Oxyheroin

superheroin

This is Super Heroin.

You and I will probably never see it. But it exists, kind of..

Its full chemical name is (5α,6α)-7,8-didehydro-4,5-epoxy-14-hydroxy-17-methylmorphinan-3,6-diol diacetate. Its chemical structure looks quite similar to that of heroin, except for the inclusion of a single oxygen atom (in the form of a hydroxy group instead of just a hydrogen) at the 14-position.

I came across this substance when I was studying the structure-activity relationship of opioid analgesics of the morphinan class (e.g. pain killers with a chemical structure similar to morphine, otherwise known as most of the prescription pain killers worth doing, and heroin of course). I quickly noted that oxycodone (the active ingredient in OxyContin and Percocet) was nothing more than hydrocodone (the active ingredient in Vicodin) but with a 14-hydroxy group added. Things really got interesting when I realized that oxymorphone (Opana) is just hydromorphone (Dilaudid) with this same 14-hydroxy group.
This trend has been backed up hundreds of times in the scientific literature, where if you take an opioid in the morphinan class and add a hydroxy group to the 14-position, the resulting drug will generally be up to twice as potent, twice as euphoric, and twice as long-lasting, but also twice as addictive and twice as deadly.

I immediately rushed to see whether or not heroin has a 14-hydroxy group in the structure and was surprised and delighted to find out that it does not.

To put this all into perspective, imagine how much better Oxys are than Vicodins… and then try to imagine something that’s that much better than heroin!

I scoured the internet trying to find even a mention of its existence, googled every key word I could think of, posted in forums, emailed drug-geek buddies of mine and spent countless hours poring through old issues of the Journal of Medical Sciences at the university library. Normally when I’m obsessed with something I can’t find, I give up after a few hours of googling, but this time I was determined. I spent every waking hour for a week and a half straight chasing one empty lead after the next before finally I found what I was looking for…

It was an obscure off-hand reference, no more than a few sentences long, but it was enough to satisfy my curiosity and tell me what I wanted to know: a team of scientists (I believe they were German and this happened in the early 1960s, and now I’m really wishing I’d bookmarked the link because hell if I can find it again) also noticed the trend of what happens if you put a 14-hydroxy group on an opioid, and they too wanted to know what would happen if you did this to the heroin molecule.

The result was everything they expected and more. They pretty much immediately concluded that something so powerful, euphoric, and addictive would be too dangerous for humanity to handle responsibly and moved on to focus their efforts on other opioids. As far as I know, no one has bothered to synthesize it since.

What strikes me most about this is that they were commenting on its euphoria. Unlike potency and duration, the qualitative high you get from a drug is not something you can measure in lab rats or test with a machine. The fact that they mentioned how euphoric it was leads me to believe that these were people who not only tried it themselves, but also had a taste for opiates and knew what to look for.
Not terribly surprising, given that in the days before lab rats became standard procedure, a scientist would often test out their new inventions on themselves or their close friends before going public with their findings. If you’re familiar with scientific and medical literature from decades or even centuries ago, it’s also not terribly surprising that a group of chemists working on developing new opioid analgesics would have dope habits. It just kind of comes with the territory. The points I just mentioned were what inspired such classics as “Dr. Jekyll and Mr. Hyde” and a big part of what led to the archetype of the “mad scientist” in the first place.
What does surprise me is the sheer power and terror this chemical caused. This was a society that was still in the throes of the Chemical Engineering Revolution. They thought that they could conquer the universe and all of life’s problems if they simply found the right technology. There was an intense push to find the most superlative form of whatever they were exploring: the fastest, the hardest, the strongest, the most efficient ways of accomplishing their goals. Addiction and long-term consequences were poorly understood or ignored completely and it was not yet recognized what a devastating effect some of their creations were having on society.
These were people who were in love with opioids and searching every nook and cranny to find the ultimate form. They were completely okay with heroin, morphine, oxycodone, fentanyl, methadone, even etorphine (a chemical that is roughly 3,000 times the potency of morphine, just not as fun), but for some reason when they found this little gem they decided that it was too much.

The next logical question to ask is, “if it’s really so awesome, why isn’t it available on the black market?”

I can think of two possible reasons for this: it’s incredibly difficult to manufacture and it’s also incredibly easy to overdose on.

Think about all the different opioid pain killers out there. Other than heroin, almost all of them are pills, e.g. pharmaceuticals that were originally made legally in a laboratory and sold with a doctor’s prescription.
Heroin is incredibly easy to make. Just refine the morphine out of the poppy plant, add acetic anhydride, and you’ve got heroin. It’s literally two easy steps away from something you can grow yourself.
Most synthetic opioids require an incredibly difficult process that involves many complicated steps, a full laboratory and dozens of reagents.
It’s quite possible that most of the people manufacturing heroin simply don’t have access to the equipment or startup capital needed for such an operation. And really, if you’re already doing just fine for yourself making heroin (a process that requires almost no effort) why would you go out of your way to do something that is many times more complicated and expensive to manufacture when it’s only twice as good???

The pharmaceutical labs producing our Vicodin and Percocet could easily produce this drug, but no one working in the legal opioid industry is going to touch this one. We as a species simply got too good at Chemical Engineering and eventually reached the limits of how far we could take our quest for the best. The most potent, longest lasting grotesquely powerful drugs aren’t always the best ones out there for society at large. Today’s drug designers are feverishly searching for the ones they overlooked in the middle ground, the ones that offer the least euphoria and recreational value while still accomplishing their “intended medical purpose”.

The other reason I can think of as to why no one on the black market has bothered with this one yet is that it is so addictive and easy to overdose on.
Heroin already causes enough overdoses. Many people who sell it are constantly afraid that their customers are going to overdose and die and attract attention. A wave of deaths not only attracts attention from the police and FBI but can even cause national media coverage.
On top of this is the simple fact that dead people don’t make good repeat-customers.
Plus, it can ruin your reputation. Drug dealers have wisened up to the fact that if your product has a tendency to kill the people who use it, it’s going to be more and more difficult to sell that product as time goes on.

Still though, you might rhetorically ask, “since when have people manufacturing goods for the black market ever cared whether or not their products kill people?” And that’s totally valid, the far more likely answer is that this obscure, super-awesome form of heroin requires complex chemistry and expensive lab equipment whereas just plain regular heroin can be manufactured by uneducated slaves for next to nothing.

So that’s what I meant when I said it exists, kind of, but you and I will probably never see it. But isn’t it good to know it’s there?

Pandora’s Box has been opened, and can never be closed again.

In the words of the immortal Sasha, “Go West, young man!”

[EDIT 09/23/2014]  After much deliberation I decided that, if following the conventions of opioid nomenclature, the proper shorthand or common name for this substance would be “Oxyheroin”

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