Heptor, lyophilizate. 400 mg 5 pcs

Cholecystitis, Liver damage, Alcoholism, Hepatitis, Depression, Liver cirrhosis

Indications

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

Intrahepatic cholestasis in pregnant women.

Symptoms of depression.

Pharmacological effect

Pharmacotherapeutic group: Hepatoprotective agent

Pharmacological action

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

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.

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.

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 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.

Active ingredient

Ademetionine

Composition

Active substance: ademetionine

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.

Pregnancy

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 for the mother outweighs the potential risk for the child.

Contraindications

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

Side Effects

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.

Manufacturer

Veropharm LLC, Russia