HEALTH
From left to right: carfentanil, furanyl fen- tanyl, acryl fentanyl
the University of Texas at Austin, US, says counterfeit opioids are ‘adding another layer of complexity to the crisis’. ‘The counterfeit pill epidemic is so new and fast moving that even the experts we work with don’t appreciate how widespread it is,’ he says. A recent report published by the PSM, says the organisation has identified, through news coverage, 40 states where counterfeit pills containing fentanyl have been found, with deaths from fake fentanyl pills verified in at least 16 of those states. ‘People purchasing counterfeit fentanyl pills believe they’re getting legitimate medications from shady sources, not deadly doses of fentanyl,’ Shepherd says. A report published in 2016
by the DEA reports that the counterfeit pill phenomenon is now widespread and is exacerbating the crisis. ‘This is becoming a trend, not a series of isolated incidents,’ the report says. The agency warns that the problem is likely to escalate because of the profit margins – 1kg of illicit fentanyl, costing a few thousand dollars, can make an estimated 666,666 counterfeit pills, which can be sold between $10 and $20 each, resulting in revenue of potentially more than $13m. ‘Fentanyls will continue to appear in counterfeit opioid medications and will likely appear in a variety of non- opiate drugs as traffickers seek to expand the market in search of higher profits,’ the report concludes. ‘Overdoses and deaths from counterfeit drugs containing fentanyls will increase
as users continue to inaccurately dose themselves with imitation medications.’ Under US pressure, China has
now started to regulate against fentanyl and several analogues, which have been listed as controlled substances. But the DEA has noticed production has gone underground, with the chemicals tweaked to avoid prosecution. Furthermore, the DEA warns that counterfeit pills ‘threaten to circumvent efforts by law enforcement and public health officials to reduce the abuse of opioid medications’.
Drugs to fight drugs Attention is finally being given to the epidemic. US president Donald Trump recently declared a public health emergency, although no new funds will be assigned to deal with the crisis (C&I, 2017, 9, 40). The National Institute on Drug Abuse, however, has already been leading an effort to reduce opioid abuse and overdose, looking at surveillance, prescribing practices, access to addiction and overdose treatment including methadone and naloxone, and developing faster methods for screening for fentanyl. Research into non-opioid and abuse-resistant pain treatments is also moving forward. There is particular interest
around research into a vaccine against fentanyl. Developed by Kim Janda at The Scripps Research Institute, California, US, the vaccine, which has only been tested in rodents, can protect against six different fentanyl analogues, even at lethal doses.
‘What we see with the epidemic, is the need to find alternatives that can work in conjunction with what is used right now,’ he says. The vaccine works by taking
> 40 2mg
of fentanyl – equivalent to 1/50th of 0.1g of heroin – can be lethal
10,000x
More potent than heroin, carfentanil is used as a tranquiliser for large animals. Just 0.02mg can kill a human
666,666
Estimated number of counterfeit pills that can be made from 1kg of illicit fentanyl – generating a potential revenue of >$13m
advantage of the body’s immune system to block fentanyl from reaching the brain. Its magic ingredient is a molecule that mimics fentanyl’s core structure, meaning the vaccine trains the immune system to recognise the drug and produce antibodies in its presence. These antibodies bind to fentanyl when someone takes the drug, which stops it from reaching the brain and creating the ‘high’. Results in mice showed the vaccine
Number of fentanyl analogues, of varying strength, currently being manufactured, according to the US- based Partnership for Safe Medicines
neutralised fentanyl for months after the last injection and protected against overdoses. It’s early days. Trials in non- human primates are scheduled for early 2018, but the vaccine is promising. Janda is also working on a heroin vaccine with the same mode of action, and which has been found to block heroin getting to monkey brains. In both cases, further development is dependent on Big Pharma taking an interest. Yet Janda is cautiously optimistic: ‘Is a vaccine going to be a panacea to fix everything? No. But will we see it assist? Definitely.’ Indeed, trying to counter the
burgeoning opioid epidemic will require not just innovative approaches and changing attitudes to prescription opioids and pain treatment, but also buy- in from all sectors – the general public, medical community and Big Pharma, as well as regulatory and enforcement authorities in targeting the booming counterfeit trade. Reducing the chronic use
of prescription opioids will be just the first step in a long and complex journey that will also touch on the black market, which threatens to undermine efforts to reduce abuse of prescription opioids. But Shepherd is optimistic, despite the upward direction of overdose figures: ‘I do believe we can greatly reduce the spread of fentanyl and the harm from this opioid.’ It won’t be easy, notes Janda. ‘I look at this like looking at [the experience with] HIV,’ he says. ‘I think it’s going to take a number of years to deal with this crisis.
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