The science behind naloxone

Drug overdose is the leading cause of unintentional death in the US, and most of these overdoses involve opioids.1 Naloxone is a life-saving medicine that can be used to quickly reverse opioid overdose and help the victim start breathing within minutes.2 Naloxone is available in a variety of forms, including intranasal spray, which virtually anyone can use to save the life of someone suffering an opioid overdose.2 Read on to learn more about what naloxone is and how it works.

What is naloxone?

Naloxone is a medicine called an opioid antagonist.3 It can be used to quickly reverse the effects of opioids and help restore breathing in a person who has experienced an overdose.3 Naloxone was patented in 1961, approved by the US Food and Drug Administration 10 years later and is considered an essentialmedicine by the World Health Organization.4,5 Naloxone is available as an intranasal spray that is easy to carry and use in an emergency situation.3 One brand of naloxone nasal spray is called Kloxxado® (naloxone HCl) nasal spray 8 mg.3,6 Another is Narcan® (naloxone HCl) Nasal Spray 4 mg.3,7

How is naloxone administered?

Naloxone can be given as a shot (in a muscle or under the skin), as an IV (in a vein) or as a nasal spray.4 The introduction of naloxone nasal spray in 2015 was a critical development because it enabled people without medical training to safely and effectively administer this life-saving medicine.2,4

What happens during an opioid overdose?

Opioids include prescription drugs such as fentanyl, oxycodone (Oxycontin®), hydrocodone (Vicodin®), codeine and morphine, as well as illegal substances such as heroin and illicitly manufactured fentanyl.3,4 Opioids work (to relieve pain, for example) by binding to opioid receptors.8 (Opioid receptors are found on nerve cells throughout the body, including the brain.8,9) When opioids bind to opioid receptors in the respiratory center of the brain, they can potentially interfere with the body’s natural urge to breathe.8,9 This situation, which is called opioid-induced respiratory depression, can quickly progress to a decreased level of consciousness.10 If and when this happens, a person could slip into a coma, suffer brain damage and/or die.11

How does naloxone affect opioids?

Naloxone works by moving opioids off the opioid receptors in the brain.12 When naloxone is administered soon after someone starts experiencing an overdose, the person will usually wake up within one to three minutes.13 Repeat administration of naloxone may be necessary.13

How much naloxone does it take to reverse an opioid overdose?

The amount of naloxone needed to reverse an opioid overdose often depends on the opioid involved.14 It may take multiple doses of naloxone to revive a person who has overdosed on a larger quantity of an opioid or on a more potent opioid (ie, fentanyl).14 Fentanyl and other synthetic opioids are the drugs most often involved in overdose deaths,15 and research shows that 78% of opioid overdose reversals involve at least 8 mg of naloxone.16

What happens if I give naloxone to someone who is not overdosing on opioids?

Naloxone won’t harm someone if they are not overdosing on opioids, so it’s best to use it even if you only suspect that an overdose is occurring.14 (If the person is, in fact, overdosing on opioids, naloxone can [but does not always] cause unpleasant opioid withdrawal symptoms like anxiety or irritability and/or nausea or vomiting.14) These symptoms and reactions, however, are nothing compared to the devastation of permanent brain damage (which can occur within 4 minutes of oxygen deprivation) and/or death that can occur when a life-saving intervention like naloxone is not used.17

Does naloxone work on non-opioids?

Naloxone works only on overdoses caused by opioids.18 It will not reverse overdose resulting from non-opioid drugs such as cocaine.18 That said, it is important to keep in mind that it is not uncommon for non-opioids to be laced with fentanyl.15,19 Some drug dealers do this to enhance the “high” and promote the addictive properties of the substances they sell.15 It takes only 2 mg of fentanyl to cause a deadly opioid overdose, and when drug dealers misjudge how much fentanyl to add, the results can be fatal.15,20 If multiple drugs are suspected to be involved in an overdose, always to try to revive the victim with naloxone.18

Who should keep naloxone on hand?

It’s possible for nearly anyone to be involved in an opioid overdose emergency—either as a victim or bystander/rescuer.1 If you’re taking an opioid, your risk for accidental opioid overdose may be higher if:21

  • You’re taking a benzodiazepine (certain anxiety, insomnia or seizure medicines)
  • You have a respiratory condition like COPD or sleep apnea
  • You’re currently in recovery for or have a history of substance use disorder (SUD)
  • You’re being treated for mental illness

If you or someone you live with takes opioids and meets one or more of the criteria above, be prepared. Make sure an intranasal naloxone spray like Kloxxado® is part of your first aid kit.

Where can I get naloxone?

Your doctor can tell you more about naloxone and may write you a prescription (if naloxone is covered by your health insurance, having a prescription may enable you to get it at a lower cost or maybe even at no cost). Naloxone intranasal spray is available at pharmacies across the United States under the brand names Kloxxado® and Narcan®. If your pharmacy doesn’t carry naloxone, they should be able to order it for you. You may also be able to get naloxone through a community program in your city or state.

