Opioids

Opioids are a class of drugs that include the illegal drug heroin, synthetic opioids such as Fentanyl, and pain relievers available by prescription such as codeine, oxycodone, Vicodin, morphine, and others.

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All opioids are chemically related and interact with opioid receptors on nerve cells in the brain and on the spinal column. Opioid pain relievers are generally safe when taken for a short time and as prescribed by a doctor, but because they produce euphoria in addition to pain relief, they can be misused (taken in a different way or in a larger quantity than prescribed, or taken without a doctor’s prescription). Regular use—even as prescribed by a doctor—can lead to dependence and, when misused, opioid pain relievers can lead to addiction, overdose, and death. 

An opioid overdose can be reversed with the drug naloxone (Narcan) when given right away. Improvements have been seen in some regions of the country in the form of decreasing availability of prescription opioid pain relievers and decreasing misuse among the Nation’s teens. However, since 2007, overdose deaths related to heroin have been increasing. Fortunately, effective medications exist to treat opioid use disorders including methadone, Buprenex and Vivitrol. 

A National Institute of Drug Abuse (NIDA) study found that once treatment is initiated, both a Buprenex/Vivitrol combination and an extended-release Vivitrol formulation are similarly effective in treating opioid addiction. However, Vivitrol requires full detoxification, so initiating treatment among active users is difficult. These medications help many people recover from opioid addiction.

What are Prescription Opioids?

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Opioids are a class of drugs naturally found in the opium poppy plant. Some prescription opioids are made from the plant directly, and others are made by scientists in labs using the same chemical structure. Opioids are often used as medicines because they contain chemicals that relax the body and can relieve pain. Prescription opioids are used mostly to treat moderate to severe pain, though some opioids can be used to treat coughing and diarrhea. Opioids can also make people feel very relaxed and high, which is why they are sometimes used for non-medical reasons. This can be dangerous because opioids can be highly addictive. Overdoses and death are common. Heroin is one of the world’s most dangerous opioids, and is never used as a medicine in the United States.

How Do People Misuse Opioids?

Prescription opioids used for pain relief are generally safe when taken for a short time and as directed by a doctor, but they can be misused. People misuse prescription opioids by:

  • taking the medicine in a way or dose other than prescribed
  • taking someone else’s prescription medicine
  • taking the medicine for the effect it causes—getting high

How Do Prescription Opioids Affect the Brain?

Opioids bind to and activate opioid receptors on cells located in many areas of the brain, spinal cord, and other organs in the body, especially those involved in feelings of pain and pleasure. When opioids attach to these receptors, they block pain signals sent from the brain to the body and release large amounts of dopamine throughout the body. This release can strongly reinforce the act of taking the drug, making the user want to repeat the experience.

Opioid misuse can cause slowed breathing, which can cause hypoxia, a condition that results when too little oxygen reaches the brain. Hypoxia can have short- and long-term psychological and neurological effects, including coma, permanent brain damage, or death. Researchers are also investigating the long-term effects of opioid addiction on the brain, including whether damage can be reversed.

What are Other Health Effects of Opioid Medications?

Older adults are at higher risk of accidental misuse or abuse because they typically have multiple prescriptions and chronic diseases, increasing the risk of drug-drug and drug-disease interactions, as well as a slowed metabolism that affects the breakdown of drugs. Sharing drug injection equipment and having impaired judgment from drug use can increase the risk of contracting infectious diseases such as HIV.

Prescription Opioids and Heroin

Prescription opioids and heroin are chemically similar and can produce a similar high. Heroin is typically cheaper and easier to get than prescription opioids, so some people switch to using heroin instead. Nearly 80 percent of Americans using heroin (including those in treatment) reported misusing prescription opioids prior to using heroin. However, while prescription opioid misuse is a risk factor for starting heroin use, only a small fraction of people who misuse pain relievers switch to heroin. This suggests that prescription opioid misuse is just one factor leading to heroin use.

The Numbers

More than 64,000 Americans died from drug overdoses in 2016, including illicit drugs and prescription opioids. This number has nearly doubled over the past ten years. 2015 was the worst year for drug overdoses in U.S. history. Then 2016 came along. In that year alone, drug overdoses killed more people than the entire Vietnam War did.

A chart of US drug overdoses going back to 1999.

The Opioid Epidemic Explained

This latest drug epidemic is not solely about illegal drugs. It began, in fact, with a legal drug. Back in the 1990s, doctors were persuaded to treat pain as a serious medical issue. There’s a good reason for that: About 100 million U. S. adults suffer from chronic pain, according to a report from the Institute of Medicine.

