Heptral lyophilized powder for the preparation of injection solution 500 mg (complete with 5 ml solvent) No. 5

Popular questions about Heptral

How to take Heptral?

Treatment begins with injections, then the patient is transferred to oral administration. The tablets are swallowed whole. The daily dose is divided into 2-3 doses. The dosage is calculated based on the recommendations given in the instructions.

Heptral: how often can I take it?

Tablets are taken 2-3 times a day at equal intervals, distributed between meals. Injections can be given 2 times a day, morning and evening. The duration of treatment is determined by the doctor individually.

How to inject Heptral?

Heptral ampoules are administered intravenously or intramuscularly. The dosage is prescribed depending on the patient's weight. The solution is prepared immediately before injection. The average course duration is 2 weeks.

Where can I buy Heptral?

The medicine is sold by prescription. The drug can be purchased at any pharmacy or ordered delivery through specialized online services.

Heptral®

Ademetionine belongs to the group of hepatoprotectors and also has antidepressant activity.

It has choleretic and cholekinetic effects, has detoxification, regenerating, antioxidant, antifibrosing and neuroprotective properties.

Replenishes the deficiency of S-adenosyl-L-methionine (ademetionine) and stimulates its production in the body; it is found in all environments of the body. The highest concentration of ademetionine was observed in the liver and brain.

Plays a key role in the metabolic processes of the body, takes part in important biochemical reactions: transmethylation, transsulfurization, transamination. In transmethylation reactions, ademetionine donates a methyl group for the synthesis of cell membrane phospholipids, neurotransmitters, nucleic acids, proteins, hormones, etc. In transsulfuration reactions, ademetionine is a precursor of cysteine, taurine, glutathione (providing a redox mechanism of cellular detoxification), coenzyme A (included in 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 plasma; reduces the content of methionine in serum, normalizing metabolic reactions in the liver. After decarboxylation, it participates in aminopropylation reactions as a precursor of the polyamines putrescine (stimulator of cell regeneration and hepatocyte proliferation), spermidine and spermine, which are part of the ribosome structure, which reduces the risk of fibrosis.

Has a choleretic effect.

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 hepatocyte membranes and promotes the passage of bile acids into the biliary tract. Effective for intralobular cholestasis (impaired synthesis and flow of bile). Ademetionine reduces the toxicity of bile acids in hepatocytes by conjugating and sulfating them. Conjugation with taurine increases the solubility of bile acids and their removal from the hepatocyte. The process of sulfation of bile acids facilitates their elimination by the kidneys, facilitates their passage through the hepatocyte membrane and excretion in the bile. In addition, sulfated bile acids themselves additionally protect liver cell membranes from the toxic effects of non-sulfated bile acids (present in high concentrations in hepatocytes during intrahepatic cholestasis).

In patients with diffuse liver diseases (cirrhosis, hepatitis) with intrahepatic cholestasis syndrome, ademetionine reduces the severity of skin itching and changes in biochemical parameters, incl. concentration of direct bilirubin, activity of alkaline phosphatase, aminotransferases, etc.

The choleretic and hepatoprotective effect lasts up to 3 months after cessation of treatment.

It has been shown to be effective against hepatopathy caused by various hepatotoxic drugs.

Antidepressant activity appears gradually, starting from the end of the first week of treatment, and stabilizes within 2 weeks of treatment.

A number of studies have confirmed the effectiveness of ademetionine in the treatment of fatigue in patients with chronic liver diseases. A pooled analysis of data obtained in patients with symptoms of increased fatigue before treatment showed the effect of treatment with ademetionine in reducing symptoms of increased fatigue in combination with a number of other symptoms, such as depression, icterus of the skin and mucous membranes, malaise and itching.

Treatment with ademetionine significantly improved mood in patients with alcoholic liver disease, who simultaneously achieved a positive response to symptoms of increased fatigue. In addition, in patients with alcoholic liver disease and non-alcoholic fatty liver disease who achieved a response to treatment with ademetionine in terms of symptoms of increased fatigue, there was also a significant reduction in symptoms such as icterus of the skin and mucous membranes, malaise and itching.

Note!

The description of the drug Heptral on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.

Compound

Pharmacokinetics

Bioavailability when taken orally - 5%. With a single oral dose of 400 mg, Cmax is 0.7 mg/l; Tmax - 2–6 hours.

Communication with plasma proteins is insignificant, penetrates the BBB. There is a significant increase in the concentration of the drug in the cerebrospinal fluid.

Metabolized in the liver. T1/2 - 1.5 hours. Excreted by the kidneys.

The tablets are coated with a special coating that dissolves only in the intestines, due to which ademetionine is released in the duodenum.

What's happening

In a systematic review, researchers report that 20-40% of coronavirus patients experience psychiatric disorders:

• insomnia - in 42% of patients
• impaired attention and concentration - in 38%
• anxiety - 36%
• memory impairment - 34%
• depression - 33%
• impaired consciousness - in 21%
• post-traumatic stress disorder - in 4-7%

Every fourth patient experiences severe headache and dizziness, 69% have psychomotor agitation, and 0.7% have seizures and movement disorders. Elderly people may develop delirium, a disorder of consciousness in which thinking, attention, and perception of the world around them are impaired. However, delirium most often occurs in older patients with dementia, a syndrome of cognitive decline. Sometimes this is their only symptom of coronavirus without any disturbances in the respiratory system.

“People with coronavirus infection often experience negative psychological reactions: an acute reaction to stress, depression, emotional disturbances, obsessions and dysphoria - a combination of gloomy mood and irritability,” says Olga Markina, candidate of psychological sciences, SberHealth consultant.”

