Opiates:History,Use,Abuse,Addiction

Opioids: History, Use, Abuse, Addiction

How Did We Get Here?

Anchored in the history, culture, religion, mythology, biology, genetics, and psychology of the earliest civilizations to the societies of present day, humans have long tried to balance the positive medicinal properties of opioids with the euphoric effects that have so often led to their use and abuse.

Before we get into their history, first a quick fyi lesson in the semantics of the terms opiates vs opioids vs narcotics. While the terms are often used interchangeably, they are technically different things. 

The term opiate refers to any drug that is derived from a naturally occurring substance, ie from opium alkaloid compounds found in the poppy plant. Types of opiate drugs include opium, codeine, and morphine. The term opioid is broader, and refers to any synthetic or partially synthetic drug created from an opiate. Examples of opioid drugs include heroin, methadone, oxycodone, and hydrocodone. Narcotics is an older term that originally referred to any mind altering compound with sleep-inducing properties.

For the general public, only the term opioid is really necessary, as it includes all opi- substances. In my practice and in my blogs, I sometimes make a distiction between the terms, but if you’re looking for a safe bet, or maybe a trivia win, the term opioid is the best and most accurate choice. Regardless of the word used, one is not any safer than the other; any opiate or opioid has the potential to treat pain, to be abused, and to cause dependence.

Following are some of the most common opioids and their generic names, listed in order of increasing strength.

Codeine

Hydrocodone (Vicodin, Hycodan)

Morphine (MS Contin, Kadian)

Oxycodone (Oxycontin, Percocet)

Hydromorphone (Dilaudid)

Fentanyl (Duragesic)

Carfentanyl (Wildnyl)

History of Opiates

A long, long time ago, opiate use began with Papaver somniferum, otherwise known as the opium poppy. Native to the Mediterranean, it grew well in subtropical and tropical regions fairly easily, a fact that contributed to its historical popularity. Unripe poppy seed pods were cut, and the milky fluid that seeped from the cuts was scraped off, air-dried, and treated to produce opium. 

In case you’re wondering… today, legal growing of opium poppies for medicinal use primarily takes place in India, Turkey, and Australia. Two thousand tons of opium are produced annually, and this supplies the entire world with the raw material needed to make the medicinal components. Papaver somniferum plants grow from the very same legal and widely available poppy seeds found in today’s many seed catalogues. But, planting these seeds is less legal, with the DEA classifying them as a Schedule II drug, meaning that technically, they can press charges against anyone growing this poppy variety in their backyard. You can ask this one dude in North Carolina about it, as he was busted for having one acre of these big blooming beauties behind his house. At about 9 feet tall and topped with big red blooms, they’re not exactly inconspicuous. Another grow was discovered after an Oregon state patrol officer stopped to look at a field of beautiful “wildflowers,” wanting to cut a bouquet for his wife… a story that I personally find totally hilarious. Evidently, when he cut the first one, he was surprised by the sap that got all over his hands, so instead of taking some home to his wife, he took one to a fellow cop friend that was big on horticulture, and she enlightened him on what it was. Good thing too, because he had even thought about how cool it would be to dry the “wildflowers” to seed and plant them in his side yard! You just can’t make this stuff up.

Archaeologists have found 8,000 year-old Sumerian clay tablets that were really the earliest “prescriptions” for opium. The Sumerians called the opium poppy “Hul Gil,” meaning the “Joy Plant,” which was regularly smoked in opium dens. Around 460-357 B.C. Hippocrates, known as the “Father of Medicine” acknowledged opium’s usefulness as a narcotic, and prescribed drinking the juice of the poppy mixed with nettle seed. Alexander the Great took opium with him as he expanded his empire- it’s surprising that he was so great, because some accounts seem to suggest that he was a raging addict. Arabs, Greeks, and Romans commonly used opium as a sedative, presumably for treating psychiatric disorders. In the 15th and 16th centuries, Arabic traders brought opium to the Far East. From there, opium made its way to Europe, where it was used as a panacea for every malady under the sun, from physical ailments to a wide variety of psych issues. Biblical and literary references, and opium’s use by known and respected writers, leaders, and thinkers throughout history, including Homer, Franklin, Napoleon, Coleridge, Poe, Shelly, Quincy, and many more, made opium use perfectly acceptable, even fashionable. 

