When prescription opioids started getting too difficult or too expensive to procure, people addicted to them started turning to heroin – a shift that’s created an “epidemic” of heroin use in whole new groups of people. Now, a new opioid is rising in use and overdose: Fentanyl, a synthetic opioid, is 50-100 times more potent than morphine, according to a recent statement on fentanyl by the Drug Enforcement Administration (DEA), and 25-50 times more potent than heroin. And its presence seems to be rising sharply, which means that, given its potency, deaths from the drug are also rising.
In 2014, 18,000 people died of opioids, at least half of which were prescription opioids, and the others from heroin. It’s not clear how many people are dying from fentanyl overdoses each day now, but the numbers are climbing sharply in pockets across the U.S. and Canada. Fentanyl is often, without the buyer’s knowledge, mixed with heroin or cocaine, because it’s cheaper than either of them, and much stronger. Here’s what we know about why fentanyl is so powerful, in the body and as a new presence in society.
What does fentanyl do in the brain?
There’s no difference in the way in which fentanyl works on the brain from any of the other opioids – it crosses the blood-brain barrier, just like they all do, and binds with the brain’s μ-opioid receptors. From here, it creates analgesia and euphoria.
“What makes it more or less euphoric than other opioids is how quickly it binds” says Lewis Nelson, Medical Toxicologist and Emergency physician at NYU’s School of Medicine. “If I give you morphine intravenously, it circulates in the blood, then it crosses blood-brain barrier, and binds the opioid receptors. But it takes a little while. Heroin crosses much more rapidly – so it’s really euphoric. And fentanyl is very, very rapid, and very euphoric.”
And fentanyl’s potency is much greater than the other opioids’ – that is, it takes much, much less of the drug to have the same effect. So it’s also lethal at much lower doses than even heroin. Micrograms of fentanyl are effective, rather than milligrams of the other opioids.
“The difference in fentanyl is that it’s very potent – it takes very little to have same effect. This has nothing to do with how it works. The reason so many are dying is because the dose is uncontrolled. It’s just how it’s used, and sold. There’s nothing more dangerous about these drugs except around the way they’re used.”
The physical effects
Aside from producing an intense high quickly, Fentanyl also produces a number of other effects – nausea, vomiting, analgesia, sedation, and respiratory depression among them, according to drugabuse.gov. And like other opioids, it causes death via respiratory arrest (one’s breathing slows to a stop), rather than cardiac arrest.
“Only thing killing you is respiratory arrest,” says Nelson. “If I took a therapeutic dose of an opioid, my breathing would slow, and I might die in six hours – it’s sort of a slow spiral toward death.” But he adds that fentanyl is just a more rapid version of the same kind of death. “If you took twice a dose of fentanyl, you might live. If you took 10 times the dose, you’d definitely die, and if you took 100 times, you’d die immediately.” This is all to say that fentanyl is potent; and its effects strong, and fast.
Where it comes from and where it’s going
Fentanyl was once largely extracted from pharmaceuticals – the fentanyl patch, for instance, used to have a reservoir of the drug that was plainly visible, so one could simply suck the liquid out with a syringe. But now the patches are “tamper proof,” in that the drug is embedded in a mesh. So fentanyl for street sale often seems to be made in China and imported to the U.S. through Mexico. And because it’s synthesized, rather than plant-derived, it’s worth the effort.
“From the dealer’s perspective, heroin is still hard to make,” says Nelson. “You have to grow it, extract it, convert it, transport into the country. Fentanyl is so much easier. And because it’s 50x more potent than heroin, the volumes are much easier to transport – you can put it in a car instead of truck, or a plane instead of a boat.” Labs in China that were previously cranking out different forms of synthetic marijuana are now making various forms of fentanyl, like acetyl and butyryl fentanyl.
And use of the drug, and of course overdoses, are rising in pockets around the country. Northern California just reported a spike in fentanyl-related deaths – and 48 overdoses and 12 deaths since late March 2016 alone. In Philadelphia, there was a 300% rise in fentanyl deaths from 2013 to 2014. Young people are trying the drug, just like with heroin, but so are middle-aged people, either wittingly or unwittingly. The problem is that not everyone is going out to buy it intentionally – many are in the market for something else, but getting the drug cut with fentanyl. Or worse, only fentanyl.
“In Sacramento, it’s not fentanyl being sold as heroin even, but it’s being pressed into pill and sold as Norco [a combination of hydrocodone and acetaminophen],” says Nelson. “If suddenly counterfeit pills are out there, then that’s a real problem.” Again, in some of these cases, there’s only fentanyl present, and none of the drug that’s being marketed.
Long-term use of fentanyl is probably somewhat rarer than heroin or other opioids, just by virtue of the fact that it’s so potent that the margin of error is quite small. “A milligram of a drug is a the size of a pinhead. A microgram is thousand times less than that,” says Nelson. “Fentanyl is always mixed into something else. Within that mixture could be hotspots of fentanyl. So you’re putting a lot of trust in your dealer. If you make a batch with just a little more, then you see overdose increases in spots in city.” So there are a lot of ways in which the use of fentanyl can go wrong.
Fentanyl will likely grow much more widespread before it peters out. And the fix probably lies not on the street or drug labs, but in exam rooms in doctor’s offices. Changing our prescribing practices would prevent many more addictions than any other avenue, says Nelson. “We are turning out opioid addicts pretty quickly in this country. De novo use is always going to be around – kids are curious and they try something – and the DEA can’t really do anything about that. It’s a Sisyphean task. But stopping the other addicts that form – those who get addicted through prescribing practices – happens by improving the way we practice medicine.”
It would take a lot of people working together to shift how we use opioids in this country. It’s possible, but it won’t happen overnight. “Constituencies on both sides are lining up. But it’s hard, because there’s so many players,” says Nelson. “Pharma is involved, the government is involved. The problem is incredibly complicated.”
By Alice G. Walton - Forbes/April 9, 2016
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