Heptral 0.5 №20 tab.
Oval tablets, biconvex, smooth, from white to light yellow in color, film-coated.
Composition Each tablet contains:
Active ingredient: Ademethionine 1,4-butanedisulfonate 949.0 mg (corresponding to 500 mg of ademetionine ion). Excipients: colloidal silicon dioxide - 5.50 mg, microcrystalline cellulose - 118.00 mg, sodium carboxymethyl starch (type A) - 22.00 mg, magnesium stearate - 5.50 mg; tablet shell: methacrylic acid and ethyl acrylate copolymer (1: 1) - 32.63 mg, macrogol-6000 - 9.56 mg, polysorbate-80 - 0.52 mg, simethicone emulsion (30%) - 0.40 mg, sodium hydroxide - 0.44 mg, talc - 21.77 mg.
Ademethionine belongs to the group of hepatoprotectors, also has antidepressant activity. It has a choleretic and cholekinetic effect, has detoxification, regenerating, antioxidant, antifibrosing and neuroprotective properties. It compensates for the deficiency of S-adenosyl-L-methionine (ademethionine) and stimulates its production in the body, found in all body environments. The highest concentration of ademetionine is noted in the liver and brain. It plays a key role in the metabolic processes of the body, takes part in important biochemical reactions: transmethylation, transulfurization, transamination. In the transmethylation reactions, ademetionine donates a methyl group for the synthesis of phospholipids of cell membranes, neurotransmitters, nucleic acids, proteins, hormones, etc. In the transmerization reactions of ademetionine, it is a precursor of cysteine, taurine, glutathione (providing the redox mechanism of cellular detoxification (included) 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 serum methionine, normalizing metabolic reactions in the liver. After decarboxylation, it participates in aminopropylation reactions, as a precursor to putrescine polyamines (a stimulator of cell regeneration and hepatocyte proliferation), spermidine and spermine, which are part of the ribosome structure, which reduces the risk of fibrosis. It has a choleretic effect. Ademethionine normalizes the synthesis of endogenous phosphatidylcholine in hepatocytes, which increases the fluidity and polarization of the membranes. This improves the function of bile acid transport systems associated with hepatocyte membranes and promotes the passage of bile acids into the bile ducts. Effective with the intralobular variant of cholestasis (impaired synthesis and bile flow). Ademethionine 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 hepatocyte. The process of sulfation of bile acids contributes to the possibility of elimination by the kidneys, facilitates the passage through the membrane of hepatocytes and excretion with bile. In addition, sulfated bile acids themselves additionally protect the liver cell membranes from the toxic effects of non-sulfated bile acids (in high concentrations present in hepatocytes with intrahepatic cholestasis). In patients with diffuse liver diseases (cirrhosis, hepatitis) with intrahepatic cholestasis syndrome, ademetionin reduces the severity of skin itching and changes in biochemical parameters, including direct bilirubin concentrations, alkaline phosphatase activity, aminotransferases, etc. The choleretic and hepatoprotective effect lasts up to 3 months after treatment is discontinued. It has been shown to be effective in hepatopathies caused by various hepatotoxic drugs. Administration to patients with opioid addiction accompanied by liver damage leads to a regression of the clinical manifestations of withdrawal symptoms, an improvement in the functional state of the liver, and microsomal oxidation processes. Antidepressant activity manifests itself gradually, starting from the end of the first week of treatment, and stabilizes within 2 weeks of treatment. Effective in recurrent endogenous and neurotic depressions resistant to amitriptyline. It has the ability to interrupt relapse of depression. Ademethionine increases the synthesis of proteoglycans and leads to partial regeneration of cartilage tissue.
- Intrahepatic cholestasis in precirrotic and cirrhotic conditions, which can be observed with the following diseases:
- fatty degeneration of the liver;
- chronic hepatitis;
- toxic liver lesions of various etiologies, including alcoholic, viral, and medicinal (antibiotics; antitumor, anti-tuberculosis and antiviral drugs, tricyclic antidepressants, oral contraceptives);
- chronic stoneless cholecystitis;
- cirrhosis of the liver;
- encephalopathy, including associated with liver failure (alcohol, etc.).
- Intrahepatic cholestasis in pregnant women.
- Symptoms of depression.