Clinical and pharmacological group: & nbsp

Detoxifying agents, including antidotes

Opioid non-narcotic analgesics and opioid antagonists

Included in the formulation
  • Naloxone
    solution
    Kern Pharma S.L.     Spain
  • Naloxone
    solution for injections 
  • Naloxone
    solution w / m in / in PC 
  • Targin®
    pills inwards 
    Mundifarma     Switzerland
  • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    V.03.A.B.15   Naloxone

    Pharmacodynamics:

    Competitive antagonism. 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 minutes.

    Indications:

    Acute poisoning with narcotic analgesics: complete (morphine, promedol, fentanyl) and partial (buprenorphine) agonists and antagonist agonists (pentazocine, butorphanol, nalboufine and others); termination of narcotic analgesics; Restoration of respiration in newborns after the introduction of opioid analgesics to mothers; diagnosis of opioid dependence.

    XIX.T80-T88.T80.5   Anaphylactic shock associated with the administration of serum

    XIX.T79.T79.4   Traumatic shock

    XVIII.R50-R69.R57.9   Shock, unspecified

    XVIII.R50-R69.R57.8   Other types of shock

    XVIII.R50-R69.R57   Shock, not elsewhere classified

    XIX.T36-T50.T42.3   Poisoning with barbiturates

    XIX.T51-T65.T51   Toxic effect of alcohol

    V.F10-F19.F11   Mental and behavioral disorders caused by the use of opioids

    XIX.T36-T50.T40   Poisoning and Drug psychodysleptics [hallucinogens]

    Contraindications:

    Hypersensitivity, pregnancy, breastfeeding.

    Carefully:Renal, hepatic insufficiency, heart failure, elderly age, children's age till 18 years.
    Pregnancy and lactation:

    Category FDA AT.

    The use is contraindicated in pregnancy. Penetrates into breast milk, at the time of treatment should stop breastfeeding

    Dosing and Administration:

    Intravenously slowly (within 2-3 min), intramuscularly or subcutaneously.

    When poisoning with opioid analgesics: initial dose - 0,4 mg, if necessary, again at intervals of 3-5 minutes until the onset of consciousness and recovery of spontaneous breathing, the maximum dose - 10 mg; children (initial dose) - 0,005-0,01 mg / kg.

    To accelerate the withdrawal from surgical anesthesia: 0,1-0,2 mg (1.5-3 mkg / kg) every 2-3 minutes until adequate pulmonary ventilation and awakening occur; children - 0,001-0,002 mg / kg intravenously, in the absence of effect - repeatedly to 0.1 mg / kg every 2 minutes until the appearance of spontaneous breathing and recovery of consciousness. If intravenous injection is not possible, enter intramuscularly or subcutaneously with fractional doses; in newborns at the initial dose - 0,01 mg / kg.

    When depression of respiration in newborns, caused by the introduction of narcotic analgesics during labor: 0,1 mg / kg intramuscularly, subcutaneously or intravenously, thereafter possibly a prophylactic dose administration 0,2 mg (0.06 mg / kg) intramuscularly.

    For the purpose of diagnosing opioid addiction: 0,8 mg intravenously.

    Side effects:

    From the nervous system and sensory organs: trembling, convulsions.

    From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): hypertension, tachycardia, cardiac arrest.

    On the part of the digestive system: nausea, vomiting.

    Others: increased sweating.

    Overdose:

    Not described.

    Treatment is symptomatic.

    Interaction:

    Under the influence of naloxone, it is possible to reduce the antihypertensive effect of clonidine.

    Special instructions:

    Caution is used in patients who received a high dose of opioid analgesic, suffering from physical opioid dependence,and in newborns from mothers with this pathology.

    When using naloxone, you need constant monitoring of the doctor.

    Naloxone is ineffective in respiratory depression caused by non-opioid drugs.

    Naloxone can be used as a means for differential diagnosis of opioid analgesics. It is possible to use naloxone in an overdose with so-called partial antagonists of opioid receptors (pentazocine and nalboufine).

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