What is Naloxone: A Comprehensive Guide to Naloxone and its Impact

Categories: Naloxone in the Workplace, OHS TrainingPublished On: October 9, 2023
What Is Naloxone? Pronunciation Of Naloxone

What is Naloxone?

Between January 2016 and December 2022 there were 36,442 deaths in Canada related to opioid toxicity. In 2022 alone, Canada experienced 7,328 apparent opioid-related deaths. This represents an average of 20 deaths every day. If a person is experiencing an opioid overdose, the two most significant things that a bystander or first responder can do are call 9-1-1 and administer naloxone.

What is Naloxone? Naloxone is a lifesaving medication that can reverse an opioid overdose temporarily. In this post, we dive deep into what naloxone is, how it works, where to get it, how to use it, and what you can do if you suspect someone is experiencing an opioid overdose. We will also examine the impact of naloxone and harm reduction programs in Canada and the next steps to further advocate for people who use opioids.

The Evolution of Naloxone: From Development to Regulatory Approval

Historical Development of Naloxone as an Overdose Reversal Agent

Naloxone was first developed in the early 1960s and was first approved for the purpose of reversing opioid overdoses by the United States Food and Drug Administration (USFDA) in 1971.

Research and Clinical Trials: Advancement in Naloxone Effectiveness

When naloxone was first approved for use in the United States (US) for the purpose of reversing opioid overdoses, it was primarily used by healthcare providers in hospitals. The first widespread use of naloxone to reverse opioid overdoses in the community was in Italy. Harm reduction agencies began distributing naloxone kits in 1991 and became available without a prescription in 1995.

Regulatory Approvals and Distribution in Canada

Since 1995, there have been advances in reversing opioid overdose deaths around the world. The first nasal spray, naloxone, was approved for use in the US by the USFDA in 2015. To help combat the high rate of opioid overdoses, Health Canada changed how naloxone was regulated, making it available without a prescription. Further, in July 2016, Health Canada granted an emergency approval to import American naloxone nasal spray pending permanent approval in Canada.

Currently, there are several approved formulations of naloxone available in Canada. This includes some that are made for use as nasal sprays and some that are for injection only. Research is still ongoing to improve the effectiveness of and access to naloxone in times of emergency.

Naloxone Formulations: Comparing Injectables and Nasal Sprays

There are two types of naloxone available for use in Canada: injectable or nasal sprays. Both types of naloxone have the same effect. The biggest difference is how a first responder gives the medication to a person suspected of experiencing an opioid overdose.

How Naloxone Works: Mechanism of Action 

Naloxone is a medication called an opioid antagonist. The naloxone molecule binds to a part of the brain called an opioid receptor. These are the same parts of the brain that an opioid, like morphine, fentanyl, or heroin, binds to. The difference between naloxone and an opioid, however, is that naloxone doesn’t cause the same effect on the body as the opioids do. It can also remove an opioid from the opioid receptor and bind with the receptor instead of the opioid and won’t allow another opioid to bind to that receptor until it has worn off.

Essentially, naloxone kicks an opioid off the opioid receptor and blocks anything else from sticking to that receptor for a period of time. It is the opioid that is attached to these receptors in the brain that causes the life-threatening symptoms of an opioid overdose. Without the opioids attached to the receptor, the symptoms of the overdose begin to subside.

Naloxone also works very fast. After giving a dose of naloxone, a first responder could start to see the effects after as little as 2 to 5 minutes. The effects of naloxone typically last between 20 and 90 minutes. The effect of some opioids may last longer, though, so a person experiencing an opioid overdose may require more than one dose of naloxone.

Injectable Naloxone: The Original Formulation

When naloxone was introduced, it had to be administered by injection. A healthcare provider could inject the medication into a vein, which is called an intravenous injection or IV. A healthcare provider could also inject it into a muscle, which is called an intramuscular injection. This is a common way to give many medications, such as flu shots or the COVID-19 vaccine, as well as many other routine and emergency medications.

Naloxone works fastest when delivered through an IV, showing effects in as little as 2 minutes. Intramuscular injections of naloxone can start to show effects in as few as 3 minutes. Both IV and intramuscular injections require careful preparation and training. This makes these routes of administration less effective in emergencies, such as opioid overdoses, where a layperson may be the first responder.

Nasal Spray Naloxone: Ease of Use and Benefits for First Responders

Nasal spray naloxone, also known as intranasal naloxone, is a recent invention. First approved in the US in 2015 and in Canada in 2016, intranasal naloxone contains the same drug as injectable naloxone but is designed and tested to be sprayed as a mist into the nose rather than injected into a vein or muscle. Nasal spray naloxone works slower than injectable naloxone but can still take effect within 3 to 5 minutes after administration.

Nasal spray naloxone is often preferred by first aid providers and non-medical first responders, such as police, for its ease of use. Naloxone nasal sprays come prepackaged and are ready for use as soon as they are opened. Having naloxone ready to use in a single-use delivery device can reduce the time and effort needed to administer the lifesaving medication. It also reduces the risks associated with administering injectable naloxone, such as accidental needle sticks.

