Naloxone

Generic name: Naloxone
Dosage form: Injectable solution (Zimhi 5 mg/0.5 mL), Nasal spray (Narcan 4 mg, Kloxxado 8 mg)
Drug class: Antidotes

Usage of Naloxone

Naloxone is an FDA approved medicine used to quickly reverse an opioid overdose. Naloxone is a opioid antagonist that works by attaching to opioid receptors and therefore reverses and blocks the effects of other opioids. 

Naloxone should be used as soon as possible to treat a known or suspected opioid overdose emergency if there are signs of slowed breathing, severe sleepiness or the person is not able to respond (loss of consciousness). Once naloxone has been given the patient must receive emergency medical care straight away, even if they wake up.

Naloxone is not a controlled substance, according to the US Drug Enforcement Administration (DEA).

Naloxone is available as a nasal spray (Narcan 4mg, Kloxxado 8mg) or an injection (Zimhi 5 mg/0.5 mL).

Narcan nasal spray became approved by the FDA on March 29, 2023 as is an over-the-counter (OTC) medicine that is available without a prescription. Other naloxone products are still prescription medicines, but in many states, these products are available from a pharmacist without a prescription from your doctor, under state Naloxone Access Laws or alternate arrangements.

Opioids are sometimes called a narcotic. Examples of opioids are Buprenorphine, codeine, Fentanyl, oxycodone (Oxycontin), heroin, hydrocodone (Vicodin, Lortab), hydromorphone, Meperidine, morphine, methadone, oxymorphone, and tramadol. 

Naloxone side effects

Get emergency medical help if you have signs of an allergic Reaction to naloxone: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Because naloxone reverses opioid effects, the administration may cause sudden withdrawal symptoms such as:

  • nausea, vomiting, diarrhea, stomach pain;
  • fever, sweating, body aches, weakness;
  • tremors or shivering, fast heart rate, pounding heartbeats, increased blood pressure;
  • goose bumps, shivering;
  • runny nose, yawning; or
  • feeling nervous, restless, or irritable.

    • Sudden withdrawal symptoms in a baby younger than 4 weeks old may be life-threatening if not treated the right way. Symptoms include crying, stiffness, overactive reflexes, and seizures. Call your doctor or get emergency medical help if you are unsure how to properly give this medicine to a baby.

    This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

    Before taking Naloxone

    You should not be treated with this medicine if you are allergic to naloxone or any iNACtive ingredients in the injection or nasal spray.

    If possible, before you receive naloxone, tell your doctor if:

  • you have heart problems; or
  • you are pregnant or breastfeeding.

    • Using naloxone while you are pregnant may cause opioid withdrawal effects in your unborn baby. However, having an opioid overdose can be fatal to both mother and baby. It is much more important to treat an overdose in the mother. You must get emergency medical help after using this medicine. Be sure all emergency medical caregivers know that you are pregnant.

    If you use opioid medicine while you are pregnant, your baby could become Dependent on the drug. This can cause life-threatening withdrawal symptoms in the baby after it is born. Babies born dependent on opioids may need medical treatment for several weeks.

    In an emergency, you may not be able to tell caregivers if you are pregnant or breastfeeding. Make sure any doctor caring for your pregnancy or your baby knows you received this medicine.

    Relate drugs

    How to use Naloxone

    Usual Adult Dose for Opioid Overdose

    Initial dose:

  • 0.4 mg to 2 mg IV; alternatively, may give IM or suBCUTAneously
  • If the desired response is not obtained, doses should be repeated at 2 to 3 minute intervals
  • If no response is observed with a total dose of 10 mg, the diagnosis of opioid-induced or partial opioid-induced toxicity should be questioned

    • Auto-injector:

  • Administer 0.4 mg (1 actuation) IM or subcutaneously into the anterolateral aspect of the thigh (through clothing if necessary)
  • If the desired response is not achieved, a second dose may be administered after 2 or 3 minutes; additional doses may be administered every 2 to 3 minutes until emergency medical assistance arrives

    • Nasal Spray:

  • Administer 1 spray intranasally into 1 nostril
  • If the desired response is not achieved after 2 or 3 minutes, give a second dose intranasally into alternate nostril; additional doses may be administered every 2 to 3 minutes in alternating nostrils until emergency medical assistance arrives

    • Comments:

  • IV route is recommended in emergency situations since it has the most rapid onset of action.
  • The duration of action of some opioids exceed that of this drug, therefore, repeat doses may be needed; the need for repeat doses will depend on the amount, type, and route of administration of the opioid being antagonized.

