Heptor instructions for use 400 tenge tablets. Heptor: instructions for use of hepatoprotector. Administration by intramuscular route

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Pharmacological properties

Pharmacodynamics
Ademetionine belongs to the group of hepatoprotectors and also has antidepressant activity. It has choleretic and cholekinetic effects, has detoxification, regenerating, antioxidant, antifibrosing and neuroprotective properties.
Replenishes the deficiency of S-adenosyl-L-methionine (ademetionine) and stimulates its production in the body; it is found in all environments of the body. The highest concentration of ademetionine was observed in the liver and brain. Plays a key role in the metabolic processes of the body, takes part in important biochemical reactions: transmethylation, transsulfurization, transamination. In transmethylation reactions, ademetionine donates a methyl group for the synthesis of cell membrane phospholipids, neurotransmitters, nucleic acids, proteins, hormones, etc. In transsulfuration reactions, ademetionine is a precursor of cysteine, taurine, glutathione (providing a redox mechanism of cellular detoxification), coenzyme A (included in biochemical reactions of the tricarboxylic acid cycle and replenishes the energy potential of the cell).
Increases the content of glutamine in the liver, cysteine ​​and taurine in plasma; reduces the content of methionine in serum, normalizing metabolic reactions in the liver. After decarboxylation, it participates in aminopropylation reactions as a precursor of polyamines - putrescine (stimulator of cell regeneration and hepatocyte proliferation), spermidine and spermine, which are part of the ribosome structure, which reduces the risk of fibrosis. Has a choleretic effect. Ademetionine normalizes the synthesis of endogenous phosphatidylcholine in hepatocytes, which increases membrane fluidity and polarization. This improves the function of transport systems associated with hepatocyte membranes bile acids and promotes the passage of bile acids into the biliary tract.
Effective for intralobular cholestasis (impaired synthesis and flow of bile). Ademetionine reduces the toxicity of bile acids in hepatocytes by conjugating and sulfating them. Conjugation with taurine increases the solubility of bile acids and their removal from the hepatocyte. The process of sulfation of bile acids facilitates their elimination by the kidneys, facilitates their passage through the hepatocyte membrane and excretion in the bile. In addition, sulfated bile acids themselves additionally protect liver cell membranes from the toxic effects of non-sulfated bile acids (present in high concentrations in hepatocytes during intrahepatic cholestasis). In patients with diffuse liver diseases (cirrhosis, hepatitis) with intrahepatic cholestasis syndrome, ademetionine reduces the severity of skin itching and changes biochemical parameters, incl. concentration of direct bilirubin, alkaline phosphatase activity, aminotransferases, etc. The choleretic and hepatoprotective effect lasts up to 3 months after cessation of treatment. It has been shown to be effective against hepatopathy caused by various hepatotoxic drugs. Antidepressant activity appears gradually, starting from the end of the first week of treatment, and stabilizes within 2 weeks of treatment.
A number of studies have confirmed the effectiveness of ademetionine in the treatment of increased fatigue in patients with chronic diseases liver. A pooled analysis of data obtained in patients with symptoms of fatigue before treatment showed the effect of treatment with ademetionine in reducing symptoms of fatigue in combination with a number of other symptoms, such as depression, icterus skin and mucous membranes, malaise and itchy skin. Treatment with ademetionine significantly improved mood in patients with alcoholic liver disease, who simultaneously achieved a positive response to symptoms of increased fatigue. In addition, in patients with alcoholic liver disease and non-alcoholic fatty liver disease who achieved a response to treatment with ademetionine in terms of symptoms of increased fatigue, there was also a significant reduction in symptoms such as icterus of the skin and mucous membranes, malaise and itching.

