Helping authorities detect fentanyl analogues

The past several years has seen growing awareness of a drug called fentanyl, which is increasingly cited in relation to drug overdoses, including many high profile deaths, as well as becoming the focus of many law enforcement agencies, especially in the United States.

macro of pills

The U.S. Drug Enforcement Administration (DEA) have named fentanyl the most significant synthetic opioid threat in the U.S. in 2018, while the Centre for Disease Control in the United States have determined that the rate of drug overdose death from synthetic opioids, not including methadone, doubled in just one year from 2015 to 2016. In 2016, opioids caused 42,000 deaths, and nearly half of those were fentanyl-related, including the deaths of Prince, Tom Petty and Lil Peep.

But is fentanyl a new drug? And if not, why has it suddenly become a major factor in the opioid crisis?

Fentanyl was first synthesised in 1959 by Paul Janssen and has been used as a pain reliever and general anaesthetic in operating rooms. While there are legitimate uses for fentanyl, it presents a formidable public health risk, especially in the United States. While some drug users seek it out for recreational use, many are unaware that what they are buying is fentanyl, as illicit drug makers use it to adulterate more expensive pharmaceuticals and opioids, like heroin. It is 80 to 100 times more potent than morphine, and while it only costs $6,000 to purchase one kilogram of fentanyl in a lab, that one kilogram can have a distribution value of up to $1.6 million. This presents an enormous economic motive for replacing common opioids with fentanyl.

Fentanyl analogues, or compounds with a similar molecular structure, make it even more difficult to regulate. Analogues are manufactured in labs, and once one is discovered by law enforcement and outlawed, another analogue is already waiting to be put into use. Some, like carfentanil, are particularly dangerous. Carfentanil is 100 times stronger than fentanyl (making it 10,000 times stronger than a unit of morphine), and as such, is used to sedate large mammals, like elephants. These highly potent drugs can rapidly incapacitate by causing central nervous and respiratory depression.

Our Sport and Specialised Analytical Services team performs analysis for forensics laboratories, including those working with police authorities and coroners, to detect and identify drugs in body fluids and drug seizures.  Work is also performed to understand more about how the latest drugs are metabolised in the body. The study of drug metabolism, or pharmacokinetics, is vital to understanding how drugs break down in the human body.  In a forensic environment it is very important to know how the body changes a drug in order to be able to detect it in forensic tests.

Scientists at LGC Simon Hudson and Charlotte Cutler studied the metabolic fate of several analogues of fentanyl, including carfentanil, and published three white papers on their findings. Each paper goes through their methodology, which can be used as an aid to detect the analogues in biological fluids.

In one of the case studies, Simon studied carfentanil in post mortem blood samples.  Not much has been understood about the metabolism of carfentanil, which suggests that the true extent of carfentanil-related deaths is unknown. After analysing over 70 carfentanil cases, Simon found that the parent drug was always present in blood and urine post mortem and that in some cases, due to the low levels of carfentanil, extremely sensitive analytical equipment was required detect it’s presence.

In the other papers, Simon and Charlotte studied samples from UK siezures of drugs that were originally reported by authorities in Latvia and Slovenia between December 2016 and August 2017. They were able to identify many metabolites of cyclopropylfentanyl and methoxyacetylfentanyl. These studies are a beneficial tool to help authorities and scientists detect these analogues in the future.

To learn more about the history of fentanyl, its chemistry and current issues, watch our interesting webinar. And to understand more about Simon’s work and studies on the drug, read the white papers on carfentanil, methoxyacetylfentanyl, and cyclopropylfentanyl.

Helping athletes stay safe and clean with Informed Sport

The use of drugs in sport goes back a long time- all the way back to the invention of sport itself, when ancient Olympians would take herbal medicines, potions and drugs to enhance their performance. Chariot racers in Ancient Rome are believed to have fed their horses hydromel, while gladiators took stimulants to improve their abilities. But the Ancient Romans, advanced as they were, did not have mass spectrometres.

More recently, drug use in sport, or doping, has become one of the biggest problems facing sport. It’s now understood to not only oppose the spirit and integrity of sport, but also poses a danger to the athletes themselves.  And as science has moved forward, becoming more accurate and precise, we are well-placed to tackle this issue head on.

Sport is a multibillion pound industry, spanning nearly every continent and reaching billions of people, so it’s easy to forget sometimes about the individuals participating in it. A sport is only as great as the people who dedicate themselves to it and drive the sport. The industry’s top priority should be to protect these athletes and their health and integrity, which is why transparency and certification programmes like Informed Sport are so important.

 

The responsibility to stay clean rests with the athletes, who can be banned for several years, or even lifetime, from their sport if they test positive for a banned substance, whether they knowingly took it or not. Worse still, banned substances can pose serious risks to a person’s health, causing heart attacks, liver damage, and other problems.

But if people don’t know what’s in the supplements they use, how can they possibly have confidence in them or know which dangers to avoid? Surveys carried out on non-Informed Sport-certified supplements that were being sold in supermarkets suggest that as high as ten percent contained banned substances, which mean the products would not pass our certification.

The WADA banned substances list is not closed; items are added as and when new drugs are caught. So there is no way to absolutely guarantee that a product is free from these illegal ingredients, but there are definitely steps that will vastly minimise the risk posed to athletes. Ensuring that products are tested and certified is the first of these steps.

Simon Richardson of GCN visits LGC.

Global Cycling Network recently visited our labs to see first-hand how sports nutrition products are tested for banned substances.  Watch to learn for yourself how exactly our Informed Sport programme takes steps to protect athletes, giving them the option to see exactly when that protein bar they’re eyeing has been tested by experts.

We can all do our part. If we expect athletes to be informed about what exactly is going into their bodies, then supplements companies should strive to demonstrate that their products are safe.