol (PEG 6000) ( 0.130 mg), Brown Opalux (sucrose, red iron oxide, iron oxide black, methyl and propyl parahydroxybenzoate, purified water) (2.250 mg), glycerol (0.030 mg).

Description:

The dragees are biconvex, coated with an outer layer of brown color and an inner layer of white color. View of the fracture: from brownish-yellow to light-brown in color.

Pharmacotherapeutic group:Hepatoprotective agent

ATX: & nbsp

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

Pharmacodynamics:

Karsil® belongs to the group of hepatoprotective medicines. Contains a dry extract of the milk thistle (equivalent to silymarin), which is a mixture of 4 isomers of flavonolignanes: silybinin, iso-silibinin, silidianin and silicristin.

The mechanism of action of the drug is still insufficiently elucidated. It has been established that hepatoprotective action of silymarin is caused by competitive interaction with toxins at the corresponding receptors in the membrane of hepatocytes, thus demonstrating membrane-stabilizing action.

Silymarin has metabolic and cell-regulatory effects, regulating the permeability of the cell membrane, suppressing the 5-lipoxygenase pathway, especially leukotriene B₄ (LTB₄), and also by binding to free reactive oxygen radicals.Stimulates the synthesis of proteins (structural and functional) and phospholipids in the affected hepatocytes, accelerating the regenerative processes. The action of flavonoids, to which silymarin belongs, is also conditioned by their antioxidant and microcirculatory-enhancing effects. Clinically, these effects are expressed in the improvement of subjective and objective symptoms and in the normalization of indicators of the functional state of the liver (transaminases, gammaglobulin, bilirubin). This leads to an improvement in the general condition, a reduction in complaints related to digestion, and in patients with reduced digestion due to liver disease, leads to increased appetite and weight gain.

Pharmacokinetics:

After oral administration, silymarin is slowly resorbed from the gastrointestinal tract. Undergoes intestinal hepatic circulation. Do not cumulate.

In the study of silybinin labeled with C¹⁴, the highest concentrations are found in the liver and very small amounts - in the kidneys, lungs, heart and other organs.

Metabolised in the liver by conjugation. In bile, glucuronides and sulfates were detected as metabolites.

The elimination half-life is 6 hours.It is excreted mainly with bile (about 80%) in the form of glucuronides and sulfates and to a small extent (about 5%) in the urine.

Indications:

Toxic liver damage;
Conditions after acute hepatitis;
Chronic hepatitis of non-viral etiology;
Steatosis of the liver (non-alcoholic and alcoholic);
In complex therapy of cirrhosis of the liver;
Prevention of liver damage with prolonged use of drugs, alcohol, with chronic intoxication (including professional).

Contraindications:

Hypersensitivity to the active ingredient or any of the excipients of the drug.

Children younger than 12 years of age.

Pregnancy and lactation:

It is not recommended to use the drug during pregnancy and breastfeeding

Dosing and Administration:

Dragee is taken orally, before eating, with plenty of water. The course of treatment lasts not less than 3 months.

Adults and children over 12 years of age:

treatment of severe liver damage begins with a daily dose of 420 mg (4 dragees 3 times a day).

In more light cases and as maintenance therapy - 1-2 tablets 3 times a day.

Prophylactically take 2-3 tablets a day.

Side effects:

The drug is well tolerated. Rarely the following side effects are observed:

from the gastrointestinal tract: nausea, dyspepsia, diarrhea.
from the skin: in single cases, skin allergic reactions are possible - itching, rashes, alopecia

Others: it is rare to observe an increase in existing vestibular disorders.

Side effects are transient and disappear after discontinuation of the drug

Overdose:

There is no evidence of an overdose of the drug.

If you accidentally take a high dose, you must induce vomiting, do a gastric lavage, applying Activated carbon and to carry out symptomatic treatment if necessary.

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

Silymarin can enhance the effects of such drugs as diazepam, alprazolam, ketoconazole, lovastatin, vinblastine because of its inhibitory effect on the cytochrome P 450 system.

Clinical studies show little risk of possible pharmacokinetic interactions of silymarin, as an inhibitor of the isoenzyme CYP3A4 and UGT1A1, and cytostatics, which are substrates of these enzymes.

Special instructions:

Be wary 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.

The drug contains wheat starch as an auxiliary substance, which can present a risk of deterioration in patients with celiac disease (gluten enteropathy), and glycerol, which can cause a headache or irritant effect on the gastric mucosa when applying high doses.

Form release / dosage:

Dragee 35 mg.

Packaging:

10 drops in a blister of PVC film and aluminum foil.

For 8 or 18 blisters together with instructions for use in a cardboard box.

Storage conditions:

In a dry and dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children!

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:П N014839 / 01

Date of registration:09.04.2008 / 01.06.2015

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® (Carsil®)