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This Is U-47700, Once a Lab Experiment, Now a Killer Opioid

From the Wall Street Journal:

In a high-stakes game of cat-and-mouse, overseas labs are churning out new synthetic drugs at a furious pace, often staying a step ahead of authorities and helping to fuel America’s rampant opioid crisis.

The United Nations Commission on Narcotic Drugs estimates that “new psychoactive substances”—a broad list that includes synthetic opioids—are emerging globally at an average rate of one a week. As with U-47700, rogue chemists sometimes piggyback on research by legitimate scientists that was abandoned before making it to the legal market.

Synthetic opioids are often more deadly than other kinds of common designer drugs, such as artificial cannabinoids or stimulants known as bath salts. Some opioids have flared up before—fentanyl variants caused problems on the West Coast in the late 1970s and 1980s—and they are roaring back at a perilous time.

The designer opioids mainly come from Chinese labs, the DEA says, and many labs sell them openly in online drug bazaars. On online forums, people compare notes on their experiences using the synthetics.

The U.S. surveillance system for these chemicals is a largely informal network of crime labs, medical examiners and law-enforcement authorities who share clues and alert each other when they find something new. It can be a laborious task, slowed in part by the challenge of finding something they didn’t know they were looking for.

At least six states specifically banned U-47700 before the DEA announced plans in September to make the drug illegal. DEA spokesman Rusty Payne said the agency’s scheduling actions are subject to “exhaustive reviews,” which take time.

So far this year through September, NMS Labs, a major private lab outside Philadelphia that works with states around the U.S., has tallied 105 overdose deaths related to U-47700 and 265 fatalities related to furanyl fentanyl—an analog, or chemical compound that is closely related to fentanyl. Axis Forensic Toxicology, a private lab firm in Indianapolis, has seen another 20 deaths linked to U-47700.

The U-47700-related fatalities span at least 31 states from Alaska to Utah to Florida.

The origins of U-47700 date to 1973, when Upjohn Co. asked its scientist Jacob Szmuszkovicz to create a drug with the pain-relieving power of morphine, but without the risk, according to a chapter he wrote for a 1999 book on drug research. Researchers wanted to find the Holy Grail that is elusive to this day: potent pain relievers that don’t have dangerous side effects, such as addiction and a potentially fatal slowdown in breathing.

By about 1974, Dr. Szmuszkovicz created a chemical Upjohn dubbed U-47700 at a company lab in Kalamazoo, Mich. Researchers knew it was a morphine-like drug when it triggered erect tails in mice, a reaction known as a Straub tail, says Phil von Voigtlander, a retired Upjohn research director who worked on the project.

Another test, which involved shining a hot light on mice’s tails to judge how long it took them to move, helped measure U-47700’s potency, says Dr. von Voigtlander. He learned the compound worked on the same receptor as morphine with roughly 7.5 times the strength.

Further rodent testing also revealed a downside. “Once we saw that it just caused tolerance and dependence like opioids and had opioid side effects, we thought, well, that’s just another morphine and that’s not what we’re looking for,” Dr. von Voigtlander says.

He calls U-47700 an important research steppingstone, and Upjohn patented the chemical. The company never tested U-47700 on people.

These kinds of pharmaceutical research efforts leave behind copious patents and scientific papers, which can serve as recipes for today’s enterprising chemists. Some researchers believe Chinese labs are scouring patent literature for new synthetic compounds to produce, before selling them.

Foreign labs began making U-47700 and offering it for sale online by late 2014, according to a forum on the social-media website Reddit devoted to discussion of chemical vendors and frequented by drug users. Buyers can choose from an array of online vendors selling synthetic drugs, including opioids, dubbed “research chemicals.”

The websites typically carry warnings that the chemicals they sell are “not for human consumption”—an attempt to gain legal cover, authorities say—and that buyers are responsible for complying with their home countries’ laws.

U-47700 began claiming lives in the U.S. by May 2015, when a 28-year-old man overdosed in Knox County, Tenn. The medical examiner there initially pegged his death to oxycodone, which was in his system. It took many more months to discover U-47700 was also there.

First, labs had to figure out what the drug was. NMS Labs detected U-47700 in November 2015 while testing blood samples from four different states at its facility outside Philadelphia.

“We actually found it by accident,” says Barry Logan, chief scientist there. U-47700 closely resembles a synthetic opioid called AH-7921—another research relic—which NMS had started watching for last year.

NMS, which is now rushing to create new tests to screen for 21 different designer opioids, eventually linked U-47700 to the Knox County case.

Another Powerful Painkiller Found in Prince's System: U-47700

From Eyewitness News 5 (Minneapolis/St. Paul):

Although it was a fentanyl overdose that killed Prince April 21, the medical examiner said it was part of a deadly chemical cocktail.

A source close to the investigation says U47700 was part of the mixture.  The potent painkiller is a synthetic opioid, eight times stronger than morphine.

