The Proper Chemistry: Purdue Pharma’s OxyContin

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Within the mid-Nineteenth century, the British East India Firm had a profitable enterprise smuggling opium from India into China. The Chinese language authorities had been conscious of the addictive potential of smoking opium and had made the importing of the substance unlawful. China’s try to dam its ports from ships carrying opium led to the First Opium Battle in 1834, with the British navy breaking the blockade. 9 years later, China’s seizing a British ship triggered the Second Opium Battle, which resulted in a fast British victory and the legalization of the opium commerce.

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Right this moment, we face one other sort of opium battle. The “opioid epidemic” is destroying lives, with many pointing a finger at one particular drug, OxyContin, as being answerable for inflicting a lot of the distress. The story is a posh one, however there may be one inevitable conclusion. Purdue Pharma, the corporate that launched OxyContin to the market in 1996, has a closet filled with skeletons. Misleading advertising and marketing, the unfold of misinformation and concealment of the addictive nature of the drug have been all used to spice up gross sales. And people techniques netted Purdue Pharma billions of {dollars}.

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Opium is the white resin that seeps out of the bulb of the opium poppy when it’s lower with a knife. It has a posh chemical composition, however the physiological results that may embody euphoria, ache aid and sleep, are principally attributed to morphine, codeine and thebaine. The title “morphine” derives from Morpheus, the Greek god of sleep and, sadly, within the fallacious dose, that sleep may be everlasting.

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The opium poppy was cultivated as early as 3400 BC by the Sumerians in Mesopotamia, who referred to it because the “pleasure plant.” The Assyrians discovered concerning the poppy from the Sumerians and handed the information on to the Egyptians. By the point King Tutankhamun ascended to the throne round 1300 BC, Egypt had a flourishing commerce in opium. Round 460 BC Hippocrates acknowledged the sleep-inducing properties of opium, however curiously there may be little point out of the substance till the sixteenth century when Paracelsus launched “laudanum,” a mix of opium, citrus juice and powdered gold as a ache killer. By the Nineteenth century, smoking opium and taking morphine, remoted from opium in 1803 by German chemist Friedrich Sertürner, had grow to be standard medically and recreationally. It had additionally grow to be clear that opium was addictive.

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The problem was to seek out a substitute for morphine that retains its pain-killing properties however eliminates its addictive potential. One strategy was to make small adjustments within the compound’s molecular construction and hope for the specified final result. In 1895, Heinrich Dreser on the Bayer Firm reacted morphine with acetic anhydride and got here up with diacetylmorphine which the corporate named “heroin.” It was deemed to carry out “heroically” in eliminating ache with out inflicting dependancy. Fallacious. Heroin turned out to be much more addictive than morphine.

In 1916, Martin Freund and Edmund Speyer on the College of Frankfurt tried a unique strategy. As a substitute of morphine, they selected thebaine, one other constituent of opium, as their beginning materials. Reacting this compound with hydrogen peroxide, then with hydrogen fuel, produced oxycodone. The brand new drug didn’t remedy the dependancy downside, nevertheless it did produce ache aid at a dose equal to morphine however was much less sedating. Throughout the Second World Battle, oxycodone turned Germany’s foremost ache reliever on the battlefield and Theodor Morell, Hitler’s doctor, documented that he gave Hitler repeated injections of Eukodal, the commerce title of oxycodone, after he was injured in an assassination try.

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By 1937, oxycodone had been launched in america however didn’t make a lot of a mark till the Eighties when a little-known pharmaceutical firm that had been established in 1952 by three doctor brothers, Arthur, Mortimer and Raymond Sackler, launched a slow-release type of morphine sulphate below the title MS Contin. The “contin” was a reference to “steady.” The concept was that the lively ingredient can be launched slowly, permitting ache aid over an extended interval. This was achieved by coating the capsule in addition to the particles of the lively ingredient it contained with various thicknesses of proprietary resins and acrylic polymers that allowed for passage via the abdomen into the small gut from the place oxycodone can be slowly absorbed. MS Contin bought nicely, however its patent safety was operating out and Purdue Pharma wanted to plug a brand new drug into the pipeline.

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The corporate determined to use the identical expertise that had been utilized in MS Contin to oxycodone and got here up with OxyContin, which was permitted in 1995. An aggressive advertising and marketing marketing campaign was launched with a concentrate on OxyContin offering 12 hours of aid as an alternative of the 4 hours offered by most opiates. Moreover, due to the sluggish launch, there can be no euphoria and due to this fact a smaller chance of dependancy. There was no proof for both of those claims. The truth is, a Purdue-sponsored trial in 1989 had proven that after belly surgical procedure greater than one-third of sufferers discovered that OxyContin’s aid of ache lasted solely eight hours.

Armies of salespeople marched into medical doctors’ places of work claiming that OxyContin was excellent for any type of ache, together with again aches and knowledge enamel extractions. And so they underlined that lower than one per cent of customers turned hooked on the drug. This was blatantly unfaithful. It wasn’t lengthy earlier than it turned clear that many sufferers have been exhibiting withdrawal signs, usually simply six hours after taking OxyContin. This made them take a second dose, a recipe for dependancy. Deaths from respiratory arrest amongst OxyContin customers have been changing into frequent, however Purdue Pharma insisted that it was as a result of folks abusing the drug by grinding up and snorting the capsules. This was not true. Dependancy and deaths have been additionally seen in sufferers who have been utilizing the capsules as directed by physicians.

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Purdue Pharma’s substitute of OxyContin by OxyNeo, which was imagined to thwart abusers by making the capsule troublesome to crush and snort, was only a method to get patent safety for a brand new drug because the patent safety for OxyContin was coming to an finish.

The increase started to descend on Purdue Pharma within the early 2000s with quite a few lawsuits by sufferers and state governments being launched. Lastly, in 2019, after paying billions in fines and settlements, the corporate filed for chapter. Purdue officers maintained that the issue was not the drug, however individuals who abused it. The issue was folks all proper, individuals who labored for Purdue Pharma and unfold misinformation.

joe.schwarcz@mcgill.ca

Joe Schwarcz is director of McGill College’s Workplace for Science & Society (mcgill.ca/oss). He hosts The Dr. Joe Present on CJAD Radio 800 AM each Sunday from 3 to 4 p.m.