Heptral pills 500mg, 20pcs

Composition

>of 1 tab. contains: Active ingredients: ademetionine 1,4-butane disulfonate 949 mg, which corresponds to the content of ademetionine ion 500 mg; Excipients: colloidal silicon dioxide – 5.5 mg, microcrystalline cellulose-118 mg, sodium carboxymethyl starch (type A) – 22 mg, magnesium stearate-5.5 mg. The composition of the shell: methacrylic acid and ethylacrylate copolymer (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.

Pharmacological properties

Pharmacotherapeutic group: other drugs for the gastrointestinal tract and metabolism, amino acids and their PROIZVODNYKh ATKH: A 16 AA 02 Pharmacological properties. Pharmacodynamics . Ademetionine belongs to the group of hepatoprotectors, also possesses antidepressant activity. It has a choleretic and cholekinetic effect, has detoxifying, regenerating, antioxidant, antifibrosing and neuroprotective properties. It makes up for the deficiency of S-adenosyl-L-methionine (ademetionine) and stimulates its production in the body. It is found in all body environments. The highest concentration of ademetionine was found in the liver and brain. It plays a key role in the metabolic processes of the body, takes part in important biochemical reactions: transmethylation, transsulfurization, transamination. In transmethylation reactions, ademetionine donates a methyl group for the synthesis of phospholipids of cell membranes, neurotransmitters, nucleic acids, proteins, hormones, etc. In transulfurization reactions, ademetionine is a precursor of cysteine, taurine, glutathione (providing the redox mechanism of cellular detoxification), and coenzyme A (included in the 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 the content of methionine in serum, normalizing metabolic reactions in the liver. After decarboxylation, it participates in aminopropylation reactions as a precursor of polyamines-putrescine (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. Ademetionine normalizes the synthesis of endogenous phosphatidylcholine in hepatocytes, which increases the fluidity and polarization of membranes. This improves the function of bile acid transport systems associated with hepatocyte membranes and promotes the passage of bile acids into the biliary tract. It is effective for intralobular cholestasis (violation of bile synthesis and flow). Ademetionine reduces the toxicity of bile acids in the hepatocyte by conjugating and sulfating them. 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, the sulfated bile acids themselves additionally protect the liver cell membranes from the toxic effects of unsulfated bile acids (in high concentrations present in hepatocytes in intrahepatic cholestasis). In patients with diffuse liver diseases (cirrhosis, hepatitis) with intrahepatic cholestasis syndrome, ademetionine reduces the severity of pruritus and changes in biochemical parameters, including the concentration of direct bilirubin, the activity of alkaline phosphatase, aminotransferases, etc. Choleretic and hepatoprotective effects persist for up to 3 months after discontinuation of treatment. It is shown to be effective in hepatopathies caused by various hepatotoxic drugs. Antidepressant activity appears gradually, starting from the end of the first week of treatment, and stabilizes during 2 weeks of treatment. A number of studies have confirmed the effectiveness of ademetionine in the treatment of fatigue in patients with chronic liver disease. A pooled analysis of data obtained from patients with pre-treatment symptoms of increased fatigue demonstrated the effect of ademetionine treatment on reducing symptoms of increased fatigue in combination with a number of other symptoms, such as depression, icteric skin and mucous membranes, malaise and pruritus. Treatment with ademetionine significantly improved mood in patients with alcoholic liver disease, who simultaneously achieved a positive response from the symptoms of increased fatigue. In addition, patients with alcoholic liver disease and non-alcoholic fatty liver disease who responded to ademetionine treatment with fatigue symptoms also showed a significant reduction in symptoms such as icteric skin and mucous membranes, malaise and pruritus.

Indications

• Intrahepatic cholestasis in precirrotic and cirrhotic conditions, which can be observed in the following diseases:
  • adipose dystrophy of the liver;
  • chronic hepatitis;
  • toxic liver lesions of various etiologies, including alcoholic, viral, medicinal (antibiotics; antitumor, antituberculous and antiviral drugs, tricyclic antidepressants, oral contraceptives);
  • chronic stone-free cholecystitis;
  • cholangitis;
  • cirrhosis of the liver;
  • encephalopathy, including those associated with liver failure (alcohol, etc. ).
• Intrahepatic cholestasis in pregnant women.
• Symptoms of depression.
• Increased fatigue in chronic liver diseases.

Use during pregnancy and lactation

Clinical studies have shown that the use of ademetionine in the third trimester of pregnancy did not cause any undesirable effects. The use of Heptral® in pregnant women in the first trimester and during breastfeeding is possible only if. the potential benefit to the mother outweighs the potential risk to the fetus or baby.