Investigative sources told reporter Beth McDonough that Prince may have thought he was taking a legitimate painkiller, like hydrocodone or fentanyl, that unknowingly also had U-47700 in it.

The pills often look just like other medications.  Plus, U47700 can be resistent to the life-saving antidote Narcan. 

Because U-47700 is not considered a controlled substance by state or federal agents, it's not regulated.  The Drug Enforcement Administrations says it tends to be produced overseas in China or Eastern Europe.  It's widely available, easily accessible and affordable, about $40 online. 

New Synthetic Drug U-47700 Has States Rushing to Stop Spread

From The Associated Press:

A new synthetic drug that can be purchased online and is connected to at least 50 deaths nationwide has several states scrambling to stop its spread, with Kansas law enforcement agencies seeking an emergency ban.

At least three other states — Ohio, Wyoming and Georgia — already have taken action to ban U-47700 after it was connected to overdoses. A spokeswoman for the U.S. Drug Enforcement Administration said that the agency is studying the opioid but hasn't yet moved to control it.

Nearly eight times more potent than morphine, U-47700 comes in various forms and can be injected, snorted or taken orally.

The U in the name stands for Upjohn, a pharmaceutical manufacturer that developed the drug in the mid-1970s as scientists were looking for a synthetic alternative to morphine, said Barry Logan, chief of forensic toxicology at NMS Labs in Willow Grove, Pennsylvania, which provides lab services for government and private clients.

"They were searching for a novel painkilling drug, the holy grail of analgesics that didn't have the addictive or respiratory depression properties of opiates or heroin," said Logan, who recently spoke about synthetic opioids at an international conference in Budapest.

The Upjohn researchers devised and patented several different compounds in search of their super drug, Logan said. Some of the compounds were written about in scientific literature, including methods for making them.

Chemists in China and Eastern Europe can find recipes for many of the drugs — including U-47700 — by combing through online patent records and old scientific journals, he said.

NMS has identified about 50 deaths across the U.S. that can be connected to U-47700, which came onto the company's radar screen in December, Logan said.

A deadlier drug: Doctors suspect W-18 is spiking overdoses

From The Philadelphia Inquirer:

Legal synthetics have caused "upwards of 50 deaths" nationwide during the last four months, according to Barry Logan, director of the Center of Forensic Science and Education. The center is the nonprofit research arm of NMS Labs, which tests for the substances at its Willow Grove headquarters.

NMS confirmed one death in Illinois caused by W-18 and is investigating its role in another.

"The bigger problem right now is the designer opioid U-47700 and the designer fentanyl, furanyl, fentanyl," Logan said, adding that NMS had detected the two substances in a string of fatal overdoses that reached from Florida to Maine.


New synthetic drug shows up on streets of Northeast Ohio

From newsnet5 (Cleveland):

There is new drug is on the streets of Northeast Ohio and it can be deadly.

In fact, an overdose death in Lake County is believed to be the first in the state, said Doug Rohde, supervisor of Chemistry and Toxicology at the Lake County Crime Laboratory.

After an alert from Lorain County about a new drug and some more research Rohde discovered it was U-47700. It is a new opioid that is eight times more potent than morphine. It is also deadly. U-47700 is to blame for the deaths of 20 people in 9 states.

The synthetic opioid is so new that it has not yet been labeled illegal. But, Rohde said just because it is still legal does not mean that it is safe.

Synthetic opiate makers stay step ahead of US drug laws as overdose cases rise

From The Guardian:

W-18 is one of thousands of synthetic opiates that is not scheduled as a controlled substance and thus not subject to criminal drug penalties, and one of a handful of drugs that law enforcement officials and scientists say they have seen in increasing numbers in the last six months, as use, abuse and overdose deaths continues to rise.

Another, U-47700, which is seven to eight times stronger than morphine, has been the source of overdoses over the past year in at least 10 states since the first US incident was discovered in Knoxville, Tennessee, in June 2015.

Barry Logan, the executive director for the Center of Forensic Science and Education, said his lab has been able to track down 17 overdose cases of U-47700. And several other overdose deaths and hospitalizations have been identified by local law enforcement in Florida and northern Texas.

The uptick in overdoses and drug seizures involving opiates like W-18 and U-47700 follows actions taken by the Chinese government to criminalize more than 100 chemicals on 1 October 2015, according to Bare.

Once more traditional synthetic drugs were outlawed, chemists looked to more novel substances instead.

The banned chemicals included the makings of acetyl fentanyl, an illicit version or analogue of the powerful prescription painkiller fentanyl that is drastically exacerbating the opioid epidemic in the US. Flakka, a cathinone similar to bath salts, was also banned.

Logan said chemists are finding the recipes for these drugs from research books from the 1970s, when scientists were trying to invent alternatives to morphine.

“In order to find one drug like that you have to test hundreds of them,” said Logan. The result is that there are thousands of variations of research opiates, most of which were never meant to be tried on humans.