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Health Canada retracts claim that W-18 is an opioid stronger than fentanyl

September 8, 2016
A bag of allegedly deadly W-18 pills.—U.S. Drug Enforcement Agency

A bag of allegedly deadly W-18 pills.—U.S. Drug Enforcement Agency

Call it what you will—erring on the side of caution, assuming the worst, overreacting, going completely overboard or deliberately fear-mongering.

Canada’s trusted federal health regulator, as well U.S. and European drug control agencies and various police departments, notably in Western Canada, have all been making exaggerated and misleading statements about the classification and potency of the drug W-18, based on little or no evidence.

It turns out that W-18, which Health Canada has been calling an “extremely dangerous synthetic opioid that can be 100 times stronger than fentanyl”, not only is not an opioid but there is no conclusive clinical evidence that it’s 100 times stronger than Aspirin, let alone fentanyl.

A new study of W-18, by the North Carolina School of Medicine, indicates that if the drug has any narcotic or analgesic properties at all, they do not come from attaching to opioid receptors in the brain—which is what defines all opioid drugs, such as morphine, heroin and fentanyl. Also, the anti-opioid-overdose drug naloxone, likely has no effect whatsoever on W-18.

The study, which has been released online prior to being peer reviewed, is entitled Pharmacology of W-18 and W-15, and was led by researchers from the Department of Pharmacology at the University of North Carolina School of Medicine in Chapel Hill, North Carolina.

In a series of clinical tests, researchers were unable to pinpoint a clear mechanism for how W-18 and W-15 interacted with cells but conclusively ruled out opioid receptor activity. The two drugs did exhibit toxicity in human embryonic kidney cells after 24 hours.

The little mouse study that roared

writhing-mouse

W-18 claims were based on mouse pain writhing tests—information from torture.

On June 19, in the face of criticism and mounting evidence (or lack thereof), Health Canada finally retracted its claim that W-18 is an opioid 100 times more dangerous than fentanyl.

Canada’s drug safety watchdog still considers W-18 to be dangerous; it just doesn’t know what kind of drug it is or how dangerous it might be.

Health Canada’s Notice of Consultation, dated June 9, proposing the addition of W-18 to Schedule I of the Controlled Drugs and Substances Act, still refers to the drug as a synthetic opioid but a June 19 information update from Health Canada only refers to it as a “harmful substance”.

The update, entitled “Health Canada clarifies position on W-18“, admits that in making its original claims, the federal agency was simply relying on the word of others that W-18 was an opioid—others such as the European Monitoring Centre for Drugs and Drug Abuse, which has also wrongly classified W-18 as an opioid.

Health Canada has also relied on others to begin doing the necessary clinical research in order to answer 34-year-ld questions about the drug’s pharmacology.

Up until the North Carolina study this year, the only real scientific information on the classification and potency of W-18 has been the drug’s original 1982 patent claims, which are based on observations of pain tests conducted on mice (male Swiss albino mice, to be precise).

Canada’s would-be super-safe pain-killer

W-18 was the most potent of a series of 32 compounds (W-1 to W-32) developed by researchers at the University of Alberta in 1981. The goal of the academic project was to create a powerful non-addictive analgesic (pain-killing) medication on a par with morphine.

No one can really say whether the effort was successful or not.

That’s because after it was patented no pharmaceutical company chose to license W-18, or any of the rest of its series. Therefore none of the clinical trials that would’ve really shown the drug’s capabilities, one way of the other, were ever carried out.

The patent finally expired and the research ended up in the public domain, with the result that—although W-18 is largely an unknown quantity with no clinical uses—several companies, mostly in China, manufacture and sell it.

The 1982 patent for W-18, titled Analgesic substituted piperidylidene-2-sulfon(cyan)amide derivatives(US 4468403 A), never actually claims that the drug is an opioid, it only compares the analgesic (pain-killing) effects to the opioid morphine.

The patent says that the opioid blocker naloxone was only tested on the W-3 compound (not W-18) and that the result was a partial reversal of its observed painkilling effects.

As for W-18’s potency, the patent claims that it was comparatively effective in reducing the writhing (from induced pain) of mice at 1/10,000 of the dose of morphine (0.0000037 mg of W-18, to 0.038 mg of morphine).

