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Created by a brilliant, well-intentioned Belgian chemist, the potent opioid now kills 20 people a day

This country is in the grip of the worst drug crisis it has ever seen.

The Public Health Agency of Canada reports that, in the first half of last year, 3,556 people died of apparent opioid overdoses, a rate of about 20 deaths per day. In other words, on average, someone was dying somewhere in Canada nearly every hour, day and night. In the worst-hit province, British Columbia, deaths from illegal narcotics exceed those from murders, suicides, car accidents and prescription-drug overdoses combined.

The cause, in a nutshell, is fentanyl, the potent synthetic opioid that has shouldered aside cocaine and oxycontin and heroin to become the undisputed king of street drugs. In all, says PHAC, 32,632 people died of overdoses between January 2016 and June 2022, two-thirds as many as have perished from COVID-19 in the course of the pandemic. Three out of four recent deaths involved fentanyl.

You can see the drug’s power most starkly on the streets of Vancouver’s Downtown Eastside, the epicentre of the crisis, where it is smoked and injected openly on city sidewalks. But it is everywhere now, from Victoria to Halifax to Whitehorse.

Saskatchewan just reported a new record for overdoses: 421 for 2022, more than double the annual figure from just three years ago in 2019. Hamilton saw 100 deaths in the first half of last year alone, a staggering increase from the 26 recorded before fentanyl back in 2005. Opioids are even reaching places as far from gritty big-city streets as Harbour Grace, N.L., where police raised the alarm after three recent overdoses, one fatal.

To understand why, flip the calendar back to the 1950s, when a brilliant Belgian drug researcher began fiddling with the molecular structure of morphine. Born the son of a physician in the town of Turnhout, Paul Janssen was a teenager when his four-year-old sister died of tubercular meningitis. The tragedy inspired him to search for new medicines.

He studied chemistry, founded his own company and began turning out an arsenal of successful drugs for combating everything from schizophrenia to athlete’s foot. One of them was a variation on morphine many times more powerful than the famous painkiller. The fast-acting new wonder drug calmed even the extreme pain of surgery and cancer. He called it fentanyl.

It was the latest and most sophisticated member of the opioid family. The founding member of this medicinal dynasty was opium. Humans discovered thousands of years ago that the opium poppy had unusual powers. Those who consumed it found that it not only took away their aches and pains but gave them a burst of euphoria and a feeling of calm in the bargain.

Alexander the Great’s troops brought it with them on their tours of conquest. Romans mixed it in their wine and put it in poppy cakes. Arab physicians used it in creams, plasters and suppositories. Christian Crusaders carried it back from the Holy Land.

Opium’s first offspring was morphine. At the start of the 19th century, Friedrich Sertuerner of Germany managed to isolate the alkaloid that gives opium its punch. He named it after the Greek god of dreams, Morpheus. Morphine was 10 times more potent than opium. Soon, doctors were using it to treat everything from pain to asthma to menstrual cramps. The downside, as with opium, was that those who took it found they could not stop. Morphine could bring on nausea and slow patients’ breathing, too. Mr. Janssen thought he could create a more effective painkiller.

Opioids – such as morphine, named for the Greek god of dreams – have helped people ease their pain for generations. But as Paul Janssen studied the molecules that gave them their potency, he saw room for improvement.

Few people could have been better suited to the task. In his recent book The Least of Us, American journalist Sam Quinones describes the Belgian as “among the most fertile scientific minds of the 20th century.”

Mr. Janssen started playing with a six-sided piece of the morphine molecule called the piperidine ring – often known as the “enchanted ring.” He managed to produce a tweaked molecule that was better at binding with certain receptors in the brain. When the endorphins produced when we laugh or go for a run bind with those receptors, we feel a burst of pleasure. Opioids have the same effect, but on a grander scale.

Fentanyl worked quicker than morphine and patients bounced back from its effects faster, so it was ideal for surgical anesthesia. It spawned a whole new family of synthetic opioids, among them sufentanil, remifentanil and carfentanil.

Because fentanyl was 50 to 100 times stronger than morphine, even tiny amounts could be fatal. Mr. Quinones writes that at first, Mr. Janssen’s company allowed only those trained in administering anesthetics to obtain the drug, isolated in special glass vials. Some of the first to become addicted to it, in fact, were the curious anesthetists who chose to experiment with it on themselves.

Already in use for medical anesthesia by the late 1960s, the drug was so effective that it soon spread beyond the operating theatre. Doctors prescribed it in pills, slow-release pain-relief patches applied to the skin and even a fast-acting flavoured lollipop.

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Fentanyl pills are one of many ways for users to consume the drug.Alberta Law Enforcement Response Teams/The Canadian Press

It didn’t take long until it found its way into the street market. In the late 1970s investigators in California began investigating a spate of overdose deaths from a drug called China White. Although they suspected some high-potency heroin was to blame, they could find no trace of heroin – or any other known drug – in the victims’ bodies. It turned out to be a variation of fentanyl cooked up by a clever amateur.

In his 2019 book Fentanyl Inc., journalist Ben Westhoff says the appearance of China White represented “a fish-crawling-onto-land moment: it was the first popular illicit drug synthesized by a rogue chemist.”

It popped up sporadically on the streets of North America over the next few decades. Some users found a way to get high by smoking or chewing the prescription skin patches. Others extracted the gel from the patch and injected it.

But it wasn’t until the 2010s that fentanyl really began to take off. Dealers were looking for an alternative to heroin, which was sometimes hard to get because of supply-chain problems such as a sudden decline in poppy cultivation in Mexico. Users were finding it tougher to get prescription painkillers like oxycontin that stoked the first wave of the opioids crisis. Doctors were becoming wary of prescribing them and new, tamper-proof formulations made it harder to break the pills down for illicit use.