Pharmacokinetics

The tablets are film-coated, dissolving only in the intestines, due to which ademetionine is released into the intestines. duodenum.
Suction
Bioavailability when taken orally is 5%, increases when taken on an empty stomach. The maximum concentrations (Cmax) of ademetionine in plasma are dose-dependent and are 0.5-1 mg/l 3-5 hours after a single oral dose of 400 to 1000 mg. Cmax of ademetionine in plasma decreases to the initial level within 24 hours.
Distribution
The connection with blood plasma proteins is insignificant, amounts to< 5 %.
Penetrates the blood-brain barrier. There is a significant increase in the concentration of ademetionine in the cerebrospinal fluid.
Metabolism
Metabolized in the liver. The process of formation, consumption and re-formation of ademetionine is called the ademetionine cycle. In the first step of this cycle, ademetionine-dependent methylases use ademetionine as a substrate to produce S-adenosylhomocysteine, which is then hydrolyzed to homocysteine ​​and adenosine by S-adenosylhomocysteine ​​hydrolase. Homocysteine, in turn, undergoes reverse transformation to methionine by transfer of a methyl group from 5-methyltetrahydrofolate. Eventually, methionine can be converted to ademetionine, completing the cycle.
Removal
Half-life (T½) - 1.5 hours. Excreted by the kidneys. In studies of healthy volunteers, ingestion of labeled (methyl 14 C) S-adenosyl-L-methionine showed 15.5 ± 1.5% radioactivity in urine after 48 hours and 23.5 ± 3.5% in feces. radioactivity after 72 hours. Thus, about 60% was deposited.

Indications for use

• Intrahepatic cholestasis in pre-cirrhotic and cirrhotic conditions, which can be observed in the following diseases:
  • fatty liver;
  • chronic hepatitis;
  • toxic liver damage of various etiologies, including alcoholic, viral, medicinal (antibiotics; antitumor, antituberculosis and antiviral drugs, tricyclic antidepressants, oral contraceptives);
  • chronic acalculous cholecystitis;
  • cholangitis;
  • cirrhosis of the liver;
  • encephalopathy, incl. associated with liver failure (alcohol, etc.).
• Intrahepatic cholestasis in pregnant women.
• Symptoms of depression.
• Increased fatigue in chronic liver diseases.

Contraindications

Pregnancy (1st trimester) and period breastfeeding(use is possible only if the potential benefit to the mother outweighs the possible risk to the fetus or child).
Concomitant use with selective serotonin reuptake inhibitors (SSRIs), tricyclic antidepressants (such as clomipramine), and drugs plant origin and drugs containing tryptophan (see section “Interaction with other drugs”).
Elderly age.
Kidney failure.

Use during pregnancy and breastfeeding

Directions for use and doses

The recommended dose is 10-25 mg/kg/day orally.
Intrahepatic cholestasis/increased fatigue in chronic liver diseases
Depression
The dose ranges from 800 mg/day to 1600 mg/day.
The duration of therapy is determined by the doctor.
Therapy with Heptral® can be started with intravenous or intramuscular administration, followed by the use of Heptral® in tablet form, or immediately with the use of Heptral® in tablet form.
Elderly patients
Clinical experience The use of the drug Heptral® did not reveal any differences in its effectiveness in elderly patients and younger patients. However, given the high likelihood of existing liver, kidney or cardiac dysfunction, other concomitant pathology or concomitant therapy with other drugs, the dose of Heptral® in elderly patients should be selected with caution, starting the use of the drug from the lower limit of the dose range.
Kidney failure
There are limited clinical data on the use of Heptral® in patients with renal failure Therefore, it is recommended to exercise caution when using Heptral® in such patients.
Liver failure
The pharmacokinetic parameters of ademetionine are similar in healthy volunteers and in patients with chronic liver diseases.
Children
The use of Heptral® in children is contraindicated (efficacy and safety have not been established).

Impact on the ability to drive a car and operate machinery

Some patients may experience dizziness while taking Heptral®. It is not recommended to drive a car or operate machinery while taking the drug until the patient is confident that the therapy does not affect the ability to engage in these types of activities.