Contraindications

Genetic disorders affecting the methionine cycle and / or causing homocystinuria and/or hyperhomocysteinemia (cystathionine betasynthase deficiency, impaired vitamin B12 metabolism). Hypersensitivity to any of the components of the drug. Under 18 years of age (limited medical experience in children). Bipolar disorders. With caution:

Pregnancy (First trimester) and breast-feeding (use only if the potential benefit to the mother exceeds the possible risk to the fetus or child).

Concomitant use with selective serotonin reuptake inhibitors (SSRIs), tricyclic antidepressants (such as clomipramine), as well as herbal and tryptophan-containing medications.

Advanced age.

Kidney failure.

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. Musculoskeletal disorders: rarely-arthralgia, muscle cramps. From the urinary system: rarely-urinary tract infections. From the skin: rarely-hyperhidrosis, pruritus, skin rash. Local reactions: rarely-injection site reactions; very rarely-injection site reactions, 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

No known interactions with other drugs have been observed. There is a report of an excess serotonin syndrome in a patient taking ademetionine and clomipramine. It is considered that such an interaction is possible and caution should be exercised when prescribing ademetionine together with selective serotonin reuptake inhibitors, tricyclic antidepressants (such as clomipramine), as well as herbs and drugs containing tryptophan.

How to take, course of use and dosage

Inside. Tablets should be taken whole, without chewing, preferably in the morning between meals. Tablets of Heptral® should be removed from the blister immediately before ingestion. If the tablets have a color other than white to white with a yellowish tinge (due to leakage of aluminum foil), the drug Heptral® is not recommended. Initial therapy:

• The recommended oral dose is 10-25 mg/kg/day.
• Intrahepatic cholestasis/ increased fatigue in chronic liver diseases
• The dose ranges from 800 mg / day to 1600 mg / day.

Depression

• The dose ranges from 800 mg / day to 1600 mg / day.
• The duration of therapy is determined by the doctor.

Therapy with Heptral® can be initiated with intravenous or intramuscular use, followed by the use of Heptral® in tablet form, or immediately with the use of Heptral® in tablet form.

Elderly patients:

Clinical experience with the use of Heptral® has not revealed any differences in its effectiveness in elderly and younger patients. However, given the high probability of existing liver, kidney or heart disorders, other comorbidities, or concomitant therapy with other medications, the dose of Heptral® in elderly patients should be selected with caution, starting with the lower limit of the dose range.

Kidney failure:

There are limited clinical data on the use of Heptral® in patients with renal insufficiency, and therefore caution is recommended when using Heptral® in such patients.

Liver failure:

The pharmacokinetic parameters of ademetionine are similar in healthy volunteers and in patients with chronic liver disease.

Children:

The use of Heptral® in children is contraindicated (efficacy and safety have not been established).

Overdose

In case of overdose, it is recommended to monitor the patient and conduct symptomatic therapy.

Description

Tablets coated with an enteric coating, film, white to white with a yellowish tinge of color, oval, biconvex.

Special instructions

Given the tonic effect of the drug, it is not recommended to take it before bedtime. When using the drug Heptral® in patients with cirrhosis of the liver on the background of hyperazotemia, systematic monitoring of the nitrogen content in the blood is necessary. During long-term therapy, it is necessary to determine the content of urea and creatinine in the blood serum. There have been reports of depression turning into hypomania or mania in patients taking ademetionine. Patients with depression have an increased risk of suicide and other serious adverse events, so during treatment with ademetionine, such patients should be constantly monitored by a doctor to assess and treat symptoms of depression. Patients should inform the doctor if their symptoms of depression do not decrease or worsen with ademetionine therapy. There have also been reports of sudden onset or increased anxiety in patients taking ademetionine. In most cases, discontinuation of therapy is not required; in some cases, anxiety disappeared after reducing the dose or discontinuing the drug. Since cyanocobalamin and folic acid deficiency can reduce ademetionine levels in patients at risk (with anemia, liver disease, pregnancy or the likelihood of vitamin deficiency, due to other diseases or diet, for example, in vegetarians), the content of vitamins in the blood plasma should be monitored. If insufficiency is detected, it is recommended to take cyanocobalamin and folic acid before starting treatment with ademetionine or simultaneously with ademetionine. In an immunological analysis, the use of ademetionine may contribute to a false determination of the indicator of high homocysteine content in the blood. For patients taking ademetionine, it is recommended to use non-immunological methods of analysis to determine the content of homocysteine.

Influence on the ability to drive a car and work with mechanisms

Some patients may experience dizziness while taking Heptral®. It is not recommended to drive a car or work with mechanisms while taking the drug until the patient is sure that the therapy does not affect the ability to engage in this type of activity.

Form of production

Enteric coated tablets,500 mg.

Storage conditions

In a dark place at a temperature of 15°C to 25°C. Keep out of reach of children.

Shelf life

1 year

Active ingredient

Ademetionine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets