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Naloxone

Medical and Pharmacy Editor:

Brand Name: Narcan, Evzio

Generic Name: naloxone

Drug Class: Opioid Reversal Agents; Opioid Antagonists

What Is Naloxone and How Does It Work?

Naloxone is used for the emergency treatment of known or suspected opioid (narcotic) overdose.

Serious overdose symptoms may include unusual sleepiness, unusual difficulty waking up, or breathing problems (ranging from slow/shallow breathing to no breathing).

Other symptoms of overdose may include very small "pinpoint" pupils, slow heartbeat, or low blood pressure.

If someone has serious overdose symptoms but you are not sure if he or she has overdosed, give this medication right away anyway, since prolonged slow/shallow breathing may cause permanent damage to the brain or death.

Naloxone belongs to a class of drugs known as opioid antagonists.

It works by blocking the effects of the opioid in the brain.

This medication may not work as well to block the effects of certain types of opioids (mixed agonist/antagonists such as buprenorphine, pentazocine).

With these types of opioids, blocking may be incomplete or you may need a higher dose of naloxone.

The effects of naloxone will not last as long as the effects of the opioid.

Since treatment with this medication is not long-lasting, be sure to get medical help right away after giving the first dose of naloxone.

Treatment of opioid overdose should also include breathing treatment (such as oxygen given through tubes in the nose, mechanical ventilation, artificial respiration).

Naloxone is available under the following different brand names: Narcan, and Evzio.

Dosages of Naloxone:

Adult and Pediatric Dosage Forms and Strengths

Injectable solution

  • 0.4 mg/mL
  • 1 mg/mL

IM/SC auto-injector

  • 20 mg

Injection, powder for reconstitution

  • 0.4 mg/0.4mL (2 auto-injectors/package)

Dosage Considerations – Should be Given as Follows:

Opioid Overdose

  • Indicated for the complete or partial reversal of opioid depression (including respiratory depression) induced by natural and synthetic opioids
  • 0.4-4 mg intravenously/intramuscularly/subcutaneously (IV/IM/SC); repeat every 2-3 minutes as needed; not to exceed 10 mg (0.01 mg/kg)
  • Consider other causes of respiratory depression if desired response not achieved after 0.8 mg total
  • Endotracheal: 2-2.5 times (0.8-1 mg) initial intravenous (IV) dose
  • For chronic opioid abuse, use smallest doses (0.1-0.2 mg) and titrate to reversal of respiratory depression

Opioid Reversal, Pediatric

Postanesthesia (acute) opioid reversal

  • Neonates: 0.01 mg/kg intravenously (IV) into umbilical vein/IM/SC; give subsequent dose of 0.1 mg/kg if needed
  • Children: 0.01 mg/kg IV x1; may repeat with 0.1 mg/kg

Therapeutic opioid dosing

Acute opioid overdose

  • Up to 20 kg or under 5 years: 0.1 mg/kg/dose intravenously/intramuscularly/subcutaneously/endotracheal tube (IV/IM/SC/ET); if needed, repeat every 2-3 minutes as needed; not to exceed 2 mg/dose
  • Greater than 20 kg or 5 years and older: 2 mg IV/IM/SC/ET; if needed, repeat every 2-3 minutes as needed

Continuous IV infusion

  • For use in patients exposed to long acting opioids (e.g., methadone), sustained release products
  • Calculate dose/hour based on effective intermittent dose used and duration of adequate response seen
  • Alternatively, use two-thirds of initial effective naloxone bolus on an hourly basis (0.25-6.25 mg/hour); administer one-half of initial bolus dose 15 min after initiating continuous IV infusion to prevent drop in naloxone levels

Evzio Auto-Injector

  • Indicated for immediate administration as emergency treatment of known or suspected opioid overdose, as manifested by respiratory and/or central nervous system depression
  • Adult and pediatric: 0.4 mg or 2 mg IM/SC into anterolateral aspect of the thigh (through clothing if necessary)
  • If child is under 1 year, pinch the thigh muscle while administering the dose
  • Seek emergency medical care immediately after use
  • Additional doses may be administered every 2-3 minutes until EMS arrives

Dosing considerations (Evzio)

  • Take-home, single-use auto-injector with visual and voice instruction for guidance
  • May be prescribed to a family member or caregiver
  • Compact size for portability with retractable needle system
  • Intended for immediate administration as emergency therapy in settings where opioids may be present
  • Not a substitute for emergency medical care
  • Also see Administration
Prescription Drug Abuse: Statistics, Facts, and Symptoms

What Are Side Effects Associated with Using Naloxone?

Side effects of naloxone include:

Abrupt reversal of narcotic depression may result in:

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

What Other Drugs Interact with Naloxone?

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

Severe interactions of naloxone include:

  • None

Serious interactions of naloxone include:

  • naloxegol

Moderate interactions of naloxone include:

  • buprenorphine
  • buprenorphine buccal

Naloxone has mild interactions with at least 25 different drugs.

This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns or for more information about this medicine.

Prescription Drug Abuse: Statistics, Facts, and Symptoms

What Are Warnings and Precautions for Naloxone?

Warnings

  • This medication contains naloxone. Do not take Narcan or Evzio if you are allergic to naloxone or any ingredients contained in this drug.
  • Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

  • Hypersensitivity

Effects of Drug Abuse

Opioid withdrawal:

  • Use in patients who are opioid dependent may precipitate acute abstinence syndrome
  • Syndrome characterized by body aches, diarrhea, tachycardia, fever, runny nose, sneezing, goose bumps, sweating, yawning, nausea or vomiting, nervousness, restlessness, or irritability, shivering or trembling, abdominal cramps, weakness, and hypertension
  • In neonates, opioid withdrawal may be life-threatening if not recognized and properly treated and may include convulsions, excessive crying, and hyperactive reflexes

Short-Term Effects

  • See "What Are Side Effects Associated with Using Naloxone?"

Long-Term Effects

  • See "What Are Side Effects Associated with Using Naloxone?"

Cautions

  • Caution in patients with cardiovascular disease or seizures
  • Avoid excessive dose after use of opioids in surgery; abrupt postoperative reversal may cause nausea/vomiting, swelling (edema), fast heart rate, sweating, and may unmask pain
  • Recurrence of respiratory depression may occur if opioid involved is long-acting or a partial agonist (e.g., methadone, buprenorphine)
  • Opioid withdrawal:
    • Use in patients who are opioid dependent may precipitate acute abstinence syndrome
    • Syndrome characterized by body aches, diarrhea, tachycardia, fever, runny nose, sneezing, goose bumps, sweating, yawning, nausea or vomiting, nervousness, restlessness, or irritability, shivering or trembling, abdominal cramps, weakness, and hypertension
    • In neonates, opioid withdrawal may be life-threatening if not recognized and properly treated and may include convulsions, excessive crying, and hyperactive reflexes

Pregnancy and Lactation

  • Use naloxone with caution during pregnancy if benefits outweigh risks
  • Animal studies show risk and human studies are not available or neither animal nor human studies were done
  • It is not known if naloxone is distributed in milk; use caution if breastfeeding
Reviewed on 5/3/2017

Medscape. Naloxone.
https://reference.medscape.com/drug/narcan-naloxone-evzio-343741
RxList. Evzio Side Effects Center.
https://www.rxlist.com/evzio-side-effects-drug-center.htm

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