Samelix, 400 mg 20 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

After a single oral dose of 400 mg, C_max of ademetionine in plasma is reached after 2-6 hours and is 0.7 mg/l. Bioavailability of the drug when administered orally is 5%, when administered by injection – 95%.

The binding to serum proteins is insignificant.

It penetrates through the barrier. Regardless of the route of administration there is a significant increase in concentration of ademetionine in cerebrospinal fluid. It is metabolized in the liver. T_1/2 – 1.5 h. It is excreted with the kidneys.

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 film-coated, enteric-soluble tablet contains:

Active ingredient:
ademetionine 1,4-butanedisulfonate 760 mg (in terms of ademetionine 400 mg);

Excipients:

sodium carboxymethyl starch 18 mg,

colloidal silica 9 mg,

Magnesium stearate 4.5 mg,

microcrystalline cellulose 108.5 mg;

film coating composition: Opadray transparent 15 mg, including: hypromellose (hydroxypropyl methylcellulose) 12 mg, macrogol (polyethylene glycol) 3 mg; Acryl-Iz white 60 mg, including: methacrylic acid and ethyl acrylate copolymer [1:1] 39.6 mg, colloidal silica 0.6 mg, sodium hydrocarbonate 0.6 mg, sodium lauryl sulfate 0.3 mg, talc 9.9 mg, titanium dioxide 9 mg; Triethylcitrate 5 mg.

How to take, the dosage

Orally. Tablets should be taken whole without chewing, preferably in the morning between meals.

Tablets of the preparation Samelix® should be removed from the blister immediately before oral intake. If the color of tablets is different from white to white with yellowish tint (due to aluminum foil leakage) Samelix® should not be used.

Initial therapy

The recommended dose is 10-25 mg/kg/day.

Intrahepatic cholestasis

The dose is 800 mg/day to 1600 mg/day.

Depression

The dose is from 800 mg/day to 1600 mg/day.

The duration of therapy is determined by the physician. Therapy with ademetionine may be initiated by intravenous or intramuscular injection followed by the use of Samelix® tablets or directly from the use of Samelix® tablets.

In elderly patients

Clinical experience of using Samelix® did not reveal any differences in its effectiveness in elderly patients and in younger patients. However, taking into account high probability of hepatic, renal or cardiac impairment, other concomitant pathology or concomitant therapy with other medicinal products, the dose of Samelix® should be adjusted with caution in elderly patients starting from the lower limit of the dose range.

Renal impairment

There are limited clinical data on the use of ademetionine in patients with renal impairment, therefore, caution is recommended when using Samelix® in such patients.

Hepatic failure

Parameters of pharmacokinetics of ademetionine are similar in healthy volunteers and in patients with chronic liver disease.

Children

The use of the drug Samelix® in children is contraindicated (efficacy and safety are not established).

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.

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.

Similarities

Heptral, Heptor, Irritable bowel