Kloxxado® is a registered trademark of Hikma Pharmaceuticals USA Inc.

All other trademarks are the property of their respective owners.

Please see the Full Prescribing Information and Medication Guide for Kloxxado® for complete product details.

NOTE: This article was not written by a medical professional and is not intended to substitute for the guidance of a physician. These are not Hikma’s recommendations, but rather facts and data collected from various reliable medical sources. For a full list of resources and their attributing links, see below.

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References

  1. Addressing the Opioid Crisis. National Safety Council website. Available at: https://www.nsc.org/home-safety/safety-topics/opioids. Accessed December 2, 2023.
  2. Jordan MR, Morrisonponce D. Naloxone. [Updated 2023 Apr 29]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2023 Jan. Available at: https://www.ncbi.nlm.nih.gov/books/NBK441910/#article-25518.s3. Accessed December 2, 2023.
  3. Naloxone DrugFacts/What is naloxone? National Institutes of Health/National Institute on Drug Abuse website. Available at: https://nida.nih.gov/publications/drugfacts/naloxone. Accessed December 2, 2023.
  4. Naloxone. Brittanica website. Available at: https://www.britannica.com/science/naloxone. Accessed December 2, 2023.
  5. World Health Organization Model List of Essential Medicines, 21st List, 2019. Geneva: World Health Organization; 2019. Licence: CC BY-NC-SA 3.0 IGO. Available at: https://iris.who.int/bitstream/handle/10665/325771/WHO-MVP-EMP-IAU-2019.06-eng.pdf?sequence=1&isAllowed=y. Accessed December 2, 2023.
  6. Kloxxado® (naloxone HCl) nasal spray 8 mg [prescribing information]. Columbus, OH: Hikma Pharmaceuticals USA Inc.; 2021.
  7. Narcan® (naloxone HCl) nasal spray 4 mg [prescribing information]. Plymouth Meeting, PA: Emergent Devices Inc.; 2021.
  8. Schiller EY, Goyal A, Mechanic OJ. Opioid Overdose. [Updated 2023 Jul 21]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2023 Jan. Available at: https://www.ncbi.nlm.nih.gov/books/NBK470415/. Accessed December 2, 2023.
  9. How opioid drugs activate receptors. National Institutes of Health website. Available at: https://stagetestdomain3.nih.gov/news-events/nih-research-matters/how-opioid-drugs-activate-receptors. Accessed December 2, 2023.
  10. Baldo BA, Rose MA. Mechanisms of opioid-induced respiratory depression. Arch Toxicol. 2022;96(8):2247-2260.
  11. Prescription Opioids DrugFacts/What are prescription opioids? National Institutes of Health/National Institute on Drug Abuse website. Available at: https://nida.nih.gov/publications/drugfacts/prescription-opioids. Accessed December 2, 2023.
  12. Facing Addiction in America: The Surgeon General’s Report on Alcohol, Drugs, and Health. US Department of Health and Human Services (HHS), Office of the Surgeon General, Washington, DC: HHS, November 2016.
  13. Access to Naloxone Can Save a Life During an Opioid Overdose. US Food and Drug Administration website. Available at: https://www.fda.gov/consumers/consumer-updates/access-naloxone-can-save-life-during-opioid-overdose. Accessed December 2, 2023.
  14. Frequently Asked Questions about Naloxone. Centers for Disease Control and Prevention website. Available at: https://www.cdc.gov/stopoverdose/naloxone/faq.html. Accessed December 2, 2023.
  15. Fentanyl Facts. Centers for Disease Control and Prevention website. Available at: https://www.cdc.gov/stopoverdose/fentanyl/index.html. Accessed December 2, 2023.
  16. Abdelal R, Banerjee R. Real-world study of multiple naloxone administration for opioid overdose reversal among bystanders. Harm Reduct J. 2022. 19:49.
  17. CPR – adult and child after onset of puberty. MedlinePlus website. Available at: https://medlineplus.gov/ency/article/000013.htm#:~:text=Time%20is%20very%20important%20when,4%20to%206%20minutes%20later. Accessed February 15, 2024.
  18. Law Enforcement Toolkit/Does naloxone reverse any overdose? Bureau of Justice Assistance/US Department of Justice National Training and Technical Assistance Center website. Available at: https://bjatta.bja.ojp.gov/naloxone/does-naloxone-reverse-any-overdose. Accessed December 2, 2023.
  19. Drug Overdose Death Rates. National Institute on Drug Abuse website. Available at: https://nida.nih.gov/research-topics/trends-statistics/overdose-death-rates. Accessed December 2, 2023.
  20. One Pill Can Kill. US Drug Enforcement Administration website. Available at: https://www.dea.gov/onepill. Accessed December 2, 2023.
  21. Naloxone: The Opioid Reversal Drug that Saves Lives. US Department of Health and Human Services website. Available at: https://www.hhs.gov/system/files/naloxone-coprescribing-guidance.pdf. Accessed December 2, 2023.