HEPTOR 400 mg 20 pcs. enteric-coated tablets

Heptor 400 mg 20 pcs. enteric-coated tablets

pharmachologic effect

Hepatoprotective agent.

Composition and release form Heptor 400 mg 20 pcs. enteric-coated tablets

Tablets - 1 tablet:

Active substance: Ademetionine tosylate disulfate in terms of ademetionine ion - 400 mg;
Excipients to obtain a tablet weighing 0.95 g (without shell): polyplasdon X El-10 (crospovidone) - 19 mg, microcrystalline cellulose - 53 mg, mannitol (mannitol) - 53 mg, magnesium stearate - 15 mg;
There is a sufficient amount of excipients to obtain a tablet with a shell weighing 1.045 g: yellow acrylic - [methacrylic acid and ethyl acrylate copolymer (1:1), talc, titanium dioxide, colloidal silicon dioxide, triethyl citrate, sodium bicarbonate, sodium lauryl sulfate, yellow iron oxide , quinoline yellow aluminum varnish], hydroxypropyl methylcellulose, plasdon ES-630 (copovidone), polyethylene glycol 6000.

10 tablets per blister pack.

20, 40 or 50 tablets per polymer jar.

Each jar contains either 1 or 2 blister packs along with instructions for use in a pack.

Description of the dosage form

Enteric-coated tablets are yellow, oblong, biconvex.

Directions for use and doses

During the period of maintenance therapy, a daily dose of 800-1600 mg (2-4 tablets) is recommended. The duration of maintenance therapy is on average 2-4 weeks. The tablets should be swallowed whole without chewing. To improve the therapeutic effect, it is recommended to take the tablets in the first half of the day between meals.

Pharmacodynamics

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) donates a methyl group in methylation reactions of phospholipids of cell membranes, proteins, hormones, neurotransmitters, etc.; transsulfation - a precursor of cysteine, taurine, glutathione (provides a redox mechanism of cellular detoxification), coenzyme A. Increases the content of glutamine in the liver, cysteine and taurine in the plasma; reduces the content of methionine in the blood serum, normalizing metabolic reactions in the liver. After decarboxylation, it participates in aminopropylation processes as a precursor of polyamines - putrescine (stimulator of cell regeneration and hepatocyte proliferation), spermidine and spermine, which are part of the ribosome structure. It has a choleretic effect due to increased mobility and polarization of hepatocyte membranes due to stimulation and 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 hepatocytes. The process of sulfation of bile acids promotes their elimination by the kidneys, facilitates their passage through the hepatocyte membrane and excretion with bile. In addition, sulfated bile acids protect liver cell membranes from the toxic effects of non-sulfated bile acids, which are 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. concentrations of direct and total bilirubin, activity of alkaline phosphatase, g-glutamyl transpeptidase, aminotransferases. The choleretic and hepatoprotective effect lasts up to 3 months after cessation of treatment. Shown to be effective in hepatopathy caused by hepatotoxic drugs. Prescribing ademetionine to patients with opioid addiction accompanied by liver damage leads to regression of clinical manifestations of withdrawal, improvement of the functional state of the liver and microsomal oxidation processes. Antidepressant activity appears gradually, starting from the end of 1 week of treatment and stabilizes within 2 weeks of treatment. Effective for recurrent endogenous and neurotic depressions resistant to amitriptyline. Has the ability to interrupt relapses of depression. Prescription for osteoarthritis reduces the severity of pain, increases the synthesis of proteoglycans and leads to partial regeneration of cartilage tissue.

Pharmacokinetics

Bioavailability when taken orally - 5%. With a single oral dose of 400 mg, the maximum plasma concentration (Cmax) is 0.7 mg/l. Time to reach maximum concentration (TCmax) - 2-6 hours. Binding to plasma proteins is insignificant, penetrates the blood-brain barrier. When taken, there is a significant increase in the concentration of ademetionine in the cerebrospinal fluid. Metabolized in the liver. Half-life (T1/2) - 1.5 hours.

