Active substanceAdemethionineAdemethionine
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  • Dosage form: & nbsplyophilizate for the preparation of solution for intravenous and intramuscular administration
    Composition:

    1 bottle of lyophilizate contains:

    active substance: ademethionine butahydisulfonate - 760 mg in terms of ademetionine ion -400 mg;

    In 1 ml of solvent contains:

    L-lysine monohydrate in terms of L-lysine-68.48 mg, sodium hydroxide solution to pH 9.8-10.3, water for injection up to 1 ml.

    Description:

    Lyophilizate: porous mass of white or almost white color.

    Solvent: clear liquid from colorless to yellowish color with a characteristic odor.

    Pharmacotherapeutic group:Hepatoprotective agent
    ATX: & nbsp

    A.16.A.A.02   Ademethionine

    Pharmacodynamics:

    Heptor belongs to the group of hepatoprotectors with antidepressant activity. Has choleretic and cholekinetic effect.Has detoxification, regenerating, antioxidant, antifibrozing and neuroprotective effect.

    Replenishes the deficit of ademetionine and stimulates its production in the body, primarily in the liver and brain. Participates in biological reactions of transmethylation (a methyl group donor) - a molecule S-adenosyl-Lmethionine (ademethionine) donates the methyl group in the reactions of methylation of phospholipids of cell membranes, proteins, hormones, neutromediators, etc .; transsulfation - the precursor of cysteine, taurine, glutathione, (provides oxidation-reduction mechanism of cellular detoxification), coenzyme A. Increases glutamine content 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 aminopropylation processes as a precursor of polyamines-putrescine (stimulator of cell regeneration and proliferation of hepatocytes), spermidine and spermine, which are part of the ribosome structure. Has a choleretic effect due to increased mobility and polarization of hepatocyte membranes due to stimulation of synthesis of phosphatidylcholine in them.This improves the function of hepatocyte-associated transport systems of bile acids and promotes the passage of bile acids into the biliary system. Effective with intraloble variant of cholestasis (a violation of synthesis and current of bile). It contributes to 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 hepatocytes. The process of sulphation of bile acids facilitates their elimination by the kidneys, facilitates passage through the membrane of the hepatocyte and excretion bile. In addition, sulfated bile acids protect the liver cell membranes from the toxic effect of non-sulphated bile acids present in high concentrations in hepatocytes with intrahepatic cholestasis. In patients with diffuse liver disease (cirrhosis, hepatitis) with intrahepatic cholestasis syndrome reduces the severity of skin itching and changes in biochemical parameters, incl. concentration of direct bilirubin, activity of alkaline phosphatase, g-glutamyltranspeptidase, aminotransferases.Choleretic and hepatoprotective effects persist up to 3 months after discontinuation of treatment. Efficacy is shown for hepatopathies due to hepatotoxic drugs. The appointment of ademetionine to patients with opioid addiction, accompanied by liver damage, leads to regression of clinical manifestations of abstinence, improvement of the functional state of the liver and the processes of microsomal oxidation. Antidepressant activity manifests itself gradually, beginning at the end of 1 week of treatment and stabilizing within 2 weeks of treatment. Effective in recurrent endogenous and neurotic depressions resistant to amitriptyline. Has the ability to interrupt recurrence of depression. The appointment in osteoarthritis reduces the severity of pain syndrome, increases the synthesis of proteoglycans and leads to partial regeneration of cartilaginous tissue.

    Pharmacokinetics:

    Bioavailability for intramuscular (IM) administration is 95%. Binding to plasma proteins is insignificant, it penetrates the blood-brain barrier. Regardless of the route of administration, a significant increase in the concentration of ademetionine in the cerebrospinal fluid is noted. Metabolised in the liver.Half-life (T1/2) - 1.5 hours. It is excreted by the kidneys.

    Indications:

    - chronic non-calculous cholecystitis;

    - cholangitis;

    - intrahepatic cholestasis, including in pregnant women;

    - Hepatitis of various genesis: viral, toxic, incl. alcoholic and medicinal origin (antibiotics, antitumor, antituberculosis and antiviral drugs, tricyclic antidepressants, oral contraceptives);

    - fatty degeneration of the liver;

    - cirrhosis of the liver;

    - encephalopathy, incl. associated with hepatic insufficiency (alcohol and other);

    - alcoholic liver disease;

    - depression (including secondary);

    - abstinence syndrome (alcoholic, etc.)