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Registration Certificate Holder

Heptor is a medicine that is intended for effective treatment patients with various pathologies. The drug is available in the form of tablets and lyophilisate for preparing a solution. Has a hepatoprotective effect.

In patients, the resistance of the liver to the development of pathological diseases increases. Detoxifying properties are additionally enhanced. The drug is embedded in the membrane of hepatocytes, stabilizing their structure.

Composition and release form

The lyophilisate is intended for preparing a solution. The active component is ademetionine 1,4-butane disulfonate in an amount of 760 mg. This dosage corresponds to an ademetionine concentration of 400 mg. For the drug solution, you can use L-lysine in the form of monohydrate, sodium hydroxide.

The manufacturer also offers the medicine in tablet form. The main potent substance is ademetionine in the form of S-adenosylmethionine in an amount of 400 mg. Auxiliary components are crospovidin, microcrystalline cellulose, mannitol, magnesium stearate.

The tablet shell is made from copovidone, polyethylene glycol, hydroxypropyl methylcellulose, acrylic. She quickly dissolves into gastrointestinal tract and releases the active component. Price of Heptor tablets 50 pcs. - 1200 rubles.

Pharmacological properties

Heptor is a hepatoprotector that has antidepressant activity. The medicine additionally has regenerating, detoxifying, antioxidant, antifibrosing and neuroprotective properties.

After administration, ademetionine begins to act actively. It gradually invades the biochemical processes of the body. There is intense stimulation of the production of endogenous ademetionine. The main component is a biological substance that can be found in the body or soft tissues.

The molecule of this component is involved in many biological reactions. This is a kind of methyl group donor. It is a precursor to physiological antitoxic agents. The drug is released in the duodenum. The official instructions for use of Heptor do not contain confirmed information about the pharmacokinetic properties of the drug.

Indications for use

The drug Heptor is prescribed to patients as a primary or complex therapy. Indications for use are the following condition:

• cirrhosis of the liver;
• intrahepatic cholestasis;
• cirrhotic conditions.

Heptor is prescribed to patients diagnosed with hepatitis of various origins. It can be toxic, medicinal and viral. Hepatitis can occur during long-term treatment with antibiotic, antituberculosis and antitumor medications. This list includes contraceptives and tricyclic antidepressants.

The drug Heptor is indicated for patients in whom encephalopathic secondary genesis progresses in the body. And also for patients with withdrawal syndrome, depressive states and disorders.

Instructions for use

Heptor is a drug that is intended exclusively for oral administration. The tablets should not be split, chewed or crushed. They are swallowed whole and washed down with plenty of water. The tablet is removed from the package only before administration. Before starting therapy, you should read the instructions for use.

To get the most positive result, you need to take Heptor between main meals. The duration of therapy and dosage of the drug are determined by the doctor, who necessarily takes into account the patient’s condition, as well as the use of additional drugs.

As a prophylaxis or maintenance therapy, adults are prescribed 2-4 tablets per day. This norm is divided into several main parts. The course of treatment is 1 month. According to the doctor's indications, an additional appointment may be prescribed after a short break.

It is strictly forbidden to take tablets before bed or late in the evening. This recommendation is due to the fact that the drug has a tonic effect, so patients may have problems sleeping.

At intravenous administration The average dosage of the drug is no more than 4 ampoules or 40 ml per day. If the patient is in a coma, then the patient is given up to 8 ampoules in the form of injections. When prescribing a dosage, the doctor takes into account the severity of the condition. Before administering the injection, the ampoules are dissolved in 500 ml of infusion solution. No more than 6 ampoules are allowed to be diluted in this quantity.

Side effects

In most cases, the drug Heptor is well tolerated by patients. Some patients experienced the following side effects:

• discomfort in the gastrointestinal tract;
• allergic reaction;
• skin rash.

In rare cases, nausea or vomiting may occur. Such symptoms are short-lived and do not require special treatment with the help of medications. They may disappear if the patient's dosage is reduced or the rate of administration of the drug is adjusted.

