Heptral pills coated 400mg N20
Condition: New product
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Active ingredients
Ademetionine
Release form
Pills
Composition
Ademetionine 1,4-butane disulfonate 760 mg, which corresponds to the content of ademetionine ion 400 mg. Additional substances: colloidal dioxide silicon - 4.4 mg, microcrystalline cellulose - 93.6 mg, sodium carboxymethyl starch (type A) - 17.6 mg, magnesium stearate - 4.4 mg. Composition shells: copolymer of methacrylic acid and ethyl acrylate (1: 1) - 27.6 mg, macrogol 6000 - 8.07 mg, polysorbate 80 - 0.44 mg, simethicone (30% emulsion) - 0.13 mg, sodium hydroxide - 0.36 mg, talc - 18.4 mg, water - QS
Pharmacological effect
Hepatoprotector, has antidepressant activity. It has choleretic and cholekinetic effects. It has detoxification, regenerating, antioxidant, antifibrosis and neuroprotective properties. It compensates for the deficiency of ademetionine and stimulates its production in the body, primarily in the liver and brain. Participates in biological reactions of transmethylation (a donor of the methyl group) - S-adenosyl-L-methionine molecule (ademetionine), is a donor of the methyl group in the methylation reactions of phospholipids of cell membranes, proteins, hormones, neurotransmitters; participates in trans-sulfation reactions as a precursor of cysteine, taurine, glutathione (provides the redox mechanism of cellular detoxification), acetylation coenzyme. Increases the content of glutamine in the liver, cysteine and taurine in plasma; reduces serum methionine, 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 included in the structure of ribosomes. It has 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 transport systems of bile acids associated with membranes of hepatocytes and facilitates the passage of bile acids into the biliary system. Effective with intralobular cholestasis (violation of the synthesis and flow of bile). It promotes the 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 contributes to the possibility of their elimination by the kidneys, facilitates the passage of hepatocyte through the membrane and the excretion of bile. In addition, sulfated bile acids protect 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 reduces the severity of pruritus and changes in biochemical parameters, including direct bilirubin level, activity of alkaline phosphatase, aminotransferases.
Pharmacokinetics
After a single oral dose of 400 mg Cmax of ademetionine in plasma is reached in 2-6 hours and is 0.7 mg / l. The bioavailability of the drug when administered is 5%, with the i / m administration - 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 h. It is derived from the kidneys.
Indications
Intrahepatic cholestasis in pre-cirrhotic and cirrhotic conditions, including: fatty degeneration of the liver; chronic hepatitis; toxic liver damage of various etiologies, including alcohol, viral, drugs (antibiotics, anticancer, antituberculosis and antiviral drugs, tricyclic antidepressants, oral contraceptives); chronic cholecystitis without stones; cholangitis; cirrhosis of the liver; encephalopathy, incl. associated with liver failure (including alcohol). Intrahepatic cholestasis in pregnant women. Symptoms of depression.
Contraindications
Genetic disorders affecting the methionine cycle, and / or causing homocystinuria and / or hyperhomocysteinemia (cystathione beta-synthetase deficiency, disruption of cyanocobalamin metabolism) children and adolescents under 18, hypersensitivity to ademethionine.
Use during pregnancy and lactation
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.Lack of vitamin B12 and folic acid can lead to a decrease in the concentrations of ademetionine, therefore their concomitant use in usual doses is recommended. Depressed patients need careful monitoring and ongoing psychiatric care in the treatment with ademetionine in order to monitor the effectiveness of treatment. When used in patients with liver cirrhosis and 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. Influence on ability to drive motor vehicles and control mechanisms When using ademetionine, dizziness is possible. Patients should not drive vehicles or work with other mechanisms until the complete disappearance of symptoms that may affect the reaction rate during these activities.
Dosage and administration
Applied orally, in / m or / in (very slowly). When ingested, the daily dose is 800-1600 mg. In case of intravenous or intramuscular injection, the daily dose is 400-800 mg. the severity and course of the disease. In elderly patients, treatment is recommended to begin with the lowest recommended dose, taking into account the decrease in hepatic, renal or cardiac function, the presence of associated pathological conditions and the use of other drugs.
Side effects
On the part of the digestive system: often - nausea, abdominal pain, diarrhea; rarely - vomiting, dry mouth, esophagitis, dyspepsia, flatulence, gastrointestinal pain, gastrointestinal bleeding, hepatic colic. On the part of the nervous system: rarely - confusion, insomnia, dizziness, headache, paresthesia. From the musculoskeletal system: rarely - arthralgia, muscle cramps. Urinary system disorders: rarely, urinary tract infections. On the part of 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 - angioedema, laryngeal edema.Other: rarely - hot flashes, superficial phlebitis, asthenia, chills, flu-like symptoms, weakness, peripheral edema, hyperthermia.
Interaction with other drugs
There is a message about the development of serotonin syndrome in a patient using ademetionine and clomipramine. Addemetionine should be used with caution simultaneously with selective serotonin reuptake inhibitors, tricyclic antidepressants, drugs and herbal remedies containing tryptophan.
special instructions
Overdose