    Contraindications:

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

    Carefully:

    Pregnancy (I term)

    Lactation period

    Bipolar disorders (see section "Special instructions")

    Pregnancy and lactation:

    Possible use of the drug in the II trimester of pregnancy with intrahepatic cholestasis. Admission of high doses of ademetionine in the III trimester of pregnancy did not cause undesirable effects. Admission in the first trimester of pregnancy and in the lactation period is possible if the potential benefit to the mother exceeds the possible risk to the fetus or the baby.

    Dosing and Administration:

    Intramuscularly (in / m), intravenously (iv). With intensive therapy - in the first 2-3 weeks of treatment, heptorum is prescribed in a dose of 400-800 mg / day IV in a drip (very slow) or in / m. The lyophilizate is dissolved only in a special applied solvent (solution Llysine). After the completion of intensive care, maintenance therapy is performed using a medicinal form of heptor for oral administration (400 mg tablets ademethionine).

    Side effects:

    Among the most frequent adverse reactions noted: nausea, abdominal pain and diarrhea.

    From the immune system: hypersensitivity reactions, anaphylactoid or anaphylactic reactions (including hyperemia of the skin, dyspnea, bronchospasm, back pain, discomfort in the chest, lowering blood pressure, increasing blood pressure, tachycardia, bradycardia).

    From the respiratory system: swelling of the larynx.

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

    Infections and infestations: urinary tract infections.

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

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

    From the digestive system: bloating, abdominal pain, diarrhea, dry mouth, indigestion, 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.

    Overdose:

    There were no cases of overdose.

    Interaction:Interaction with other drugs was not observed.
    Special instructions:

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

    When using ademetionin in patients with cirrhosis of the liver against a background of hyperaemia, a systematic control of the nitrogen content in the blood is necessary, during prolonged 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 lyophilizate differs from the proper one (see section "Description"), it is necessary to refrain from using it.

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

    Patients with depression have an increased risk of suicide and other serious adverse events, so during treatment with ademethionine, such patients should be under constant medical supervision to evaluate and treat the symptoms of depression. Patients should inform the doctor if their symptoms of depression do not decrease or worsen with ademethionine therapy. There are also reports of sudden onset or worsening of anxiety in patients taking ademethionine. In most cases, cancellation of therapy is not required, in several cases, anxiety disappeared after a dose reduction or drug withdrawal.

    Since the deficiency of cyanocobalamin and folic acid can reduce ademetionin in patients at risk (with anemia, liver disease,when pregnancy or the probability of vitamin deficiency, in connection with other diseases or diet, for example, in vegetarians), you should control the vitamin content in the blood plasma. If insufficiency is detected, the administration of cyanocobalamin and folic acid is recommended before treatment with ademethionine or simultaneous administration with ademethionine. In immunoassay, the use of ademetionine may contribute to a false determination of the high homocysteine ​​content in the blood.

    For patients receiving ademethionine, it is recommended to use non-immunological assays to determine the content of homocysteine.

    Form release / dosage:Lyophilizate for the preparation of solution for intravenous and intramuscular injection 400 mg.

    Solvent on 5 ml.

    Packaging:

    Lyophilizate for the preparation of a solution for intravenous and intramuscular administration of 400 mg in bottles of colorless, neutral glass.

    Solvent on 5 ml in bottles of colorless, neutral glass or in ampoules of neutral glass.

    5 vials with lyophilizate and 5 vials or ampoules with a solvent in a contour squamous packaging.1 contour pack together with instructions for use in a cardboard pack. For 30, 50 vials with lyophilizate with an equivalent number of vials or ampoules with a solvent together with instructions for use in a cardboard box (for hospitals).

    Storage conditions:

    At a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:2 years (for lyophilizate). 3 years (for solvent). Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-006254/10
    Date of registration:01.07.2010 / 27.07.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:LENS-PHARM, LLC LENS-PHARM, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp02.04.2017
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