Weekly Dose: ephylone, the dangerous designer stimulant found at Groovin the Moo

Australia’s first pill testing service was successfully trialled on Sunday at the Groovin the Moo music festival in Canberra. The group Safety and Testing and Advisory Service at Festivals and Events tested 128 samples and identified 85 substances, including paint, toothpaste, and a dangerous drug called ephylone.

While this is the first time ephylone has been detected in Australia, it has been growing in popularity in New Zealand. Festival drug testers from Know Your Stuff NZ detected ephylone at every event they attended over summer. In March, 13 New Zealanders were hospitalised for ephylone overdoses and police seized six kilograms of the drug worth around NZD$600,000.

Ephylone was also responsible for deaths in South Africa and the the United States in recent years.

Read more: Weekly Dose: phenibut – the Russian anti-anxiety drug linked to Gold Coast teens' overdoses

What type of drug is it?

Ephylone, also known as N-ethylpentylone and beta-keto-1,3-benzodioxolyl-N-ethylbutanamine (bk-EBDP), is a so-called “new psychoactive substance”. It belongs to the growing class of designer stimulants termed synthetic cathinones.

Synthetic cathinones are sometimes sold as “bath salts” or “plant food”, but are intended to be snorted or swallowed for their psychoactive effects.

According to the United Nations Office on Drugs and Crime, more than 140 individual cathinone derivatives have been identified as illicit drugs.

Although synthetic cathinones share a common chemical template, the potency, effects, and toxicity of these stimulants can vary enormously. Based on user reports of these substances, some synthetic cathinones produce experiences that are a mix between MDMA (ecstasy) and cocaine, while others are described as being similar to methamphetamine (ice).

How was it developed?

Ephylone was first described in a 1967 patent by the pharmaceutical firm Boehringer Ingelheim. It was originally designed to treat mild depression and fatigue, and researchers of the time showed that it produced stimulant activity in mice.

No formal scientific study of ephylone has occurred since then, so we can’t be certain about its effects in humans.

Read more: Flakka is a dangerous drug, but it doesn't turn you into a zombie

The closest chemical cousins of ephylone, such as pentylone, increase levels of the neurotransmitters (brain signalling molecules) dopamine, norepinephrine, and serotonin in cellular tests. Stimulants such as MDMA, cocaine, and methamphetamine can affect these three neurotransmitters to varying extents.

These neurotransmitters are highly involved in the processes underlying mood, arousal, appetite, and addiction. Modulation of the levels of these neurotransmitters in certain brain regions is key to the effects of stimulant drugs, but also clinically useful antidepressants and pharmaceuticals for attention deficit hyperactivity disorder (ADHD).

What does it do?

Although scientists have not yet investigated ephylone specifically, its chemical relative pentylone produces cocaine- and methamphetamine-like effects in rats lasting up to six hours. At higher doses, it causes fatal seizures. Rodent studies also suggest that pentylone and related molecules are likely addictive.

Online user reports posted to the websites Erowid and Reddit describe the effects of ephylone as euphoric, stimulating, and mildly empathogenic (producing a feeling of emotional openness), similar to MDMA.

As with other stimulants, overdose of ephylone can lead to overheating, dangerous changes to blood acidity, cardiotoxicity, and multiple organ failure.

How is it sold?

The active dose of ephylone is unknown, and it is often sold as MDMA, which has a typical dosage of around 100 mg.

According to one pill testing website, ephylone capsules have been found to contain anywhere from tens of milligrams to almost half a gram. The variability of ephylone dosages, and its misrepresentation as MDMA, increases the risk of overdose.

Although ephylone was only reported as an illicit drug for the first time in 2016, it was the most common cathinone drug in the United States by 2017, making up more than half of all synthetic cathinone seizures.

Read more: The rise and fall of Russia's 'flesh-eating drug' krokodil

Individual synthetic cathinones appear on the illicit drug market faster than we can comprehensively study them, and are often deceptively sold as other substances; a situation we have seen with other classes of designer drugs such as synthetic cannabinoids and fentanyl derivatives.

As the recent success of pill testing at Groovin the Moo shows, proactive approaches to the identification and study of new designer drugs can empower governments to respond quickly and effectively to emerging threats while minimising harms to users.