Active substanceNaloxoneNaloxone
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  • Naloxone
    solution
    Kern Pharma S.L.     Spain
  • Naloxone
    solution for injections 
  • Naloxone
    solution w / m in / in PC 
  • Targin®
    pills inwards 
    Mundifarma     Switzerland
  • Dosage form: & nbsp

    injection

    Composition:

    1 ml of solution:

    Active substance: 400 μg of naloxone hydrochloride dihydrate (in terms of naloxone hydrochloride)

    Excipients: sodium chloride - 8.55 mg, hydrochloric acid diluted (to pH 3 - 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:

    Naloxone is a specific antagonist of opioid receptors. Competitively communicates with the main types of opioid receptors and prevents or eliminates central (including respiratory depression) and peripheral effects as endogenous opioid peptides, and exogenous opioids - narcotic analgesics and their surrogates.

    It also affects the dopaminergic and GABA-ergic system of the brain. Does not cause tolerance and drug dependence. People with drug dependence provoke the development of withdrawal symptoms.

    With intravenous administration, the effect develops within the first 2 minutes, with intramuscular and subcutaneous injection - after 2-5 minutes and reaches a maximum after 5-15 minutes. The duration of action is from 20-45 minutes after intravenous administration and 2.5-3 hours after intramuscular and subcutaneous administration.

    Practical value has the ability to restore breathing, reduce the sedative and euphorizing effect, weaken the hypotensive effect.

    The psychotomimetic effects and dystrophy caused by narcotic analgesics of the agonist-antagonist group (pentazocine, butofanol) naloxone has no pronounced effect. Not effective as a tramadol antagonist. Completely does not eliminate the effects of buprenorphine.

    Naloxone provokes a withdrawal syndrome in patients with drug dependence for opioids. Naloxone does not cause addiction and drug dependence.
    Pharmacokinetics:

    Penetrates through blood-brain and placental barriers. The half-life of blood plasma (T1/2) - about 1 hour (30-80 minutes). In adults T1/2 - about 64 +/- 12 minutes; in newborns (after injection into the umbilical vein) - about 3.1 +/- 0.5 hours; in premature infants T1/2 - about 51.8 +/- 9.2 minutes. Naloxone is metabolized in the liver with the formation of predominantly glucuronides and is excreted through the kidneys (within 72 hours 70% of the administered dose is excreted).

    Indications:

    - ABOUTthe structure of poisoning (overdose) with narcotic analgesics (morphine, trimperidine, fentanyl) and other medicines, the mechanism of toxic effect of which has an opioid component (opioid substitutes, methadone, pentazocine, buprenorphine, butorphanol, nalboufine and others) in combination with other resuscitation measures;

    - postoperative application: acceleration of the exit from general anesthesia, before the end of controlled breathing (the drug is used only if narcotic analgesics were used during the operation);

    - Restoration of respiration in newborns after the introduction of opioid analgesics to mothers;

    - as a diagnostic tool in patients with suspected drug (opioid) dependence - naloxone test.

    Contraindications:Hypersensitivity to naloxone in a history of patients.
    Carefully:

    When using naloxone, oxygen therapy and resuscitation should be provided, as well as access to equipment that allows cardiopulmonary resuscitation.

    Caution should be exercised when using naloxone in patients with heart, lung, liver and / or kidney problems, during pregnancy, lactation, childhood, in persons with established or suspected physical dependence on opioids, and in newborns whose mothers indicated in the history of dependence on opioids (sudden and complete abolition of narcotic action can cause acute withdrawal syndrome).

    Carefully apply naloxone in the treatment of respiratory depression caused by the use of buprenorphine, since the response to the use of naloxone may be incomplete. In this case, artificial ventilation should be used.

    Since the duration of action of naloxone is shorter than the duration of opioids, there is a risk of a decrease in respiratory activity.

    Sudden abolition of opioids after surgery can cause nausea, vomiting, sweating, shaking, tachycardia and other symptoms. Unwanted effects are possible.

    Pregnancy and lactation:

    During pregnancy and during breastfeeding, the drug should be used only in cases of acute need.

    Dosing and Administration:

    The rate of administration of the drug should be selected individually, depending on the patient's response to the use of naloxone and the previously administered single doses.

    Naloxone is used intravenously, intramuscularly or subcutaneously.

    In the case of infusion, a solution of naloxone is diluted in 0.9 % solution of sodium chloride or 5% dextrose solution as follows: 2000 μg (5_ ml solution containing 400 μg / ml naloxone) is added to 500 ml of infusion medium. The solution obtained after dilution contains 4 μg of naloxone in 1 ml. The solution is prepared immediately before use.

    Dosing regimen

    The dose of naloxone and the method of application depend on the patient's condition, type and amount of opioid taken.

    In acute poisoning ('overdose') with narcotic analgesics.

    Adults

    The initial single dose is 400-2000 μg intravenously slowly (within 2-3 minutes). If necessary, the dose can be repeated after 2-3 minutes, until the restoration of consciousness and even breathing. If after the introduction of a total dose of naloxone 10 mg there was no recovery of consciousness and breathing, we should assume another (non-opioid) cause of poisoning.

    Naloxone can also be administered intramuscularly or subcutaneously. In menacing states of life, an intravenous route of administration is preferred.

    Children

    The initial single dose is 10 μg / kg intravenously slowly (within 2-3 minutes). If necessary, after 2-3 minutes, an additional dose of 100 μg / kg can be administered.

