Opioids, also called opiates or narcotics, are one of the oldest painkillers in existence. In fact, some sources suggest that opiates have been used since 1500 B.C. Today the use and abuse of opioids is a hot topic. However, because some of the forms of opioids go by other names, many people aren’t clear on how many types of opioids a physician is able to prescribe or what conditions are best suited to each type of opioid. Further, they carry risks of dependence, abuse, and addiction. How do opioids work, and more importantly, do their risks outweigh their benefits when it comes to treating pain?

How do opioids work?

All opioids work similarly. Sensory information, such as temperature or pressure, is transmitted from the body along nerves to the spinal cord and, from there, to the brain.

Along the way, groups of specialized nerve cells transmit pain signals as well. These nerve cells are partially controlled by mu receptors, a type of biological sensor. When these mu receptors are activated, they’re able to stop pain signals from going any further. Other receptors in the body include delta and kappa ones.

Naturally-occurring molecules like endorphin bind to mu receptors in order to regulate your pain perception. These natural molecules produce an “opioid effect” that helps to block pain signals, and also leads to a calming effect. It also has the side effect of slowing breathing and other functions. However, as the NAABT explains, “The body cannot produce enough natural opioids to stop severe or chronic pain nor can it produce enough to cause an overdose.”

Synthetic opioids

Naturally-derived opioids from poppies have been used for hundreds of years. It was only in the last few decades that healthcare professionals began using artificially-created, or synthetic, opioids to help treat pain. These opioids, also known as opiates or prescription painkillers, work through the same mechanisms as naturally-occurring opioids in our body.

These synthetic opioids mimic these natural molecules. And because of that, they can bind to mu receptors too. This essentially “tricks” the body’s receptors and suppresses part of the nervous system, thereby delaying pain signals. Since they don’t work in the same way as our natural brain chemicals, they lead to abnormal messages and floods of dopamine throughout the brain. The brain chemical, dopamine, is responsible for feelings of pleasure. And, as we’ll see, this flood of pleasure by users is the major reason opioids have such a high risk for addiction and abuse.

As the National Institute on Drug Abuse explains, these opioids affect more than the brain. They also affect:

  • The limbic system, which controls emotions
  • The brainstem, which controls automatic functions like breathing
  • The spinal cord, which controls pain transmission

The following video by Healthcare Triage (and backed by the National Institute for Healthcare Management) goes into a deeper explanation of how opioids work in the body and brain.


What are the different types of opioids?

There are several types of opioid prescription painkillers. To regulate opioid use and hopefully reduce the risk of abuse and dependence, the U.S. Drug Enforcement Agency (DEA) arranges potentially-harmful medications into groups called schedules. The higher the risk of abuse in each schedule, the more strict the regulations are surrounding its prescription and use.

Types of opioids include:

  • Low-risk Schedule V opioids, like cough medications with small amounts of codeine
  • Codeine, a Schedule II opioid
  • Schedule II opioids, including hydrocodone, meperidine, oxycodone, hydromorphone, fentanyl, methadone, and morphine
  • Schedule I street drugs like heroin that have no approved medical uses

Heroin is a type of opioid that’s synthesized from morphine. After entering the bloodstream, it converts back into morphine. Because heroin is so closely related to prescription opioids, the abuse of or addiction to prescription painkillers is often considered a first step to eventual heroin addiction.

What do opioids feel like? 

Opioids don’t stop pain — they inhibit your brain from experiencing those pain sensations. Typically, those who take opioids will feel:

  • Relaxed
  • Slightly warm
  • Foggy
  • Numbness
  • Slowed breathing
  • Drowsiness
  • Lethargy

Other side effects and risks include:

  • Dizziness
  • Nausea or vomiting
  • Constipation
  • Hearing loss
  • Opioid-induced hyperalgesia, or heightened sensitivity to pain
  • Sedation
  • Stopped or slowed breathing, that can lead to overdose and death

Opioid characteristics

Different opioids also have different characteristics. Because of this, pain doctors will prescribe different opioids based on what type of pain their patients are experiencing.

