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.

opiate painkillers

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.

America’s Fentanyl Crisis

Every day 91 Americans fatally overdose on an opioid drug. It may be a prescription analgesic or heroin–4 to 8 percent of people who misuse painkillers transition to heroin–but increasingly it is likely to be heroin’s much more potent synthetic cousin fentanyl. In the space of only two years, fentanyl has tragically escalated the opioid crisis. This drug is 50 to 100 times more potent than morphine and able to enter the brain especially quickly because of its high fat solubility; just 2 milligrams can kill a person, and emergency personnel who touch or breathe it may even be put in danger. Unfortunately, many people addicted to opioids as well as other drugs like cocaine are accidentally being poisoned by fentanyl-laced products.

Although fentanyl is a medicine prescribed for post-surgical pain and palliative care, most of the fentanyl responsible for this surge of deaths is made illicitly in China and imported to the United States via the mail or Mexican drug cartels. Its high potency and ease of manufacture make it enormously profitable to produce and sell. According to the Drug Enforcement Agency (DEA), one kilogram of fentanyl can be purchased in China for $3,000 to $5,000 and then generate over $1.5 million in revenue through illicit sales in America. Thus, distributors of illicit drugs are eager to adulterate heroin or cocaine powder with fentanyl or put it in counterfeit prescription drugs, such as pills made to look like prescription pain relievers or sedatives. Last month, for example, a wave of deaths in Florida was linked to fake Xanax pills containing fentanyl.

Deaths from fentanyl and a handful of other synthetic opioids tripled from 3,105 in 2013 to 9,580 in 2015, and those numbers are likely underestimates; some medical examiners do not test for fentanyl and many overdose death certificates do not list specific drugs involved. Thus far, New Hampshire has recorded the most fentanyl overdoses per capita; an NIDA-funded study found that in 2015, almost two-thirds of the 439 drug deaths in that state involved fentanyl. Although most who fatally overdose on fentanyl are unaware of what they have taken, news of such fatalities has unbelievably driven some people with severe opioid addictions to seek it out. Part of the cycle of an opioid use disorder is increased tolerance, causing diminished response to the drug, which leads users to seek products with higher potency so they can experience the euphoria they initially felt. Roughly one-third of opioid users interviewed as part of the study in New Hampshire knowingly sought fentanyl.

The fentanyl problem is already a high priority for policymakers. Last month, NIDA’s Deputy Director Wilson Compton testified before Congress on the science of fentanyl, accompanied by representatives from the DEA, the Office of National Drug Control Policy (ONDCP), the CDC, and other agencies. Diplomatic and law enforcement efforts to cut off the supply of illicit fentanyl and the chemicals needed to manufacture it will be important, but the emergence of very high potency opioids–which can be transported in smaller volumes–will make addressing supply increasingly difficult. Thus, a public health strategy to address the opioid crisis and overdose epidemic is more important than ever.

First, we must improve pain management and minimize our reliance on existing opioid pain medications. Second, treatment centers and healthcare systems must make much wider use of available, effective medications for opioid addiction (Buprenorphine, Methadone, and extended-release Vivitrol). Third, the opioid-overdose reversing drug naloxone needs to be made as widely available as possible, both to emergency first responders as well as to opioid users and other laypeople who may find themselves in a position to save a life. In cases of fentanyl overdose, multiple doses of naloxone may be needed to reverse an overdose, and additional hospital care may be needed. All individuals who overdose on opioids need to be linked to a treatment program to prevent it from happening again.

From the blog of Dr. Nora Volkow, Dir., National Institute on Drug Abuse
April 6, 2017