Discovery Central - Morphine, Opium and Heroin

Welcome back to all my Snoopers. This time I'll be giving you discoveries, mainly scientific ones. This new collection of articles called "Discovery Central" will be your link to the origins of the most common and used chemicals around. And the one I'm going to talk about this time is probably one of the most effective painkiller ever used. To be properly clear, Morphine (formula on the right) is an analgesic drug derived from opium but far more reliable and powerful. Like other chemicals of the same family, called opioids, morphine acts directly on the central nervous system (CNS) to relieve pain. As everybody know, it's highly addictive and the abuse can reverse the effects fairly rapidly, worsening pain through Hyperalgesia.

The discovery of Morphine changed pharmacology and pain relief. But to start talking about it, we have to begin with the origins and use of opium. Derived from the seedpods of the poppy, opium (scientifically called Papaver somniferum) has been used since early civilizations, first cultivated from a wild strain, Papaver setigerum. The very first evidence of its use can be found in a 6000 years old Sumerian tablet and all the ancient populations (Egyptians, Romans and Greek) enjoyed it to a very insane point. This ancient powder was placed in pharaohs tombs and also mentioned in The Odyssey, the extremely famous classic poem. By the 700s AD, opium use had spread to include India, China and Arabia, the latter eventually becoming part of its trade.

Opium has long been prized for its medicinal purposes, even if its power cannot be compared with Morphine. The famous Greek physician Galen used opium to treat a variety of ailments, including poison, venom, headache, vertigo, epilepsy, vision problems, deafness,asthma, jaundice, urinary problems, fever, leprosy and melancholia. Although its efficacy as a cure for most of these complaints is questionable, the treatment probably put the patient in such a crazy state of mind that he didn't worry about his problems anymore. By the 1800s in Europe, opium was the painkiller of choice for physicians, but its effects were hard to predict. This was because each batch of opium would have its own unique and different qualities, including potency.

But now let's archive opium and start check out the discovery of its powerful friend. It all started in an old pharmacy in Paderborn, Germany. The young apprentice Friedrich Sertürner (1783-1841) was watching frustrated physicians complaining about the unpredictability of opium to his boss, who could do little more than entreat his suppliers for better quality. Realizing that the problem would never be solved until dosages could become standardized, Friedrich tried to isolate the active ingredient in opium, from which predictable and reliable doses could then be produced. Working in the evenings on the pharmacist’s old equipment, Friedrich eventually isolated a yellow-white crystal after submerging it in ammoniated water. Confounding conventional wisdom at the time, the substance produced was an alkaloid (the crystal in the photo is actually Piperine, an alkaloid), the first ever derived from a plant source.
After conducting animal experiments (including on a few dogs who died) and adjusting the dosages, Friedrich named his new drug for the Greek god of dreams, Morpheus, but to keep it consistent with standard naming conventions, labeled it morphine.

As all new scientific discoveries, Friedrich’s discovery was not well received at first by the medical community because of his lack of credentials and poor scientific method. Discouraged, he abandoned the work for several years until, while enduring a painful tooth ache, he treated himself with a small amount of his morphine. After a nice nap, he believed his product was safe for human consumption. But just to be sure about what he was doing, he began tests on local children. Luckily, it turned out to be effective, relatively safe and reliable, and his second round of experiments spurred interest, including that of French physician François Magendie. In 1818, Magendie published a paper on morphine’s pain relieving and sleep-inducing qualities, and by the mid-1820s, pharmaceutical companies, including that founded by Heinrich Emanuel Merck, were producing standardized doses of the drug.

In addition to being sold as an analgesic, initially morphine was also marketed as a non-addictive cure for addiction to both alcohol and opium, and by 1853, the drug was being administered via the newly invented hypodermic needle directly into the bloodstream, increasing the potency.
It turns out, the cure was far worse than the disease. After its heavy use in the American Civil War, people began to realize morphine was even more addictive than opium. So scientists began a research, in order to find a non-addictive opiate alternative to morphine.

But during that searching, London chemist C.R. Alder Wright synthesized diacetylmorphine from morphine in 1874. What a shame that this fantastic new formula was Heroin (on the right). Sure of a great success when he saw it, chemist Heinrich Dreser, with Bayer Labs, further developed diacetylmorphine and tested it on animals, himself (yes, chemists are so mad) and other people. They eventually commercialized it not only as a general cure, but also as a non-addictive cure for morphine addiction… Again, it turned out this amazing cure was even more addictive than its predecessor. Not a complete failure anyway. A new drug can sometimes be more useful, even if you're not actually searching for that.

Both morphine and heroin (as well as cocaine) were designated as controlled substances with the Harrison Narcotics Tax Act of 1914, which limited their distribution. Heroin was later banned even for medicinal use with the Heroin Act of 1924. Today, under U.S. federal law, both Opium and Morphine are listed as Schedule II controlled substances, meaning they have some medical use but also a “high potential for abuse.”
Heroin, on the other hand, is listed as a Schedule I controlled substance, which means it has no currently accepted medical use in the United States, even though some countries still use it for medicinal purposes. Recent statistics show that heroin and opioid analgesic abuse has reached huge levels in the U.S. lately, and drug overdose deaths from these have increased 400% from 1999 to 2010.

SO BE CAREFUL WHAT YOU INJECT IN YOUR VEINS.