Fentanyl offered the perfect solution. Because it could be cooked up in a lab by manipulating chemicals instead of refining opium, traffickers didn’t have to worry about a poppy blight in Afghanistan, a heroin eradication program in Thailand or a drug enforcement crackdown at North American ports.

Underground chemists invented new, simplified ways of making fentanyl. One that appeared online in the 1990s, the Siegfried method, gave easy-to-follow, step-by-step instructions on how to make the drug without advanced equipment or expensive raw materials. Several other even easier recipes followed.

Traffickers could produce a drug of unparalleled power in the lab. Before long they were using pill presses to turn fentanyl into fake prescription painkillers or mixing it into heroin and cocaine to increase their strength. They could get a million pills from just a kilogram of fentanyl, the RCMP reported.

Fentanyl, once a tool for medical professionals, soon became a lucrative street drug that traffickers could use to give an extra kick to their other products – with unpredictable and dangerous results.

Today, fentanyl is no longer just a dangerous adulterant, polluting other drugs. It is the mainstream street narcotic, ubiquitous, commonplace, a market leader. People who work in safe-injection sites or drug-testing labs say they rarely see heroin anymore. It is fentanyl, fentanyl, fentanyl.

Users seek it out. They can buy a “point” (a tenth of a gram) for as little as $20 on the streets. One convicted B.C. dealer told a forensic examiner that when someone suffers an overdose, others will try to buy from the victim’s dealer because they can be sure they are getting strong stuff.

The craving for the drug is so powerful and fear of becoming “dopesick” without it is so great that many users continue to use it even though they can never be quite sure what they are buying.

Street fentanyl often contains many other things – not just inert substances used to cut it, like powdered caffeine or fibre supplements, but a variety of other drugs, like carfentanil, fentanyl’s much more powerful cousin, and xylazine, an animal tranquilizer. Sedatives mixed with fentanyl can make it harder to revive those who suffer an overdose.

Just as other drugs are mixed into fentanyl, fentanyl is often mixed into other drugs. Weekend warriors doing lines of cocaine at a party may find they have taken fentanyl. These days, fentanyl is in everything and everything is in fentanyl.

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A Vancouver drug-testing centre takes samples from a patron last spring.Jimmy Jeong/The Canadian Press

“I’m never really too sure what’s in my product,” the B.C. dealer told the forensic examiner in 2020, according to a report by University of British Columbia psychiatrist Nickie Mathew in the B.C. Medical Journal. He said some dealers mix fentanyl with carfentanil and other agents, microwave the mixture then mash it into clumps with a fork.

Sloppy mixing means that some drug doses have “hot spots” of pure fentanyl. Just two milligrams, the equivalent of a few grains of salt, can be deadly.

Overdose victims typically lapse into a deep stupor. Those around them sometimes think they are simply “sleeping it off.” Their skin becomes pale and clammy, their lips or nails blue. They may make a snoring or gurgling sound.

Margaret Thompson, medical director of the Ontario, Manitoba and Nunavut Poison Centres, says fentanyl and other opioids affect the brain’s ability to detect high levels of carbon dioxide. In normal breathing, a person breathes out to expel carbon dioxide and in to get oxygen. Fenantyl disrupts that process. Breathing slows and, if the dose is big enough, eventually stops.

Fentanyl is strong and fast-acting, but doesn’t stay in the system long, so most users need more daily hits than they did with earlier, weaker drugs to stave off the agony of withdrawal. More hits means more risk. Deaths often happen in clusters, when batches of bad drugs find their way to the street.

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Packets of contaminant-free heroin are given out by the Vancouver Area Network of Drug Users on Jan. 31, after the legalizaiton of some drugs.Jennifer Gauthier/Reuters

Authorities have been struggling for years to stop the fentanyl plague. Police manage to seize some drugs before they reach the street. Last year Canadian border authorities intercepted a suspicious shipment from China declared as “toys.” It had 1,133 kilograms of a chemical precursor used to produce fentanyl, enough to make a billion doses of the opioid.

But much of the illegal cargo evades law enforcement. American authorities estimate they stop only five to 10 per cent of the fentanyl that crosses the border with Mexico, much of it in the form of fake prescription pain pills manufactured by drug cartels.

Many health officials say that, with drugs so easy to get, the best way to save lives is by making it safer to use them: the strategy known as harm reduction. Dozens of safe injection sites have sprung up across the country since the first opened in Vancouver in 2003. Pharmacies and clinics hand out free naloxone, the drug that can quickly reverse an overdose.

British Columbia is going a step further. Starting Jan. 31, it decriminalized the possession of small amounts of illicit narcotics. It is also permitting doctors to prescribe safe opioids to users so they don’t have to turn to dangerous street drugs – the strategy known as “safe-supply.”

Provinces are spending more on treating addictions, too. Alberta’s United Conservative Party government, which rejects safe supply, has made addiction treatment free.

Some places are seeing the death rate ease a little, though it it hard to know for sure whether that is due to health strategy or other factors such as changes in the drug supply. The number of deaths fell below 100 a month in Alberta in the last few months on record. But that is still far higher than before the start of the COVID-19 pandemic, which brought on a surge in overdose deaths across the country.

Paul Janssen died in his hotel room while attending a conference in Rome in 2003. He was 77. A New York Times obituary noted his many achievements, but omitted what was to become his most consequential invention: the wonder drug he called fentanyl.

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