Discomfort or pain in the gastrointestinal tract is directly related to the fact that active substance can increase the pH balance towards increased acidity. This condition does not require treatment. The discomfort goes away on its own, without taking medications.

Contraindications

The medicine Heptor is not prescribed to patients if they have a history of a negative reaction to the main or additional components contained in the composition. It is important to exercise caution when prescribing the drug to people who have liver cirrhosis with hyperazotemia.

In this case, therapy is carried out only under the strict control and supervision of the attending physician. Professionals should regularly monitor plasma nitrogen levels. Contraindication is pregnancy in the first and second trimester.

After 30 weeks of pregnancy, the doctor may decide to prescribe medication. But the woman must regularly stay in the hospital. Doctors will monitor her condition and also monitor important indicators of fetal development. During lactation, you can take the drug Heptor only after consulting a doctor.

In most cases, the doctor prohibits continued breastfeeding in favor of treating the mother. There is no experience in prescribing to children, so the medicine is not used in pediatric practice.

Overdose and compatibility

IN medical practice There are no official data on cases of intoxication resulting from an overdose of L-carnitine and L-aspartate. These are safe substances that do not cause serious harm to health. But patients do not need to exceed the established daily norm. In case of overdose, it is recommended to consult a doctor who will prescribe symptomatic treatment.

Scientists have not conducted studies to determine interactions with other medications. Because of this, it is not recommended to use the drug in complex therapy without consultation or full examination. Only in rare cases can specialists prescribe a medicine containing complex treatment, if there is evidence for this.

Analogs

The following can be distinguished effective analogues Heptora:

1. Karsil. This drug is prescribed to patients with liver disease. It reliably protects the organ from toxins that damage the nuclei as a result of alcoholism, cirrhosis, and hepatitis. At correct use lipid metabolism is adjusted.
2. Holosas. The drug has a choleretic and hepatoprotective effect on the body. Holosas helps maintain normal hepatocyte function and is an excellent means of preventing inflammatory processes liver. It has a diuretic effect and enhances intestinal motility.
3. Heptral. This is a proven medicine that was developed to restore the structure of liver tissue. It has a pronounced antioxidant, regenerating, and neuroprotective effect. It is prescribed to patients when dystrophic changes in liver tissue.
4. Galstena. This is a complex homeopathic medicine. It has a hepatoprotective effect, performs choleretic and cholekinetic properties, and has an antispasmodic and anti-inflammatory effect on the hepatobiliary system.
5. Ursosan. The drug promotes effective reduction cholesterol production. These processes often occur in the liver as a result pathological processes. With regular use, cholesterol stones dissolve. The main indications are liver diseases and cholestatic diseases.
6. Ursodes. This is a hepatoprotective medicine that affects the body choleretic effect. A decrease in synthesis occurs inside the liver, and the concentration of bile in the intestine decreases. Thanks to this drug, the formation and secretion of secretions begins to be stimulated. It reduces lithogenicity, increases acidity and lipase activity.

All drugs that are included in the list of analogues have an immunomodulatory effect on the body. In the liver, the expression of some antigens in the hepatocyte membrane decreases.

The presented medications dissolve cholesterol stones inside the gallbladder, stop the development of biliary cirrhosis, primary sclerosing cholangitis, cystic fibrosis, non-alcoholic steatohepatitis, and alcoholic liver disease.

The medicine should be taken only after complex diagnostics and examinations to avoid serious complications and negative consequences.

Hepatoprotective agents are used in the treatment of many diseases, as well as prophylactic drugs. They help the main cleansing organ of the body to work correctly, performing all the functions assigned to it. One of these drugs is Heptor (400 mg). The instructions for use will tell you why and how the medicine is used.

In what form is the medicine available?

