Active substanceNaltrexoneNaltrexone
Similar drugsTo uncover
  • Antakson
    capsules inwards 
    Zambon SpA     Italy
  • Vivitrol
    powder w / m 
  • Naltrexone
    capsules inwards 
  • Naltrexone
    pills inwards 
  • Naltrexone
    pills inwards 
  • Naltrexone FV
    capsules inwards 
  • Dosage form: & nbsppills
    Composition:

    For one tablet.

    Active substance:

    naltrexone hydrochloride in terms of 100% of the substance - 50.0 mg.

    Excipients:

    lactose monohydrate-179.6 mg,

    potato starch - 44.9 mg,

    povidone (low molecular weight polyvinylpyrrolidone) - 10.5 mg,

    crospovidone XL-10), 9.0 mg,

    magnesium stearate - 3.0 mg,

    Silica colloidal dioxide -3.0 mg.(aerosil)

    Description:

    Tablets from white to almost white in a flat-cylindrical shape with a facet and a risk.

    Pharmacotherapeutic group:Opioid receptor antagonist
    ATX: & nbsp

    N.07.B.B.04   Naltrexone

    Pharmacodynamics:

    Competitively blocks the binding of agonists or displaces them from opiate receptors. Reduces or removes symptoms caused by intravenous administration of opiates. The greatest affinity for mu-and kappa-receptors.

    Pharmacokinetics:

    Effective when ingested, in the gastrointestinal tract absorbed at 96 %. In the liver, almost completely (95%) is converted into pharmacologically active metabolites, incl. in 6-beta-naltrexone. The half-life of naltrexone is 3.9 hours, 6-beta-naltrexone is 12.9 hours; the average half-life is dose dependent and increases with prolonged use. Naltrexone and its metabolites are excreted mainly by the kidneys and intestines (undergoes intestinal-hepatic circulation). The total ground clearance is 1.5 l / min.

    Begins to act after 1-2 hours. With simultaneous long-term administration, prevents the development of physical dependence on morphine, heroin and other opiates. In a dose of 50 mg blocks the pharmacological effects of 25 mg iv injected heroin for 24 hours, a double dose (100 mg) for 48 hours, and 150 mg for 3 days.

    Long-term appointment does not cause tolerance and dependence. The combination with large doses of opioids leads to an increased release of histamine with a characteristic clinical picture (facial flushing, itching, rash).

    In patients with opioid dependence causes an attack of abstinence.

    When alcoholism is associated with opioid receptors and blocks the effects of endorphins.Reduces alcohol consumption and prevents relapses within 6 months after a 12-week course of therapy (the success of treatment depends on the patient's consent and his interaction with the doctor).
    Indications:

    Naltrexone is used to prevent the pharmacological effects of exogenous opioids and to maintain a non-opioid state in patients with opioid dependence. The drug is prescribed only after relief of the withdrawal syndrome and after a preliminary detoxification.

    The use of naltrexone is started in specialized drug treatment units 7-10 days after the last intake of the opioid drug. In the future, the patient must be under strict medical supervision, a positive attitude is necessary for the treatment of drug addiction in the patient.

    Naltrexone is prescribed in the complex treatment of alcohol dependence (with the patient's consent and in combination with psychotherapeutic and social methods), including with maintenance therapy in the same dosages as with heroin addiction.

    Contraindications:

    Hypersensitivity (including naloxone), taking opiates, a positive test for the presence of opioids in the urine, withdrawal symptoms,acute hepatitis, hepatic insufficiency, pregnancy, breast-feeding (for the period of treatment is excluded), children and adolescence (under 18 years).

    Carefully:

    Impaired renal function.

    Dosing and Administration:

    Treatment of alcoholism: inside of 50 mg once a day, a 12-week course of treatment prevents relapse within 6 months (the success of treatment depends on the patient's consent).

    Therapy of drug dependence begins only after a 7-10 day abstinence from the use of opioids, confirmed by a provocative test and urine analysis for the content of opioids. The patient should have no "withdrawal" syndrome and signs of abstinence. Treatment does not begin until a provocative trial with an intravenous injection of 0.5 mg of naloxone becomes negative. The initial dose of 25 mg, for 1 hour should monitor the patient's condition, in the absence of withdrawal syndrome - appoint 50 mg once a day, this dose blocks 25 mg of heroin administered intravenously.

