Heptor
Heptor: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Heptor
ATX code: A16AA02
Active ingredient: ademetionine (ademetionine)
Producer: Veropharm, LLC (Russia), Microgen NPO FGUP (NPO Virion) (Russia), Lens-Pharm, LLC (Russia)
Description and photo update: 2019-09-09
Prices in pharmacies: from 832 rubles.
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Heptor is a hepatoprotective agent with antidepressant activity.
Release form and composition
Dosage forms of Heptor release:
- enteric-coated tablets: biconvex, oblong, yellow (10 pcs. in blisters, 1 or 2 packs in a cardboard box; 20, 40 or 50 pcs. in polymer cans, 1 can in a cardboard box);
- lyophilisate for preparation of a solution for intravenous and intramuscular administration: almost white or white porous mass; solvent - transparent, from yellowish to colorless, has a characteristic odor (in colorless glass vials complete with solvent in ampoules of 5 ml, in a cardboard box 5 vials with lyophilisate and 5 ampoules with solvent).
Each pack also contains instructions for the use of Heptor.
Composition of 1 tablet:
- active substance: ademetionine (in the form of S-adenosylmethionine) - 400 mg;
- auxiliary components: crospovidone - 19 mg, magnesium stearate - 15 mg, microcrystalline cellulose - 53 mg, mannitol - 53 mg;
- shell: polyethylene glycol 6000 - 3.7 mg, acrylysis - 61.3 mg, copovidone - 9 mg, hydroxypropyl methylcellulose - 21 mg.
The active substance in 1 bottle of lyophilisate: ademetionine - 400 mg (1,4-butanedisulfonate ademetionine - 760 mg).
Composition of 1 ml of solvent: L-lysine (in the form of monohydrate) - 68.48 mg, sodium hydroxide solution - up to pH 9.8-10.3, water for injection - up to 1 ml.
Pharmacological properties
Pharmacodynamics
The heptor has a stimulating effect on liver cells, helps to restore their structure, normalizes the basic functions of the liver, protects hepatocytes from the pathogenic effects of toxins, and has antidepressant activity. The drug has a detoxifying, regenerating, choleretic, cholekinetic, antioxidant, antifibrosing and neuroprotective effect.
Replenishing the lack of ademetionine in the body, Heptor stimulates its production, the highest concentration is noted in the liver parenchyma and brain cells. As a donor of the methyl group, the S-adenosyl-L-methionine (ademetionine) molecule takes part in transmethylation by donating the methyl group in the methylation reactions of proteins, hormones, phospholipids of cell membranes, neurotransmitters, etc. As a precursor of cysteine, taurine, glutathione, coenzyme A ademetionine through transsulfation provides redox detoxification of cells. The heptor increases the concentration of glutamine in the liver, cysteine and taurine in the plasma, lowers the level of methionine in the blood serum, thereby normalizing hepatic metabolism.
Following decarboxylation, ademetionine takes part in aminopropylation as a precursor of polyamines - putrescine (a stimulator of hepatocyte proliferation and cell regeneration), spermine and spermidine, which are part of the ribosome structure. The choleretic effect of Heptor is due to an increase in the mobility and polarization of hepatocyte membranes as a result of stimulation of the synthesis of phosphatidylcholine in them. This improves the function of the transport systems of bile acids associated with the membranes of hepatocytes, and promotes the release of bile acids into the biliary system. Ademetionine is effective in disrupting the synthesis and flow of bile, the so-called. intralobular, or intralobular, cholestasis. It detoxifies bile acids, increases the content of sulfated and conjugated bile acids in hepatocytes. When conjugated with taurine, it increases the solubility of bile acids, thereby improving their excretion from hepatocytes. Sulfation of bile acids promotes their elimination, and also facilitates the passage through the hepatocyte membrane and excretion with bile. Sulfated bile acids also have a protective effect on the membranes of liver cells during the toxic effect of unsulfated bile acids, which are present in high concentrations in hepatocytes during intrahepatic cholestasis. Sulfated bile acids also have a protective effect on the membranes of liver cells during the toxic effect of unsulfated bile acids, which are present in high concentrations in hepatocytes during intrahepatic cholestasis. Sulfated bile acids also have a protective effect on the membranes of liver cells against the toxic effect of unsulfated bile acids, which are present in high concentrations in hepatocytes during intrahepatic cholestasis.