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Naloxone Access Programs: Community Distribution and Pharmacy Initiatives

Increased access to naloxone has been recognized to prevent deaths associated with opioids. The more people who use drugs, or who are around people who use drugs, who have access to naloxone and are trained to recognize and respond to an opioid overdose, the greater the chance that someone will survive if they experience one. Many provinces offer programs aimed to get naloxone to the people who may benefit from having a kit, whether they use drugs themselves or support someone who does.

Community-Based Naloxone Access Programs: Targeting At-Risk Populations

The Ontario Harm Reduction Network (OHRN) is a group of harm reduction, public health, social services, and other charitable organizations across Ontario that support harm reduction initiatives. Many member organizations focus on specific vulnerable or at-risk populations that are underrepresented in other areas. For example, a study published by the Library of Parliament noted that individuals who identified as Indigenous and living on reserve experienced opioid overdoses at a rate 5.6 times higher than the rate among non-indigenous people.

Further, in British Columbia, Indigenous women died due to opioid poisoning at a rate 9.9 times higher than non-Indigenous women in the province while Indigenous men died at a rate 4.3 times higher than non-Indigenous men.

A second report by Statistics Canada reviewed data from British Columbia to identify high-risk populations. The report identified several high-risk groups which showed higher levels of overdose deaths than the remainder of the population. These high-risk groups included males working in construction, middle-aged women who access social assistance, and young males who are precariously employed or unemployed.

By identifying high-risk populations, it allows public health officials to target resources where they will be most effective. Many member organizations of the OHRN work closely with specific vulnerable populations. Providing accessible harm reduction at a place and in a way that is appropriate for the individual is key to reducing opioid-related deaths.

Pharmacy Dispensing of Naloxone: Increasing Availability and Accessibility

Many pharmacies across Canada offer naloxone kits free of charge to anyone who may experience an opioid overdose themselves or who believes they are likely to witness someone experience an opioid overdose. In many cases, a person who wants to have a naloxone kit must talk to someone at the pharmacy and then receive training from the pharmacist on how to recognize an opioid overdose and how to administer the naloxone if it is required.

To make it easier for residents to find a naloxone kit, the Ontario Ministry of Health and Long-Term Care publishes an interactive list and map of all locations offering naloxone kits. The list and map can be found by clicking the link here.

Overcoming Barriers: Funding, Legislation, and Public Support for Naloxone Access

One of the most significant barriers to increasing access to naloxone is stigma and public attitude towards drugs and people who use drugs. A literature review published in 2022 found that the most commonly reported barrier to accessing naloxone was stigma from healthcare providers. Additionally, stigma was a significant factor in the general public, with 89.7% of people saying they do not want to have “drug addicts” living nearby.

Some suggested solutions identified in the research included providing naloxone kits any time a person accessed any harm reduction services, even if they did not specifically request one, or creating other spaces that were judgment-free to reduce the stigma associated with requesting naloxone.

In addition to increasing access to naloxone, the Canadian government changed the law to reduce barriers to accessing care for people experiencing opioid overdoses in 2017. The Good Samaritan Drug Overdose Act became law in May 2017. The law provides legal protection against charges for drug possession when accessing emergency medical support for a suspected overdose.

This means that a person who witnesses a suspected opioid overdose can call 9-1-1 without fear they will be arrested because they possess or have taken drugs. The act does not protect a person who is selling or trafficking drugs; it only provides protection to people who use drugs and possess them for their own use.

Some other policies that are currently being considered or that have been implemented in Canada include the decriminalization of personal drug possession, the establishment of supervised consumption sites, and safe supply programs.

British Columbia decriminalized the possession of small amounts of some controlled substances on January 31, 2023. This means that a person who is found to have a drug in their possession will not be charged criminally and may be offered medical help. Safe supply programs are being considered in many areas across Canada. A safe supply program connects a person who uses drugs with a physician, who may prescribe a substance.

The person who uses drugs can then access that drug through a pharmacy or other regulated supplier. This guarantees that the person who consumes the drug knows exactly what is in it. This is done to reduce the impact of contaminants, such as fentanyl or benzodiazepines, in the illicit drug supply. Connecting with a physician also increases the opportunity to provide other medical resources to the person consuming drugs.

Naloxone Training and Education: Empowering Individuals to Respond

A pillar of the current strategy to prevent opioid overdose deaths includes providing training on how to prevent a potential overdose and how to respond if one does occur. Training should be tailored to the specific audience. Medical professionals receive training on topics such as prescribing opioids, harm reduction techniques, counselling patients, and more.

First responders, such as police, firefighters, and paramedics, receive training on how to accurately recognize and respond to an overdose quickly. People who use drugs and people who directly support them may receive training on harm reduction techniques, where to get safe supplies such as naloxone, how to prevent an opioid overdose when they are consuming drugs, and how to use naloxone if it is needed.

Importance of Naloxone Training: Recognizing Opioid Overdose Signs and Symptoms

It is very important to act quickly if you suspect an opioid overdose. The most common cause of death related to opioid overdose is respiratory depression or arrest. This means that a person’s breathing slows or stops entirely. Permanent damage to the organs, including the heart and brain, can occur in as little as 4 to 5 minutes after a person stops breathing.

