Heptor [S-Adenosyl methionine]

Contents

Enteric coated tablets, 20 tablets per pack.

Active ingredient: ademetionine 400 mg

Inactive ingredients: crospovidone 19 mg, microcrystalline cellulose 53 mg, mannitol 53 mg and magnesium stearate 15 mg.

Administration and doses

The average daily dose is 800–1,600 mg (2-4 pills). The treatment period duration is 2-4 weeks.

Drug interaction

To be used with caution when co-administered with selective serotonin reuptake inhibitors, tricyclic antidepressants or drugs containing tryptophan.

Side effects

In the digestive system: nausea, abdominal pain or diarrhea.

In the nervous system: insomnia or headache.

Allergic response.

Storage conditions

Store in a cool dark place at a temperature not higher than 25°C (77°F). Keep out of the reach of children. Shelf life is 3 years.

Heptor is a drug based on ademetionine (S-Adenosyl methionine), which is currently considered one of the most powerful hepatoprotectors. Ademetionine takes part in transmethylation and is a biosynthetic precursor of cysteine, taurine and glutathione. Apart from its hepatoprotective properties, ademetionine also has anti-inflammatory, painkiller and antidepressant effects. Heptor is a choleretic and cholekinetic drug.

The use of drug in patients with osteoarthritis helps relieve pain and stimulates proteoglycan synthesis and cartilage tissue regeneration.

Heptor also has detoxifying, regenerating, antioxidant, antifibrotic and neuroprotective properties.

The drug was shown to be effective in patients with hepatopathy caused by hepatotoxic drugs.

Pharmacodynamic properties

As a hepatoprotector, Heptor replenishes ademetionine deficiency and stimulates its production in brain and liver. As a part of transmethylation, it elevates glutamine levels in the liver and increases plasma cysteine and taurine concentration. It also lowers the concentration of methionine in serum; this helps stabilize the metabolic functions of the liver. Heptor acts as a precursor of polyamines: putrescine which stimulates cell regeneration, spermidine and spermine that are compounds of ribosomes and living tissues.

Choleretic effect of the drug is driven by synthesis of phosphatidylcholine in hepatocyte membranes which increases their mobility. This enhances the function of biliary system. The drug is effective in case of bile secretion disorders, including cholestasis.

The use of Heptor in patients with opioid addiction accompanied by liver damage helps reduce manifestations of withdrawal symptoms and improves the functional state of the liver.

Antidepressant effects of the drug increase gradually starting from the 2nd week of the treatment course. Heptor treatment is recommended in case of recurrent endogenous and neurotic depressions. Research demonstrated that the drug is effective in treating depression relapse.

Indications (on-label uses)

  • hepatitis of various origins: toxic, viral, drug-induced (caused by antibiotics, anticancer drugs, anti-tuberculosis and antiviral drugs, tricyclic antidepressants and oral contraceptives);
  • intrahepatic cholestasis;
  • cirrhosis;
  • secondary metabolic encephalopathy;
  • depressive disorder;
  • alcohol withdrawal syndrome.
  • Counterindications

  • genetic disorders affecting the methionine cycle and/or causing homocystinuria/hyperhomocysteinemia;
  • children under 18 years of age;
  • hypersensitivity to the components of the drug.
    1. Cozens et al (1988) Reproductive toxicity studies of ademetionine https://www.ncbi.nlm.nih.gov/pubmed/3214447
    2. Domljan et al (1989) A double-blind trial of ademetionine vs naproxen in activated gonarthrosis https://www.ncbi.nlm.nih.gov/pubmed/2674027
    3. P Almasio, L Pagliaro (1993) Ademetionine: the state of the art and future prospects https://www.ncbi.nlm.nih.gov/pubmed/8117523
    4. M Frezza (1993) A meta-analysis of therapeutic trials with ademetionine in the treatment of intrahepatic cholestasis https://www.ncbi.nlm.nih.gov/pubmed/8117521
    5. Bottiglieri et al (1994) The clinical potential of ademetionine (S-adenosylmethionine) in neurological disorders https://www.ncbi.nlm.nih.gov/pubmed/7527320
    6. T Bottiglieri (1997) Ademetionine (S-adenosylmethionine) neuropharmacology: implications for drug therapies in psychiatric and neurological disorders https://www.ncbi.nlm.nih.gov/pubmed/15989609
    7. Qin et al (2000) A trial of ademetionine in the treatment of intrahepatic biliary stasis viral hepatitis https://www.ncbi.nlm.nih.gov/pubmed/10880165
    8. L Il'chenko, E Vinnitskaia (2002) Metabolism pathways and use of heptral in chronic liver diseases https://www.ncbi.nlm.nih.gov/pubmed/12046390
    9. G Vostrikov, A Toporkov (2002) Use of heptral in chronic liver diseases https://www.ncbi.nlm.nih.gov/pubmed/12685015
    10. Arnold et al (2005) Double-blind, placebo-controlled pharmacodynamic studies with a nutraceutical and a pharmaceutical dose of ademetionine(SAMe) in elderly subjects, utilizing EEG mapping and psychometry https://www.ncbi.nlm.nih.gov/pubmed/16046102
    11. Tkachenko et al (2008) Clinical efficacy of ademetionine "Heptor" in the therapy of alcohol-dependent liver disease https://www.ncbi.nlm.nih.gov/pubmed/19145875
    12. Zhu et al (2010) Efficacy and safety of ademetionine for treatment of drug-induced liver disease in children https://www.ncbi.nlm.nih.gov/pubmed/21110437
    13. Shilov et al (2012) Comparative evaluation of clinical efficacy of drugs remaxol and ademetionine in patients with acute ethanol poisoning complicated by the toxic damage of the liver https://www.ncbi.nlm.nih.gov/pubmed/22665730
    14. Sukhanov et al (2013) Hepato- and endothelioprotective action of runihol and ademetionine in experimental liver injury induced by TB drugs in combination with alcohol https://www.ncbi.nlm.nih.gov/pubmed/24000714
    15. Tian et al (2013) Protective effect of ademetionine 1, 4-butanedisulfonate on liver injury caused by chemotherapeutic agents https://www.ncbi.nlm.nih.gov/pubmed/24156455
    16. D Sukhanov (2013) Antioxidant properties of remaxol, reamberin, and ademetioninein patients with drug-induced liver injury on the background of antituberculous therapy https://www.ncbi.nlm.nih.gov/pubmed/23762990
    17. Virukalpattigopalratnam et al (2013) Heptral (ademetionine) in patients with intrahepatic cholestasis in chronic liver disease due to non-alcoholic liver disease: results of a multicentre observational study in India https://www.ncbi.nlm.nih.gov/pubmed/25154164
    18. Guo et al (2015) S-Adenosyl-L-Methionine for the Treatment of Chronic Liver Disease: A Systematic Review and Meta-Analysis https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4361566/
    19. Tong et al (2015) Effect of ademetionine on cytochrome P450 isoforms activity in rats https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4538182/
    20. Stelmakh et al (2015) Efficacy of the infusion hepatotropic drug remaxol in the pathogenetic therapy for cirrhotic stage chronic viral hepatitides https://www.ncbi.nlm.nih.gov/pubmed/26824818
    21. Sharma et al (2017) S-Adenosylmethionine (SAMe) for Neuropsychiatric Disorders: A Clinician-Oriented Review of Research https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5501081/
    22. Ivashkin et al (2018) Open-label study of ademetionine for the treatment of intrahepatic cholestasis associated with alcoholic liver disease https://www.ncbi.nlm.nih.gov/pubmed/29431335


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