In diffuse liver diseases, such as cirrhosis and hepatitis, with intrahepatic cholestasis syndrome, taking Heptor reduces the degree of changes in biochemical parameters (concentration of direct bilirubin, aminotransferase activity, alkaline phosphatase, g-glutamyl transpeptidase) and reduces the severity of itching. The choleretic and hepatoprotective effect of the drug after termination of treatment lasts up to 3 months. The effectiveness of therapy for patients with hepatopathies caused by hepatotoxic drugs has been proven.
The use of ademetionine by patients with opioid addiction with concomitant liver damage causes regression of the clinical manifestations of withdrawal symptoms, improves liver function and stimulates microsomal oxidation processes.
The antidepressant efficacy of the drug manifests itself gradually, starting from the end of the first week of the course, and stabilizes within two weeks of therapy. Heptor is effective in recurrent depression, endogenous and neurotic, which are resistant to amitriptyline. It has the ability to stop relapses of depression.
In osteoarthritis, ademetionine reduces the severity of pain, enhances the synthesis of proteoglycans, and partially regenerates cartilage tissue.
Pharmacokinetics
Oral bioavailability of ademetionine is 5%. A single intake of 400 mg of the substance provides a maximum plasma concentration (C max) of 0.7 mg / l, the time to reach (T C max) of which varies from 2 to 6 hours.
Bioavailability with intramuscular injection of the drug is 95%.
The binding of ademetionine to plasma proteins is insignificant, the substance penetrates the blood-brain barrier. A significant increase in the level of ademetionine in the cerebrospinal fluid is noted regardless of the route of administration of the drug.
The metabolism of the substance occurs in the liver. Ademetionine is excreted by the kidneys, T 1/2 (half-life) - 1.5 hours.
Indications for use
- chronic non-calculous cholecystitis;
- encephalopathy, including those associated with liver failure (alcoholic and others);
- intrahepatic cholestasis, including in pregnant women;
- cirrhosis of the liver;
- fatty degeneration of the liver;
- cholangitis;
- hepatitis of various etiologies: viral, toxic, including drug (oral contraceptives, antibiotics, tricyclic antidepressants, drugs with antitumor, anti-tuberculosis and antiviral effects) and alcoholic origin;
- withdrawal syndrome (alcoholic, etc.);
- depression, including secondary.
Contraindications
Injection solution
Absolute:
- children and adolescents up to 18 years of age (due to limited experience in medical use);
- increased individual sensitivity to ademetionine and / or solvent components.
Lyophilisate is used with caution in the treatment of patients with bipolar disorders. In the first trimester of pregnancy and during breastfeeding (lactation), the appointment is possible only if the potential benefit to the mother exceeds the possible risk to the fetus.
Pills
Absolute:
- genetic pathologies affecting the methionine cycle, as well as causing homocystinuria / hyperhomocysteinemia, such as a lack of cystathionine beta synthase, impaired metabolism of cyanocobalamin (vitamin B 12);
- children and adolescents up to 18 years of age (due to limited experience in medical use);
- I – II trimesters of pregnancy;
- period of breastfeeding;
- increased individual sensitivity to ademetionine and / or Heptor auxiliary components.
Relative (Heptor is used with caution):
- bipolar disorder;
- renal failure;
- simultaneous use with tricyclic antidepressants (for example, clomipramine), selective serotonin reuptake inhibitors, herbal medicines and drugs with tryptophan;
- elderly age.
Heptor, instructions for use: method and dosage
Injection solution
Route of Heptor administration: intramuscularly (intramuscularly) or intravenously (intravenously).
During the period of intensive therapy during the first 2-3 weeks of use, the drug is prescribed in a daily dose of 400-800 mg IM or IV drip (very slowly).
The lyophilisate should only be dissolved in the accompanying solvent (L-lysine solution).
At the end of the course of intensive therapy, the patient is transferred to take the drug inside.
Pills
Heptor tablets are taken orally, without chewing, whole. In order to improve the therapeutic effect, the tablets are recommended to be taken between meals in the morning.
The recommended daily dose during maintenance therapy is 2–4 tablets. The duration of the course is from 2 to 4 weeks.
Side effects
Injection solution
- heartburn;
- gastralgia;
- allergic reactions;
- dyspepsia.
