Clinical and pharmacological group: & nbsp

Detoxifying agents, including antidotes

Opioid non-narcotic analgesics and opioid antagonists

Included in the formulation
  • Antakson
    capsules inwards 
    Zambon SpA     Italy
  • Vivitrol
    powder w / m 
  • Naltrexone
    capsules inwards 
  • Naltrexone
    pills inwards 
  • Naltrexone
    pills inwards 
  • Naltrexone FV
    capsules inwards 
  • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    N.07.B.B.04   Naltrexone

    Pharmacodynamics:

    Competitive antagonist. It blocks μ-, δ- and κ-receptors, therefore eliminates both the analgesic effect of narcotic analgesics, and the euphoria caused by them, respiratory depression and other effects.

    Pharmacokinetics:

    The connection with plasma proteins is weak. Passes through the placenta and the blood-brain barrier. Biotransformation in the liver. Elimination by the kidneys (70% for 72 hours). Half-life 64 min.

    Indications:

    Opioid addiction (as an auxiliary drug after the abolition of opioid analgesics), alcoholism.

    XIX.T51-T65.T51   Toxic effect of alcohol

    V.F10-F19.F14.4   Mental and behavioral disorders caused by cocaine use - abstinent state with delirium

    V.F10-F19.F14.3   Mental and behavioral disorders caused by the use of cocaine - the abstinence state

    Contraindications:

    Hypersensitivity (including naloxone), the condition of withdrawal from the background of opioid dependence, a positive test for the presence of opioids in the urine, acute hepatitis, hepatic insufficiency, pregnancy, breast-feeding.

    Carefully:

    Renal failure, heart failure, elderly age, children under 18 years.

    Pregnancy and lactation:

    Category FDA C.

    The use is contraindicated in pregnancy. When naltrexone was orally taken, naltrexone and 6-β-naltrexol were isolated from breast milk. Because of potential carcinogenicity and the likelihood of serious side effects in infants, a decision should be made to discontinue drug therapy during breastfeeding or to stop lactation during drug treatment, depending on the importance of therapy for the mother.

    Dosing and Administration:

    Inside. Single dose is 25-50 mg. The scheme and duration of treatment are set individually.

    Side effects:

    From the side of the central nervous system: agitation, a state of prostration, irritability, dizziness; rarely - depression, paranoia, fatigue, confusion, disorientation in time and space, hallucinations, nightmares, drowsiness, decreased visual acuity, pain and burning sensation in the eyes, photophobia, pain and a feeling of stuffiness in the ears, tinnitus.

    From the digestive system: decreased appetite, diarrhea, constipation; rarely - dry mouth, flatulence, aggravation of hemorrhoid symptoms, erosive and ulcerative lesions of the gastrointestinal tract, increased activity of hepatic transaminases.

    On the part of the urinary system: rarely - frequent or violated urination.

    On the part of the reproductive system: delayed ejaculation, reduction of sexual potency; rarely - increased or decreased libido.

    Dermatological reactions: rash; rarely - increased secretion of sebaceous glands, epidermophytic feet, skin changes, corresponding to the first stage of frostbite.

    On the part of the respiratory system: rarely - hyperemia of the vessels of the nasal cavity, nosebleeds, rhinorrhea, sneezing, dryness in the throat, increased mucus, sinusitis, shortness of breath, tracheophone, cough, shortness of breath.

    From the cardiovascular system: rarely - phlebitis, swelling, increased blood pressure, nonspecific changes in the cardiogram, tachycardia, a feeling of heat in the limbs, a sudden sensation of blood flow to the face.

    Others: chills are possible; rarely - increase or loss of appetite, weight gain, pathological yawning, fever, pain in the groin, lymphadenopathy, lymphocytosis; describes one case of idiopathic thrombocytopenic purpura in a patient who appears to have been sensitized to naltrexone during the previous treatment.

    Overdose:

    Not described.

    Interaction:

    With simultaneous use with naltrexone, the effectiveness of opioid receptor agonists (antitussives, analgesics) decreases.

    Special instructions:

    Naltrexone can be used only in cases where the patient does not take opioid analgesics for at least 7-10 days.

    Naltrexone can be effective in the treatment of chronic alcoholism.

    Use with caution in patients with impaired liver and / or kidney function. During the treatment period, regular monitoring of liver function is recommended.

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

    It should be borne in mind that with the use of naltrexone the probability of complete recovery from opioid dependence is variable.

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