Chronic Pain The Silent Condition

Pharmaceutical companies took advantage of this concern. Through a big marketing campaign they got doctors to prescribe products like OxyContin and Percocet in droves — even though the evidence for opioids treating long-term non-cancer related chronic pain is very weak despite their effectiveness for severe short-term, acute pain—while the evidence that opioids cause harm in the long term is very strong. So painkillers inundated society, landing in the hands of not just patients but also teens rummaging through their parents’ medicine cabinets, other family members and friends of patients, and the black market.

As a result, opioid overdose deaths trended up — sometimes involving opioids alone, other times involving drugs like alcohol and benzodiazepines (Xanax, Ativan, Valium) typically prescribed to relieve anxiety. By 2015, opioid overdose deaths totaled more than 33,000 — close to two-thirds of all drug overdose deaths. The numbers have grown exponentially over the past three years.

What Can We Do?

Seeing the rise in opioid misuse and deaths, officials have cracked down on prescription painkillers. Law enforcement, for instance, now threaten doctors with incarceration and loss of their medical licenses if they prescribed the drugs unscrupulously. Ideally, doctors should still be able to get painkillers to patients who truly need them — after, for example, evaluating whether the patient has a history of drug addiction. But doctors, who weren’t conducting even such basic checks, are now being instructed to give more thought to their prescriptions.

Yet many people who lost access to painkillers are still addicted. So some who could no longer obtain prescribed painkillers turned to cheaper, more potent opioids bought off the street, such as heroin and Fentanyl. Not all painkiller users went this direction, and not all opioid users started with painkillers. But statistics suggest many did. A 2014 study in JAMA Psychiatry found many painkiller users were moving on to heroin, and a 2015 analysis by the Centers for Disease Control and Prevention (CDC) found that people who are addicted to prescription painkillers are 40 times more likely to be addicted to heroin.

So other types of opioid overdoses, excluding painkillers, also rose. That doesn’t mean cracking down on painkillers was a mistake. It appears to have slowed the rise in painkiller deaths, and it may have prevented doctors from prescribing the drugs to new generations of people with drug use disorders. But the likely solution is to get opioid users into treatment. According to a 2016 report by the Surgeon General of the United States, just 10 percent of Americans with a drug use disorder obtain specialty treatment. The report found that the low rate was largely explained by a shortage of treatment options. Given the exorbitant cost of health care in America today, that is simply unacceptable. Federal and state officials have pushed for more treatment funding, including medication-assisted treatment like methadone and Buprenex.

Source: National Institute on Drug Abuse; National Institutes of Health; U. S. Department of Health and Human Services.

The Molecule

Andy Coop very nearly spent his career watching paint dry. The son of a machinist and school cafeteria worker, Coop hailed from Halifax in Northern England. He finished his undergraduate work in chemistry at Oxford University in 1991. He was given a choice of where to continue his studies. At Cardiff University was a professor whose specialty was the chemistry of paint. Industry at the time was aiming to find a new paint that dried at a certain temperature. At the University of Bristol was John Lewis, who studied the chemistry of drugs and addiction. In the 1960s, Lewis had discovered buprenorphine, an opiate that he later helped develop into a treatment for heroin addicts.

Coop didn’t remember giving the choice much thought. Drugs sounded more interesting than paint, so off to Bristol and John Lewis he went. It was there, in 1991, in a lab at Bristol, that Andy Coop encountered the morphine molecule – the essential element in all opiates. In time, Andy Coop got hooked on the morphine molecule – figuratively, of course, for he only once took a drug that contained it, and that was following surgery.

Like no other particle on Earth, the morphine molecule seemed to possess heaven and hell. It allowed for modern surgery, saving and improving too many lives to count. It stunted and ended too many lives to count with addiction and overdose. Discussing it, you could invoke some of humankind’s greatest cultural creations and deepest questions: Faust, Dr. Jekyll and Mr. Hyde, discussions on the fundamental nature of man and human behavior, of free will and slavery, of God and evolution. Studying the molecule, you naturally wandered into questions like, Can mankind achieve happiness without pain? Would that happiness even be worth it? Can we have it all?

In heroin addicts, there is a certain debasement that comes from the loss of free will and enslavement to what amounts to an idea: permanent pleasure, numbness, and the avoidance of pain. But man’s decay has always begun as soon as he has it all, and is free of friction, pain, and the deprivation that temper his behavior. In fact, the United States achieved something like this state of affairs during the last decade of the twentieth century and the first decade of the twenty-first century. It was first observable in widespread obesity. It wasn’t just people. Everything seemed obese and excessive. Massive Hummers and SUVs were cars on steroids. In some of the Southern California suburbs, on plots laid out with three-bedroom houses in the 1950s, seven-thousand-square-foot mansions barely squeezed between the lot lines, leaving no place for yards in which to enjoy the California sun.