Indications for use Heptor 400 mg 20 pcs. enteric-coated tablets

chronic non-calculous cholecystitis;
cholangitis;
intrahepatic cholestasis;
hepatitis of various origins: viral, toxic, incl. alcoholic and medicinal origin (antibiotics, antitumor, antituberculosis and antiviral drugs, tricyclic antidepressants, oral contraceptives);
fatty liver;
cirrhosis of the liver;
encephalopathy, incl. associated with liver failure (alcohol, etc.);
depression (including secondary);
withdrawal syndrome (alcohol, etc.).

Contraindications

Hypersensitivity.

Children under 18 years of age.

Pregnancy I-II trimester, lactation period.

Application of Heptor 400 mg 20 pcs. Enteric-coated tablets during pregnancy and breastfeeding

Taking the drug is contraindicated in the I-II trimester of pregnancy and during lactation.

special instructions

Given the tonic effect of the drug, it is not recommended to take it before bedtime. Oral use of the drug in patients with liver cirrhosis associated with hyperazotemia should be carried out under medical supervision with monitoring of nitrogen levels. The tablets of the drug are coated with a special coating that dissolves only in the intestines, due to which ademetionine is released in the duodenum. In patients with bipolar affective disorder, taking ademetionine can induce an inversion of affect (the development of hypomania or mania).

Impact on the ability to drive vehicles and operate machinery

When used in this dosage form, the drug does not affect the ability to drive a car or operate machinery.

Overdose

There were no clinical cases of overdose.

Side effects Heptor 400 mg 20 pcs. enteric-coated tablets

For this dosage form:

From the nervous system: headache, insomnia.

From the digestive system: abdominal pain, diarrhea, dry mouth, dyspepsia, flatulence, nausea.

Drug interactions

No interactions with other drugs were observed.

Heptor

Hepatoprotective agent, has choleretic and cholekinetic, as well as some antidepressant effects.

Taking the drug replenishes the deficiency of ademetionine and stimulates its production in the body, primarily in the liver and brain. Participates in biological transmethylation reactions (methyl group donor), donates a methyl group in methylation reactions of phospholipids of cell membranes of proteins, hormones, neurotransmitters, etc.; transsulfation - a precursor of cysteine, taurine, glutathione (provides a redox mechanism for cellular detoxification), acetylation coenzyme.

Therapy with the drug increases the content of glutamine in the liver, cysteine and taurine in plasma; reduces the content of methionine in the blood serum, normalizing metabolic reactions in the liver. After 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 ribosome structure.

The active ingredient of the drug 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 hepatocytes. 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, treatment with the drug reduces the severity of skin itching and changes in the concentration of direct bilirubin, alkaline phosphatase activity, “liver” transaminases, etc.

The choleretic and hepatoprotective effect lasts up to 3 months after cessation of treatment.

Shown to be effective in hepatopathy caused by hepatotoxic drugs.

Prescribing the drug to patients with opioid addiction accompanied by liver damage leads to regression of clinical manifestations of withdrawal, improvement of the functional state of the liver and microsomal oxidation processes.

Antidepressant activity appears gradually, starting from the end of 1 week of treatment, and stabilizes within 2 weeks of treatment. Effective for recurrent endogenous and neurotic depressions resistant to amitriptyline. Has the ability to interrupt relapses of depression.

Prescribing treatment with the drug for osteoarthritis reduces the severity of pain, increases the synthesis of proteoglycans and leads to partial regeneration of cartilage tissue.

Heptor lyophilisate for intravenous and intramuscular injection 400 mg No. 5 + solution

Compound

Active substance: ademetionine 1,4-butane disulfonate 760 mg, which corresponds to the content of ademetionine 400 mg.
Solvent: L-lysine (in the form of monohydrate) - 68.48 mg, sodium hydroxide solution - up to pH 9.8-10.3, water for injection - up to 1 ml.

