Heparsil

Geparsil is included in the category of medicines with hepatoprotective effect. It contains the active element silymarin, which is obtained from the fruits of spotted milk thistle. The substance is a mixture of 4 different isomers of flavonolignans: isosilibinin with silibinin, as well as silychristin with silidanin.

The drug has antitoxic and hepatoprotective activity. The antihepatotoxic effect of silymarin develops with its competitive interaction with the endings of relatively corresponding toxins inside the walls of hepatocytes. This leads to the development of a membrane-stabilizing effect. As a result, liver fibrosis and steatosis slow down.

Indications Heparsila

It is used in cases of liver intoxication, as well as for maintenance therapy in people with inflammation affecting the liver (chronic) or with liver cirrhosis.

Release form

The medicinal component is released in capsules - 12 pieces inside a cellular package, 5 or 10 packages inside a box. It can also be released inside containers - 30 or 50 capsules.

Pharmacodynamics

Silymarin has a cell-regulating and metabolic effect, inhibits the function of the 5-lipoxygenase pathway (especially the LTB4 component), and also stabilizes the permeability of the cell wall and is synthesized with reactive oxygen free radicals.

The active substance also stimulates phospholipid and protein binding (functional and structural proteins) inside the affected liver cells (stabilizing lipid metabolism) and normalizes the activity of their walls, and at the same time synthesizes free radicals (has an antioxidant effect), thereby protecting liver cells from negative influences, helping to restore them.

The effect of flavonoids is due to their antioxidant activity and ability to improve microcirculation. The clinical manifestation of these effects is an improvement in objective and subjective signs, as well as stabilization of liver function values (reduction in bilirubin, transaminase, and γ-globulin). As a result, health improves and symptoms associated with digestive activity are alleviated, and in people with impaired food absorption (due to liver damage), appetite improves.

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Pharmacokinetics

When taken orally, silymarin is absorbed at a low rate in the gastrointestinal tract. It participates in the processes of circulation in the liver and intestines. There is no accumulation of the substance.

It is subject to intensive distribution within the body. Tests conducted using 14C-labeled silibinin showed that the component is found in large quantities in the liver; its levels are very low in the lungs, kidneys, heart and other organs.

The metabolic processes of silymarin develop inside the liver by means of conjugation. Sulfates and glucuronides (metabolic components) are found inside the bile.

The half-life of silymarin is 6 hours. Excretion occurs mainly with bile (approximately 80%) in the form of sulfates with glucuronides. Only a small part of the drug is excreted with urine (approximately 5%).

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Dosing and administration

The medicine is taken orally, after meals. The capsules are swallowed whole, without chewing, with plain water.

It is necessary to take 1-2 capsules of the medicine 3 times a day (equivalent to 0.07-0.14 g of silymarin).

The duration of therapy is selected individually by the attending physician, taking into account the progression of the pathology, as well as its nature.

On average, the therapeutic course usually lasts 3 months.

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Use Heparsila during pregnancy

There is no information regarding the therapeutic efficacy and safety of Heparsil when used during breastfeeding or pregnancy.

Contraindications

Contraindicated for use in cases of severe intolerance to the components of the drug, as well as in cases of intoxication of various origins in the active phase.

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Side effects Heparsila

The medication is usually tolerated without complications. Only occasionally, with strong personal sensitivity, the patient may experience side effects:

• damage to the digestive function: vomiting, diarrhea, heartburn, nausea and dyspepsia;
• disorders affecting subcutaneous tissues and the epidermis: epidermal signs of allergy appear sporadically - rashes or itching, as well as potentiation of alopecia;
• disorders affecting the urinary system: potentiation of diuresis occurs occasionally;
• problems with the respiratory system: dyspnea appears occasionally;
• other symptoms: occasionally, there is a potentiation of existing vestibular disorders.

Negative manifestations are temporary and disappear after discontinuation of the drug, without the use of additional special measures.

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Overdose

If too much of the drug is consumed, vomiting should be induced, gastric lavage should be performed, and activated carbon should be given to the patient. Symptomatic treatment procedures should be performed if necessary.

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Interactions with other drugs

Combined use of the drug with oral contraception and medications used in estrogen replacement therapy may lead to a weakening of the therapeutic activity of the latter.

Since silymarin suppresses the activity of the hemoprotein P450 system, it causes potentiation of the action of individual drugs:

• anticoagulants (including warfarin with clopidogrel);
• anti-allergy medications (for example, fexofenadine);
• hypocholesterolemic agents (such as lovastatin);
• antipsychotics (diazepam and alprozolam with lorazepam);
• antifungals (including ketoconazole);
• certain agents used in carcinoma (for example, vinblastine).

Storage conditions

Geparsil should be stored in a place closed to small children. Temperature – not higher than 25°C.

Shelf life

Heparsil can be used for a period of 24 months from the date of sale of the drug.

Application for children

Experience with the use of the drug in children under 14 years of age is limited, which is why it is not prescribed to this age subgroup.

Analogues

The analogues of the drug are Darsil, Legalon and Karsil with Silibor, as well as Karsil Forte and Silibor Max.

Reviews

Geparsil receives good reviews from patients - the medication demonstrates high therapeutic effectiveness, helping to treat the disorders prescribed by the indications. The disadvantages include the high cost of the drug.