If a first responder or bystander does not respond within a few minutes of when a person starts experiencing symptoms of an overdose, the damage could be permanent or even lethal. This is also why take-home naloxone is so critical. If a person has naloxone with them at the scene of a suspected overdose, this removes the wait time associated with calling 9-1-1 and waiting for paramedics to arrive with the lifesaving medication.

Training Programs for Laypersons: Equipping Bystanders to Administer Naloxone

Many first aid training curriculums now recognize opioid overdose as a major medical emergency and include training on recognizing and responding to a suspected opioid overdose. Both the Canadian Red Cross and St. Johns Ambulance, which are among the largest first aid training organizations in Canada, provide training on how to recognize an opioid overdose and administer naloxone as part of their regular first aid programming and as standalone courses. Many other first aid providers also offer training on responding to an opioid overdose.

Additionally, the Ontario Ministry of Labour, Immigration, Training and Skills Development has established the Workplace Naloxone Program. Through this program, eligible employers can receive a free naloxone kit and training for two workers at each workplace free of charge.

Healthcare Professional Training: Prescribing, Counselling, and Naloxone Education

There is research currently ongoing in the United States to examine the impact of prescribing and dispensing naloxone at the same time as prescribed opioids. Earlier research suggested that the rate of opioid overdoses decreased if naloxone was prescribed by a physician at the same time as opioids, even if the patient never filled the naloxone prescription.

Additionally, many physicians are now trained to look for the signs of drug abuse in patients who are prescribed opioids. If a physician suspects that their patient may be misusing a prescribed substance, they can develop a treatment plan to reduce the use of a substance or change the way that pain is treated by prescribing other medications or treatments.

Assessing the Impact: Evaluating Naloxone’s Role in Overdose Response and Public Health

Quantitative and Qualitative Measures: Tracking Naloxone Administration and Outcomes

The Ontario HIV Treatment Network (OHTN) published a review of a large number of academic studies that show naloxone can be effective at reducing opioid overdose deaths. However, accurately tracking data was found to be a challenge. This is because of multiple factors.

One major factor is that data is tracked differently depending on the jurisdiction. Additionally, accurately tracking the identity of an individual who has received naloxone was a challenge. To more accurately track the success of naloxone programs, researchers and policymakers need to establish guidelines for data collection to guide future research.

Naloxone Program Evaluation: Successes, Challenges, and Lessons Learned

The report by OHTN also discussed some lessons learned from naloxone programs around the world. Consuming opioids or other drugs at home alone was a factor in a significant number of deaths. A person cannot administer naloxone to themselves if they believe they are experiencing an overdose. If a person is experiencing an opioid overdose, they need to have another person present to administer the naloxone to them.

Another significant challenge that has been identified recently is the composition of the drugs that are publicly available. A recently published study showed a significant increase in the number of drugs being sold as opioids also containing benzodiazepines. Benzodiazepines are a medication that is used to treat anxiety, insomnia, or seizures.

Naloxone does not have an impact on benzodiazepines. When combined with benzodiazepines, the risk of death related to opioid overdose is significantly higher, possibly even double, when compared to opioids alone.

Public Health Implications: Naloxone’s Contribution to Harm Reduction Strategies

Naloxone is just one piece of the public health strategy that is needed to combat the opioid overdose crisis in Canada. Naloxone works to prevent an opioid overdose that has already occurred. Given the recent increase in benzodiazepines and other drugs in the illicit drug market, it is not always effective. Implementing multiple public health initiatives is critical to prevent opioid overdoses before they occur.

Resources and References:

Opioid- and Stimulant-related Harms – canada.ca

Naloxone – canada.ca

The Opioid Crisis in Canada – lop.parl.ca

Exploring the intersectionality of characteristics among those who experienced opioid overdoses: A cluster analysis – statcan.ca

Naloxone – Drugs and Devices – health.gov.on.ca

Perspectives of Stakeholders of Equitable Access to Community Naloxone Programs: A Literature Review – ncbi.nlm.nig.gov

About the Good Samaritan Drug Overdose Act – canada.ca

CPR – adult and child after onset of puberty – MedlinePlus Medical Encyclopedia

Effectiveness of take-home naloxone programs and availability of naloxone nasal spray in different jurisdictions – ohtn.on.ca

The increase in benzodiazepine-laced drugs and related risks in Canada: The urgent need for effective and sustainable solutions – sciencedirect.com

About the Author

Matthew Budau Bscn, Bba (Hons), Rn - Hspi

Matthew Budau
OHS Advisor

Matthew is a Registered Nurse, with a Bachelor of Science in Nursing from Laurentian University. Matthew also holds an Honours Bachelor of Business Administration with a Specialization in Human Resources Management from Algoma University. Matthew draws from his experience across both the public and private sector to develop custom solutions for HSPI’s clients ranging from policy development, to training program development and delivery. Matthew integrates technology using innovative safety software packages to effectively merge health and safety into client business plans.


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