Pharmacokinetics

Bioavailability after intramuscular (IM) administration is 95%. Plasma protein binding is negligible and penetrates the blood-brain barrier. Regardless of the route of administration, there is a significant increase in the concentration of ademetionine in the cerebrospinal fluid. Metabolized in the liver. The half-life (T1/2) is 1.5 hours. It is excreted by the kidneys.

Indications for use

Chronic non-calculous cholecystitis,
cholangitis,
intrahepatic cholestasis, including in pregnant women,
hepatitis of various origins: viral, toxic, incl. alcoholic and medicinal origin (antibiotics, antitumor, antituberculosis and antiviral drugs, tricyclic antidepressants, oral contraceptives),
fatty liver degeneration,
cirrhosis of the liver,
encephalopathy, incl. associated with liver failure (alcoholic, etc.),
alcoholic liver disease,
depression (including secondary),
withdrawal syndrome (alcohol, etc.)

Contraindications

Hypersensitivity to ademetionine and/or solvent components, age under 18 years.

Carefully:

Pregnancy (1st trimester).
Lactation period.
Bipolar disorders (see section "Special instructions").

Directions for use and doses

Intramuscular (IM), intravenous (IV). In intensive therapy, in the first 2-3 weeks of treatment, Heptor is prescribed at a dose of 400-800 mg/day intravenously (very slowly) or intramuscularly. The lyophilisate is dissolved only in the special supplied solvent (L-lysine solution). After completion of intensive therapy, maintenance therapy is carried out using the dosage form of Heptor for oral administration (400 mg tablets of ademetionine).

Storage conditions

At a temperature not higher than 25 °C. Keep out of the reach of children.

Best before date

2 years (for lyophilisate). 3 years (for solvent). Do not use after the expiration date stated on the package.

special instructions

Given the tonic effect of the drug, it is not recommended to take it before bed.

When using ademetionine in patients with cirrhosis of the liver against the background of hyperazotemia, systematic monitoring of nitrogen content in the blood is necessary; during long-term therapy, it is necessary to determine the content of urea and creatinine in the blood serum. The drug solution is prepared immediately before use; if the color of the lyophilisate differs from what it should be (see section “Description”), you must refrain from using it.

It is not recommended to use ademetionine in patients with bipolar disorders. There are reports of the transition of depression to hypomania or mania in patients taking ademetionine.

Patients with depression have an increased risk of suicide and other serious adverse events, therefore, during treatment with ademetionine, such patients should be closely monitored by a physician to evaluate and treat symptoms of depression. Patients should inform their physician if their symptoms of depression do not improve or worsen with ademetionine therapy. There are also reports of sudden onset or worsening anxiety in patients taking ademetionine. In most cases, discontinuation of therapy is not required; in several cases, anxiety disappeared after reducing the dose or discontinuing the drug.

Since deficiency of cyanocobalamin and folic acid can reduce the level of ademetionine in patients at risk (with anemia, liver disease, pregnancy or the likelihood of vitamin deficiency due to other diseases or diet, for example, vegetarians), the content of vitamins in the blood plasma should be monitored. If deficiency is detected, it is recommended to take cyanocobalamin and folic acid before starting treatment with ademetionine or simultaneous use with ademetionine. In immunological analysis, the use of ademetionine may contribute to the false determination of high homocysteine levels in the blood.

For patients taking ademetionine, it is recommended to use non-immunological methods of analysis to determine homocysteine levels.

Description

Hepatoprotective agent.