The patent’s comparison to the effects of morphine, the slight effect of naloxone on one of the other W compounds and the dosage ratio between W-18 and morphine was all the evidence that Health Canada (along with other groups and agencies around the world) needed to declare that W-18 was an opioid 100 times more potent than fentanyl.

The making of a fearful new drug terror

Drug aficionados were already discussing W-18 on Drugs-Forum website in 2010, referring to it as an opioid with potential for synthesis as a legal recreational drug.

Significantly, perhaps—given the alarming estimates of W-18’s potency—one 2014 post to the original 2010 thread wrote of taking W-18 in rather high oral doses of 600-plus micrograms and finding that it didn’t deliver the “euphoria (fun) of more classic opiates”.

The poster elaborated in a follow-up reply that it “just wasn’t a good opiate-esque high, or any high for that matter”.

In 2013, according (only) to Health Canada: “The use of W-18 as a ‘legal’ substitute for other controlled substances was first detected in Europe”.

In August of 2015, police in Calgary, Alberta, announced finding 110 pills of W-18 in a house on the city’s rural outskirts. Police declared that W-18 was an opioid “about 100 times more powerful than fentanyl”.

On April 24, 2016, Alberta police and RCMP announced finding W-18 in powder form during the take-down of a clandestine drug lab, apparently in Edmonton, Alberta.

The CBC News piece on the drug lab raid (conducted, we are told, in haz-mat suits) quotes an associate professor with the department of pharmacology at the University of Alberta as calling W-18 one of the most dangerous drugs in a whole spectrum of synthetics, or analogs.

On May 23, 2016, the Globe & Mail reported “Western Canada’s first fatal overdose of W-18“, after a man who died of a fatal overdose in south Calgary in March was found to have heroin, the fentanyl analog 3-Methylfentanyl and W-18 in his system.

It was the media, in this case and not authorities, that pinned the blame in W-18. As Calgary police Staff Sgt. Martin Schiavetta told Canadian Press:

“As far as which one [of the three drugs] resulted in the person’s death, we cannot say.”

Also in May, an anesthesiologist, pharmacist, and pain specialist at Drexel University College of Medicine, named Anita Gupta, was quoted as suggested that W-18 was behind a spike in overdoses in Philadelphia, Pennsylvania, in the United States:

“The symptoms were worse than we were used to seeing. We were getting patients with symptoms of near-death, and often required multiple doses of the antidote naloxone.”

This reminded the healthcare professional of a recent Drug Enforcement Administration bulletin warning that W-18 increased the strength of heroin and cocaine.

“It put a name to what was already going on. My suspicion is, W-18 is something we’re already dealing with.”

People naturally put a lot of trust in what agencies such as the DEA and Health Canada say. It’s assumed that such federal regulators base their findings on research and testing, not guesswork.

Noloxone, being an opioid antagonist drug, should only be expected to block the effects of opioid drugs and there has never been clinical evidence that W-18 is an opioid drug, as both agencies should’ve known.

Never say never but it’s much more within the realm of the possible that the tougher overdoses that Anita Gupta was referring to were caused by one of the well-documented synthetic opioid analogs of fentanyl, such as the ridiculously powerful carfentanil.

A recent spate of overdoses last month in Ohio, shown to be caused by carfentanil, likewise only responded to multiple shots of naloxone.

This is not to say that W-18 isn’t potentially toxic on its own or that it may not somehow increase the toxicity of other drugs.

For example, antihistamines, which act on histamine receptors in the body, are known to be able to boost, or potentiate, the sedation and respiratory depression caused by opioids, sometimes quite dangerously.

For what little it’s worth, W-18 showed weak activity at H3-histamine receptors in the South Carolina tests.

Here in Vancouver, B.C. the supervised safe injection site Insite has never encountered an overdose that it wasn’t able to handle and I do not believe that it has seen an overdose involving W-18.

Ignorance certainly boosts the dangerous effects of drugs

Health Canada may like to argue that it was erring on the side of caution when it decided to hype the heck out of W-18 but it’s more accurate, I think, to say that the public agency jumped to a false conclusion, which generally does more harm than good.

For instance, the researchers behind the South Carolina study pointedly suggest that erroneously assuming and telling people that W-18 is an opioid could actually endangers lives.

Abusers of the compound may feel a false sense of safety, trusting that any negative effects of W-18 can be revered by naloxone. But, given the lack of opioid receptor activity, that is also likely to be an erroneous assumption. Click the images to enlarge them.

From → Canada

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