There were no clinical cases of overdose.
genetic disorders that affect the methionine cycle and / or cause homocystinuria and / or hyperhomocysteinemia (cystathionine beta-synthase deficiency, impaired vitamin B metabolism12),
hypersensitivity to any of the components of the drug,
age up to 18 years.
With caution: bipolar disorders (see "Special instructions"), pregnancy (first trimester), breast-feeding period.
No known interactions with other drugs were observed.
There is a report of an excess serotonin syndrome in a patient taking ademetionine and clomipramine. It is believed that such an interaction is possible, and ademetionine should be prescribed with caution together with SSRIs, tricyclic antidepressants (such as clomipramine), as well as herbs and drugs containing tryptophan..
Enteric-coated tablets
The most common adverse reactions are nausea, abdominal pain, and diarrhea. The following are generalized data on adverse reactions that were observed against the background of the use of ademetionine both in tablets and in injectable dosage form.
From the immune system: laryngeal edema, allergic reactions.
On the skin side: sweating, itching, rash, Quincke's edema, skin reactions.
Infections and infestations: urinary tract infections.
From the nervous system: dizziness, headache, paresthesia, restlessness, confusion, insomnia.
From the CCC side: hot flushes, phlebitis of the superficial veins, cardiovascular disorders.
From the digestive system: bloating, abdominal pain, diarrhea, dry mouth, dyspepsia, esophagitis, flatulence, gastrointestinal disorders, gastrointestinal bleeding, nausea, vomiting, hepatic colic, cirrhosis of the liver.
From the musculoskeletal system: arthralgia, muscle spasms.
Other: asthenia, chills, flu-like syndrome, malaise, peripheral edema, fever.
intrahepatic cholestasis in precirrotic and cirrhotic conditions, which can be observed in the following diseases:
- fatty degeneration of the liver,
- chronic hepatitis,
- toxic liver lesions of various etiologies, including alcoholic, viral, medicinal (antibiotics, antitumor, anti-tuberculosis 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.
Ademetionine belongs to the group of hepatoprotectors, it also has 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 observed in the liver and brain.
It plays a key role in the metabolic processes of the body, takes part in important biochemical reactions: transmethylation, transulfation, transamination.
In transmethylation reactions, ademetionine donates a methyl group for the synthesis of cell membrane phospholipids, neurotransmitters, nucleic acids, proteins, hormones, etc. In the trans-sulfation reactions, ademetionine is a precursor of cysteine, taurine, glutathione (providing the redox mechanism of cellular detoxification), coenzyme acetylation (it is 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 the plasma, reduces the content of methionine in the 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 spermin, 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 the bile acid transport systems associated with the hepatocyte membranes and promotes the passage of bile acids into the biliary system. It is effective in the intrahepatic (intra-lobular and inter-lobular) variant of cholestasis (violation of the synthesis and flow of bile). 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 excretion from the hepatocyte. The process of sulfation of bile acids contributes to the possibility of their elimination by the kidneys, facilitates the passage through the hepatocyte membrane 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 with intrahepatic cholestasis).
In patients with diffuse liver diseases (cirrhosis, hepatitis) with intrahepatic cholestasis syndrome, ademetionine reduces the severity of itching and changes in biochemical parameters, including the level of direct bilirubin, the activity of alkaline phosphatase, aminotransferases, etc. The 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. Administration to patients with opioid addiction, accompanied by liver damage, leads to regression of clinical manifestations of abstinence, improvement of the functional state of the liver and the processes of microsomal oxidation.
Antidepressant activity manifests itself gradually, starting from the end of the first week of treatment, and stabilizes within 2 weeks of treatment. It is effective in recurrent endogenous and neurotic depression, resistant to amitriptyline. It has the ability to interrupt the relapse of depression.
Administration in osteoarthritis reduces the severity of pain, increases the synthesis of proteoglycans and leads to partial regeneration of cartilage tissue.
The oral bioavailability is 5%. With a single oral dose of 400 mg Smax - 0.7 mg/l, Tmax - 2-6 hours —
The connection with plasma proteins is insignificant, it penetrates through the BBB. There is a significant increase in the concentration of the drug in the cerebrospinal fluid.
It is metabolized in the liver. T1/2 - 1.5 hours — It is excreted by the kidneys.
The tablets are coated with a special coating that dissolves only in the intestine, so that ademetionine is released in the duodenum.
Ademetionine-Vial
Ademetionine
Inside. Tablets should be taken whole, without chewing, preferably in the morning, between meals.
Tablets of the drug Heptral® it should be removed from the blister immediately before ingestion. The dose is from 800 to 1600 mg/day.
The duration of therapy is determined by the doctor.
A16AA02 Ademetionine
