Searching For The Next Naloxone

By Kelly Burch 07/03/18
Experts are concerned that naloxone may not be strong enough for synthetic opioids such as fentanyl and carfentanil.
a box of naloxone vials

Naloxone is—at times—a seemingly miraculous drug. Within minutes of naloxone being administered, someone who was unresponsive because of an opioid overdose can start breathing on their own and regain consciousness.

However, despite its strengths, there are issues with the drug that have left healthcare professionals and policy makers pushing for alternatives. 

One of the biggest issues with naloxone today is that it is reportedly not as effective at reversing overdoses from powerful synthetic opioids like fentanyl and carfentanil.

In these cases, a person might need multiple doses of the opioid reversal drug in order to see a benefit. This isn’t just expensive, but can also cost someone their life if there aren’t enough doses immediately available. 

Another issue is that opioids remain active in the body for longer than naloxone does. Because of this, someone can be revived using the opioid reversal drug, but later slip back into an overdose when the effects of naloxone have worn off. 

Both of these concerns have led to the search for alternatives to naloxone. 

“The strategies we’ve done in the past for reversing overdoses may not be sufficient,” Nora Volkow, director of the National Institute on Drug Abuse (NIDA), recently said in a speech at the 2018 National Rx Drug Abuse and Heroin Summit, according to STAT News. “We need to develop alternative solutions to reversing overdoses.”

Dr. Jay Kuchera, a Florida-based addiction medicine specialist for Resolute Pain Solutions, said that “naloxone is being outgunned” by synthetic opioids that have largely replaced heroin in many areas of the country. 

“Naloxone seemed to be great for the older opioids,” Kuchera said. “But now that we’re encountering these nonmedical, ungodly [opioids] like carfentanil… we need to get with the times.”

In 2016, one report found that the market for opioid reversal drugs was valued at nearly $1 billion, so there are good economic incentives for companies to find alternatives to naloxone.

Opiant Pharmaceuticals, which developed Narcan (the nasal spray version of naloxone), has had early success with a drug that works the same way as naloxone but lasts longer, so that the victim would be less likely to slip into another overdose after administration. 

“Compounds like fentanyl, carfentanil, and other synthetic opioids act for longer periods of time,” said Dr. Roger Crystal, CEO of Opiant. “The concern is that naloxone’s half-life doesn’t provide sufficient cover to prevailing amounts of fentanyl in the blood.”

Because many overdose deaths occur when a person stops breathing, scientists are also examining whether they can use drugs to keep a person breathing even while not reversing the overdose itself. For this, researchers are looking at ampakines, a class of drugs that can counteract respiratory depression. 

Some people argue that funds would be better used to address the causes of addiction or to further study naloxone to see if it is indeed less effective against synthetic opioids, but Volkow said that having new and potentially better options for saving people from overdose is critical.  

“There are so many people dying that we have to recognize the urgency,” Volkow said. “We obviously value basic science, but at the same time we have to recognize because of the current situation, the development of medication the can help address the crisis has become our top priority.”

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Kelly Burch writes about addiction and mental health issues, particularly as they affect families. Follow her on TwitterFacebook, and LinkedIn.