Ademetionine for Injection 500mg, Ademetionine Tablet

1.Product name:Ademetionine for injection
2.Specification:ademetionine 500mg
                      L-Lysine injection 5ml
3.Package:5 ampoules+5 vials/tray/box
4.Shelf life:36 months
5.Registration dossiers are available.
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Composition, structure and packing
Lyophilisate for solution for IV and IM administration from almost white to white with a yellowish tint without inclusions; solvent - a clear, colorless to pale yellow, with no inclusions; reconstituted solution - Transparent, colorless to yellow color with no visible precipitate.
Solvent: L-lysine, Sodium hydroxide, Water for injections.
Pharmacological action
Pharmacological action - hepatoprotective, anti-depressant, detoxifying, stimulating regeneration, antioxidant, neuroprotective.
Hepatoprotector has antidepressant activity. Has choleretic and cholekinetic action. Has detoxifying, regenerating, antioxidant, antifibrosing and neuroprotective properties.
Fills deficit ademetionine and stimulates its production in the body, is found in all environments of the body. The highest concentration of ademetionine noted in the liver and brain. Plays a key role in the metabolic processes of the body, is involved in important biochemical reactions: transmethylation, transsulfuration, transamination. In transmethylation reactions ademethionine sends a methyl group for the synthesis of cell membrane phospholipids, neurotransmitters, nucleic acids, proteins, hormones, and others. Transsulfation reactions of ademetionine ia a precursor of cysteine, taurine, glutathione (providing a redox mechanism cellular detoxification), acetylation coenzyme (involved in biochemical reactions of the citric acid cycle and replenishes the energy potential of the cell).
Increases of glutamine in the liver, cysteine and taurine in the plasma; reduces the amount of methionine in serum, normalizing the metabolic reaction in the liver. After decarboxylation involved in the process aminopropylation as precursor of polyamines - putrescine (stimulator of cell regeneration and proliferation of hepatocytes), spermidine, and spermine, within the structure of the ribosome, which reduces the risk of fibrosis.
Has choleretic action. Ademetionine normalizes endogenous synthesis of phosphatidylcholine in hepatocytes, which increases the fluidity and membrane polarization. This improves the function of membrane-associated hepatocyte transport systems of bile acids and facilitates passage of bile acids in the biliary system. Effective with intrahepatic (intralobular and interlobular) variant of cholestasis (impaired bile flow and synthesis). Ademetionine reduces the toxicity of bile acids in the hepatocyte, exercising their conjugation and sulfation. Conjugation with taurine increases the solubility of bile acids and removing them 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 membrane of hepatocytes and excretion in the bile. Besides themselves sulfated bile acids also protect membranes of liver cells from the toxic action nonsulphated bile acids (present in high concentrations in hepatocytes in intrahepatic cholestasis). In patients with diffuse liver disease (cirrhosis, hepatitis) with intrahepatic cholestasis syndrome ademetionine reduces the severity of itching and changes in biochemical parameters, including the level of direct bilirubin, alkaline phosphatase activity, aminotransferases. Choleretic and hepatoprotective effect lasts up to 3 months after cessation of treatment.
The efficiency with hepatopathies caused by hepatotoxic drugs.
Appointment of patients with opioid addiction, accompanied by liver disease, leading to regression of clinical manifestations of withdrawal, improves the functional state of the liver and microsomal oxidation processes.
Antidepressant activity is manifested gradually, starting from the first week of treatment and stabilized for 2 weeks of treatment. The drug is effective in recurrent endogenous and neurotic depression that is resistant to amitriptyline. Has the ability to interrupt recurrences of depression.
Use of the drug in osteoarthritis reduces the severity of pain, increases the synthesis of proteoglycans and leads to partial regeneration of cartilage tissue.
Pharmacokinetics
Absorption
Bioavailability after parenteral injection - 96%, C max is reached in the plasma after 45 min.
Distribution
Binding to serum proteins is negligible.
Penetrate the BBB. Has been a significant increase in the concentration of ademetionine in the cerebrospinal fluid.
Metabolism
Biotransformed in the liver.
Excretion
T 1/2 - 1.5 h. Write kidney.
Dosage
Used IV or IM.
Necessary to dissolve the lyophilisate in a specially attached solvent just prior to administration. The residue of the drug should be disposed of.
