This new street drug is 10,000 times more potent than morphine, and now it’s showing

[neversickanymore]

This new street drug is 10,000 times more potent than morphine, and now it’s showing up in Canada and the U.S.
By Katie Mettler April 27

It was first developed in a Canadian lab more than three decades ago, promising and potent — and intended to relieve pain in a less addictive way.

Labeled W-18, the synthetic opioid was the most powerful in a series of about 30 compounds concocted at the University of Alberta and patented in the U.S. and Canada in 1984.

But no pharmaceutical company would pick it up, so on a shelf the recipe sat, the research chronicled in medical journals but never put to use. The compound was largely forgotten.

Then a Chinese chemist found it, and in labs halfway around the world started developing the drug for consumers in search of a cheap and legal high — one experts say is 100 times more potent than fentanyl and 10,000 stronger than morphine.

And now it has come to North America. The substance first surfaced in Canada last fall, when Calgary police seized pills containing traces of the drug, according to the Calgary Herald. Then more than 2.5 pounds of W-18 was discovered in the home of a Florida man, who was sentenced to 10 years in federal prison after he pleaded guilty to smuggling fentanyl from China, reported the Sun Sentinel. He faced no charges for possessing the W-18, however, because it’s not yet illegal in the U.S.

And just last week, Health Canada’s Drug Analysis Service confirmed that four kilograms of a chemical powder seized in a fentanyl investigation in December 2015 was indeed the dangerous W-18 drug.

Health officials are concerned for many reasons. There are currently no tests to detect the drug in a person’s blood or urine, according to reports, making it difficult for doctors to help someone who might be overdosing, a risk outlined in the drug’s 1984 patent.

Its effect on humans is largely unknown because W-18 was only ever tested on lab mice.

“Whenever this drug starts circulating on the streets you’re going to have deaths,” Sacramento-based forensic chemist Brian Escamilla told the Calgary Sun.

Health Canada is working to have W-18 added to its Controlled Drugs and Substances Act.

continued with many links https://www.washingtonpost.com/news...and-now-its-showing-up-in-canada-and-the-u-s/

 

[neversickanymore]

Canadian police fight a Frankenstein in new W-18 street drug
Delay identifying new W-18 drug shows need for better battle plan on synthetics
By Marion Warrnica, CBC News Posted: Apr 24, 2016

The only thing worse than having a killer in your midst is not knowing it is there.

That's why some experts say Canada's bad trip with W-18 this week reveals an urgent need for authorities to catch up to the trend that brought it here: synthetic drugs.

It took Alberta's elite policing squad, ALERT, one month to send the strange white powder discovered at a clandestine lab for testing.

It took three months for Health Canada to figure out what it was: W-18, a deadly experimental opioid not intended for human use, resurrected for the recreational drug circuit.

A Frankenstein.

And as rogue chemists get better at producing and shipping W-18 through our borders, some say Canada cannot eliminate the monster drug — without also tackling its family.

'We thought it was meth'

A Health Canada spokesperson said Alberta police called their office to help dismantle the lab on Dec. 10 last year, then on Jan. 12, RCMP requested that Health Canada test the unknown white powder.

Three months later, on April 8, Health Canada officials said they confirmed it was W-18 and notified the RCMP "immediately."

On April 19, a memo to emergency room doctors warning them about the discovery of W-18 in Edmonton was leaked to media. On April 20, ALERT held a press conference to tell the public about the threat.

ALERT spokesperson Mike Tucker admitted that the December lab takedown involved "unusual circumstances." While an ongoing investigation prevents him from saying much more, he did explain RCMP used a special team wearing haz-mat suits to clear out the lab.

Tucker isn't saying exactly why the team waited a month to send the then-unknown W-18 sample for testing. But he said the delay was nothing out of the ordinary.

"In hindsight it's always crystal clear, right? But at the time, this was simply seized as an unknown substance. It was actually suspected as being some form of methamphetamine," Tucker said.

"What's being added to cocaine as a buffing agent, a lot of time, are unknown white powders. So for us it's pretty difficult to make that determination to say this is a high priority drug file, versus let's just say something else that's being submitted to the lab in a homicide case."

In an email, the Health Canada representative said the W-18 sample was "one of 60 products" discovered in the lab, which needed to be analyzed separately.

Tucker said an investigator was waiting for official confirmation during the nearly two-week delay between the identification of the drug by Health Canada and telling the public about the new W-18 discovery in Alberta.

"This [April 8 confirmation] was a phone call that was received by our investigator indicating it was W-18," Tucker said. "Our investigator interpreted that that was a preliminary opinion. So on the 19th we received official confirmation in writing that it was W-18. We made the decision to hold the news conference the next day."

Too little, too late?