In Northern California’s Humbolt and Mendocino Counties, 1960s hippies became the last great American pioneers by escaping their parents’ artificial world. They lived in tepees without electricity and funded the venture by growing pot. Now their children and grandchildren, like mad scientists, were using chemicals and thousand-watt bulbs, in railroad cars buried to avoid detection, to forge hyperpotent strains of pot. Their weed rippled like the muscles of bodybuilders, and growing this stuff helped destroy the natural world that their parents once sought. Today, great new numbers of these same kids – most of them well-off and white – began consuming huge quantities of the morphine molecule, doping up and tuning out.

What gave the morphine molecule its immense power was that it evolved somehow to fit, key-in-lock, into the receptors that all mammals, especially humans, have in their brains and spines. The so-called mu-opioid receptors – designed to create pleasure sensations when they receive endorphins the body naturally produces – were especially welcoming to the morphine molecule. The receptor combines with endorphins to give us those glowing feelings at, say, the sight of an infant or the feel of a furry puppy. The morphine molecule overwhelms the receptor, creating a far more intense euphoria than anything we come by internally. It also produces drowsiness, constipation, and an end to physical pain. Aspirin had a limit to the amount of pain it could calm. But the more morphine you took, Coop said, the more pain was dulled.

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For this reason, no plant has been more studied for its medicinal properties than the opium poppy. As the mature poppy’s petals fall away, a golf-ball-sized bulb emerges atop the stem. The bulb houses a goo that contains opium. From opium, humans have derived laudanum, codeine, thebaine, hydrocodone, oxymorphone, and heroin, as well as almost two hundred other drugs – all containing the morphine molecule, or variations of it. Etorphine, derived from thebaine, is used in dart guns to tranquilize rhinoceroses and elephants. [Amazingly, Etorphine has hit the streets of America as an opiate which teens and young adults are taking to get high, only to be dropping dead due to its potency.]

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Tobacco, coca leaves, and other plants had evolved to be pleasurable and addictive to humans out of the gate. But the morphine molecule surpassed them in euphoric intensity. Then it exacted a mighty vengeance when a human dared to stop using it. In withdrawal from the drug, an addict left narcotized numbness and returned to life and to feeling. Numbed addicts were notoriously impotent; in withdrawal they had frequent orgasms as they began to feel again. Humans with the temerity to attempt to withdraw from the morphine molecule were tormented first with excruciating pain that lasted for days. If an addict was always constipated and nodding off, his withdrawals brought ferocious diarrhea and a week of sleeplessness.

The morphine molecule resembled a spoiled lover, throwing a tantrum as it left. Junkies say they often have an almost constipated tingling when trying to urinate during the end of withdrawal, as if the last of the molecule, now holed up in the kidneys, was fighting like hell to keep from being expelled. Like a lover, no other molecule in nature provided such merciful pain relief, then hooked humans so completely, and punished them so mercilessly for wanting their freedom from it.

Certain parasites in nature exert the kind of control that makes a host act contrary to its own interests. One protozoan, Toxoplasma gondii, reproduces inside the belly of a cat, and is then excreted by the feline. One way it begins the cycle again is to infect a rat passing near the excrement. Toxoplasma gondii reprograms the infected rat to love cat urine, which to healthy rats is a predator warning. An infected rat wallows in cat urine, offering itself up as an easy meal to a nearby cat. This way, the parasite again enters the cat’s stomach, reproduces, and is expelled in the cat’s excrement – and the cycle continues.

The morphine molecule exerts an analogous brainwashing on humans, pushing them to act contrary to their self-interest in pursuit of the molecule. Addicts betray loved ones, steal, live under freeways in harsh weather, and run similarly horrific risks to use the molecule.

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It became the poster molecule for an age of excess. No amount of it was ever enough. The molecule created ever-higher tolerance. Plus, it had a way of railing on when the body gathered the courage to throw it out. This wasn’t only during withdrawals. Most drugs are easily reduced to water-soluble glucose in the human body, which then expels them. Alone in nature, the morphine molecule rebelled. It resisted being turned into glucose and it stayed in the body.

“We still can’t explain why this happens. It just doesn’t follow the rules. Every other drug in the world – thousands of them – follows this rule. Morphine doesn’t,” Coop said. “It really is almost like someone designed it that way – diabolically so.”

The above is taken from Sam Quinones’ best-selling nonfiction book “Dreamland: The True Tale of America’s Opiate Epidemic.” ©2015, New York, NY: Bloomsbury Publishing.