19th Century Opiates to Opioids

There was a lot of unrest and violence around the globe throughout the 1800’s. Wounded soldiers from the American Civil War, British Crimean War, and the Prussian French War were basically allowed to abuse opium. And sure enough, beginning in the 1830’s, one-third of all lethal poisoning cases were due to opium and its opiate derivatives, and this really marked the first time that a “medicinal” substance was recognized as a social evil. Yet, most places around the world still really turned a blind eye to opium and opiate use. But, so many soldiers developed a dependency on opiates that the post-war addiction state was commonly known as “soldier’s disease.”

In 1806, German alkaloid chemist Friedrich Wilhelm Adam Sertürner isolated a substance from opium that he named “morphine,” after the god of dreams, Morpheus. The prevailing wisdom for creating morphine was to maintain the useful medicinal properties of opium while also reducing its addictive properties. Uh huh, sure. In the United States, morphine soon became the mainstay of doctors for treating pain, anxiety, and respiratory problems, as well as consumption and “female ailments,” 

(that’s old-timey for tuberculosis and menstrual moodiness/ cramps) In 1853, the hypodermic needle was invented, upon which point morphine began to be used in minor surgical procedures to treat neuralgia (old timey for nerve pain). The combination of morphine and hypodermic needles gave rise to the medicalization of opiates.

Well, morphine turned out to be more addictive than opium, wouldn’t ya know it. So, as with the opium before it, the morphine problem was “solved” by a novel “non-addictive” substitute. Of course… I mean, what could possibly go wrong? Your first clue is that this novel compound was the first opioid, and was called heroin. See where this is going? First manufactured in 1898 by the Bayer Pharmaceutical Company of Germany, heroin was marketed as a cough suppressant, a treatment for tuberculosis, and a remedy for morphine addiction. Well, as you can probably guess, that worked great, until heroin proved to be far more addictive than morphine ever thought of being. So what to do? Hmmm… what…to…do… I know! Let’s make a “non-addictive” substitute for the heroin! That’s the best plan, definitely. 

20th Century: Opiates to Opioids

By the dawning of the 20th century, the United States focused on ending the non-medicinal use of opium. In 1909, Congress finally passed the “Opium Exclusion Act” which barred the importation of opium for purposes of smoking. This legislation is considered by many to be the original and official start of the war on drugs in the United States. Take that, Nancy Reagan! In a similar manner, the “Harrison Narcotics Tax Act of 1914” placed a nominal tax on opiates and required physician and pharmacist registration for its distribution. Effectively, this was a de-facto prohibition of the drug, the first of its kind.

In 1916, a few years after Bayer stopped the mass production of heroin due to the dependence it created, German scientists at the University of Frankfurt developed oxycodone with the hope that it would retain the analgesic effects of morphine and heroin, but with less physical dependence. Of course they did, because this worked out so swimmingly before. What could possibly go wrong? 

Well, we know how this story turns out.

First developed in 1937 by German scientists searching for a surgical painkiller, what we know today as methadone was exported to the U.S. and given the trade name “Dolophine” in 1947. Later renamed methadone, the drug was soon being widely used as a treatment for heroin addiction. But shocker… unfortunately, it too proved to be even more addictive than its predecessor heroin. Captain Obvious says he’s sensing a trend here.  

In the 1990’s, pharmaceutical companies developed some new and especially powerful prescription opioid pain relievers. They then created some equally powerful marketing campaigns that assured the medical community that patients would not become addicted to these drugs. Gleefully, docs started writing for them, and as a result, this class of medications quickly became the most prescribed class in the United States- even exceeding antibiotics and heart medications- an astounding statistic. Well, we now know that the pharma co’s were full of crap: opioids were (and still are) the most addictive class of pharmaceuticals on the planet… and so in the late 90’s, the opioid crisis was born. 

Opioids: True and Freaky Facts

The real fact is that 20% to 30% of all patients who were/ are prescribed opioids for chronic pain will misuse them. Further, studies on heroin addicts report that 80% of them actually began their addiction by first misusing prescription opioids. That’s a big number people, but I think it’s actually higher. Food for thought for all the pill poppers out there saying ‘I’ll never use a street drug like heroin.’ And speaking of that, by the turn of the 21st century, the mortality rate of heroin addicts was estimated to be as high as twenty times greater than the rest of the population. Twenty times, people.