Alan Hudson, an associate professor with the department of pharmacology at the University of Alberta, called W-18 one of the most dangerous drugs in a whole spectrum of synthetics, or analogs. They often mimic the chemical structure of traditional street drugs — save for a compound or two — and that slips them through the rules.

Others include Spice or K2, a synthetic marijuana product, and fentanyl analogs.

"It really is a big challenge for the police to keep on top of this," Hudson said. "There are various people who look for new potential recreational drugs. They go through old patents and look for old opioids, and see how easy they are to synthesize."

W-18 was invented at the University of Alberta as part of a spectrum of experimental painkillers in the 1980s, then patented by three men — one of whom still lives in Edmonton and no longer picks up the phone when media call.

It was never adopted as a clinical drug, never tested on humans, and is not on the list of controlled substances in Canada — which means technically it can be sent freely through mail. And it can be found for sale on websites, typically based in China.

"Obviously somebody in China has picked up on the fact that W-18 is quite easy to make in large quantities and they're trying to sell it to the North American market," said Hudson.

But because of its potency, Hudson believes W-18 has taken the synthetic drug trend to a whole new danger level. And he said that's why law enforcement — and lawmakers — need to look more toward the source.

"The importation of W-18 from China needs to be stopped as soon as possible. If any package were to be damaged, anyone coming into contact would face being overdosed with this drug immediately and would need immediate medical attention," Hudson said.

"You only need a tiny speck of W-18, which can cause respiratory depression and can kill you," he added. "It's just too potent to even consider using."

The killer we haven't discovered yet

Some regular drug users echo his words.

In a thread on an online discussion board called "Drugs-forum," a user called "name goes here" described serious concerns.

"The risk of a bad batch is so incredibly high, why take the chance?" the person wrote, pointing out the drug's strength (said to be 100 times more potent than known killer fentanyl) and calling it "an overdose waiting to happen."

But even if drug users don't seek out W-18 specifically, they could ingest it without knowing, now that it's on the market.

Like powerful fentanyl synthetics, W-18 may be used to mimic or extend batches of more common drugs, like heroin or OxyContin.

Delayed or not, the warning is clear.

http://www.cbc.ca/news/canada/edmonton/street-drug-w18-delay-1.3550642
................................................

'We thought it was meth'

'In hindsight it's always crystal clear'

Maybe legalize medical grade heroin, before everyone is hooked on or dies from this shit .

 

[DrJay]

Potency ratios suggest that 100 mcg of W-18 is equipotent to 10,000 mcg of fentanyl, which seems insanely high, even for tolerant people. As i am very involved with naloxone distribution efforts , please help me understand how one measures the dose of non-pharmaceutical i.e.- street - fentanyl. Given the wide variability of tolerance in habituated humans, what’s the usual dose (if there is such a thing) of fentanyl in tolerant IVDU’s?

AS for harm-reduction , any ideas on testing doses before using to detect ultra-high affinity synthetics? Would this discussion better be re-posted on a different thread?

Most importantly, the potential street presence of ultra-high-affinity synthetics such as carfentanyl and w-18 certainly challenge the idea that higher plasma concentrations of the Adapt Narcan product are undesirable as they might precipitate inordinately nasty withdrawal.

Synthetic opioids, fentanyl analogues ( such as carfentanyl) , W-18 , are here . what is the advice for the consumer in this regard?

Get naloxone !!

 

[Carl Landrover]

Is it carfentanyl? It was first synthesized in 1974 and according to wiki it's 10,000 times stronger than morphine and 100x stronger than fentanyl.

 

[neversickanymore]

Basically a powerful poison? Have to be some laws about that being broken.. maybe even very big laws that carry over borders?

Yeehaa china.. talk about the west being greedy?

 

[neversickanymore]

'No one deserves to be executed': Peter Gardner's parents

China? REALLY just moving a silly worthless amount of one of your nations many illegal and quasi legal national products.. shit probably hit the next flight out?

 

[LucidSDreamr]

only companies

'No one deserves to be executed': Peter Gardner's parents

China? REALLY just moving a silly worthless amount of one of your nations many illegal and quasi legal national products.. shit probably hit the next flight out?

agreed. Its totally cool for companies in china to supply the entire world with tons of amphetamines more powerful and dangerous than meth (insert random RC amphetamine name here). Fentanyl analogues, W18, etc. As long as industry is making tons of money off of supplying the whole planet with drugs that all good.

chemical laboratories pay taxes, drug trafficers dont....you think if the drug trafficers payed taxes it would be ok?

But if a person gets caught trafficking drugs in china they get executed.....while to totally legit operational laboratory operating in plane sight that manufactures the shit gets to go on pumping away.

 

[jammin83]

prob 10000x potency is a bit much. maybe in animal models but that doesn't always translate to humans.

still, whats an active dose? 10 mics? and a lethal dose is 20 mics? slightly problematic i would say.

shit like this and bromadol, etc = death to RCs and psychoactive substance bills and so on.

