Racing Integrity’s Newest Threat: Human Designer Drugs?

by | 09.19.2017 | 4:48pm

It's no secret the challenge of post-race drug testing has always been keeping regulators one step ahead of those who use illegal drugs or illegally manipulate medication. But with the advent of Internet sales and bitcoin, one laboratory director fears his job, and that of racing commissions everywhere, is about to get a lot more difficult.

Earlier this year, Dr. Rick Sams, laboratory director at LGC Sport Science in Lexington, Ky., was asked to analyze the contents of a plastic baggie found somewhere on a backstretch in Kentucky. The Kentucky Horse Racing Commission's Equine Drug Research Council makes funding available for LGC to analyze substances seized by security personnel to help the commission learn what drugs they need to be looking out for. The baggie contained sugar cubes, slightly rounded about the edges, almost as if they had been partially dissolved.

Sams' analysis revealed the sugar cubes contained etizolam, a drug used in a handful of foreign countries for short-term treatment of insomnia and panic attacks. Etizolam has not been approved for use in the United States by the federal government, although it has been granted emergency controlled substance status in a handful of states due to problems with illegal use in humans. Etizolam is a GABA inhibitor, making its action similar to Carolina Gold, a sedation substance which has caused debate in the show horse world and in racing. Sams' quest to find out how it ended up in a baggie of sugar cubes took him down an Internet rabbit hole he hadn't expected.

Etizolam is one of hundreds of new psychoactive substances (or “designer drugs”) available online through illegal laboratories to anyone with a credit card or web-based payment system. Most of the drugs are cannabinoids (the largest group); others are opioids, benzodiazepines (sedatives), methamphetamines, or cathinones (known commonly as ‘bath salts') – newer, chemically-tweaked versions of street drugs which their makers hope will turn out to be more potent and commercially valuable than the last substance to hit the market. And there are hundreds of them.

In 2014 alone, global law enforcement seized 34 tons of new psychoactive substances. Some 644 new ones have been classified by the UN Office of Drugs and Crimes from 102 countries. In the course of one year, the office shut down 100 illegal labs in China churning out ketamine.

“That brings home the magnitude of the problem,” said Sams. “And ketamine is a legitimate substance that's still used in human and veterinary medicine and it's being made by these laboratories.”

Sams said these designer drugs escape regulatory detection by being touted as “research chemicals” and are commonly sold in vials with labels suggesting they are “not for human consumption.” This labeling often keeps them off the radar for the U.S. Postal Service, since transport of research materials isn't necessarily illegal. It's not hard to find dosing instructions online for the drugs, which often come in concentrate form and must be weighed into tiny quantities to get individual doses. Users then discuss doses, side effects, and length of symptoms openly in web forums.

These “research chemicals” are not buried in some corner of the dark web or limited to bitcoin users, either. Sams found websites selling legitimate psychoactive substances through a quick Google search as he was trying to learn more about the drugs themselves. Many retailers claimed to take mainstream payment methods.

“It blew me away,” said Sams. “I had no idea that this existed. I went on these websites where they're talking about these effects, they're talking about how they prepped the dose from a research chemical. On these websites, they'll learn what solvent is required to dissolve the chemical – not all of it is dissolvable in water – some of it is nail polish remover, rubbing alcohol.

“This whole thing has been so eye-opening for me.”

In the case of etizolam, users receive a vial of concentrated powder (Sams has analyzed these products and found that unlike many horse medications and supplements sold through sketchy online retailers, they do indeed contain the drug they're purported to). A reddit post directed users to dissolve the powder inside the original container (which is large enough to allow this). The solution can then be dried on blotting paper and divided into fractions based on the vial's concentration. Alternatively, it can be sucked, dose by dose, into small pipettes or insulin syringes. It is then dropped onto sugar cubes and allowed to dry, the crystals of the drug sitting more or less on the sugar cube and ready for oral consumption. It was this that investigators found on the backstretch in Kentucky.

New psychoactive substances are marketed to human abusers who have little concern for the way they were made; some are bought by addicts, others by athletes seeking an edge, usually with something that will act as an anabolic steroid. The drugs are on the radar for the World Anti-Doping Administration, which detected letrozole in mixed martial arts fighter Jon Jones in mid-2016. Letrozole was once used for treating breast cancer in humans by strangling the hormone supply to estrogen-dependent tumors. A side effect of its action was an androgenic effect.

What does all this have to do with horse racing? It's going to get much harder to figure out when a positive is really a positive.

Sams now has to quantify and analyze post-race samples for an exponentially-growing number of substances. At the time they discovered dermorphin could be chemically modified to escape detection, lab directors knew they would have problems finding all possible versions of certain drugs intended for horses. With hundreds of new substances out there intended for people, the challenge is far greater. Commission officials will now have a larger library of substances which could be found in horses as a result of accidental contamination, or as a result of cheating.

Designer drugs have already cropped up in racehorses, although the reason for their presence isn't often known. In 2011, MDPV (“bath salts”) were detected in horses in Oklahoma. JWH-250, a synthetic cannabinoid, was detected in Standardbreds in 2016. AH-7921 was found in a Thoroughbred in New York (though in that case, the trainer admitted he thought he had dosed the horse with a different illegal drug). And this year, nomifensine (which is no longer produced legally in the U.S.) has resulted in the suspension of the reigning American Quarter Horse Association champion trainer. All of these were designer drugs, likely cooked up in an illegal lab somewhere.

“We can't tell here from the analysis of the sample, whether it came from environmental contamination or the tail end of intentional administration. There are no tags that tell us one way or another,” said Sams.

This month, officials in Maryland held trainer Dale Capuano blameless after they determined a cocaine positive in one of his runners was caused by exposure to a groom who was in possession of the substance. In that case, the groom admitted his role in the positive, making it clear there was no intentional administration.

If you think people won't give a human drug of abuse to horses just to see if it helps, history says otherwise. Sams recalls as little as 30 to 40 years ago, trainers were known to administer methamphetamine to horses for the purpose of performance enhancement.

So what's the solution? Perhaps surprisingly, given his position, Sams doesn't think it lies in more testing. Currently, labs cannot detect a drug unless they have analyzed it and added it to their library. Hair testing is more appropriate for chronic drug administrations and unlikely to catch single uses of drugs in small quantities. He does think federal legislation placing the United States Anti-Doping Agency at the head of drug testing for racing could better disseminate new information about drugs across its network.

“I think [track surveillance] is really the answer,” he said. “I think longer than four hours from race time is needed. Maybe it comes down to out-of-competition and essentially lockdown at the racetrack before race time, maybe for as long as two or three days.”

Newer substances of human abuse may already be making their way into the horse world. In the course of his research Sams found one other item related to etizolam – a classified advertisement on a website geared toward Western pleasure riders.

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