Heptral tablets p / o enteric 500mg №10×2

Name:
Geptral tab. in pack. No. 10×2
Description:
: Tablets, enteric-coated, film-coated, from white to light yellow, oval, biconvex, smooth. The main active ingredient Ademetionine Release form Enteric-coated tablets, film-coated, from white to light yellow, oval, biconvex, smooth. 1 tab. Active substance: ademetionine 1,4-butanedisulfonate 949 mg, which corresponds to the content of ademetionine ion 500 mg . The composition of the shell: a copolymer of methacrylic acid and ethyl acrylate (1: 1) – 32.63 mg, macrogol 6000 – 9.56 mg, polysorbate 80 – 0.52 mg, simethicone emulsion (30%) – 0.4 mg, sodium hydroxide – 0.44 mg, talc – 21.77 mg. 10 pieces. – blisters (1) – packs of cardboard. 10 pieces. – blisters (2) – packs of cardboard. Dosage 500mg in bl. in pack. No. 10×2 Special instructions Use ademetionine with caution in patients with renal insufficiency, 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 at usual doses is recommended. Patients with depression require careful monitoring and ongoing psychiatric care while on ademetionine treatment to monitor the effectiveness of the treatment. When used in patients with cirrhosis of the liver on the background of 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 the ability to drive 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 in these activities. Pharmacological action Hepatoprotector, has antidepressant activity. It has a choleretic and cholekinetic effect. It has detoxifying, regenerating, antioxidant, antifibrosing and neuroprotective properties. 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 (donator of the methyl group) – the molecule of S-adenosyl-L-methionine (ademetionine), is a donator of the methyl group in the reactions of methylation of phospholipids of cell membranes, proteins, hormones, neurotransmitters; participates in transsulfation 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 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 (a stimulator of cell regeneration and hepatocyte proliferation), spermidine and spermine, which are part of the structure of ribosomes. It has a choleretic effect due to an increase in the 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. It is effective in the intralobular variant of 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 contributes to the possibility of their elimination by the kidneys, facilitates passage through the membrane of the hepatocyte and excretion with bile. In addition, sulfated bile acids protect the membranes of liver cells from the toxic effects of non-sulfated bile acids (in high concentrations present in hepatocytes in intrahepatic cholestasis). In patients with diffuse liver diseases (cirrhosis, hepatitis) with intrahepatic cholestasis syndrome, it reduces the severity of pruritus and changes in biochemical parameters, incl. level of direct bilirubin, activity of alkaline phosphatase, aminotransferases. Pharmacokinetics After a single oral dose of 400 mg, 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%, with a / m administration – 95%. Serum protein binding 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 with the kidneys. Indications for use Intrahepatic cholestasis in precirrhotic and cirrhotic conditions, including: fatty degeneration of the liver; chronic hepatitis; toxic liver damage of various etiologies, including alcoholic, viral, medicinal (antibiotics, antitumor, antituberculosis and antiviral drugs, tricyclic antidepressants, oral contraceptives); chronic acalculous cholecystitis; cholangitis; cirrhosis of the liver; encephalopathy, incl. associated with liver failure (including alcohol). Intrahepatic cholestasis in pregnant women. Symptoms of depression. Dosage and administration 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 set individually depending on the severity and course of the disease. In elderly patients, it is recommended to start treatment with the lowest recommended dose, taking into account the decrease in hepatic, renal or cardiac function, the presence of concomitant pathological conditions and the use of other drugs. Application during pregnancy and lactation In the I and II trimesters of pregnancy, ademetionine is used only if absolutely necessary, 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. Precautions Use ademetionine with caution in patients with renal insufficiency, with bipolar disorders, simultaneously with selective serotonin reuptake inhibitors, tricyclic antidepressants (such as clomipramine); herbal preparations and preparations containing tryptophan; in elderly patients. Interaction with other drugs There is a report on the development of serotonin syndrome in a patient who used ademetionine and clomipramine. Ademetionine should be used with caution concomitantly with selective serotonin reuptake inhibitors, tricyclic antidepressants, preparations and herbal remedies containing tryptophan. Contraindications Genetic disorders affecting the methionine cycle and / or causing homocystinuria and / or hyperhomocysteinemia (deficiency of cystathion beta synthetase, impaired metabolism of cyanocobalamin); children and adolescents under 18 years of age, hypersensitivity to ademetionine. Composition Active substance: ademetionine 1,4-butanedisulfonate 949 mg, which corresponds to the content of ademetionine ion 500 mg . The composition of the shell: a copolymer of methacrylic acid and ethyl acrylate (1: 1) – 32.63 mg, macrogol 6000 – 9.56 mg, polysorbate 80 – 0.52 mg, simethicone emulsion (30%) – 0.4 mg, sodium hydroxide – 0.44 mg, talc – 21.77 mg. Side effect 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. 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. 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 – Quincke’s edema, laryngeal edema. Other: rarely – hot flashes, superficial phlebitis, asthenia, chills, flu-like symptoms, weakness, peripheral edema, hyperthermia. Storage conditions At a temperature not higher than 25 °C. Keep out of the reach of children! Buy Heptral tablets p / o enteric soluble 500 mg No. 10×2