Naloxone (Naloxone)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceNaloxoneNaloxone
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    • Dosage form: & nbsp

    injection

    Composition:

    1 ml of the solution contains:

    Active substance:

    Naloxone hydrochloride in terms of anhydrous substance - 0.4 mg Excipients:
    Sodium chloride 8.6 mg, disodium edetate (disodium ethylenediaminetetraacetic acid) 0.3 mg, hydrochloric acid 0.1 M - to a pH of 3.0 to 4.5, water for injection up to 1 ml.

    Description:Transparent colorless liquid.
    Pharmacotherapeutic group:Opioid receptor antagonist
    ATX: & nbsp

    V.03.A.B.15   Naloxone

    Pharmacodynamics:

    An antagonist of opioid receptors. It blocks opioid receptors, eliminates central (including respiratory depression) and peripheral effects of opioids. It also affects the dopaminergic and GABAergic system of the brain. Does not cause tolerance and drug dependence. People with drug dependence provoke the development of withdrawal symptoms.

    After intravenous administration, the effect develops after 1-2 minutes, after intramuscular injection - 2-5 minutes; reaches a maximum after 5-15 minutes;the duration of the effect depends on the dose and route of administration - with intravenous administration of 0.4 mg, the duration of the effect is 45 minutes, with intramuscular injection, longer (up to 4 hours).

    In experiments on mice and rats, suppression of fertility and the absence of a teratogenic effect.
    Pharmacokinetics:

    Penetrates through the blood-brain and placental barrier. Metabolised in the liver. The half-life of naloxone is 30-80 min. It is excreted by the kidneys (within 72 hours 70% of the administered dose is excreted).

    Indications:

    Overdose of narcotic analgesics.

    Postoperative application: acceleration of the exit from general anesthesia, before the end of controlled breathing. Postoperatively, the drug is used only if narcotic analgesics were used during anesthesia. Naloxone Ineffective for the treatment of respiratory depression caused by substances other than opioids.

    Restoration of respiration in newborns after the introduction of narcotic analgesics. As a diagnostic drug in patients with suspected drug addiction.

    Contraindications:

    Hypersensitivity.

    Carefully:Organic heart disease, lung disease, renal / hepatic insufficiency, the use of narcotic analgesics in high doses, physical opioid dependence, children's age, use in newborns from mothers with opioid dependence.
    Pregnancy and lactation:Use during pregnancy is acceptable if the benefit to the mother exceeds the risk to the fetus. It is not known whether naloxone with breast milk. The use of the drug in the period of breastfeeding is possible by absolute indications.
    Dosing and Administration:

    The drug is administered intravenously, intramuscularly, subcutaneously.
    In case of an overdose of narcotic analgesics to adults - in a dose of 0.4-2 mg, for children - 5-10 μg / kg. If the application in this dose does not bring the expected effect, the administration in the same dose is repeated after 2-3 minutes. The maximum total dose is 10 mg / day. If recovery of consciousness and breathing does not occur, one should think about another (non-opioid) cause of poisoning.

    Postoperative administration is carried out intravenously, at a dose of 0.1-0.2 mg, after 2-3 minutes, the administration of the same dose is repeated until the patient has had satisfactory breathing.Then, if necessary, continue intramuscular injection for several hours.

    In children intravenously, the initial dose is -1-2 μg / kg. If the desired effect is not present, re-enter in doses of up to 0.1 mg / kg every 2 minutes, until spontaneous breathing and recovery of consciousness. If intravenous injection is not possible, it can be administered intramuscularly or subcutaneously in fractional doses.

    In newborns, the initial dose is 0.01 mg / kg. Introduction can be repeated in compliance with the principles of use in adults.

    When oppression of breath caused by the introduction of opioid analgesics of the mother during childbirth, the newborn is administered 0.1 mg / kg intramuscularly, subcutaneously or intravenously. Before administration, it is necessary to make sure that the airway is passable in the newborn. Possible preventive intramuscular injection of 0.2 mg (0.06 mg / kg).

    Diagnosis of opioid dependence - intravenously 0.08 mg.

    Side effects:

    From the digestive system: nausea, vomiting.

    From the cardiovascular system: tachycardia, arrhythmia, increase or decrease in blood pressure.

    After administration in doses exceeding the therapeutic dose,(especially in the postoperative period in patients with diseases of the cardiovascular system): disappearance of analgesia and agitation, decrease / increase in arterial pressure, ventricular paroxysmal tachycardia, fibrillation, ventricles, pulmonary edema, cardiac arrest.

    From the side of the central nervous system: tremor, nervousness, agitation, irritability, fatigue, convulsions, behavioral disorders.

    Other: increased sweating, allergic reactions, pulmonary edema. The withdrawal syndrome in patients with opioid dependence: vague pain, diarrhea, hyperthermia, rhinorrhea, sneezing, goosebumpia, sweating, nausea, vomiting, nervousness, fatigue, irritability, tremor, epigastric spasms, tachycardia, weakness; in newborns - convulsions, diarrhea, hyperthermia, unrestrained crying, hyperreflexia, sneezing, tremor, unusual irritability, vomiting.

    Overdose:

    See the "Side effect" section.

    Interaction:

    Reduces the hypotensive effect of clonidine.

    Reduces the effect of narcotic analgesics (including butorphanol, nal-

    bufina, pentazocine, fentanyl, remifentanil) and accelerates the appearance of the syndrome

    "cancellation".

    Incompatible with solutions of medicines containing hydrosulphates. Pharmaceutically compatible with 0.9% sodium chloride solution, 5% dextrose solution, sterile water for injection.

    Special instructions:

    Can be used as a medicine for differential diagnosis of poisoning with narcotic analgesics. In the application it is necessary to carry out constant medical supervision of the patient.

    Effect on the ability to drive transp. cf. and fur:not described
    Form release / dosage:

    Solution for injection 0.4 mg / ml in ampoules of 4 ml.

    5 ampoules in a contour mesh package made of a polyvinylchloride and-foil film of aluminum printed lacquered or flexible packaging on the basis of aluminum foil, or without foil.

    1 or 2 contiguous cell packs (with foil or without foil), along with instruction on the use of the preparation; knife or scarifier ampullum placed in a pack of cardboard.

    20, 50 or 100 contour cell packs with foil together with 10, 25 or 50 instructions for the use of the preparation respectively, knives or ampoule scalers are placed in a box of cardboard or in a box of corrugated cardboard (for inpatient).When packing ampoules with rings or break points, scarifiers or ampoule knives do not.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    4 years. Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:PL-000266
    Date of registration:16.02.2011
    The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia
    Manufacturer: & nbsp
    Information update date: & nbsp16.02.2011
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