 

[forensictoxguy]

This is a blogpost of mine... can be found here: http://dosemakespoison.blogspot.com/2016/04/what-do-we-know-about-w-18.html

What do we know about W-18?

“W18 drug is 10,000 times stronger than morphine: Calgary police warning”

“Police warn against deadly new street drug W-18”

“Alberta health official warns of deadly new street drug”

“W-18, a drug 100 times more potent than fentanyl, is now in B.C.”

“Albertans left in the dark about police seizure of deadly new street drug”

“ER doctors warned about massive seizure of suspected W-18, 100 times more powerful than fentanyl”

“A toxic drug, more powerful than fentanyl, hits the streets in Alberta”

Those are some recent headlines regarding a newly emerged drug named W-18 in North America. The substance is supposedly 10,000 times more potent than morphine or 100 times more potent than fentanyl as a central nervous system depressant.

W-18 is a compound in a series of 32 substances (named W-1 to W-32) that were first synthesized in academic research by Edward Knaus, Brent Warran, and Theodore Ondrus at the University of Alberta in 1981. These W-series compounds are covered under US patent 4468403A (August 28, 1984). The chemical name for W-18 is 4-chloro-N-[1-[2-(4-nitrophenyl)ethyl]-2-piperidinylidene]-benzenesulfonamide and it has a chemical formula C₁₉H₂₀ClN₃O₄S. Molecular weight is 421.9 g/mol.

W-18 was detected in counterfeit tablets sold as fentanyl in Calgary, Alberta, Canada in August 2015. W-18 was also identified as the constituent in four kilograms of powder in a drug seizure in Edmonton, Alberta, Canada in December 2015; purity of the powder substance was reported to be 90% by Canadian authorities. In 2016, a Florida man was found to be in possession of 2.5 pounds of a powder containing W-18.

Despite media reports and quotes from law enforcement officials, the pharmacological profile for W-18 is not established at this time. We have no data on absorption, distribution, metabolism, or excretion of the substance. We do not know on what specific receptors W-18 acts. We know nothing about receptor binding affinities. We know nothing of the acute effects of the substance. The only piece of pharmacological data that exists for W-18 was acquired via the mouse phenylquinone (PQ) writhing assay. In that test, W-18 had an IC₅₀ equal to 3.7 ng/kg and 50% inhibition. In the same test, morphine’s IC₅₀ was equal to 38,000 ng/kg and 50% inhibition. It very important to note that the PQ writhing assay is a general or non-specific test in which many compounds not considered to be analgesics, including sympathomimetics and central nervous system stimulants, protect mice against the PQ-induced writhing. The assay results should not be interpreted in any way that insinuates W-18 is approximately 10,000 times more potent than morphine as a central nervous system depressant. We currently have no pharmacological data to support that W-18 has any activity at the opioid receptors: mu (µ), kappa (κ), or delta (δ).

W-18 is not considered a controlled substance in the United States, though it may be considered a controlled substance analog under the Analog Enforcement Act. It was made illegal in Sweden in January 2016. In Canada, the government has proposed making W-18 a Schedule I controlled substance, but it currently remains uncontrolled. In clinical and postmortem toxicology, there have been no analytically confirmed W-18 associated presentations to the hospital or fatalities reported.

As with any other newly emerging psychoactive substance, many claims are made about the compound itself. Many of the headlines are meant to grab attention and readership with hysteria about the new “super potent” or “scary” drug of the day. We should guard ourselves against that sort of hyperbole. But, even though we have no data to support the supposed extreme potency of W-18, let’s not fall into the trap that it isn’t potentially dangerous. We do not have data that shows its lack of potency. This extreme lack of knowledge about the compound makes the drug potentially dangerous.

References can be found here: http://dosemakespoison.blogspot.com/2016/04/what-do-we-know-about-w-18.html

 

[neversickanymore]

^Great post.. thank you

 

[downerhead]

The figures of 10,000x the potency of morphine and 100x the potency of Fentanyl (and which version of fent are they referring to, the HCL or the more commonly administered Citrate version, which is substantially weaker than HCL version IME) are greatly exaggerated for W-18 IME (at least the batch I got ahold of). I know that different RC vendors' products can vary, sometimes widely, in the same chemical, or even batch to batch within the same manufacturer. The same is true of the big pharmaceutical companies, albeit to a much lesser extent. Before getting booted from pain management recently, I was prescribed roxy (90mg/day. Not strong enough for my pain and tolerance levels but, living where I now do, I'll take 90mg of roxy every day and be happy and thankful to get it, very happy and very grateful actually. I'd sell my soul to get that script back again, it's far better than nothing and does give some decent pain relief at those doses). Depending on the pharmacy (I used 2, which pharmacy depended on circumstances), I would get KVK Tech or Mallincrodt. I generally prefer the Mallincrodt, it seems a bit more effective for me, but I got one batch that was defective and the difference was noticeable enough that psychosomatic causes were able to be ruled out. And we all know what happened to Watson's opioid products after the Watson/Actavis merger.

