What are Opioids?

Updated: Mar 20

What are Opioids?



The word “opioids” refers to a group of chemical pain-relieving compounds that impact our body’s ability to feel pain. Our body can naturally form opioids, referred to as endogenous opioids, or we can obtain these externally, referred to exogenous opioids, in the form of prescription painkillers or illicit drugs. Neurons or nerve cells in our body, brain, and spinal cord have receptors to which opioids bind. Once an opioid attaches to these receptors, they block the ability of those nerve cells to transmit pain. Opioids are available both legally as a prescription painkiller from a physician and in illegal forms such as heroin and synthetic fentanyl.




How long have doctors been prescribing opioids?


Opioids, or at least opium derivatives, have been used and traded worldwide for centuries. In the U.S., by the mid 19 century, opioids were being used widely to treat pain in injured Civil War soldiers. Initially available as opium, they were initially taken orally or inhaled. Later, morphine had been developed and could be administered with the recently invented hypodermic needle, which was more costly but more effective. These compounds were ultimately identified to be addictive and led to drug dependence in veterans of the Civil War, later known as “Soldier’s Disease”.

In response to the addictive qualities of morphine, the Bayer company developed a new version of morphine by 1898 and marketed this analgesic as effective and far more potent than morphine without its addictive properties. This new product was called Heroin, or diacetylmorphine. It was not only used to treat pain, but was also marketed to be used as a method to detox from Morphine addiction. It was not until 1924 that the widespread use and abuse of Heroin became evident, highlighted by the high rate of heroin use amongst criminal drug addicts and crime related to Heroin, leading it to being classified as illegal.

In time, oral opioid pills were developed; including, oxycodone in 1916 and hydromorphone (Dilaudid) in 1924. Combination agents were later developed that combined an opioid with another agent such as acetaminophen; including, oxycodone with acetaminophen (ie, Percocet and Endocet), hydrocodone with acetaminophen (ie, Vicodin and Lortab), and tramadol and acetaminophen (Ultracet).



The Drug Abuse Control Amendments of 1965 and the Controlled Substances Act of 1970 sought to regulate the use of potentially addictive substances with risks of misuse and abuse. By 1973, the Drug Enforcement Agency (DEA) was formed. Now, opioids are regulated as Schedule II drugs, whereas when combined with acetaminophen or aspirin they are less stringently regulated as Schedule III drugs.





What is the Opioid Epidemic?





The current Opioid Epidemic was a result in increased prescribing and consumption of oral prescription opioids during the late 1990’s coinciding with the development of long-acting oxycodone, better known as Oxycontin. This conflucence led to what today is considered the “first wave” of the Opioid Epidemic. The “second wave” is attributed to increased Heroin abuse. More recently, the “third wave” is attributed to illicit synthetic Fentanyl use. Fentanyl, developed in the 1960s and is among the most potent opioid available today, is generally administered intravenously and used primarily as an anesthetic agent during surgeries. However, by the 1980s and 1990s, other delivery systems for Fentanyl were developed such as buccal, sublingual, intranasal, and transdermal patches leading to the potential for abuse. Today, synthetic Fentanyl is illicitly made within the US and /or smuggled in creating the dominant driver of the Opioid Epidemic today. In 2021, there were over 100,000 opioid-related deaths in America.


How does addiction develop?

Our brains produce natural opiates called endorphins that work to block pain and produce a euphoric sensation. When exogenous opioids are taken, these opioids interact with our opioid receptors on nerve cells to block pain. These opioids also block our body’s ability to produce our natural endorphins. They also decrease the production of opioid receptors on nerve cells. In this way, the brain’s chemistry is altered. Gradually, tolerance develops to exogenous opioids requiring the individual to feel the need to increase their intake of opioids to get the same effect. When an attempt is made to decrease opioid intake, symptoms of withdrawal are noted. These symptoms drive the individual to increase their intake to avoid these uncomfortable symptoms. This cycle of increasing amount of opioids needed to achieve the same euphoric feelings while avoiding the withdrawal symptoms is what leads to abuse and the risk of overdose.


What are the symptoms of opioid withdrawal?

Opioids both block the sensation of pain while also providing a general sense of euphoria. When the effects start to wear off, it is common to experience symptoms of withdrawal. These symptoms include:

  • Anxiety

  • Insomnia

  • Dilated pupils

  • Body aches

  • Excess Sweating

  • Cramps and Vomiting

  • Diarrhea

  • Fever

  • Increased heart rate and blood pressure

  • Faster breathing

  • Hallucinations

  • Seizures

These symptoms can last for days or weeks making the individual seek more opioids to alleviate the symptoms.



Why are these medications even available given the risk of addiction?

Opioids are still routinely prescribed to manage severe acute pain, surgical pain, chronic pain, and cancer pain.

Is it possible to avoid addiction?

Development of an addiction relies on a multitude of factors. The factor that is likely within our control is the time frame these medications are taken. By choosing alternative non-opioid pain management strategies as first line treatment and then supplementing with opioids only when directed and needed is most important. Ultimately, minimizing the dose, frequency, and duration of opioids is most important to reducing the chances of addiction.


What is the Rothman Opioid Foundation’s role in the Opioid Crisis?

The focus of our Foundation is research, education, and advocacy to help curb the Opioid Epidemic. Specifically, the Foundation focuses on educating patients and prescribers on evidenced-based and safe opioid consumption and prescribing, respectively; supporting and performing research focused on advancing innovative opioid-sparing pain management strategies; and advocating for evidenced-based pain management legislations to our policymakers.





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