A large-scale outbreak of coronavirus is not the first time in history. During previous epidemics, doctors observed depressed mood and anxiety in patients - the most common symptoms in the acute phase of intoxication that accompanies the disease. A small proportion of patients experience psychosis - an acute disorder of mental activity in which mental processes are desynchronized, the perception of the real world is disrupted, and behavior and emotional reactions do not correspond to the real situation.

“During illness, patients experience fear and anxiety,” neurologist and rehabilitation specialist at GMS Clinic Tigran Makichyan shares his experience. “This is due to many factors: media pressure, stories that someone you know has died, a rapid heartbeat that makes a person restless and anxious.”

Some patients also experience catatonia, a movement disorder accompanied by either complete stupor or increased agitation.

“Work experience shows that coronavirus infection, associated with intoxication and oxygen deprivation of the brain, can cause exacerbation of diseases of the neurological and psychiatric spectrum,” warns Olga Markina. — In older patients, emotional and intellectual impairment may worsen. COVID-19 can also cause a psychotic state: confusion, hallucinations and delusions. Episodes of anxiety-depressive disorder, panic attacks and obsessive-compulsive disorder occur quite often.”

If a person with a mental disorder is sick with coronavirus, then the infection and its treatment can trigger a relapse and worsen the course of the disorder. For example, medications for the treatment of COVID-19 can provoke psychosis in a patient with schizophrenia - delusions, hallucinations and inappropriate behavior, for example, the patient will think that medical staff are trying to infect him.

“Coronavirus leads to decompensation of all chronic diseases, including schizophrenia,” says Tigran Makichyan. “Against the background of hypoxia, when the brain does not have enough oxygen, patients become disoriented, but after recovery, as a rule, this goes away.”

Mental disorders are caused not only by the direct impact of infection on the brain, but by socio-psychological and economic factors associated with coronavirus. People associate a pandemic with instability and unpredictability. Quarantine, social restrictions, uninterrupted news flow about morbidity and mortality from COVID - all this affects the emotional state and mood of people. Thus, depression, anxiety, sleep disturbances, feelings of loneliness, depression and apathy can be caused by:

• high frequency of contact with infected people
• fear of infecting loved ones
• the need for physical distancing and wearing masks
• feeling of medical and social insecurity
• regular media reports about coronavirus
• lack of information about when the pandemic will end

A Chinese study demonstrates that the very fact of an outbreak of a virus pandemic is already affecting the mental state of people who have not contracted the coronavirus. Thus, approximately one in six, under the influence of the epidemic, developed symptoms of moderate and severe depression, and one in three developed signs of an anxiety disorder of moderate or severe severity.

In addition, some respondents reported symptoms of post-traumatic stress disorder and psychological distress. There are also reports that the pandemic is worsening mental health disorders in people who do not have coronavirus.

Covid affects not only the patient himself. It is reported that 50% of family members with a coronavirus patient experience symptoms of depression.

Side effects

The most common adverse reactions include nausea, abdominal pain and diarrhea. Below are summarized data on adverse reactions that were observed during the use of ademetionine both in tablets and in injection dosage form.

From the immune system: laryngeal edema, allergic reactions.

Skin: sweating, itching, rash, Quincke's edema, skin reactions.

Infections and infestations: urinary tract infections.

From the nervous system: dizziness, headache, paresthesia, anxiety, confusion, insomnia.

From the CCC side: hot flashes, phlebitis of 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.

From the musculoskeletal system: arthralgia, muscle spasms.

Others: asthenia, chills, flu-like syndrome, malaise, peripheral edema, fever.

special instructions

Given the tonic effect of the drug, it is not recommended to take it before bed. When prescribing Heptral® to patients with liver cirrhosis due to hyperazotemia, systematic monitoring of residual nitrogen is necessary. During long-term therapy, it is necessary to determine the content of urea and creatinine in the blood serum.

It is not recommended to prescribe ademetionine to patients with bipolar disorders. There are reports of the transition of depression to hypomania or mania in patients taking ademetionine.

There are also reports of sudden onset or worsening anxiety in patients taking ademetionine. In most cases, discontinuation of therapy is not required; in a few cases, anxiety resolved after dose reduction or drug discontinuation.

Since vitamin B12 and folic acid deficiency may reduce ademetionine levels in patients at risk (with anemia, liver disease, pregnancy or the possibility of vitamin deficiency due to other diseases or diet, such as vegetarians), vitamin levels should be monitored. If deficiency is detected, simultaneous administration of ademetionine with vitamin B12 and folic acid is recommended. Ademetionine interferes with homocysteine ​​immunoassay results, which may cause falsely high plasma homocysteine ​​levels. For patients taking ademetionine, it is recommended to use non-immunological methods of analysis to determine homocysteine ​​levels.

Impact on the ability to drive a car and operate machinery. Some patients may experience dizziness while taking Heptral®. It is not recommended to drive a car or operate machinery while taking the drug until patients are sure that the therapy does not affect the ability to engage in this type of activity.

Indications

intrahepatic cholestasis in pre-cirrhotic and cirrhotic conditions, which can be observed in the following diseases:

- fatty liver;

- chronic hepatitis;

- toxic liver damage of various etiologies, including alcohol, viral, drugs (antibiotics, antitumor, anti-tuberculosis and antiviral drugs, tricyclic antidepressants, oral contraceptives);

— chronic acalculous cholecystitis;

- cholangitis;

- cirrhosis of the liver;

— encephalopathy, incl. associated with liver failure (alcohol, etc.);

intrahepatic cholestasis in pregnant women;

symptoms of depression.