Diseases, whatever they may be, cause a person to feel depressed and depressed. Therefore, some drugs also have antidepressant properties in their functionality. They play a dual role - they help not only fight the disease, but also relieve nervous tension, calm down. The instructions for use for the drug "Heptor" (400 mg) describe precisely this property.

Only the attending physician chooses the form of the drug and the duration of treatment. The release form of the hepatoprotector "Heptor" (400 mg) is tablets of 20, 40 or 60 pieces per package or lyophilisate for the preparation of a solution for intravenous or intramuscular administration.

The tablets are colored yellow, which has an enteric coating. They are oval in shape, without external notches, although two parts can be seen at the break. Tablets are packaged in glass or plastic jars or in blisters.

What does the drug consist of?

"Heptor" (400 mg) contains one active substance - ademetionine. The auxiliary components of the drug include:

• magnesium stearate - formative substance;
• mannitol has diuretic properties;
• microcrystalline cellulose - formative substance
• Polyplasdon X El-10 (crospovidone) is a complexing substance with detoxification properties.

Availability of auxiliary components corresponds dosage form substances.

How does the active substance work?

A chemical compound called ademetionine is produced in human liver and brain tissue and is functionally necessary for many reactions. The synthesized substance in the form of a drug helps the production of a natural analogue and compensates for its deficiency. The coenzyme ademetionine was first studied in Italy in the middle of the last century. Scientists have found that its role in the body is very important as a precursor of many thiol physiological compounds, such as glutathione, taurine, cysteine, as well as polyamines - putrescine, which stimulates cell recovery, spermidine and spermine, which are part of the ribosome complex.

Ademetionine stimulates the production of phosphatidylcholine, which is responsible for the polarization and mobility of membranes of liver tissue cells - hepatocytes. This functionality is especially important for intralobular cholestasis - a violation of the synthesis and flow of bile. The medicinal component of the drug "Heptor" (400 mg) activates several functions of the hepatosystem:

• transport function, promoting the release of bile acids into the biliary system;
• by increasing the amount of conjugated and sulfated bile acids in hepatocytes, it stimulates the detoxification of bile acids;
• increases the solubility of bile acids due to fusion with taurine;
• activates the removal of bile acids from liver cells;
• promotes the excretion (elimination) of bile due to its ability to sulfate;
• protects liver cells from the toxic effects of damaging components during intrahepatic cholestasis.

Ademetionine has an antidepressant property that manifests itself in the second week of use of the drug. It also helps to interrupt relapses of depression.

For the drug "Heptor" (400 mg), the instructions for use also describe its ability to reduce the manifestations of symptoms of intrahepatic cholestasis syndrome, such as skin itching and biochemical blood parameters - the activity of alkaline phosphatase (a cellular enzyme, activity characterizes tissue pathology), the level of direct bilirubin.

The drug helps reduce asthenic syndrome. During clinical trials, it was found that the positive dynamics of the antiasthenic, anticholestatic and hepatoprotective effects of the drug persisted 3 months after its discontinuation. Drug-induced hepatopathy and liver disorders associated with opioid addiction successfully regress when taking the drug.

Decrease pain syndrome, as well as partial restoration of cartilage tissue in osteoarthritis due to stimulation of proteoglycan synthesis was noted with the empirical use of the drug "Heptor".

As with any other medicine, instructions for use are included with the drug "Heptor" (400 mg). It is required to be read carefully not only by the doctor prescribing the drug, but also by the patient.

Path of the active component at work

Taking the drug "Heptor" (400 mg) in tablet form allows the active component to reach the duodenum unchanged, where it is released and enters the blood through the intestinal walls. Bioavailability in this case is low - only 5%. The concentration of 400 mg of the active substance in one tablet allows the patient to receive a therapeutically significant amount of the drug. The maximum concentration of ademetionine is observed in the cerebrospinal fluid after 2-6 hours. Its metabolism occurs in the liver, and the half-life is one and a half hours.

