6 Facts About Naloxone, the Drug That Reverses Overdoses

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Six months ago, Rachel* was feeling manic, dealing with a medication imbalance related to her bipolar disorder. With an on/off history of opioid use, the 20-year-old decided to self-medicate with her “tried-and-true method” of stabilization: heroin. “I made a careless mistake, thought I was invincible, and I did a little too much,” she says. “Things started out fine, just another high. But about 30 minutes in, I was puking everywhere and uncontrollably shivering, even under a bunch of blankets.”

The Oregon resident remembers “getting higher and higher,” unable to reverse what she’d done. Rachel faded in and out of consciousness for a while, until she was fully unconscious. She can’t recall anything else—until a friend found her, and jabbed a syringe filled with naloxone into her behind. She estimates the antidote began to work in under a minute. “I took a huge gasp of air, and then everything was fine,” she recalls.

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Such are the dramatic effects of naloxone (sold under the brand names Narcan and Evzio), a drug you're hearing a lot more about these days thanks to the opioid crisis. This epidemic of addiction has left millions of people dependent on illegal narcotics such as heroin, or to prescription opioid pain relievers like oxycodone (brand name: OxyContin), codeine, and morphine.

According to a Vox analysis of CDC statistics, drug overdoses killed more people in 2015 than HIV-AIDS killed during its fatality peak in 1995. Overdoses also take more lives per year than gun violence or car crashes. Here’s everything you need to know about the lifesaving drug that can reverse an opioid overdose.

How does naloxone work?

Naloxone is an opioid antagonist, says Edwin Salsitz, MD, an addiction medicine specialist at Mount Sinai Beth Israel in New York City. When an opioid enters the brain, it attaches to neurotransmitters that give the user a hit or a high. “The naloxone goes to same opioid receptors, removes the drug, and binds to the receptors to block the opioid,” he explains. If a person is overdosing and stops breathing, administering Naloxone can restore normal breathing and save a life.

When was naloxone developed?

Researcher Jack Fishman, PhD, synthesized the drug back in 1961. The idea was that a structural adaptation to the drug oxymorphone, derived from morphine, would work tirelessly to attach to the same brain receptors that opioids like heroin attached to. In essence, naloxone does just that; it pushes harder than opioids to bind to those receptors, preventing overdoses. In 1971, the Food and Drug Administration approved the use of naloxone to counteract overdoses of illegal and prescription drugs.

How effective is it?

Naloxone is extremely successful in reversing an opioid overdose, so much so that it's on the World Health Organization’s Essential Medicines list. It is fast-acting and short-acting, meaning it does its job quickly and only stays in a person's system for roughly 30 to 90 minutes.

Naloxone should be given at the first signs of overdose.“The sooner the drug is given, the better the result, because the brain of a person who isn’t breathing is being deprived of oxygen,” says Thomas Waters, MD, an emergency medicine physician at the Cleveland Clinic. As effective as it is, Naloxone does not work on non-opioid or narcotic drugs, nor will it counteract an alcohol overdose.

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How is naloxone administered?

There are several forms of the drug available, depending on who’s administering it. On the street, Dr. Waters says it can be given as a nasal mist by either an emergency medical technician or a layperson. If an overdose victim enters a hospital ER, naloxone can be given by a medical professional as a shot under the skin or through a breathing tube. Many city police officers also carry it and are trained to use it. Rachel had obtained the injectable form of naloxone from a needle exchange program, which provides sterile needles to injectable drug users, and a friend was able to grab it and give her the shot in time.

What are the side effects?

Aside from the fact that naloxone is “always effective” in preventing overdose death if it’s administered fast enough, Dr. Salsitz says the most incredible part of the drug is that there are virtually no side effects.

“If someone is opioid-addicted, they may experience withdrawal symptoms,” he says, as naloxone blocks the effects of opioid drugs. Withdrawal symptoms include nausea, stomach pain, and anxiety.  However, "it is a great harm-reduction tool. Even the concern that, as an unintended consequence, there might be more opioid use if naloxone became more widely available has proven untrue,” says Dr, Salsitz.

How can I access It?

Thankfully, naloxone is becoming more widely available—particularly in the last decade, with the opioid crisis hitting just about every part of the nation. Dr. Salsitz says that most doctors can prescribe the drug, including primary care physicians, and it is now available at drugstores such as CVS and Walgreens without a prescription in the majority of states. Although the price is not uniform, he says it is “generally affordable” and also covered under Medicaid.

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If you know someone who is struggling with opioid addiction, you can administer the drug in an emergency situation and dial 911. “Previously, people were afraid to report an overdose, because they might get in legal trouble,” Salsitz says. “Most places now have Good Samaritan laws that will exempt someone who calls for help from getting arrested for possession.”

Dr. Waters says to contact the department of public health in your state, who can give you a list of resources on naloxone, as well as direct you to a class or program to help educate you on how to administer the drug. “Naloxone has been used safely for over 40 years,” he explains. “It really is a safe, benign drug with no other effects or uses besides reversing an opioid overdose.”

It’s a shame the drug has not been more widely available in the past, where friends and family of those struggling with addiction could gain easy access to it. The painful irony? Naloxone creator Jack Fishman’s stepson died from a likely overdose of heroin, cocaine, and fentanyl in 2003, when the drug could not have been legally obtained and used. His death didn’t have to happen. Hopefully, with opioid addiction rampant in the U.S. these days, similar tragedies will happen a whole lot less.

*name has been changed