The emergence of legal highs in the UK
The recreational drug scene in the UK has undergone rapid change over the last two years, with the growth of the so-called legal highs. These consist of psychoactive drugs that are not controlled by the Misuse of Drugs Act 1971 and are marketed as replacements for illegal drugs. Their emergence has been attributed to "a reduction in the availability (and thus purity) of illegal drugs such as ecstasy and cocaine and resultant disillusionment among users," according to a recent report in Drugs and Alcohol Today.
The legal highs produce effects similar to those of ecstasy, cocaine and amphetamines and are widely available over the Internet. At first, the active components were claimed to be cathinone derivatives such as mephedrone and mephylone which were not banned at the time. However, this is no guarantee of safety. As Phil Yates of the UK Forensic Science Service stated in the press recently, the term legal high did not mean that the Government had sanctioned them, just that they had not been tested.
Yates added "These are completely unknown quantities. They're not intended for human use, you really don't know what you're getting." That statement has been borne out by new research in the UK on the second generation of legal highs.
The emergence of second generation legal highs
On April 16, 2010, the UK government reacted to the growth in use of cathinone-based legal highs by classifying cathinone derivatives, including mephedrone, as Class B, Schedule I drugs, essentially banning them from use. The response of the drug supply community was rapid and alternative products were offered over the Internet within a very short time.
This second generation claimed to contain legal substitutes. Specifically, DMC is marketed with dimethocaine as active ingredient and NRG-1 (Energy 1) with naphyrone. The speed with which these products appeared raised the suspicions of a team of researchers, operating under Home Office licence, who set about to test the claims.
Simon Brandt and Harry Sumnall from Liverpool John Moores University, Fiona Measham from Lancaster University and Jon Cole from the University of Liverpool, acquired 24 second generation products from 18 websites following the April 2010 ban. They were analysed by NMR spectroscopy and by GC/MS to determine the compounds present.
Most of the products were powders or crystals but one was a dark oil and another consisted of green granules. They were each dissolved in methanol for GC/MS analysis using a 5% phenyl 95% dimethylpolysiloxane column and analysed using electron ionisation or positive ion chemical ionisation with methanol as the reagent.
The ingredients were identified from their mass and NMR spectra and by comparison with the spectra of standard compounds, where available.
Legal highs? most are illegal highs containing cathinones
A total of 13 samples were marketed as NRG-1 and purported to contain naphyrone. However, only one of them did, the remainder containing various cathinones, alone or in mixtures, such as mephedrone, butylone, flephedrone and 4-methyl-N-ethylcathinone. Other samples contained caffeine and local anaesthetics.
Seven samples flagged as NRG-2 actually contained mephedrone and 4-methyl-N-ethylcathinone, along with benzocaine and caffeine. The dimethocaine sample consisted of a caffeine-lidocaine mixture and contained no dimethocaine.
Overall, 15 (62.5%) of the samples contained cathinones, which are banned under current legislation.
Banned drugs remain on sale: Health and legal implications
This market testing program has revealed that many of the legal highs available online in the UK are, in fact, illegal. It remains to be seen whether online retailers are aware of the fact that they are, perhaps unwittingly, selling illegal products. Similarly, we must assume that the customer is purchasing the products under the misapprehension that they are legal when, in fact, they could be charged with the possession of illegal drugs.
A more worrying aspect is the effect that the cathinones have on human health. "Most of the so far detected cathinones have been known since the 1960s because they were patented by several pharma companies but further research and development was abandoned at that time," Brandt told spectroscopyNOW.com. There appear to be limited studies on their antidepressant and psychostimulant properties.
For the drug takers, however, there is the added risk introduced by the fact that they are not taking the drug they think they are. This could lead to excess consumption with an unpredictable outcome.
Illegal cathinones: new developments
Since the Brandt research was published, there have been several new developments. In a subsequent paper, Brandt showed that naphyrone consists of two isomers. The drug is generally associated with 1-naphthalen-2-yl-2-pyrrolidin-1-yl-pentan-1-one (beta-naphyrone) but they detected a novel isomer, the 1-naphthalen-1-yl- analogue.
"What was surprising is that the alpha-derivative appeared to be absent totally from the scientific literature and it would be interesting to evaluate its pharmacological/toxicological properties. We simply don't know anything about this compound," Brandt declared.
In a further paper soon to be published, Brandt and his team have identified further novel cathinone derivatives from the legal highs that they acquired, illustrating the complexity of the area.
The UK government has also reacted quickly to the appearance of the second generation legal highs by banning naphyrone from July 23, 2010. However, Brandt sees the legal high field as a fluid one: "I wouldn't be surprised if the cathinones were to disappear shortly, possibly, at least in part, due to lack of interest from users. New compound classes have come out already so it would be interesting to see how, and to what extent, they are going to be replaced."
*Analyses of second-generation ‘legal highs’ in the UK: Initial findings
* Drug Testing and Analysis 2010 (Article in Press): "The naphyrone story: The alpha or beta-naphthyl isomer?" (requested)
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* "Tweaking, bombing, dabbing and stockpiling: the emergence of mephedrone and the perversity of prohibition"
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October 15, 2010
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Legal highs contain illegal drugs: cathinones are the main culprits