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.

Our top 5 favourite scientific breakthroughs in history

British Science Week kicked off on the 9th March and this year’s theme is ‘Exploration & Discovery’, which encompasses the spirit of scientific enquiry. The week is a ten day celebration of science, technology, engineering and maths.

As humans, we love to celebrate big moments in history and retell stories that help us understand our own story. Famous thinkers often become legends who attain ‘larger than life’ status. But it’s important to remember that our heroes of science pursued science every day and dedicated themselves to their work. Innovations are often accomplished over the course of lifetimes with the help of many scientists.

We are constantly building on the knowledge of the past to take science into the future, and it’s exciting to think that we could each play a part in something big. After all, there are often just a few steps between ‘business as usual’ and ‘making history’. So keep up the good work!

To celebrate the spirit of exploration and discovery, here’s a look at our top five favourite scientific breakthroughs:

Genomics/DNA: While the term ‘genomics’ was only coined in 1986, by geneticist Tom Roderick, the actual study of the human genome is more extensive than that. A genome is defined as all the genetic information of an organism, and therefore genomics, the study of the complete genetic material of these organisms.

Gregor Mendel

Selective breeding has been practiced for thousands of years, but it wasn’t until the Augustinian friar Gregor Mendel undertook his studies in the mid-19th century that modern genetics as we know it was born. Do you remember practicing Mendel’s laws in school, determining traits in offspring based on dominant and recessive traits? It was the most fun to be had in biology.

Later, British Nobel Prize-winners James D. Watson and Francis Crick published the discovery of the helical structure of DNA, based on work done by Rosalind Franklin and Raymond Gosling, and then molecular biologists began to sequence nucleic acids. By 2001, the Human Genome Project completed a rough draft of the human genome, a feat which is being replicated with the 1000 Genomes Project. Now, scientists are using genomics to forge the way forward in personalised medicine, conservation, synthetic biology and gene editing. This all within the relatively short space of 150 years!

Domestication of plants & fermentation: Perhaps not a ‘discovery’, the domestication of plants definitely changed the course of human history, allowing populations to settle and grow. Plant domestication first occurred about 10,000 years ago in the Middle East. This change from hunter-gatherer societies to agricultural societies is largely seen as the beginning of the rise of civilisation.

Often, crops would go bad before they could be consumed, so in order to make the yields last longer and feed more, humans began to use a chemical process called fermentation in the Neolithic Age. This process converts sugars and carbohydrates to acids, gases or alcohol, and it was used to preserve food and beverages. Some of our favourite food and drinks were invented thanks to fermentation, including beer, wine, yoghurt, kimchi and sauerkraut (not that this is the only reason it made the list).

Alexander Fleming in his St Mary’s lab in London

Penicillin/antibiotics: Discovered in 1928 by Scottish scientist Alexander Fleming, penicillin became the world’s first true antibiotic. By the time Fleming made this discovery, scientists had reported the antibacterial properties of some moulds, including penicillium. But they were unable to successfully harness these properties. For his part, Fleming recounted that his historically famous discovery was a lucky accident. After mistakenly leaving a Petri dish containing Staphylococci exposed in his lab, he returned from holiday and noticed it had grown a blue-green mould. The mould slowed the growth of the bacteria around it, and after studying this effect, Fleming was able to use his ‘mould juice’ (blegh) to kill a range of harmful bacteria.

Ultimately, this discovery has greatly reduced the number of deaths from infection, playing an enormous role in improving the mortality rates around the globe. Today, antimicrobial resistance is a growing concern, and medical professionals warn that if we do not discover new classes of antibiotics, infections could kill as many as ten million people a year by 2050. But scientists are looking for new antibiotics in unexpected places, like toilet seats, dog food bowls, and even laptop keyboards.

Steam engine: Another British invention, the steam engine is not so much a scientific breakthrough as it is a series of breakthroughs over the course of one hundred years, and it certainly changed the course of human history. This invention has roots in Roman times, but it wasn’t until the 17th century when Englishman Thomas Savery developed a model of the steam engine that it became a promising innovation. Soon after, another Englishman, Thomas Newcomen, and Scottish engineer James Watt made the design more efficient and the rest, as they say, was history.

James Watt’s steam engine at the Thinktank museum in Birmingham (© Copyright Ashley Dace)

Connected to a piston and cylinder, a boiler filled with water is heated until the water turns to steam. Once the steam expands, it travels through the cylinder and moves the piston first forward, and then, once the steam is cooled, backward. This back-and-forth process, attached to a larger machine, moves the machine forward, in what must be one of the most rudimentary explanations ever of this amazing process. This engine was adapted for use in boats, cars, and, of course, trains. The idea that people began to cross continents in record time just by turning a liquid into a gas over and over is pretty bonkers when you think about it.

Periodic table: This one may be last on our list, but it’s definitely not last in our hearts. Chemists have spent a lot of time throughout history on the classification of chemical elements, but when Russian chemistry professor Dmitri Mendeleev got hold of it, things changed. He published his version in 1869, much to the chagrin of German chemist Julius Lothar Meyer, who published his version just one year later in 1870 and probably thought we’d all be talking about “Meyer’s Table” right now.

Like others before him, Mendeleev saw when elements were listed in order of atomic weight, elements at certain intervals shared physical and chemical properties. But Mendeleev left gaps in the table, predicting where an element hadn’t yet been discovered and it’s properties. He also took care to classify elements into ‘chemical families’. And just like any good developer, he released an updated version in 1871. Adjustments have been made from time to time, when new elements have been discovered or to make the table more easily readable, but Mendeleev is still considered the Father of the Periodic Table.

What are your favourite breakthroughs?

Science for a safer world

In the twenty-first century, science has been brought to the forefront, informing all aspects of our lives. In order for it to make our world safer, it’s especially important for science to remain steadfast, reliable and responsible. Science should not have an agenda; science is the agenda. It should not be informed by policy or opinion, but should inform policy and opinion. And at LGC, we work to ensure that our science does just that.

From our origins testing tobacco, alcohol and food products for adulteration in the 19th century, LGC has built a commitment to using science for a safer world.

This commitment underpins all of what we do. From testing drinking water and the quality of food to researching medicines and diagnostics, we work to ensure both our customers and the public benefit from our knowledge. Our scientists develop accurate methods for detecting infectious and congenital diseases and we test more than 6,000 products and supplements for banned substances, certifying that they are safe for athletes at all levels to use.  In our role as UK designated National Measurement Institute for chemical and bio-measurement, we solve measurement challenges in diagnostics, food safety, cancer research and environmental testing. At the heart of everything we do is the question, How can we make the world safer?

LGC is also looking to the future, to advance research, technologies, solutions and medicines that will build a better, more secure future.

Now, through this blog, we hope to bring our science to you, shedding light on the vital work we do every day.

What does ‘Science for a safer world’ mean to you?