Opioid Addiction and Overdose

Opioids produce a sense of wellbeing or euphoria that can be addictive to some people. Opioids are often regularly and legitimately prescribed by excellent, well-meaning physicians when treating patients for severe pain. The problem is that even when taken properly, many people develop tolerance to these opioids, meaning they need more and more to get the same effect and relieve their pain. That’s just one factor that makes them so insidious. In addition, we cannot predict who will go down this tolerance and potential addiction path, because it can happen to anyone who takes opioids. However, there are some factors that make people more susceptible to addiction, such as the presence/ prevalence of mood disorder(s) and especially a genetic/ familial history of addiction, which contributes to nearly 50% of abuse cases.

When people become addicted to opioids, they begin to obsessively think about ways they can obtain more, and in some cases they engage in illegal activities, such as doctor shopping, stealing prescriptions from friends and family, and/ or procuring them on the street. 

Another insidious facet of tolerance is that the tolerance to the euphoric effect of opioids develops faster than the tolerance to the dangerous physical effects of taking them. This often leads people to accidentally overdose as they chase the high they once felt. In this attempt to get high, they take too much and overdose, dying of cardiac or respiratory arrest. Drug overdose is the leading cause of accidental death in the United States, and there are more drug overdose deaths in America every year than deaths due to guns and car accidents combined. According to the CDC, 2019 drug overdose deaths in the United States went up 4.6% from the previous year, with a total of 70,980 overdose deaths, 50,042 of which were due to opioids. 

There’s a kahuna in Opioidland that’s so big and so bad that it bears a special mention… fentanyl. Referencing the above statistics, of the more than 50,000 opioid overdoses, fentanyl is specifically indicated in more than 20,000 of those fatalities. Again, I think it’s way higher than that. Regardless, I think we can all agree that it’s deadly. Fentanyl is so crazy dangerous because it is 50 to 100 times more potent than morphine, so it takes the teeny tiniest amount to overdose. A lethal dose of fentanyl for adults is about two milligrams- that’s the equivalent of six or seven grains of salt people! 

Obvi, there are tons of chilling statistics about fentanyl, but here’s another one for you: in one-third of fentanyl overdoses, the individual died within seconds of taking it. Get this- they died so quickly that their body didn’t have enough time to even begin to metabolize the drug, so no metabolites of fentanyl were found on toxicology screens at the time of autopsy. The moment you ingest or inject any drug/ pharmaceutical, the body immediately begins to break it down into components called metabolites. After a certain period of time (which varies according to many different factors) the drug is completely metabolized by the body, so a toxicology screen will pick up those metabolites rather than the complete molecule(s) of the drug. Every drug has a known rate of metabolism, so tox tests can tell how long ago a drug was used or ingested. This data is saying that in one-third (33%) of fentanyl overdose deaths, tox screens pick up zero metabolites, because the body had no time to even begin to start the process of making them. The screens detected the presence of the full complete molecule(s), but no breakdown products. It’s a very significant and scary hallmark of fentanyl use/ abuse/ overdose: the fact that you may not live long enough to regret using it.  

How did fentanyl become such a big part of the opioid epidemic? Around 2010, docs were getting smart to the use and abuse of opioids and the ensuing crisis, and many stopped prescribing them. This left a lot of addicted people, including many who legitimately required relief from pain, unable to get prescriptions and SOL. At the same time, buying prescription drugs on the street was crazy expensive due to increased demand and decreased supply. But also, heroin had became so abundant that it suddenly became cheaper than most other drugs, so addicts started to switch to heroin. In one survey, 94% of people in treatment for opioid addiction said they used heroin only because prescription opioids became much more expensive and harder to obtain. 

Next, to make things exponentially worse, drug cartels discovered how to make fentanyl very cheaply, so huge quantities of fentanyl started flooding the market. Because fentanyl is easier to make, more powerful, and more addictive than heroin, drug dealers recognized the opportunity, and began to lace their heroin with fentanyl. People taking fentanyl-laced heroin are more likely to overdose, because they often don’t know they’re taking a much more powerful drug. Fentanyl can be manufactured in powder or liquid forms, and it can be found in many illicit drugs, including cocaine, crack, and methamphetamine. And let’s face it folks, the people making this garbage aren’t exactly rocket scientists, so all of these drugs can (and usually do) contain toxic contaminants and/ or have different levels of fentanyl in each batch, or even varying levels within the same batch. These facts just add to the lethal potential of this stuff. 

