You can hardly go a single day anymore without reading about someone overdosing on some kind of opioid painkiller. Even worse, new opioids continue to be developed, manufactured and distributed. These man made synthetic opioids continue getting stronger and stronger, which in turn makes an effective dose cheaper and cheaper. The increasing potency also reduces the margin for error between an effective dose, and a lethal dose. These potency of opioids have become so cheap to manufacture that illicit drug traffickers add them to heroin and/or cocaine to extend the supply and sell them at higher prices. This only adds to the dosage issues because often people who think they are using heroin or cocaine are actually using a mixed substance that in mostly comprised of a super-opioid.
The use of opioids goes back centuries. You may recall hearing of the Chinese opium dens from the 17th and 18th centuries in your world history class. Opium is just one member in a family of highly addictive substances. The term opiate or opiates refer to substances derived from the opium in poppy plants. Scientist eventually learned to create substances with similar molecular structures and biological effects as opiates. These substances that are either partially or fully synthesized became known as opioids. Eventually the term opioid or opioids grew to include both the synthetic opioids and the naturally occurring opiates—becoming an umbrella term for all opium derivatives natural and synthetic. The opiate family history swings violently back and forth between medical use and recreational abuse.
Records of opium cultivation go as far back as 3400 B.C. (Some archeological evidence suggests it was widely used as far back as 5000 B.C.) The ancient Sumerians gave the opium poppy plant the name “Hul Gil,” which translates to the “Joy Plant,” because ingesting it would give people a feeling of euphoria.
Somewhere between 460 and 357 B.C., the father of modern medicine, Hippocrates, began using opium to treat internal diseases. Roughly 600 years later, sometime between 220 and 264 A.D. a Chinese surgeon named Hua began giving opium to patients before operations.
In 1527, the Swiss-German alchemist, Paracelsus, dissolved an opium derivative in an alcohol solution and created laudanum, which he used to treat pain. Today, doctors in the United States still prescribe laudanum as a painkiller.
Friedrich Wilhelm Adam Sertürner, a German chemist, isolated morphine out of opium in 1806. Throughout the 1800s, doctors used morphine to treat a multitude of medical issues, including anxiety, menstrual problems, pain, and tuberculosis (known at the time as “consumption”). During the American Civil War, medics gave morphine to injured soldiers to dull their pain. Morphine remains the standard against which the strength of other opioids is measured.
In 1832, scientists discovered codeine, which is only about two-thirds as strong as morphine, and is the main active agent in the popular over-the-counter painkiller Tylenol.
Following the Civil War, many men suffered from a condition commonly known as “Soldiers Disease.” In fact, “Soldiers Disease” was the manifestation of withdrawal symptoms experienced by soldiers who had become addicted to morphine. In 1853, following the invention of the hypodermic needle, the use of morphine during surgical procedures grew, but the abuse of morphine also increased.
Because morphine abuse was so rampant, people searched for a less addictive way to treat pain. Dihydrocodeine, an opioid about one-tenth as potent as morphine, was developed in 1882. Then, in 1898, the German chemical company, Bayer, synthesized a morphine derivative it claimed was a non-addictive morphine substitute that also acted as a cough suppressant. That new substance, heroin, is two to three times as potent as morphine.
Just two short years later, in 1900, the Saint James Society began to mail free samples of heroin to morphine addicts. It intended these samples to help people free themselves from addiction. We now know that was a faulty plan.
The turn of the century also saw the development of dihydromorphine – another opioid up to 1.5 times as potent as morphine.
In 1909, the U.S. fired what is now considered the first shot in the “war on drugs,” when Congress passed the Opium Exclusion Act, which banned importing opium for smoking. Five years later, the Harrison Narcotics Tax Act of 1914 essentially prohibited opiates by requiring doctors and pharmacists to sign a registry in order to distribute them, while at the same time taxing the distribution of opiates.
A new opioid up to three times as potent as morphine, oxymorphone, was also developed in 1914.
Near that same time, Bayer halted mass production of heroin because people became dependent upon it and thus overused it. But, in 1916, at the University of Frankfurt, German scientists synthesized oxycodone for the first time. Again, they hoped this new opioid would have the pain killing powers of morphine, without being addictive. But, oxycodone is actually up to 1.5 times stronger than morphine.