    • Usual Adult Dose for Reversal of Opioid Sedation

    Initial dose:

  • 0.1 to 0.2 mg IV at 2 to 3 minute intervals to the desired degree of reversal
  • Supplemental doses administered IM have been shown to produce a longer-lasting effect

    • Intravenous Infusion:

  • A concentration of 0.004 mg/mL may be administered by IV infusion; titrate in accordance with patient's response

    • Comments:

  • For the partial reversal of opioid depression following the use of opioids during surgery, smaller doses of naloxone are usually sufficient; larger than necessary doses may result in significant reversal of analgesia and increases in blood pressure.

    • Usual Pediatric Dose for Opioid Overdose

    Neonates:

  • Initial dose: 0.01 mg/kg IV, IM, or subcutaneously; repeat dose every 2 to 3 minutes as needed

    • Children:

  • Initial dose: 0.01 mg/kg IV; if desired response is not obtained, may give 0.1 mg/kg IV
  • If IV route is not available may give IM or subcutaneously in divided doses.
  • Administer 0.4 mg (1 actuation) IM or subcutaneously into the anterolateral aspect of the thigh (through clothing if necessary); if desired response is not achieved, a second dose may be administered after 2 or 3 minutes; additional doses may be administered every 2 to 3 minutes until emergency medical assistance arrives
  • Under 1 year of age: Thigh muscle should be pinched while administering injection

    • Comments:

  • Neonatal opioid withdrawal syndrome may be life-threatening and should be treated according to protocols developed by neonatology experts.
  • To avoid precipitating opioid withdrawal symptoms, consider use of a naloxone product that can be dosed according to weight and titrated to effect.
  • The duration of action of some opioids will exceed that of this drug, therefore, repeat doses may be needed; the need for repeat doses will depend on the amount, type, and route of administration of the opioid being antagonized.
  • Patients should remain under continued surveillance; if a patients responds and relapses back into respiratory depression, additional doses should be given.
  • Additional supportive and/or resuscitative measures may be helpful while awaiting emergency medical assistance.

    • Usual Pediatric Dose for Reversal of Opioid Sedation

    Neonates:

  • Initial dose: 0.01 mg/kg IV, IM or subcutaneously at 2 to 3 minute intervals to the desired degree of reversal

    • Children:

  • 0.005 mg to 0.01 mg IV at 2 to 3 minute intervals to the desired degree of reversal

    • Intravenous Infusion:

  • A concentration of 0.004 mg/mL may be administered by IV infusion; titrate in accordance with patient's response

    • Comments:

  • For the partial reversal of opioid depression following the use of opioids during surgery, smaller doses of naloxone are usually sufficient; larger than necessary doses may result in significant reversal of analgesia and increases in blood pressure.

    • Warnings

    In an emergency situation it may not be possible before you are treated to tell your caregivers about your health conditions or if you are pregnant or breast feeding. Make sure any doctor caring for you afterward knows that you have received this medicine. A person caring for you can give the naloxone if you stop breathing or don't wake up. Make sure any person caring for you knows where you keep this medicine and how to use it.

    Your caregiver must get emergency help after giving you this medicine. You may need another injection every 2 to 3 minutes until emergency help arrives.

    Drinking alcohol can increase certain side effects of naloxone.

    Naloxone may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

    If you are using any narcotic pain medication, the pain-relieving effects of the narcotic will be reversed while you are also receiving this medicine.

    What other drugs will affect Naloxone

    Other drugs may interact with naloxone, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell your doctor about all your current medicines and any medicine you start or stop using.

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