Heptral, 400 mg 20 pcs

Pharmacotherapeutic group Other drugs for gastrointestinal tract and metabolism, amino acids and their derivatives

ATC code A16AA02

Pharmacological properties.

Pharmacodynamic

Ademetionine belongs to the group of hepatoprotectors, also has antidepressant activity. It has choleretic and cholokinetic effect, has detoxifying, regenerating, antioxidant, antifibrotic and neuroprotective properties.

It replenishes the S-adenosyl-L-methionine (ademetionine) deficiency and stimulates its production in the body, contained in all body fluids. The highest concentration of ademetionine is found in the liver and brain. Ademetionine plays a key role in the metabolic processes of the body and takes part in major biochemical reactions: transmethylation, transsulfurization and transamination.

In transmethylation reactions ademetionine donates methyl groups for the synthesis of cell membrane phospholipids, neurotransmitters, nucleic acids, proteins, hormones and others. In transsulfurization reactions ademetionine is a precursor of cysteine, taurine, glutathione (providing redox mechanism of cellular detoxification), coenzyme A (is included into biochemical reactions of tricarboxylic acid cycle and fills the cell energy potential).

Increases glutamine content in the liver, plasma cysteine and taurine, decreases methionine content in the serum, normalizing metabolic reactions in the liver. After decarboxylation it participates in aminopropylation reactions as a precursor of polyamines – putrescine (promoter of cell regeneration and hepatocyte proliferation), spermidine and spermin, included in the structure of ribosomes, which reduces the risk of fibrosis.

It has choleretic action. Ademetionine normalizes the synthesis of endogenous phosphatidylcholine in hepatocytes, which increases membrane fluidity and polarization. This improves the function of bile acid transport systems associated with membranes of hepatocytes and contributes to bile acid passage to biliary tracts.

Effective with intradolocular variant of cholestasis (disorders of bile synthesis and flow). Ademetionine reduces the toxicity of bile acids in the hepatocyte by performing their conjugation and sulfation. Conjugation with taurine increases solubility of bile acids and their excretion from the hepatocyte. The process of sulfation of bile acids promotes the possibility of their elimination by the kidneys, facilitates the passage through the hepatocyte membrane and excretion with bile. In addition, sulfated bile acids themselves additionally protect liver cell membranes from toxic effects of nonsulfated bile acids (in high concentrations present in hepatocytes with intrahepatic cholestasis).

In patients with diffuse liver diseases (cirrhosis, hepatitis) with intrahepatic cholestasis syndrome, ademetionine reduces the severity of skin itching and changes of biochemical parameters, including the concentration of direct bilirubin, alkaline phosphatase activity, aminotransferases and others. Choleretic and hepatoprotective effect persists 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 from the end of the first week of treatment and stabilizes during 2 weeks of treatment.

Several studies have confirmed the effectiveness of ademetionine in treatment of increased fatigability in patients with chronic liver disease. A pooled analysis of data from patients with pre-treatment symptoms of fatigue proved the effect of ademetionine treatment in reducing symptoms of increased fatigue in conjunction with a number of other symptoms, such as depression, hiccuria of the skin and mucous membranes, malaise and skin itching.

Ademetionine treatment significantly improved mood in patients with alcoholic liver disease who had a simultaneous positive response from symptoms of increased fatigue. In addition, in patients with alcoholic liver disease and nonalcoholic fatty liver disease with achieved response to ademetionine treatment on the side of fatigue symptoms there was also observed a significant reduction in such symptoms as acidity of the skin and mucous membranes, malaise and skin itching.

Indications

The drug Heptral® is used in adults over the age of 18 years as an adjuvant therapy for established chronic liver diseases, to improve and maintain its functions; with increased fatigue and established chronic liver diseases.

If there is no improvement or you feel worse, you should consult a doctor.