Now fentanyl has found its way onto the street in yet another form: pills. When fentanyl pills are created for the street, they’re pressed and dyed to look like oxycodone. Talk about insidious! If you go looking to buy oxy’s on the street and the dealer is selling them dirt cheap because they don’t know any better, or care is probably more accurate, you’ll probably think ‘Wow- these oxy’s are cheap! Let me get those!’ If your body is accustomed to using real oxy’s and you unknowingly take fentanyl, you will absolutely overdose. Like see ya later, bye overdose.

But believe it or not, it gets worse… A new variation of fentanyl is finding its way into the drug trade. Carfentanil is 100 times stronger than fenatanyl, which makes it 10,000 times more potent than morphine. While it was originally developed as an elephant tranquilizer (hel-looo??!!) the powdered form of carfentanil is now commonly used as a cutting agent in illicit drugs like heroin, cocaine, and methamphetamine.

Opioid Withdrawal

Opioid withdrawal can be extremely uncomfortable. But an important thing to remember is that opioid withdrawal is not generally life threatening if you are withdrawing only from opioids and not a combination of drugs. This is because each drug class is pharmacologically different, so withdrawal is different for each one. FYI, the most dangerous withdrawls are from benzodiazepines (Valium, Xanax, etc) and alcohol, even though alcohol isn’t technically a drug, it reacts, is metabolized, and physically withdraws from the body like any drug. Individually, either can be lethal in withdrawl and require medical supervision. 

Opioid Withdrawal Symptoms

Withdrawal typically includes the following symptoms to varying degrees:

Low energy

Irritability

Anxiety

Agitation

Insomnia

Runny nose

Teary eyes

Hot and cold sweats 

Goose bumps

Yawning

Muscle aches and pains

Abdominal cramping

Nausea

Vomiting

Diarrhea

Stages of Opioid Withdrawal

-The first phase (called acute withdrawal) begins about 12 hours after the last opioid use. It peaks at around 3 – 5 days, and lasts for approximately 1 – 4 weeks. This acute stage has mostly physical symptoms.

-The second phase (post-acute withdrawal) can last for a long time, with some references documenting up to two years. The symptoms during this phase are mostly emotional, and while they are considered less severe, they last longer.

Symptoms include mood swings, anxiety, variable energy, low enthusiasm, variable concentration, and disturbed sleep.

But, don’t let concern over withdrawl symptoms keep you from getting off of opioids. There are medications that can significantly decrease all of these. Two of the most common are methadone and buprenorphine. Being that drug detox is one of my specialties, in next week’s blog, I’ll outline both of these and tell you my reccommendations.

Until then…

Now that we’ve covered the history and background on opioids, if you think you might have an opioid addiction, I have a separate quiz that will bring some clarity to you on that question. I will upload a more detailed assessment as a separate blog, but for now, here’s a short generalized screen to take first. 

Do You Have an Opioid Addiction?

Answer yes or no to each of the following questions. If you answer yes to at least three of these questions, then you are likely addicted to opioids and should definitely take the detailed addiction self-assessment test which follows. I also suggest that you print the assessment and answers and take them with you for a professional evaluation.

Addiction: Basic Screen1) Has your use of opioids increased over time?2) Do you experience withdrawal symptoms when you stop using?3) Do you use more than you would like, or more than is prescribed?4) Have you experienced negative consequences to your using?5) Have you put off doing things because of your drug use?6) Do you find yourself thinking obsessively about getting or using your drug?7) Have you made unsuccessful attempts at cutting down your drug use?

Again, if you answered yes to at least three of these questions, then you are likely addicted to opioids and should take the detailed addiction self-assessment test which follows as a separate blog. Be sure to print both with you for a professional evaluation. 

I hope you enjoyed this blog and found it to be interesting and educational. Please feel free to share it with family and friends. Be sure to check out my YouTube channel with all of my videos, and I’d appreciate it if you would like, subscribe, leave comments, and share those vids! As always, my book Tales from the Couch has more educational topics and patient stories, and is available in office and on Amazon. 

Thank you and be well people!

MGA

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