Pharmacodynamics

Heptor belongs to the group of hepatoprotectors with antidepressant activity.
It has choleretic and cholekinetic effects. It has detoxifying, regenerating, antioxidant, antifibrosing and neuroprotective effects. 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) donates a methyl group in methylation reactions of phospholipids of cell membranes, proteins, hormones, neurotransmitters, etc.; transsulfation - a precursor of cysteine, taurine, glutathione (provides a redox mechanism of cellular detoxification), coenzyme A. Increases the content of glutamine in the liver, cysteine and taurine in the plasma; reduces the content of methionine in the blood serum, normalizing metabolic reactions in the liver. After 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 ribosome structure. 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 hepatocytes. The process of sulfation of bile acids promotes their elimination by the kidneys, facilitates their passage through the hepatocyte membrane and excretion with bile. In addition, sulfated bile acids protect liver cell membranes from the toxic effects of non-sulfated bile acids, which are 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. concentration of direct bilirubin, activity of alkaline phosphatase, g-glutamyl transpeptidase, aminotransferases. The choleretic and hepatoprotective effect lasts up to 3 months after cessation of treatment. Shown to be effective in hepatopathy caused by hepatotoxic drugs. Prescribing ademetionine to patients with opioid addiction accompanied by liver damage leads to regression of clinical manifestations of withdrawal, improvement of the functional state of the liver and microsomal oxidation processes. Antidepressant activity appears gradually, starting from the end of 1 week of treatment and stabilizes within 2 weeks of treatment. Effective for recurrent endogenous and neurotic depressions resistant to amitriptyline. Has the ability to interrupt relapses of depression. Prescription for osteoarthritis reduces the severity of pain, increases the synthesis of proteoglycans and leads to partial regeneration of cartilage tissue.

Side effects

The most common adverse reactions include nausea, abdominal pain and diarrhea.
From the immune system: hypersensitivity reactions, anaphylactoid or anaphylactic reactions (including skin hyperemia, shortness of breath, bronchospasm, back pain, discomfort in the chest, decreased blood pressure, increased blood pressure, tachycardia, bradycardia).

From the respiratory system: laryngeal edema.

From the skin: reactions at the injection site (very rarely with skin necrosis), Quincke's edema, increased sweating, allergic skin reactions (including rash, itching, urticaria, erythema).

Infections and infestations: urinary tract infections.

From the nervous system: dizziness, headache, paresthesia, anxiety, confusion, insomnia.

From the cardiovascular system: hot flashes, phlebitis of the superficial veins, cardiovascular disorders.

From the digestive system: bloating, abdominal pain, diarrhea, dry mouth, dyspepsia, esophagitis, flatulence, gastrointestinal disorders, gastrointestinal bleeding, nausea, vomiting, hepatic colic, cirrhosis.

From the musculoskeletal system: arthralgia, muscle spasms.

Other: asthenia, chills, flu-like syndrome, malaise, peripheral edema, fever.

Use during pregnancy and breastfeeding

It is possible to use the drug in the second trimester of pregnancy with intrahepatic cholestasis. Taking high doses of ademetionine in the third trimester of pregnancy did not cause undesirable effects. Use in the first trimester of pregnancy and lactation is possible if the potential benefit to the mother outweighs the possible risk to the fetus or child.

Interaction

No interactions with other drugs were observed.

Overdose

There were no cases of overdose.

Impact on the ability to drive vehicles and operate machinery

Dizziness may occur when using ademetionine. Patients should not drive or operate machinery until symptoms that may affect reaction time during these activities have completely resolved.

Heptor tablet p o intestinal 400 mg pack cont cell/pack card x40

Description of the active components of the drug Heptor The scientific information provided is general and cannot be used to make a decision about the possibility of using a particular drug. Update date: 2018.02.21

Release form, packaging and composition Clinical-pharmacological. group Pharmacotherapeutic group Pharmacological action Pharmacokinetics Indications of the drug Dosage regimen Side effects Contraindications for use Special instructions Drug interactions

Marketing authorization holder: VEROPHARM, JSC (Russia) ATX code: A16AA02 (Ademetionine) Active substance: ademetionine Rec.INN registered by WHO

Dosage form

Heptor

Tab., cover. enteric coated, 400 mg: 20 pcs.reg. No.: LS-001820 from 08/22/11 - Indefinitely

Release form, packaging and composition

Enteric-coated tablets are yellow, oblong, biconvex.

1 tab.

ademetionine (in the form of S-adenosylmethionine) 400 mg

Excipients: crospovidone (polyplasdon X El-10) - 19 mg, microcrystalline cellulose - 53 mg, mannitol (mannitol) - 53 mg, magnesium stearate - 15 mg.