Pharmaceutical group of the drug

As the instructions for use say about the drug "Heptor" (400 mg) (ampoules or tablets - it doesn’t matter), the medicine belongs to two pharmacological groups- antidepressants and hepatoprotectors due to the functional characteristics of the active component - ademetionine. Therefore, the list of areas of its application is quite extensive.

In what cases is the drug indicated?

Double-action drug - "Geptor" (400 mg). Indications for the use of this product are based on the work of its active component - ademetionine. It is thanks to him that it is used in the following cases:

• withdrawal syndrome;
• biliary tract disease of unspecified etiology;
• intrahepatic cholestasis;
• depressive syndrome;
• liver damage: alcoholic, viral, drugs (antibiotics, oral contraceptives, antiviral, antitumor, anti-tuberculosis drugs, tricyclic antidepressants), toxic;
• behavioral and mental disorders caused by opioid use;
• liver fibrosis;
• cirrhosis of the liver;
• encephalopathy, including those caused by liver failure.

What if the drug cannot be used?

Like all medicines, the drug "Heptor" (400 mg), tablets or lyophilisate, has undergone clinical trials to help identify contraindications for use. There are not many of them for this medicine - hypersensitivity and intolerance to the components. The drug is also not recommended for the treatment of patients with diagnosed liver cirrhosis associated with hyperazotemia - an excess of nitrogenous products of protein metabolism in the blood. This drug is not prescribed to children under 18 years of age due to the lack of appropriate clinical trials.

Pregnancy and lactation period

Pregnancy and the period of breastfeeding a newborn child require a maximum of useful substances from the woman’s body, a full return of all vital forces, and it seems that products that have the ability to help during this period should be in demand. But this does not apply to the hepatoprotector "Geptor" (400 mg). This drug is strictly contraindicated in the 1st and 2nd trimesters of pregnancy. If, for medical reasons, a woman needs to take this medicine in the 3rd trimester of pregnancy, then it is carried out only under constant monitoring attending physician.

The lactation period is incompatible with treatment with a hepatoprotector based on ademetionine, since the active substance passes into breast milk and can have an extremely negative effect on the baby’s body. If treatment with Heptor (400 mg) is necessary, the instructions for use of the medicine recommend stopping breastfeeding and transferring the baby to artificial formula in advance.

Possible side effects

He will tell you what side effects the drug "Heptor" (400 mg) can cause, instructions for use. In the form of tablets or lyophilisate, it does not cause many side effects:

• allergic reactions to the components of the drug;
• pain or discomfort in the epigastrium, which are caused by an increase in the acidity of gastric secretions against the background of the acidic pH of ademetionine.

As a rule, the pain goes away on its own, but allergies can provoke a deterioration in health, so you need to inform your doctor about side effect means to adjust treatment.

How to take the drug

Any drug should be taken in accordance with the instructions for use and as prescribed by the attending physician. Hepatoprotector "Heptor" (400 mg), ampoules of which contain lyophilisate of ademetionine, is used to prepare a solution. This form The drug is most often used for lyophilisate dissolved only in a special substance based on L-lysine. 400 or 800 mg of the drug is administered per day. It can be administered either intramuscularly or intravenously, very slowly. The course of intensive treatment with lyophilisate is 2-4 weeks, the specific duration is determined by the attending physician. Therapy is then carried out using tablets, the same form of medication used for standard treatment that does not require emergency drug action. The tablet is removed from the package immediately before ingestion. The mode of use of this form of the drug is between breakfast and lunch, lunch and dinner. It is advisable to avoid using the drug in the evening, as it has some stimulating effect. The tablet should be swallowed whole, without chewing, dissolving or crushing. The drug is taken per day in a dosage of 2-4 tablets, exact dosage determined by the doctor based on the patient’s condition.

Overdose

Instructions for use describe injections or tablets "Geptor" (400 mg) quite clearly. But information about an overdose of the drug in any form is not indicated, since there is none and no tests have been conducted on this matter. It should be remembered that the medicine must be used strictly as prescribed by the doctor in the specified dosage and mode of administration.

