Heptral, 500 mg 20 pcs.

Indications

• Intrahepatic cholestasis in precirrhotic and cirrhotic conditions, which may be observed in the following diseases:
  • fatty liver dystrophy;
  • chronic hepatitis;
  • toxic liver lesions of various etiologies, including alcoholic, viral, drug (antibiotics; anticancer, anti-tuberculosis and antiviral drugs, tricyclic antidepressants, oral contraceptives);
  • chronic acute cholecystitis;
  • cholangitis;
  • liver cirrhosis;
  • encephalopathy, including those associated with hepatic
• Encephalopathy including that associated with liver failure (alcoholic, etc.).

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Active ingredient

Ademetionine

Composition

1 tablet contains:

Active ingredients: Ademetionine 1,4-butanedisulfonate 949 mg, corresponding to the content of ademetionine ion 500 mg;

Excipients:

Colloidal silicon dioxide – 5 mg,
microcrystalline cellulose – 118 mg,
sodium carboxymethyl starch (type A) – 22 mg,

Sodium metabisulfonate – 10 mg.5 mg,

microcrystalline cellulose – 118 mg,

sodium carboxymethyl starch (type A) – 22 mg,

magnesium stearate – 5.5 mg.

Shell composition: 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.

How to take, the dosage

Orally.

Tablets should be taken whole without chewing, preferably in the morning between meals.
Tablets of the drug Heptral® should be removed from the blister immediately before oral intake. If the color of tablets is different from white to white with yellowish tint (because of aluminum foil leakage), Heptral® preparation is not recommended.

Initial therapy:

• Recommended dose is 10-25 mg/kg/day orally.
• Intrahepatic cholestasis/ increased fatigue in chronic liver disease
• Dose is 800 mg/day to 1600 mg/day.

Depression

• Dose is 800 mg/d to 1600 mg/d.
• Duration of therapy is determined by the physician.

The therapy with Heptral® may be initiated by intravenous or intramuscular injection followed by administration of Heptral® tablets or directly with Heptral® tablets.

Patients in elderly patients:

Clinical experience with Heptral® has not shown any difference in efficacy between elderly patients and younger patients. However, taking into account high possibility of existing hepatic, renal or cardiac impairment, other comorbidities or concomitant therapy with other medicinal products, the dosage of Heptral® should be adjusted with caution in elderly patients starting from the lowest dose range.

Renal Impairment:

There are limited clinical data available on the use of Heptral® in patients with renal impairment; therefore, caution is recommended when using Heptral® in these patients.

Hepatic failure:

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

Children:

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

Interaction

No known interactions with other drugs have been observed.

There is a report of serotonin excess syndrome in a patient taking ademetionine and clomipramine. It is believed that this interaction is possible and ademetionine should be prescribed with caution together with selective serotonin reuptake inhibitors, tricyclic antidepressants (such as clomipramine), and herbs and drugs containing tryptophan.

Special Instructions

Taking into account the tonic effect of the drug, it is not recommended to take it before going to bed. When using Heptral® by patients with liver cirrhosis against hyperazotemia background, systematic monitoring of blood nitrogen content is required. During long-term therapy it is necessary to determine the serum urea and creatinine content.

There are reports about the conversion of depression into hypomania or mania in patients taking Ademetionine.

Patients with depression have an increased risk of suicide and other serious adverse events, so such patients should be under constant medical supervision during ademetionine treatment for evaluation and treatment of depression symptoms. Patients should inform the doctor if their symptoms of depression do not decrease or worsen during ademetionine therapy.

There are also reports of the sudden appearance or increase in anxiety in patients taking ademetionine. In most cases it is not necessary to cancel the therapy, in a few cases the anxiety disappeared after reducing the dose or canceling the drug.

Since cyanocobalamin and folic acid deficiency may decrease the content of ademetionine in patients at risk (with anemia, liver disease, pregnancy or the possibility of vitamin deficiency due to other diseases or diet, such as vegetarians), the plasma vitamin content should be controlled. If insufficiency is detected, cyanocobalamin and folic acid intake prior to ademetionine treatment or concomitant administration with ademetionine is recommended.

In immunological analysis, the use of ademetionine may contribute to the false detection of high homocysteine content in the blood.

For patients taking ademetionine, it is recommended to use non-immunological methods of analysis to determine homocysteine content.

Influence on the ability to drive and operate machinery

In some patients dizziness may occur while taking Heptral®. It is not recommended to drive a vehicle or operate machinery while taking this medicine until the patient is sure that the therapy does not affect the ability to perform this type of activity.

Synopsis

Intestine-coated, film-coated, white to white with a yellowish tint, oval, biconvex.

Contraindications

Genetic disorders that affect the methionine cycle, and/or cause homocystinuria and/or hyperhomocysteinemia (cystathionine betasynthase deficiency, disorder of vitamin B12 metabolism).

Hypersensitivity to any of the drug components.

Age under 18 years (experience of medical use in children is limited).

Bipolar disorders.

With caution:

Pregnancy (first trimester) and the period of breastfeeding (use is possible only if the potential benefit to the mother exceeds the possible risk to the fetus or baby).

Simultaneous use with selective serotonin reuptake inhibitors (SSRIs), tricyclic antidepressants (such as clomipramine), and herbal and tryptophan preparations.

Elderly age.

Renal insufficiency.

Side effects

The digestive system: frequently – nausea, abdominal pain, diarrhea; rarely – vomiting, dry mouth, esophagitis, dyspepsia, flatulence, gastrointestinal pain, gastrointestinal bleeding, liver colic.

Nervous system: rare – confusion, insomnia, dizziness, headache, paresthesia.

Musculoskeletal system: rare – arthralgia, muscle cramps.

Urinary system: rare – urinary tract infections.

Skin: rare – hyperhidrosis, itching, skin rash.

Local reactions: rare – reactions at the injection site, very rare – reactions at the injection site, necrosis of the skin at the injection site.

Allergic reactions: rare – anaphylactic reactions, very rare – Quincke’s edema, laryngeal edema.

Other: rare – flushes, superficial phlebitis, asthenia, chills, flu-like symptoms, weakness, peripheral edema, hyperthermia.

Overdose

In case of overdose, patient monitoring and symptomatic therapy are recommended.

Pregnancy use

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

Similarities

Heptral, Heptor, Samelix, Irritable bowel