PillsNaloxone is an opioid antagonist used to stop overdoses of opioid drugs, such as prescription painkillers or heroin. Opioid medications or drugs can slow or stop a person’s breathing, a symptom called depressed breathing, and this can eventually lead to hypoxia and death. Naloxone stops opiates from binding to receptors in the brain, which can lead to symptoms of drug withdrawal, but will also allow an individual who is overdosing to breathe normally until help arrives.
This medication has been shown to stop or slow opioid overdoses at the time of the overdose, but further medical research has not shown it to be effective in stopping overdoses of other drugs. While the long-term effects of the drug are still being studied, one-time use to stop an opioid overdose has been shown to be completely safe, nonaddictive, and effective for many patients. Naloxone can affect individuals who are taking other prescription medications, or who have certain physical conditions, so it is important to speak with a doctor about any concerns.


How Is Naloxone Used?

While medical research seeks a greater understanding of possible uses for naloxone, the Food and Drug Administration has only approved this medication to treat immediate known or suspected overdoses of opioid drugs, such as morphine, hydrocodone, oxycodone, or heroin. Naloxone can be administered to a person via a nasal spray or an injection, and the injection may go either directly into the bloodstream or into a large muscle group, like the thigh muscle. Trained medical professionals, such as emergency room doctors, as well as an increasing number of first responders and law enforcement officers, use syringes. Injections work within two minutes, while inhalants work within five minutes. Current medical guidance states that, if the patient does not wake up after one dose, the person may receive a second dose without any physical harm.

Medical professionals caution that civilians who find an individual suffering an opioid overdose should also call 911. Although naloxone is considered an effective treatment to stop or slow overdoses, the effects will wear off within 30-60 minutes after administration.  Anyone who is not a medical professional, and who is assisting a person suffering from an overdose, should always get emergency medical help.


How Does It Work?

Naloxone binds to the same receptors in the brain as opioid drugs, which effectively blocks opiates for a certain period of time. The drug is categorized as a competitive antagonist, meaning it will bind to these receptors faster than opioid drugs will. Naloxone is effective in treating overdoses temporarily because it acts quickly after administration to stop opiates from binding to the brain’s receptors; however, the medication leaves the body faster than opiates do, so the effects will wear off after about an hour. This is why it is important for caregivers or first responders to ensure the individual receives medical care as soon as possible after administering naloxone; otherwise, overdose symptoms will likely recur.

Overdose is a potential concern for anyone using opioid drugs, because of an addiction or because of a chronic pain issue. Accidental overdoses do occur, especially if the person takes a prescribed painkiller alongside other medications that might enhance the opioid’s effect. Doctors sometimes prescribe a dose of naloxone to patients taking these medications to prevent an overdose in the event the medication is accidentally misused or combined with other medications. Naloxone will stop the opioid overdose, but it will not interact with most other medications.

This drug is a pure antagonist, meaning it only competes with opioid drugs and stops their effectiveness, but medical research has not shown naloxone to produce its own effect. This means naloxone is not addictive, which, in the face of a nationwide opioid abuse epidemic, has made the drug increasingly popular in the media.


Does It Have an Impact on Overdoses?

Naloxone has consistently worked to slow or stop opioid overdose symptoms long enough for emergency responders to get medical help for the individual. However, this drug is not effective against other types of overdoses, such as overdoses on alcohol, benzodiazepines, cocaine, or synthetic marijuana.

The Centers for Disease Control and Prevention (CDC) concluded that, between 1996 and 2010, naloxone stopped opioid overdoses in 15 states and the District of Columbia, which resulted in 10,171 overdose reversals – over 10,000 lives were saved thanks to this opioid antagonist.


Physical Effects

Although scientific studies and statistics about naloxone have shown it to be effective in stopping opioid overdoses, or preventing them from becoming fatal, the drug is not prescribed as a treatment for opioid addiction. People who suffer from opioid addiction must seek long-term medical treatment with trained therapists and doctors, and inpatient rehabilitation facilities often work for these individuals.

As mentioned, naloxone only temporarily binds to opioid receptors, and it does not remain in the bloodstream as long as opiates, so overdose symptoms can return after one dose of naloxone wears off. The drug also does not prevent cravings for opiates or the physiological drive to use them; it simply stops the drug from acting in the body for a short period of time.