Drug interactions

Ademetionine, which is the active substance of the hepatoprotector drug "Geptor", has not been studied in the field of interaction with other medicinal substances. When taking tablets or giving injections, you should take into account the manufacturer's recommendation - use the drug between meals. Since the majority medicines taken half an hour before or after meals, this allows you to eliminate meaningful interaction active substances.

Features of drug treatment

For the drug "Heptor" (400 mg), the instructions for use indicate some features. They must be taken into account during therapy with this drug:

• You should not take the medicine in the evening, as it has a tonic effect;
• treatment of liver cirrhosis with hyperazotemic etiology should be accompanied by regular checking of the content of nitrogenous compounds in the blood;
• The medication tablets are enclosed in a special coating that dissolves only in the duodenum, so tablets cannot be crushed for oral administration;
• treatment with the drug and drinking alcoholic beverages are incompatible;
• the lyophilisate solution is prepared just before administration, the tablet is removed from the package immediately before ingestion. A change in the color of the solution or the color of the tablet warns of the impossibility of using it;
• the medicinal product does not affect concentration or memory, and therefore control is not prohibited during treatment vehicles and performing work that requires increased concentration.

How to buy and store medicine?

The drug "Heptor" is a hepatoprotector that also has an antidepressant effect. That is why its purchase in pharmacy chains is only possible with a doctor’s prescription. The purchased medicine must be stored away from sunlight and excess moisture, at a temperature from +5 to +25 0 C. The solution should be prepared and the tablet should be removed from the package immediately before use.

What do doctors and patients say about the medicine?

The hepatoprotector "Heptor" (400 mg) receives mostly positive reviews from both doctors and patients. The drug helps to cope with health problems if the course of treatment is completed according to the regimen specified by the doctor. Many patients compare the medicine "Geptor" (400 mg), the instructions for use of which speak of it as a hepatoprotector and antidepressant, with similar ones, similar drugs, noting its slightly lower price.

The use of the drug "Heptor" allows you to effectively solve health problems and at the same time obtain an antidepressant effect. But only the attending physician can prescribe this medicine!

Instructions for use

Active ingredients

Release form

Pills

Compound

Active ingredient: Ademetionine Concentration active substance: 400mg

Pharmacological effect

Hepatoprotector, has antidepressant activity. It has choleretic and cholekinetic effects. It has detoxifying, regenerating, antioxidant, antifibrosing and neuroprotective properties. It replenishes ademetionine deficiency and stimulates its production in the body, primarily in the liver and brain. Participates in biological transmethylation reactions (methyl group donor) - the S-adenosyl-L-methionine molecule (ademetionine), is a methyl group donor in methylation reactions of phospholipids of cell membranes, proteins, hormones, neurotransmitters; participates in transsulfation reactions as a precursor of cysteine, taurine, glutathione (provides a redox mechanism for cellular detoxification), and acetylation coenzyme. Increases the content of glutamine in the liver, cysteine ​​and taurine in plasma; reduces the content of methionine in serum, normalizing metabolic reactions in the liver. In addition to decarboxylation, it participates in the processes of aminopropylation as a precursor of polyamines - putrescine (stimulator of cell regeneration and proliferation of hepatocytes), spermidine and spermine, which are part of the structure of ribosomes. It has a choleretic effect due to increased mobility and polarization of hepatocyte membranes, due to stimulation of the synthesis of phosphatidylcholine in them. This improves the function of bile acid transport systems associated with hepatocyte membranes and promotes the passage of bile acids into the biliary system. Effective for intralobular cholestasis (impaired synthesis and flow of bile). Promotes detoxification of bile acids, increases the content of conjugated and sulfated bile acids in hepatocytes. Conjugation with taurine increases the solubility of bile acids and their removal from the hepatocyte. The process of sulfation of bile acids facilitates their elimination by the kidneys, facilitates their passage through the hepatocyte membrane and excretion in the bile. In addition, sulfated bile acids protect liver cell membranes from the toxic effects of non-sulfated bile acids (present in high concentrations in hepatocytes during intrahepatic cholestasis). In patients with diffuse liver diseases (cirrhosis, hepatitis) with intrahepatic cholestasis syndrome, it reduces the severity of skin itching and changes in biochemical parameters, incl. level of direct bilirubin, alkaline phosphatase activity, aminotransferases.