I found W-18 to be kind of disappointing thb. And this was in doses far bigger than ug levels. Since I haven't seen it mentioned here, I will add that W-18 has been shown, according to medical reports(mostly gleaned from users iirc) and long-term user experiences I've read, to cause deafness and hair loss with long term use. It would seem this stuff is pretty toxic in the long-run, in ways that weren't noticed for a great while because of the lack of human experience with the stuff until fairly recently. Now that it seems to be hitting the streets more, as the good fent analogs disappear from the reputable Chinese vendors (is there even such a thing as legit Chinese vendors these days?) at an alarming rate, we'll probably hear of more and more weird side effects of W-18. I think it's weird (and fucked up) that vendors seem to be able to freely and openly sell all kinds of hallucinogens and speed (including analogs of acid, meth, and caine), but woe unto those who dare produce quality opioid analogs to help people in pain that either can't afford or get effective treatment for pain from a doctor or pain clinic. I've been running into the exact problem. No doctor, NP, or pain clinic will treat me, but you can get analogs of PCP, MDA/MDMA, hosts of speeds, etc... very easily for cheap. The only useful thing I see online is benzo analogs and thienodiazapines. For some reason, those are everywhere, but I'm RXd plenty of xanny bars per month so, I don't really have a use for some benzo analog/thieno which is less effective than what I get. Instead of having to look online and roll the dice, the U.S. should do like Portugal and decriminalize everything, or at least do like a thing I saw on the U.K., where you can become a registered heroin addict (probably on the government's dime) and get your dope and fresh rigs from the pharmacy once you're issued your card. That would be a good option for chronic pain patients IMO.

 

[Sturnam]

W-18 does not act on opioid receptors

I can't believe this stuff is still making the rounds. The whole "10,000x morphine potency" claim, that is. W-18 does not affect opioid receptors!

W-18 (1-(4-Nitrophenylethyl)piperidylidene-2-(4-chlorophenyl)sulfonamide) and W-15 (4-chloro-N-[1-(2-phenylethyl)-2-piperidinylidene]-benzenesulfonamide) represent two emerging drugs of abuse chemically related to the potent opioid agonist fentanyl (N-(1-(2-phenylethyl)-4-piperidinyl)-N-phenylpropanamide). Here we describe the comprehensive pharmacological profiles of W-18 and W-15. Although W-18 and W-15 have been described as having potent anti-nociceptive activity and are presumed to interact with opioid receptors, we found them to be without detectible opioid activity at μ, δ, κ and nociception opioid receptors in a variety of assays. We also tested W-18 and W-15 for activity as allosteric modulators at opioid receptors and found them devoid of significant positive or negative allosteric modulatory activity. Comprehensive profiling at essentially all the druggable G-protein coupled receptors in the human genome using the PRESTO-Tango platform revealed no significant activity. In silico predictions using the Similarity Ensemble Approach suggested activity for W-18 only weakly at H3-histamine receptors, which was not confirmed in radioligand binding studies. Weak activity at the sigma receptors and the peripheral benzodiazepine receptor were found for W-18 (Ki=271 nM); W-15 displayed weak antagonist activity at 5-HT2-family serotonin receptors. W-18 is extensively metabolized, but its metabolites also lack opioid activity. W-18 and W-15 did inhibit hERG binding suggesting possible cardiovascular side-effects with high doses. Thus although W-18 and W-15 have been suggested to be potent opioid agonists, our results reveal no significant activity at these or other known targets for psychoactive drugs.

 

[Jabberwocky]

That is fascinating Sturnam. Do we have any idea how something like W-18 works? I mean, that is asking a lot of any substance without a lot of human use, so I don't have my hopes up.

 

[downerhead]

Yeah, I would say to not get your hopes up about W-18, Toothpaste. The stuff is toxic, and it sucks effects wise. I really don't even see the point in synthesizing/manufacturing W-18. Better to keep your hair, equilibrium, and hearing than a toxic substance that isn't effective. Why it's hitting the streets and people continually buy it is a mystery to me.

 

[Limpet_Chicken]

Wonder if its an epsilon ligand. Theres another putative opioid receptor, although I'm unaware of any selective agonists, the main compounds acting as agonists being etorphine, dihydroetorphine (AFAIK) and beta-endorphin, as well as severaw of the benzomorphan opioids (the -azocines of which pentazocine is probably the only one used, occasionally in medical practice( and buprenorphine is an antagonist