Still desperate to stem the growth of addiction, The U.S. passed The Heroin Act in 1924. The Heroin Act prohibited all importation, manufacture, and possession of heroin in the United States. This made even medical use of heroin illegal, however many other medications derived from opium were still legal.
Hydromorphone, an opioid five times stronger than morphine, was also developed in 1924.
In 1937, scientists developed methadone. Commonly known today for its use in treating heroin addiction, this member of the opioid family can be up to 7.5 times as potent as morphine.
The United State established the Food and Drug Administration (FDA) in 1938 to make sure consumables were safe before they could be sold in America. However, some opioid based medications were already being used, including, codeine, morphine, and oxycodone.
In 1950, the FDA approved oxycodone and it became widely available under the brand name Percodan®. The abuse of prescription oxycodone began as early as the 1960s.
Scientists discovered Etonitazene, the first of the super-powerful opioids, in the late 1950s. Etonitazene is up to 1,500 times as potent as morphine.
1960 saw the development of more opioids, some of which are among the most potent. Clonitazene which is up to three times as potent as morphine, fentanyl, which is up to 80 times more potent than morphine, and etorphine, which is up to 3,000 times more potent than morphine.
The 1960s also saw a rise in the use heroin. This prompted The Controlled Substances Act in 1970, which categorized all illegal or controlled substances into five different schedules. Drugs were sorted based on known medical uses and potential for abuse, with Schedule I being the most severe and recognized as having no known medical use and a high potential for abuse. The high rates of drug abuse in the 1960s also led President Nixon to declare War on Drugs and establish the Drug Enforcement Agency in 1973.
The creation of increasingly strong opioids continued through the 1970s. In 1974, scientists developed two super-strength opioids, 3-methylfentanyl and carfentanil. At up to 6,000 times the potency of morphine, 3-methylfantanyl is one of the strongest opioids in existence, but it pales in comparison to the other super opioid developed the same year.
Carfentanil may be the strongest opioid ever created. At up to 10,000 times the potency of morphine, it can sedate large animals. If you want to knock out an elephant, all you need is 2mg of carfentanil. What happens when humans ingest such a strong substance? In a word, overdose. In a two-week period during the summer of 2016, carfentanil caused over 100 overdoses and as many as nine deaths in the Midwestern United States. In nearly all of these cases, the carfentanil was found either disguised as or mixed with other drugs.
In 1978, the German pharmaceutical company, Knoll, began selling Vicodin®, a mix of hydrocodone (an opioid up to 2.5 times as strong as morphine in some forms) and acetaminophen. Along with Vicodin, hydrocodone is found in Hycet, Lorcet, Lortab, Maxidone, Norco, Stagesic, Verdrocet, Xodol, Zamicet, and Zolvit.
Despite some hesitation to prescribe opioid painkillers in the early 1980s, by the end of the decade doctor started prescribing them to patients with chronic pain.
In the 1990s, the number of opioid painkiller prescriptions grew significantly. The marketing push made by pharmaceutical companies manufacturing the medications contributed to the boom.
The family of super-strength opioids continued to grow through the 1990s. 14-Methoxymetopon, an opioid up to 500 times as potent as morphine (and up to 1 million times the potency of morphine if injected spinally) was developed in the mid-1990s. In 1995, Ohmefentanyl, was discovered. It’s 6,300 times more potent than morphine. Fentanyl was also made available by prescription for the first time in the 1990s.
Abuse of prescription opioids doubled between 1998 and 2008. As of 2002 more than 6 million Americans abused prescription drugs.
In efforts to quell abuse, many opioid manufacturers started developing slow release or extended release forms of their respective products. These efforts have had mixed results.
2016 saw a rash of overdoses caused by substances referred to as W-15 and W-18. Initially these substances were believed to be extremely strong opioids. W-18 was actually thought to be the strongest opioid ever known. However, recent evidence shows that these substances do not share most of the characteristics associated with opioids.
As the opioid family tree grows the potential harm to humans seems to grow as well. Not only are more and more opioids becoming available, but they are becoming more and more potent. The prevalence of any specific opioid seems to come from a combination of its potency and its ease of synthesis. You can see the results of this economic combination in the rising rates of fentanyl and carfentanil found in street drugs and the consequential rise in overdoses on these opioids.
People addicted to opioid painkillers, tempted to find cheaper opioid alternatives on the street, are susceptible to these killers in disguise. If you or someone you know are addicted to pain pills, don’t hesitate to get help.
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