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      Hamilton's Pharmacopeia

      April 2, 2009

      By Hamilton Morris

      Photo by Maggie Lee

      SYNTHETIC OPIOIDS: THE MOST ADDICTIVE DRUGS IN THE WORLD
      I have never been that into opiates. Sure, the drug train has made a brief stop at heroin junction, but it’s honestly not my thing. It’s not like I hate the effect—I like swimming through a sea of warm blankets fresh from the euphoria dryer as much as the next person. You know, sometimes you have a shitty day, you stub your toe or your cat knocks something over, and you think, “Wow, a line of heroin would really do the trick right now!” but that’s just asking for trouble. Scientists have spent over a hundred years trying to figure out a way to cure pain without making people high. When heroin was first synthesized, they marketed it as a nonaddictive alternative to morphine. Whoops. But heroin was just the beginning of the itchy and constipated history of synthetic painkillers.


      ETONITAZENE
      It has been suggested that etonitazene is the most addictive substance on the planet. As an opioid, it exhibits 1,500 times the potency of morphine, but it’s also a stimulant on par with ecstasy. Basically, it’s a molecular speedball. Although etonitazene has appeared as a street drug on a few occasions, the vast majority of the world’s supply is consumed by mice and monkeys in addiction studies. Scientists know that rhesus monkeys lick their little furry lips with delight when you spike their water dish with etonitazene, but monkeys like a lot of shit, and as the old saying goes, never send a rhesus monkey to do a man’s job.

      Thomas Highsmith worked at a prestigious laboratory in Salt Lake City designing low-friction laminates for high-performance skis. In 2003, he started spending long nights in his lab secretly manufacturing a personal supply of etonitazene. Shortly after completing the synthesis, he became hopelessly addicted. He would show up for work clutching a 12-ounce spray bottle of etonitazene and fiendishly snort it throughout the day. Over the course of a couple of months, his tolerance escalated to the point where he was taking 300 times his starting dose. A coworker became suspicious of Highsmith’s odd behavior and reported him to the police. His etonitazene supply was seized, and he was prescribed methadone to combat the withdrawal. At that point, his addiction equated to 500 bags of heroin a day, and the methadone umbrella did nothing to deflect the 10,000-pound etonitazene anvil hurtling toward his head. Highsmith never received a criminal sentence because he was found dead in his home before his first court date. The withdrawals were so severe that he had killed himself to escape the pain.


      FENTANYL
      Etonitazene is hardly the most potent opioid known to man. Another class of opioids called the fentanyls is routinely much stronger. A classic example is carfentanyl, which is 7,000 times more potent than morphine. Carfentanyl was famously used to anesthetize a Tyrannosaurus rex in Jurassic Park 3, but it’s actually a real drug used to knock out bears and rhinos. Fentanyls have historically been a popular choice for naughty chemists because just a few grams can be cut and sold as thousands of bags of “heroin” at a tremendous profit, but this ruse has resulted in the deaths of hundreds of junkies who have overdosed on improperly cut fentanyl. Thus, fentanyl chemists are considered the slimiest scum of the drug-synthesis underworld. They make meth cooks look like hospice nurses. A junkie friend of mine said that he would not hesitate a moment before turning a fentanyl chemist in to the police.

      Two years ago, a young Canadian guy made a post on an internet drug forum begging for help withdrawing from an unknown opioid he called pharaohfentanyl, a synthesis of a new fentanyl derivative that he claimed to be 4,000 times more potent than morphine—the strongest opioid a human had ever tasted. He was generally mocked and assumed to be a liar, but after asking around a bit, I’ve come to the conclusion that his story was probably true. Although his original intention had been to deal the drug on blotter paper, he started using and spent the next six months on a nonstop pharaohfentanyl binge. His dosage increased 675-fold, and by the end he was using amounts that would equate to 3,300 bags of heroin a day. His breath alone was strong enough to make someone nod. He destroyed his entire supply and quit cold turkey. Here is how he described the withdrawal: “I cannot feel my FACE! It’s like touching a brick wall. It feels like I took a bath in MENTHOL, my insides feel like ice… that will shift after a few seconds to MENOPAUSE-ESQUE INSANE hot flash like a wave of lava under my skin with profuse sweating… I’M SOOO WEAK AND SOOO TIRED AND SOOO DRAINED I JUST WANT IT TO GO AWAY RIGHT NOW!”

      The general consensus is that if you’re smart enough to be making designer opioids, you should be using your skill to make LSD or a similar tool for enlightenment, but the temptation is hard to beat. I called up a chemist friend in England who has dabbled in the field. He said, “I’ve accumulated a shitload of data on designer opiates, but hopefully it will never see the light of day. I truly don’t want to encourage people to make these things that are effectively in the realm of psychochemical weapons, but they are so damn interesting that sometimes my judgment goes out the window and I start to chunter on about potential routes of synthesis and… oh well, sometimes I wish I could just shut the fuck up.”

      But guess what? Pharaohfentanyl is still not the most potent opioid ever discovered. The strongest painkiller in the world has only an abbreviated chemical name, 4-F-Ohmefentanyl, and it has 18,000 times the potency of morphine. After that, there is very little room left for improvement. It’s the hydrogen bomb of painkillers, and as far as I can tell, no human has ever tasted it. A suitcase full of this stuff could cure all the pain on Earth, which is sort of a pleasant thought. I tried contacting the Chinese chemists who discovered it but got no reply. I assume that either they don’t speak English or they aren’t willing to discuss their invention with the press. Or maybe, just maybe, their curiosity has already gotten the best of them.

       

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