New hope for fentanyl overdose

Fentanyl overdose is a significant and growing issue, particularly in the United States. Fentanyl is a powerful synthetic opioid that is 50 to 100 times more potent than morphine. Due to its potency, even a small amount can lead to a fatal overdose. The rapid onset of its effects and the narrow window for treatment make it especially dangerous.

Current Treatments for Fentanyl Overdose

1. Naloxone: This is the primary treatment for opioid overdoses, including fentanyl. Naloxone can quickly reverse the effects of an overdose by binding to opioid receptors and blocking the effects of the drug. However, due to fentanyl’s potency, multiple doses of naloxone may be required.
2. Supportive Care: This includes providing oxygen and fluids to help the person breathe and maintain blood pressure. In severe cases, CPR may be necessary.
3. Advanced Treatments: Research is ongoing into other treatments, such as nalmefene (another opioid receptor antagonist), respiratory stimulants, and wearable naloxone delivery devices that can provide continuous monitoring and automatic administration of naloxone.

The fentanyl crisis is part of the broader opioid epidemic, which has had devastating effects on communities and healthcare systems. Efforts to combat this crisis include increasing access to naloxone, improving public awareness, and enhancing addiction treatment services.

Cyclodextrin: new hope on the horizon

Lawrence Livermore National Laboratory has a program to develop countermeasures to fentanyl, an opioid 10,000 times more potent than morphine. Very recently, this and related compounds have been associated with post-therapeutic chemical dependencies and as unanticipated components of illicit drugs. They are investigating the ability of cyclodextrins, cyclic carbohydrates, to neutralize the effects of fentanyl by binding it within its hollow central cavity thereby reducing its bioavailability. Starting with commercially available cyclodextrins, they used a combined experimental and computational approach to screen modified cyclodextrins with enhanced affinity for fentanyl and its analogues.

This work has resulted in the identification of a specialized cyclodextrin with an affinity for fentanyl approximately 250 times greater than its commercial counterparts, signifying that significantly less countermeasure is necessary to neutralize a given amount of fentanyl. Perhaps more importantly, this cyclodextrin, called Subetadex (SBX), was observed to be generally applicable to a wide range of fentanyl-type compounds suggesting it would be a broad-spectrum therapeutic to fentanyl misuse. The FSC is currently working on patenting this technology and hopes to test these compounds in both?in vivo?and?in vitro?systems. This and related research was recently featured in an article in?Vice.

Evaluation of polyanionic cyclodextrins as high affinity binding scaffolds for fentanyl

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In the coming weeks, we will continue focusing on using cyclodextrins as active ingredients, disease by disease. Stay tuned!

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