Naloxone in itself is not addictive, nor does it have side effects on an average person. However, naloxone has been shown to impact people with heart conditions, and, in some cases, has been shown to interact with medications or supplements used to treat high blood pressure or heart disease. Medical research is also being conducted into the potential effects on patients with liver or kidney disease.

While naloxone itself has not been shown to become addictive, the drug can pose some danger for some people who suffer from opioid addictions, because the drug can shock the body into withdrawal. Symptoms of withdrawal commonly include:

  • Shivering or trembling
  • Nervousness or restlessness
  • Body or muscle aches
  • Goosebumps
  • Physical weakness or exhaustion
  • Sweating
  • Watery eyes
  • Runny nose
  • Fever
  • Nausea or vomiting
  • Stomach cramps
  • Diarrhea

In extreme cases, a person may suffer seizures due to opioid withdrawal, but this is a rare side effect. Because opiate withdrawal can be intense, medical detox is always recommended to ensure the safety and comfort of clients.


More Medical Professionals Use and Prescribe Naloxone

The CDC’s first naloxone study concluded in 2010, and it examined 48 organizations that had trained over 53,000 nonmedical personnel, like caregivers, to properly administer the medication. After their findings were published, numerous other organizations began to use naloxone to stop opioid overdoses. By 2014, the CDC found that 136 organizations had trained more than 150,000 nonmedical personnel to administer naloxone to patients. An estimated 26,000 lives have been saved because naloxone was administered in an emergency opioid overdose situation.

The agency also found that people using opioid drugs can be trained to properly administer naloxone to themselves. Distribution programs set up to train these individuals and give them naloxone prescriptions reported that 82.8 percent of overdose reversals occurred because patients administered naloxone themselves. Another 9.6 percent of naloxone administrations came from family or friends of patients. Although emergency responders and hospital staff have used similar opioid antagonists to stop overdoses, they made up only 0.2 percent of naloxone administrations.


Changing Attitudes to Addiction and Recovery with Naloxone

Although naloxone is a prescription medication, the drug is not restricted under any schedule per federal law. This has helped pharmaceutical companies rapidly develop new forms of the drug and distribute this potentially lifesaving medication to caregivers, parents, teachers, and other nonmedical professionals who know someone taking prescription painkillers or who is suffering from opioid addiction. Laws differ in other countries, but the World Health Organization (WHO) recently placed naloxone on their Model List of Essential Medicines.

In the past two years, new forms of naloxone have received FDA approval, including a handheld auto-injector containing a single dose of prescription named Evzio. The small container with automatic syringe allows the patient or caregiver to rapidly administer naloxone in an overdose situation.

In November 2015, the FDA fast-tracked its approval for a new nasal spray form of naloxone, under the brand name Narcan. The spray became the first non-injectable form of naloxone to enter the market. While it still requires a medical professional or a prescription, the drug is considered safer than injectable forms because there is less potential for the needle to become contaminated.

Narcan has become so popular with first responders and emergency room doctors that Adapt Pharma, the company that manufactures Narcan, has partnered with the Clinton Health Matters initiative to fund a supply of the nasal spray to high schools across the country. Abuse of and addiction to prescription pain medication can start early, and the initiative aims to prevent that.

As of September 2015, only seven states in the US had not granted wider access to naloxone for medical professionals, first responders, and nonmedical caregivers, such as teachers and family members. The year prior, based on medical research and the CDC’s statistics, US Attorney General Eric Holder announced that he would like the Department of Justice to allow greater access to the drug to help prevent overdose deaths. Now, 651 law enforcement departments all over the country have armed themselves with naloxone to prevent opioid overdose deaths.

Some skeptics fear that naloxone’s wider availability might encourage more people to misuse or abuse opioid drugs, but most medical professionals disagree. The potential of an accidental overdose is greater with patients who routinely take prescription painkillers, and naloxone helps reduce an overdose’s fatal potential. For patients suffering from an opioid addiction, naloxone is not used as a way to stop the addiction, but only to stop the overdose for a short time.

Medical researchers strongly recommend greater education about naloxone’s properties as it becomes more popular. Naloxone can save lives when used in specific situations, and by saving lives, more people have the chance to find help for addiction through rehabilitation and therapy.