Shell composition: acryliz - 61.3 mg, hydroxypropyl methylcellulose - 21 mg, copovidone (plasdon ES-630) - 9 mg, polyethylene glycol 6000 - 3.7 mg.

10 pieces. — contour cell packaging (2) — cardboard packs.

Clinical and pharmacological group: Hepatoprotector. Drug with antidepressant activity Pharmacotherapeutic group: Hepatoprotective agent

pharmachologic effect

Hepatoprotector, has antidepressant activity. It has choleretic and cholekinetic effects. It has detoxifying, regenerating, antioxidant, antifibrosing and neuroprotective properties.

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 of the drug

Intrahepatic cholestasis in pre-cirrhotic and cirrhotic conditions, including: fatty liver, chronic hepatitis, toxic liver damage of various etiologies, including alcohol, viral, drugs (antibiotics, antitumor, anti-tuberculosis and antiviral drugs, tricyclic antidepressants, oral contraceptives), chronic acalculous cholecystitis, cholangitis, liver cirrhosis, encephalopathy, incl. associated with liver failure (including alcoholic).

Intrahepatic cholestasis in pregnant women.

Symptoms of depression.

ICD-10 codes

Dosage regimen The method of administration and dosage regimen of a particular drug depend on its release form and other factors. The optimal dosage regimen is determined by the doctor. The compliance of the dosage form of a particular drug with the indications for use and dosage regimen should be strictly observed.

Apply orally, intramuscularly or intravenously (very slowly).

When taken orally, the daily dose is 800-1600 mg.

When administered intravenously or intramuscularly, the daily dose is 400-800 mg.

The duration of treatment is determined individually depending on the severity and course of the disease.

In elderly patients, it is recommended to begin treatment with the lowest recommended dose, taking into account decreased hepatic, renal or cardiac function, the presence of concomitant pathological conditions and the use of other drugs.

Side effect

From the digestive system: often - nausea, abdominal pain, diarrhea; rarely - vomiting, dry mouth, esophagitis, dyspepsia, flatulence, gastrointestinal pain, gastrointestinal bleeding, hepatic colic.

From the nervous system: rarely - confusion, insomnia, dizziness, headache, paresthesia.

From the musculoskeletal system: rarely - arthralgia, muscle cramps.

From the urinary system: rarely - urinary tract infections.

From the skin: rarely - hyperhidrosis, itching, skin rash.

Local reactions: rarely - reactions at the injection site, very rarely - reactions at the injection site, skin necrosis at the injection site.

Allergic reactions: rarely - anaphylactic reactions, very rarely - Quincke's edema, laryngeal edema.

Other: rarely - hot flashes, superficial phlebitis, asthenia, chills, flu-like symptoms, weakness, peripheral edema, hyperthermia.

Contraindications for use

Genetic disorders affecting the methionine cycle and/or causing homocystinuria and/or hyperhomocysteinemia (cystathione beta synthetase deficiency, cyanocobalamin metabolism disorder), children and adolescents under 18 years of age, hypersensitivity to ademetionine.

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. The use 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.

Use in children Contraindication: children and adolescents under 18 years of age.

special instructions

Use ademetionine with caution in patients with renal failure, with bipolar disorders, concomitantly with selective serotonin reuptake inhibitors, tricyclic antidepressants (such as clomipramine), herbal preparations and drugs containing tryptophan in elderly patients.

Insufficiency of vitamin B12 and folic acid can lead to a decrease in ademetionine concentrations, so their concomitant use in normal doses is recommended.

Patients with depression require careful monitoring and ongoing psychiatric care when treated with ademetionine to monitor the effectiveness of treatment.

When used in patients with cirrhosis of the liver against the background of hyperazotemia, systematic monitoring of nitrogen levels in the blood is necessary. During long-term therapy, it is necessary to determine the content of urea and creatinine in the blood serum.

Impact on the ability to drive vehicles and operate machinery

Dizziness may occur when using ademetionine. Patients should not drive or operate machinery until symptoms that may affect reaction time during these activities have completely resolved.

Drug interactions

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.