For example, short-acting opioids are typically effective for four to six hours, so they’re well-suited to conditions that don’t require round-the-clock medication. Short-acting opioids available in pill form include codeine and hydrocodone pills. There are other forms of short-acting opioids available, too, such as a fentanyl lollipop. These help with “breakthrough pain” that occurs despite regular pain medications.

Long-acting opioids are better for longer-lasting pain. Some of these opioids are available in pills. For example, oxycodone is available in both short-acting and long-acting form. Additionally, some opioids are available in long-acting form through patches or suppositories. Fentanyl, for instance, is available in a long-acting patch that can work for up to 72 hours. Some stronger opioids are given as injections, like morphine.

What Are Opioids? | PainDoctor.com

Why are opioids addictive?

Not everyone who takes opioids is an addict. But, opioid use carries a high risk for misuse, dependence, abuse, and addiction. As the National Institute on Drug Abuse explains:

“When properly managed, short-term medical use of opioid pain relievers—taken for a few days following oral surgery, for instance—rarely leads to an opioid use disorder or addiction. But regular (e.g., several times a day, for several weeks or more) or longer-term use of opioids can lead to dependence (physical discomfort when not taking the drug), tolerance (diminished effect from the original dose, leading to increasing the amount taken), and, in some cases, addiction (compulsive drug seeking and use).”

It’s important to know the facts. In 2016, over two million people in the U.S. had a substance abuse disorder involving opioids. 20,101 overdose deaths in 2015 were found to be related to opioids. Science Line explains why addiction occurs:

“An opioid’s ability to bind to the brain’s pleasure receptors makes it extremely effective in managing pain. But it also makes it very prone to abuse because the opioids also attach to non-pleasure receptors in the brain and on the spinal cord. When they bind in these other spots, they eliminate the sensation of pain. And because opioids impact the brain regions related to reward, some people experience euphoria. While it can take a while before heavy use leads to a physical dependence, psychological addiction can take place in under three days.”

Why are opioids deadly? 

There’s a few reasons addiction to opioids can be so deadly:

  • The difference between a lethal dose and the amount needed for pain relief is small, especially for those taking higher doses of the drug for pain
  • Mixing with alcohol, sleeping pills, or anti-anxiety medications heightens respiratory depression
  • Long-time users often develop tolerance, or less of an ability to feel the drug’s effects, and require higher doses

To repeat, not everyone who takes opioids is an addict. Certain factors can influence a person’s risk for becoming addicted. These include a family history of addiction as well as environmental and social factors. Further, working with a dedicated pain management team can help a patient find the lowest dosage needed, while incorporating complementary therapies to reduce pain safely.

Are opioids a good option for pain management? 

No. Opioids have been used in the past to treat chronic pain conditions like headaches, lower back pain, or fibromyalgia. However, many leading healthcare organizations, including the CDC, NIH, and the American Academy of Neurology (AAN) have all spent considerable resources studying the use of these medications. And one after the other have come to the conclusion that opioids are not a good option for chronic pain management. Here’s what they say.

How Do Opioids Work To Relieve Pain? | PainDoctor.com

The American Academy of Neurology 

The AAN notes that the risks outweigh the benefits when treating these conditions with opioids. Serious side effects, addiction, overdose, and death are all potential risks of opioid use. Risks increase with longer use. According to the AAN’s press release statement:

“Studies have shown that 50 percent of patients taking opioids for at least three months are still on opioids five years later. A review of the available studies showed that while opioids may provide significant short-term pain relief, there is no substantial evidence for maintaining pain relief or improved function over long periods of time without serious risk of overdose, dependence or addiction.”

Pain journal study 

In November of 2014, a report published by the medical journal PAIN demonstrated the correlation between prescribed painkillers and mortality rates among chronic pain patients. Researchers made associations between opioid-related overdoses and the increase of prescriptions for these types of medications to chronic pain patients not diagnosed with cancer. The higher risk of mortality was found among patients prescribed opioids for long-term use as opposed to individuals who used them on a short-term basis.