    If it is impossible to apply naloxone intravenously, injected intramuscularly or subcutaneously in divided doses at intervals of 2-3 minutes. With intramuscular injection, the effect of the drug manifests itself more slowly. A dose of about 200 μg (i.e., about 60 μg / kg) can be administered once, resulting in a longer duration of action.

    Postoperative use: to accelerate the recovery from general anesthesia / if narcotic analgesics were used during the operation.

    Adults

    Intravenously, 100-200 μg (1.5-3 μg / kg) of naloxone solution every 2-3 minutes until adequate pulmonary ventilation and awakening of the patient occur, but without distinct pain and discomfort. A dose that exceeds the minimum required may cause the analgesia to stop and increase blood pressure, as well as other symptoms: nausea, vomiting, increased sweating, dyscirculatory crisis.

    In some cases, especially after taking opioid analgesics with a long duration of action, intramuscular injection of an additional dose of naloxone is necessary within 1-2 hours.

    The drug is also administered by intravenous infusion.

    Children

    Intravenously 10 μg / kg naloxone solution. If necessary, an additional dose of 100 mcg / kg can be administered.

    If it is impossible to apply naloxone intravenously, injected intramuscularly or subcutaneously in divided doses at intervals of 2-3 minutes. With intramuscular injection, the effect of the drug manifests itself more slowly. A dose of about 200 μg (i.e., about 60 μg / kg) can be administered once, resulting in a longer duration of action.

    The drug is also administered by intravenous infusion.

    Restoration of respiration in newborns after the introduction of opioid analgesics

    Newborns

    Before the introduction of the drug, it is necessary to check the patency of the airway of the newborn.

    Intravenously, intramuscularly or subcutaneously, 10 μg / kg. If necessary, the dose can be repeated after 2-3 minutes.

    After the birth of a child, one can administer 200 mg (ie, about 60 μg / kg) of naloxone for intramuscular injection.

    As a diagnostic tool in patients with suspected drug (opioid) dependence

    An intravenous dose of 0.5 mcg / kg allows us to decide whether respiratory depression or difficulty in urinating with opioids is caused. Then the dose of naloxone can be increased, avoiding too large doses. Large doses remove any action of the opioid, including pain medication, and also lead to the excitation of the systems of the sympathetic system and the circulatory system.

    Side effects:

    When using the drug in the postoperative period: lowering blood pressure, increasing blood pressure, ventricular tachycardia and ventricular fibrillation, choking, pulmonary edema, cardiac arrest. These effects sometimes lead to death, coma and encephalopathy. When using doses of the drug that exceed the minimum required, the disappearance of analgesia and psychomotor agitation may occur.

    In case of sudden withdrawal of opioids, nausea, vomiting, sweating may appear; tachycardia, increased blood pressure, tremors, cramps, ventricular tachycardia and ventricular fibrillation, pulmonary edema and cardiac arrest, which can lead to death.

    The withdrawal syndrome in patients with opioid dependence: nausea, vomiting, diarrhea, weakness, tachycardia, increased blood pressure, fever, runny nose, sneezing, goosebump (piloorexia), sweating, yawning, nervousness, anxiety, irritability, trembling, spasm in the epigastric region, pain of unclear localization.

    In newborns - cramps, unrestrained crying, hyperreflexia.

    If any of the side effects listed in the manual are aggravated, you will notice any other side effects not listed in the instructions, inform your doctor.

    Overdose:

    There were no cases of acute overdose with Naloxone.

    However, when the drug is administered at high doses (4 mg / kg and above), nausea, vomiting, chills, hyperventilation, convulsions, marked increase or decrease in blood pressure and / or bradycardia may occur.

    When these symptoms appear, conservative treatment is recommended (in intensive care settings).

    Doses of 2 mg / kg can cause cognitive impairment and behavioral symptoms, including irritability, anxiety, stress, suspicion, depression, difficulty concentrating and lack of appetite. Behavioral symptoms can last 2-3 days.

    Somatic symptoms can also be observed, such as dizziness, sweating, nausea and stomach pain, a feeling of heaviness.

    Patients with an overdose of naloxone should be treated symptomatically, under strict supervision.
    Interaction:

    Naloxone should not be used intravenously with other medicines.

    The drug reduces the hypotensive effect of the cladidine; reduces the effect of opioid analgesics (including butorphanol, nalbuphine, pentazocine, fentanyl, remifentanil) and speeds up the appearance of the "withdrawal" syndrome. Incompatible with solutions of drugs containing bisulfites. Pharmaceutically compatible with sodium chloride solution 0,9 %, solution of dextrose 5%, sterile water for injections. Methohexital (a short-acting barbituric acid derivative) blocks the acute onset of withdrawal caused by naloxone in persons with drug dependence.

    Effect on the ability to drive transp. cf. and fur:When using the drug, it is forbidden to operate vehicles and other moving mechanical devices.
    Form release / dosage:

    Solution for injection 400 mcg / ml.

    Packaging:1 ml per ampoule of colorless glass.Above the point of the ampulla fracture is a point of white or red color, as well as strips in the form of rings: the upper ring is yellow, and the lower ring is pink-violet. 5 ampoules are placed in a tray for ampoules made of PVC. In a cardboard bundle there are two pallets (10 ampoules) with instructions for use.
    Storage conditions:

    Store in a 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:П N011962 / 01
    Date of registration:10.08.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:Warsaw Pharmaceutical Plant Polfa, JSCWarsaw Pharmaceutical Plant Polfa, JSC Poland
    Manufacturer: & nbsp
    Representation: & nbspAKRIKHIN OJSC AKRIKHIN OJSC Russia
    Information update date: & nbsp28.05.2018
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