Pharmacokinetics

After a single oral dose of 400 mg, the Cmax of ademetionine in plasma is reached after 2-6 hours and is 0.7 mg/l. The bioavailability of the drug when taken orally is 5%, when administered intramuscularly - 95%. Binding to serum proteins is negligible. Penetrates through the BBB. Regardless of the route of administration, there is a significant increase in the concentration of ademetionine in the cerebrospinal fluid. Metabolized in the liver. T1/2 - 1.5 hours. Excreted by the kidneys.

Indications

intrahepatic cholestasis; hepatitis of various origins: toxic (including alcoholic), viral, medicinal (antibiotics, antitumor, antituberculosis and antiviral drugs, tricyclic antidepressants, oral contraceptives); precirrhotic conditions; liver cirrhosis; encephalopathies of secondary origin; depressive syndromes, including secondary; alcohol withdrawal syndrome .

Contraindications

Hypersensitivity.

Use during pregnancy and breastfeeding

In the first and second trimesters of pregnancy, ademetionine is used only in cases of extreme necessity, when the expected benefit to the mother outweighs the potential risk to the fetus. Application of ademetionine in high doses in the third trimester of pregnancy did not cause any undesirable effects. The use of ademetionine during breastfeeding is possible only if the expected benefit to the mother outweighs the potential risk to the child.

Directions for use and doses

Inside, swallowing whole, without chewing. To improve the therapeutic effect, it is recommended to take the tablets between meals. During the period of maintenance therapy, the recommended daily dose is 800–1600 mg (2–4 tables). The duration of maintenance therapy is on average 2–4 weeks.

Side effects

Due to the fact that the active substance of the drug has an acidic pH, some patients may experience discomfort in the epigastric region when using the tablets. In any case, these sensations are short-term, are not pronounced and should not serve as a reason for stopping the course of treatment.

Overdose

There were no clinical cases of overdose.

Interaction with other drugs

There is a report of the development of serotonin syndrome in a patient who used ademetionine and clomipramine. Ademetionine should be used with caution simultaneously with selective serotonin reuptake inhibitors, tricyclic antidepressants, drugs and herbal remedies containing tryptophan.

special instructions

Use ademetionine with caution in patients with renal failure, with bipolar disorders, simultaneously with selective serotonin reuptake inhibitors, tricyclic antidepressants (such as clomipramine); herbal preparations and preparations containing tryptophan; in elderly patients. Vitamin B12 deficiency and folic acid may lead to a decrease in ademetionine concentrations, therefore their concomitant use in normal doses is recommended. Patients with depression require careful monitoring and constant psychiatric care during treatment with ademetionine in order to monitor the effectiveness of treatment. When used in patients with cirrhosis of the liver against the background of hyperazotemia, systematic monitoring of the level of nitrogen in the blood is necessary. During long-term therapy, it is necessary to determine the content of urea and creatinine in the blood serum. Effect on the ability to drive vehicles and operate machinery When using ademetionine, dizziness is possible. Patients should not drive or operate machinery until symptoms have completely resolved, which may affect reaction time. specified types activities.

Heptor: instructions for use and reviews

Latin name: Heptor

ATX code: A16AA02

Active substance: ademetionine

Manufacturer: Veropharm, LLC (Russia), Microgen NPO FSUE (NPO Virion) (Russia), Lance-Pharm, LLC (Russia)

Updating the description and photo: 09.09.2019