There were a number of factors in these deaths, including a higher risk of poisoning. In fact, long-term opioid users had a four times higher risk of poisoning than individuals without a chronic pain diagnosis. From Drs. Harald Breivik and Audun Stubhaug from the Department of Pain Management and Research at the University of Oslo:

“Safe and effective treatment of opioid-sensitive pain is possible but continues to be a double-edged sword that is difficult to handle. It requires deep pharmacological knowledge, experience, resources, considerable patience, and mental energy from a group of helpers who are able to take care of the whole bio-psycho-social conundrum of the chronic pain patient.”

Cleveland Clinic research 

The Cleveland Clinic backs up this research, noting that for too long doctors were prescribing opioids to patients without considering the long-term effects in their effort to stem chronic pain. The years since that trend became popular demonstrated that this approach was not only ineffective but also dangerous. Dependence on these painkillers develops very quickly and, without the right support, patients are at a high risk of addiction and death.

In fact, between 15,000-18,000 deaths occur each year from the overdose of prescription medications. A phenomenon known as “pill mills” became prevalent which helped individuals get access to these drugs even without the care of a physician. Luckily, most states are implementing programs to crack down on these for-profit drug centers.

In truth, opioid medications do not provide adequate pain relief when used long-term due to the body’s ability to process these chemicals and develop a tolerance. Patients using the drugs over long periods of time typically need to increase their dose to get the same relief they felt at the beginning of treatment. They also carry with them a whole host of side effects including addiction.

When are opioids an option? 

For the vast majority of chronic pain patients, opioids provide little pain relief benefits and a host of risks. However, there are some patients who do benefit from their use. Opioids should only be an option for acute pain, terminal conditions, or when other therapies simply do not work. If your pain specialist approves their use, develop a plan that can help you safely and effectively use these drugs. Our partners at PainDoctor offer this 12-step checklist for patients and their care providers to use to help manage their treatment.

How Do Opioids Work To Relieve Pain? | PainDoctor.com

Short-term pain relief

Due to the potential of developing an opioid addiction when using the medication for an extended period of time, one of the better uses is for short-term pain relief only. Opioid medications can be effective if they are prescribed for individuals who are undergoing surgery or are experiencing isolated pain due to an injury. As soon as the medication begins to be ineffective, however, there is greater risk for the patient.

The best use of this medication for acute pain is to utilize it only during a very short period of time immediately following the illness or injury. Often your doctor will prescribe them “as needed.” If other types of pain relievers provide relief, you can avoid opioids altogether.

Of course, for some patients other therapies, treatments, or medications may not have an effect. If this is the case, it is appropriate to talk to your doctor about alternatives such as opioid painkillers. Your doctor should closely monitor this kind of treatment.

Terminal cancers

Painkiller medications may be used effectively for individuals dealing with the effects of a terminal disease, such as cancer, who are in hospice or receiving palliative care. The use of these medications can help with the reduction of pain caused by the disease and its treatments.

In spite of science’s best advancements in the treatment of cancer, some forms remain terminal and untreatable. In these cases, opioids can provide some pain relief.

Last resort 

Some patients find that a reduced dose of opioids, along with complementary pain management therapies, can help them get back to their life. Living with pain is never easy, which is why doctors work hard to find treatments that do work for each specific patient. Before trying opioids for your pain, your pain doctor can try:

  • Therapies like physical therapy and chiropractic to correct underlying muscular issues that are leading to pain
  • Assistive devices like braces or orthotics to provide pain relief
  • Minimally-interventional techniques like epidural steroid injections or radiofrequency ablation to target pain at its source
  • Semi-permanent implants, like spinal cord stimulation, to provide ongoing pain relief
  • Surgeries, in cases with structural abnormalities

If none of these pain management therapies provide relief, talk to your doctor. Low or moderate doses of opioids could help manage your pain. Always work with a highly-trained pain specialist. They have a number of tools to help you in your fight against pain. Opioids can work for some, but only when used under the guidance of a trusted pain specialist.

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