The drug should not be mixed with alkaline solutions and solutions containing calcium ions. Drug Geptral at IV application is introduced very slowly.
When intrahepatic cholestasis drug is administered 400 mg/day to 800 mg/day (2.1 fl./Day) for 2 weeks.
When depression drug is administered at a dose of 400 mg/day (1 fl./Day) Within 15-20 days.
If necessary, maintenance therapy is recommended to continue taking the drug in tablet form Geptral in a dose of 800-1600 mg/day for 2-4 weeks.
Overdose
Clinical cases of overdose were reported.
Drug Interactions
Known drug interactions Geptral drug with other drugs was not observed.
There is a report of the syndrome of excess serotonin in patients taking ademetionine and clomipramine. It is believed that such an interaction is possible, and should be used with caution ademetionine with selective serotonin reuptake inhibitors, tricyclic antidepressants (such as clomipramine), as well as herbal remedies and drugs containing tryptophan.
Pregnancy and lactation
Application ademetionine in high doses in the III trimester of pregnancy did not cause any adverse effects.
Use of the drug Geptral I trimester of pregnancy and during breast-feeding is possible only if the potential benefit to the mother outweighs the potential risk to the fetus or child.
Side effects
Among the most frequent adverse reactions observed: nausea, abdominal pain and diarrhea. Below are summaries of the adverse reactions that were observed during treatment in ademetionine tablets and injectable dosage form.
By the immune system: laryngeal edema, allergic reactions.
Skin: injection site reactions (very rarely with necrosis of the skin), sweating, itching, rash, angioedema, skin reactions.
Infections and infestations: urinary tract infection.
The nervous system: dizziness, headache, paresthesia, confusion, and insomnia.
Cardio-vascular system: flushing, phlebitis superficial veins, cardiovascular disorders.
From the digestive system: bloating, pain in the abdominal pain, diarrhea, dry mouth, dyspepsia, esophagitis, flatulence, gastrointestinal disorder, gastrointestinal bleeding, nausea, vomiting, hepatic colic, liver cirrhosis.
On the part of the musculoskeletal system: arthralgia, muscle spasms.
Other: asthenia, chills, flu-like symptoms, malaise, peripheral edema, fever. Conditions and terms
The drug should be stored in a dark place, out of reach of children at a temperature of 15° to 25° C. Shelf life - 3 years.
Indications
Intrahepatic cholestasis with pretsirroticheskih and cirrhotic conditions that may occur in the following diseases:
Fatty liver;
Chronic hepatitis;
Toxic liver disease of various etiologies, including alcoholic, viral, drugs (antibiotics, anti-cancer, anti-tuberculosis and anti-viral drugs, tricyclic antidepressants, oral contraceptives);
Chronic cholecystitis without stones;
Cholangitis;
Cirrhosis of the liver;
Encephalopathy, including associated with hepatic impairment (including alcohol).
Intrahepatic cholestasis in pregnancy.
Symptoms of depression.
Contraindications
Age 18 years;
Hypersensitivity to the drug.
Precautions should be prescribed the drug for bipolar disorder, I trimester of pregnancy, lactation (breastfeeding).
Cautions
Given Heptral tonic effect, it is not recommended to use at bedtime.
In the appointment of Geptral patients with cirrhosis of the liver on the background hyperasotemia requires systematic monitoring of the level of nitrogen in the blood. During prolonged therapy is necessary to determine the content of urea and serum creatinine.
Do not appoint ademetionine patients with bipolar disorder. There are reports on the transition depression into hypomania or mania in patients taking ademetionine.
Patients receiving Geptral recommended to assign cyanocobalamin (vitamin B 12) and folic acid deficiency as cyanocobalamin and folic acid can reduce the concentration of ademetionine.
Use in Pediatrics
Safety of the drug in children Geptral poorly understood.
Effects on ability to drive vehicles and management mechanisms
In some patients, while taking the drug Geptral may dizziness. It is not recommended to drive a car and operate machinery while taking the drug for as long as the patient is not sure that the therapy does not affect the ability to engage in this type of activity.
Renal impairment
In appointing Heptral patients with cirrhosis on the background hyperasotemia requires systematic monitoring of the level of nitrogen in the blood. During prolonged therapy is necessary to determine the content of urea and serum creatinine.
In hepatic dysfunction
Applied on the testimony
Application in childhood
Safety of the drug in children Geptral poorly understood.