Hard News by Russell Brown

Ecstasy for grownups

The sudden suspension of the sale of Ease by Stargate International isn't news in the same sense that, say, yesterday's ripsnorting lead in the Herald on Sunday is news, but it is worth discussing.

The suspension of Stargate's "clinical trial" of its ecstasy substitute took place after Great Southern Television commissioned ESR to analyse the tablets for its forthcoming TV2 show, Truth Files. The analysis determined that they contained, well, exactly what Stargate said they did.

The impression that there was some undeclared ingredient in Ease should be dispelled. I obtained the ministerial advisory from Stargate under NDA some time ago; that is, the documentation the company supplied to Jim Anderton and his officials. As I see it, the NDA is now inoperative, so I'll quote the opening paragraph of the 'Substance identification and similarity to known substances' section:

Methylone is structurally and pharmacologically similar in some respects to the illegal and neurotoxic drug of abuse MDMA, although its structure falls outside the definition of "Amphetamine analogues" as defined in Part 7 of Schedule C of New Zealand's Misuse of Drugs Act.

Oh no it doesn't, says ESR. From the Herald:

Yesterday, Associate Health Minister Jim Anderton said advice from the chair of the Expert Advisory Committee on Drugs, Dr Ashley Bloomfield, showed Ease contained a substance called called methylone, an "analogue" - similar to - cathinone, which is a Class B amphetamine controlled under the Misuse of Drugs Act.

"On this basis, the so-called clinical trial being conducted via the Stargate website might well be a breach of the Misuse of Drugs Act, and accordingly the police have been informed," Mr Anderton said.

Matt Bowden says his company cleared the legal status of methylone for importation last year with government agencies, including the Ministry of Health. So it's less the case of something new being brought to light than an apparent change of mind by official experts. So which decision was the correct one?

The Wikipedia entry on methylone describes it as "a designer drug that is a methcathinone analog of MDMA (Ecstasy). It is also known as bk-MDMA, or MDMC. It is more properly known as methylenedioxymethcathinone. MDMC is related to methcathinone just as MDMA is related to methamphetamine, and as MDA is related to amphetamine."

But we run into naming issues. In that entry, methylone is described as 2-methylamino-1-(3,4-methylenedioxyphenyl)propan-1-one. Bowden's documentation describes a slightly different substance: 1-(1,3-benzodioxol-5-yl)-2-(methylamino)propan-1-one. The difference is apparent in the respective chemical structure diagrams: the methylone used by Bowden lacks two CH3 molecules. I don't know enough about chemistry to properly interpret this.

UPDATE:It's definitely the same chemical. The difference in diagrams comes down purely to the use of different conventions (and probably different software) for drawing molecules. Told you I didn't know much about chemistry - RB.

The full schedule of drugs controlled under our Misuse of Drugs Act is here. It lists both cathinone (which can be derived from the plant khat) and methylcathinone as Class B controlled drugs. My impression is that the legal argument on whether methylone was of a "substantially similar structure" to those controlled drugs rested on the presence or otherwise of the CH3 molecules.

In a way, this misses the point: you're saying that something should be illegal because it's against the law. What, you may be wondering, is this stuff, what does it do and how dangerous is it? Alright: methylone was first synthesised in 1997 by the US Drug Enforcement Agency (yes, really) and then, independently, by Dr Alexander Shulgin.

Like ecstasy (MDMA), methylone works by triggering serotonin release in the brain. Unlike ecstasy, it is selective and does not release the monoamines dopamine and noradrenalin, which are responsible for the amphetamine-like effects of ecstasy.

In practical terms, the effect is one of elevated mood, empathy and sociability, without the out-of-it-ness of ecstasy, the intensity of physical effect, or the hangover. As a friend of mine put it, "ecstasy for grownups". There are quite a number of experience reports at Erowid. (To answer the obvious questions: yes, I have tried Ease and I am not the only journalist to have done so, and, yes, I found it highly effective.)

But the monoamine dump triggered by ecstasy is also linked to its neurotoxicity: depending on dosage, frequency and recovery time, ecstasy really can hurt your brain. With its more selective effect, methylone would seem to lack ecstasy's neurotoxic effects, even at high doses. This is the argument Bowden made in the ministerial advisory, also suggesting that it lacked the mechanisms to cause addiction or acute hyperthermia, which is the main cause of (very rare)ecstasy deaths.

As part of a trial programme involving "several hundred individuals with a total of only a few thousand doses consumed", Bowden had volunteers take up to 2500mg under supervision (a standard dose is 100-400mg). They became confused but didn't need medical attention. He points out in the ministerial advisory that a comparable dose of MDMA would have been fatal.

From there, Ease went public, in what was called a "non-therapeutic clinical trial" but really looked a lot like a direct marketing business. Customers were required to be over 21 and to complete a questionnaire on their existing drug use (in particular, they had to warrant that they were ecstasy users) before being able to buy Ease in tidy little branded packets of four 100mg tablets for $50. Those who gave their mobile numbers got text messages every week, letting them know where the Stargate team would be in advance of the weekend's club nights and dance parties. Ease was also available to registered customers via the Stargate website.

Until, that is, last Friday. That afternoon, a text message went out to customers:

STARGATE: Regrets to inform, due to conflicting legal opinions, the EASE trial is withdrawn. Thanks to all participants. More info on TV1 news 6pm tonight.

The One News video is online here.

So it would seem to be over. And perhaps Bowden knew that it wouldn't last. The fact that methylone is less harmful than ecstasy is not in itself an argument for its legalisation. But the weekend's regional rioting would seem to suggest that another popular social lubricant isn't exactly harmless either. One thing's for sure: the ecstasy dealers will be relieved.