Pills
- nervous system: headache, insomnia;
- digestive system: dyspepsia, nausea, flatulence, abdominal pain, dryness of the oral mucosa, diarrhea.
Overdose
Clinical cases of ademetionine overdose have not been reported.
special instructions
It should be taken into account that the Heptor produces a tonic effect. Therefore, its use before bed is not recommended.
With cirrhosis of the liver, which is associated with hyperazotemia, systematic control of azotemia should be carried out.
During long-term treatment, the serum content of urea and creatinine in the blood should be determined.
The solution of the drug must be prepared immediately before use. If the color of the lyophilisate changes, it cannot be used.
When prescribing Heptor to patients with bipolar disorders, it should be borne in mind that there is information about the transition during therapy of depression to mania / hypomania.
Influence on the ability to drive vehicles and complex mechanisms
Since some patients, when taking ademetionine inside (Heptor tablets), may experience dizziness, they should refrain from performing potentially dangerous types of work until the ability to concentrate and psychomotor speed is restored.
Application during pregnancy and lactation
Injection solution
In the first trimester of pregnancy and during breastfeeding (lactation period), Heptor should be used only as directed by a doctor, taking precautions, provided that the potential benefit to the mother exceeds the possible risk to the fetus / child.
In the second trimester of pregnancy, the drug is used mainly for the treatment of intrahepatic cholestasis, caution is recommended. The use of Heptor in high doses in the third trimester of pregnancy did not cause undesirable side effects.
Pills
Use in the I – II trimesters of pregnancy and during breastfeeding is contraindicated.
Pediatric use
Due to the limited experience of medical use, it is contraindicated to use Heptor for the treatment of children and adolescents under the age of 18 years.
With impaired renal function
Heptor tablets are prescribed with caution to patients with renal insufficiency (due to the limited clinical data on the use of ademetionine inside for such diseases).
For violations of liver function
Correction of the Heptor dosage regimen in hepatic failure is not required, since the pharmacokinetic characteristics of ademetionine are similar in patients with chronic liver disease and in healthy volunteers.
Use in the elderly
According to the results of clinical studies of the use of Heptor tablets, no differences were found in the effectiveness of tablets in elderly and younger patients. But, given the high likelihood of liver, kidney, heart dysfunction and other concomitant pathologies in elderly patients, as well as the simultaneous use of various drugs for their therapy, the dose of ademetionine for patients of this age group is recommended to be selected with caution, starting taking Heptor with the lowest effective dose.
Drug interactions
No significant interaction with other drugs / substances was observed.
Analogs
Analogues of Heptor are: Ademetionine-Vial, Heptor N, Heptral.
Terms and conditions of storage
Store in a place protected from light and moisture at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life:
- tablets, lyophilisate - 2 years;
- solvent - 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Heptor
In most reviews, Heptor is characterized as a high-quality domestic analogue of an imported drug, not inferior to it in efficiency, but having a cost of 2.5 times cheaper. The drug has proven itself well in the prevention of liver diseases, the treatment of cholecystitis, psoriasis, and fatty hepatosis. It has a mild antidepressant and tonic effect.
Patients are warned not to use the Heptor before bed, as it can cause insomnia.
Patients who have not previously used more expensive analogues consider the cost of Heptor very high, while others argue that it is 2-3 times cheaper than imported analogues.
Price for Heptor in pharmacies
Estimated price of Heptor:
- enteric-coated tablets, 400 mg, 20 pcs. in the package - 940-1028 rubles;
- lyophilisate for the preparation of a solution for intravenous and intramuscular administration, 400 mg, 5 ampoules in a package - 1248-1339 rubles.
Heptor: prices in online pharmacies
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Drug name Price Pharmacy |
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Heptor 400 mg enteric-coated tablets 20 pcs. 832 RUB Buy |
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Heptor tablets p.p. enteric solution. 400mg 20 pcs. 866 RUB Buy |
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Heptor 400 mg lyophilisate for preparation of a solution for intravenous and intramuscular administration complete with a solvent 5 pcs. 1199 RUB Buy |
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Heptor lyoph. for prigot. solution for intravenous and intramuscular injection. 400mg 5 pcs. (with Lysine solvent) 1214 RUB Buy |
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Heptor tablets p.p. enteric solution. 400mg 40 pcs. 1736 RUB Buy |
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Heptor 400 mg enteric-coated tablets 40 pcs. 1736 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