    Alternative treatment regimens:

    1. 50 mg every weekday and 100 mg on a Saturday;

    2. 100 mg every other day;

    3. 150 mg after 2 days;

    4. for example, 100 mg (on Monday), 100 mg (on Wednesday) and 150 mg (on Friday).

    It should be borne in mind that the use of these regimens increases the risk of hepatotoxicity. The course of treatment is determined individually.

    Side effects:

    From the digestive system: rarely - increased appetite, dry mouth, flatulence, aggravation of symptoms of hemorrhoids, erosive and ulcerative lesions of the gastrointestinal tract, abdominal pain, increased activity of "liver enzymes."

    From the nervous system and sense organs: more often - unusual fatigue, rarely - blurred vision, confusion, hallucinations, central nervous system depression, ringing and feeling of stuffiness in the ears, pain and burning sensation in the eyes, photophobia, irritability, drowsiness, disorientation in time and space.

    From the respiratory system: rarely hoarseness, nasal congestion (hyperemia of the vessels of the nasal cavity), sneezing, shortness of breath, dryness in the throat, increased separation of mucous sputum, sinusitis.

    From the side of the cardiovascular system: rarely - chest pain, nonspecific ECG changes.

    From the genitourinary system: discomfort with urination, increased frequency of urination.

    Allergic reactions: less often - skin rash, rarely - hyperthermia, itchy skin, Rarely - increased secretion of sebaceous glands.

    Other: rarely - thirst, increase or loss of body weight, pain in the groin, enlargement of lymph nodes, lymphocytosis; in one case, the development of idiopathic thrombocytopenic purpura is described against a background of preliminary sensitization to the drug.

    The syndrome of "withdrawal" of opioids: abdominal pain, epigastric cramps, anxiety, nervousness, fatigue, irritability, diarrhea, tachycardia, hyperthermia, rhinorrhea, sneezing, goosebumpia, sweating, yawning, arthralgia, myalgia, anorexia, nausea and / or vomiting, tremor, general weakness.

    Interaction:

    Increases (mutually) the risk of liver damage when combined with hepatotoxic drugs. Possible lethargy or increased drowsiness when combined with thioridazine. Reduces the effectiveness of medicines containing opioids (antitussive drugs, analgesics).

    Accelerates the appearance of the symptoms of "withdrawal syndrome" against the background of drug dependence (symptoms can appear as early as 5 minutes after drug administration, last for 48 hours, are characterized by persistence and difficulty of their elimination).

    Special instructions:

    Before use, subclinical hepatic insufficiency must be excluded, during the treatment should periodically monitor the level of transaminases; Do not combine with drugs that have hepatotoxic properties.

    To prevent the development of an acute withdrawal syndrome, patients should at least 7-10 days later stop taking opioids and drugs containing them, be sure to identify opioids in the urine and conduct a provocative test with naloxone; if these requirements are not complied with, withdrawal symptoms may appear 5 minutes after taking the drug and continue for 48 hours.

    Naltrexone should be discontinued at least 48 hours before surgery, which requires the use of opioid analgesics.

    In case of emergency analgesia, caution is prescribed for opioids in a higher dosage (to overcome antagonism), since respiratory depression will be deeper and more prolonged.

    A persistent decrease in appetite and progressive weight loss require discontinuation of therapy.

    Ineffective in the treatment of cocaine, as well as non-opioid drug dependence.

    Patients should be warned that

    - when seeking medical help, they are obliged to inform medical workers about treatment with naltrexone;

    - In case of abdominal pain, darkening of urine, yellowing of the sclera, it is necessary to stop taking the medicine and consult a doctor;

    - with independent use of heroin and other drugs in small doses, the effect of their use will not be, and further increase in the dose of drugs will lead to death (stopping breathing).
    Form release / dosage:

    Tablets 50 mg.

    Packaging:

    10 tablets per contour cell packaging made of polyvinylchloride film and foil of aluminum printed lacquered or flexible packaging on the basis of aluminum foil.

    For 1,2 or 5 contour squares with instructions for use in a cardboard bundle. For 100, 200, 300 contour squares with an equal number of instructions for use, respectively, in a box or box (for hospitals).

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C. Keep out of reach of people for children.

    Shelf life:
    5 years. Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-004678/07
    Date of registration:11.12.2007 / 04.02.2015
    Expiration Date:Unlimited
    The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia
    Manufacturer: & nbsp
    Information update date: & nbsp27.05.2018
    Illustrated instructions
      Instructions
      Up