Samelix, lyophilizate 400 mg 5 pcs

Hepatoprotector, has antidepressant activity. It has choleretic and cholekinetic effect. It has detoxifying, regenerating, antioxidant, antifibrotic and neuroprotective properties.

Makes up for the lack of ademetionine and stimulates its production in the body, especially in the liver and brain. S-adenosyl-L-methionine (ademetionine) is a donor of methyl groups in biological reactions of methylation of phospholipids of cell membranes, proteins, hormones and neurotransmitters; It participates in transsulfation reactions as a precursor of cysteine, taurine, glutathione (provides redox mechanism of cellular detoxification), acetylation coenzyme.

Enhances glutamine in the liver, cysteine and taurine in the plasma; decreases methionine in the serum, normalizing metabolic reactions in the liver. Except decarboxylation it participates in processes of aminopropylation as precursor of polyamines – putrescine (stimulator of cell regeneration and proliferation of hepatocytes), spermidine and spermin, entering the structure of ribosomes.

It has choleretic effect caused by increase of motility and polarization of hepatocyte membranes due to stimulation of phosphatidylcholine synthesis in them. This improves function of bile acid transport systems associated with hepatocyte membranes and promotes bile acid passage into bile-excretory system. It is effective in intradolocular variant of cholestasis (disorder of bile synthesis and flow).

It 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 excretion from the hepatocyte. The process of sulfation of bile acids promotes the possibility of their elimination by the kidneys and facilitates their passage through the hepatocyte membrane and excretion with bile.

In addition, sulfated bile acids 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 it reduces severity of skin itching and changes of biochemical indices, including level of direct bilirubin, alkaline phosphate activity, aminotransferases.

Pharmacokinetics

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 etiology, including alcoholic, viral, drug (antibiotics, anti-tumor, anti-tuberculosis and antiviral drugs, tricyclic antidepressants, oral contraceptives);
– Chronic acalculous cholecystitis;
– cholangitis;
– cirrhosis;
– encephalopathy, including those associated with liver.

• Intrahepatic cholestasis in pregnant women;

• Symptoms of depression.

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Active ingredient

Ademetionine

Composition

1 vial of lyophilizate contains:

Active ingredient:

Ademetionine 1,4-butanedisulfonate 760.0 mg, in terms of ademetionine 400.0 mg.

1 ampoule of the solvent contains:

L-lysine monohydrate 384.5 mg, in terms of L-lysine 342.4 mg,

sodium hydroxide solution 1 M to pH 9.8-10.3,

water for injection to 5 ml.

Interaction

There has been a report of serotonin syndrome in a patient using ademetionine and clomipramine.

Ademetionine should be used with caution concomitantly with selective serotonin reuptake inhibitors, tricyclic antidepressants, drugs and herbal products containing tryptophan.

Directions for use

It is used orally, v/m or intravenously (very slowly).

The daily dose is 800-1600 mg when taken orally.

In intravenous or intravenous administration the daily dose is 400-800 mg.

The duration of treatment is determined individually depending on the severity and course of the disease.

In elderly patients, treatment should be started with the lowest recommended dose, taking into account decreased hepatic, renal, or cardiac function, comorbid conditions, and use of other medications.

Special Instructions

Ademetionine should be used with caution in patients with renal impairment, bipolar disorders, concomitantly with selective serotonin reuptake inhibitors, tricyclic antidepressants (such as clomipramine); herbal and tryptophan preparations; in elderly patients.

Deficiency of vitamin B₁₂ and folic acid may lead to decreased concentrations of ademetionine, so their concomitant use at normal doses is recommended.

Patients with depression need close monitoring and ongoing psychiatric care during ademetionine treatment to monitor the effectiveness of treatment.

When used in patients with cirrhosis with a background of hyperazotemia, systematic monitoring of blood nitrogen levels is necessary. Serum urea and creatinine levels should be determined during long-term therapy.

Impact on driving and operating machinery

Ademetionine administration may cause dizziness. Patients should not drive vehicles or operate other mechanisms until symptoms that may affect reaction speed during the above activities have completely disappeared.

Contraindications

Genetic disorders affecting the methionine cycle and/or causing homocystinuria and/or hyperhomocysteinemia (cystathionine beta synthase deficiency, impaired vitamin B12 metabolism);

Hypersensitivity to any of the drug components;

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

Cautions

• Bipolar disorders.
• Pregnancy (first trimester) and breastfeeding period (use possible only if potential benefit to mother exceeds possible risk to fetus and baby).
• Simultaneous use with selective serotonin reuptake inhibitors (SSRIs), tricyclic antidepressants (such as clomipramine), and herbal and tryptophan preparations.
• Elderly age
• Renal insufficiency

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Side effects

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

Nervous system disorders: rarely – confusion, insomnia, dizziness, headache, paresthesias.

Muscular system disorders: rare – arthralgia, muscle cramps.

Urinary system disorders: rarely – urinary tract infections.

The skin: rarely – 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.

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

Pregnancy use

In I and II trimesters of pregnancy, ademetionine is used only when absolutely necessary, when the expected benefit to the mother exceeds the potential risk to the fetus. The use of ademetionine in high doses in the third trimester of pregnancy has not caused any adverse effects.

The use of ademetionine during breastfeeding is possible only if the expected benefit to the mother exceeds the potential risk to the baby.

Similarities

Heptral, Heptor, Irritable bowel