Special instructions

Before taking Heptral®, consult your doctor or pharmacist. This is especially important if:
if you have impaired kidney function;
if you are an elderly person;
if you suffer from depression or are taking antidepressants from the group of selective serotonin reuptake inhibitors (SSRIs), tricyclic antidepressants (such as clomipramine) or medicines containing the amino acid tryptophan, including herbal ones;
if you have a deficiency of vitamin B12 and/or folic acid.
You should not take Heptral® before bed due to its tonic effect. Heptral® may cause a false increase in plasma homocysteine ​​levels.

Children

Heptral® is contraindicated in children under 18 years of age.

Driving or operating machinery

The drug Heptral® can rarely cause dizziness and a decrease in blood pressure. If you feel dizzy, refrain from driving or operating machinery.

Active ingredient

Ademetionine

Composition

The active ingredient is ademetionine.

Each enteric film-coated tablet contains 400 mg of ademetionine (as ademetionine 1,4-butane disulfonate 760 mg).

Other ingredients (auxiliary substances) are colloidal silicon dioxide, microcrystalline cellulose, sodium carboxymethyl starch (type A), magnesium stearate, methacrylic acid and ethyl acrylate copolymer (1:1), macrogol-6000, polysorbate-80, simethicone emulsion (30%), sodium hydroxide, talc, water.

Pregnancy

If you are pregnant or breastfeeding, think you may be pregnant, or are planning a pregnancy, consult your doctor or pharmacist before using this drug.

The use of Heptral® during pregnancy and breastfeeding is not recommended without medical supervision.

Contraindications

Do not take Heptral®:
if you are allergic to ademetionine or any of the other ingredients of the medicine listed in section 6 of the leaflet;
if you have genetic disorders that affect the methionine cycle and/or cause homocystinuria and/or hyperhomocysteinemia (for example, deficiency of the enzyme cystathionine beta synthetase, impaired metabolism of vitamin B12);
if you have bipolar disorder;
if you are under 18 years old

Side Effects

Like all medicines, Heptral® can cause side effects, although not everyone gets them.

Possible adverse reactions that may occur when taking Heptral®:

Common (may affect up to 1 in 10 people):
anxiety,
insomnia,
headache,
stomach pain,
diarrhea,
nausea,
skin itching,
severe fatigue (asthenia).

Uncommon (may affect up to 1 in 100 people):
urinary tract infections (eg cystitis),
hypersensitivity reactions,
anaphylactoid or anaphylactic reactions (including redness of the skin, shortness of breath, bronchospasm, back pain, chest discomfort, changes in blood pressure [decreased blood pressure, increased blood pressure] or pulse rate [increased, decreased]),
strong emotional arousal accompanied by motor restlessness (agitation),
confusion,
dizziness,
disturbance of sensitivity, manifested by tingling or burning (paresthesia),
taste disorders characterized by loss of taste or distortion of taste perception (dysgeusia),
“tides”
difficulty breathing due to swelling of the throat (laryngeal edema),
decrease in blood (arterial) pressure,
inflammation of the venous vessels (phlebitis)
dry mouth,
indigestion (dyspepsia),
increased gas formation in the intestines (flatulence),
gastrointestinal pain,
gastrointestinal bleeding,
gastrointestinal disorders,
vomit,
inflammation of the esophageal mucosa (esophagitis),
increased sweating,
angioedema (rapidly developing swelling of the skin, mucous membranes and subcutaneous fat),
allergic reactions (redness of the skin, severe itching of the skin, rash or very itchy blisters on the skin (urticaria)),
joint pain (arthralgia),
muscle spasms,
edema,
increased body temperature (fever),
chills.

Rare (may affect up to 1 in 1000 people):
bloating,
malaise.

Interaction

Tell your doctor or pharmacist if you are taking, have recently taken, or may start taking any other medications.

This is especially important:
if you are taking SSRI antidepressants (such as citalopram, fluoxetine, paroxetine and sertraline), tricyclic antidepressants (such as clomipramine) or medicines containing the amino acid tryptophan, including herbal ones.

Storage conditions

Store the drug at a temperature not exceeding 25 °C.

Manufacturer

EbbVee S.r.L., Italy