Opioids Overview

The United States is in the midst of an “opioid epidemic,” aptly named considering that opioids are responsible for nearly 130 deaths every day in the United States. The drugs involved in the opioid epidemic range from illegal drugs such as heroin to legal, prescription drugs that can be bought at a pharmacy. Regardless of their legality, all opioids carry the potential for addiction.

 Opiate vs Opioid

While often used interchangeably, the term opioid refers to any substance that binds to opioid receptors and includes natural, synthetic (man-made) and semi-synthetic drugs. The term opiate refers to a drug derived directly from the opium poppy, such as morphine and codeine. All opiates are opioids, but not all opioids are opiates.

A Brief Overview

Opioids are some of the most effective analgesics available and often the backbone of treatment regimens for chronic pain, particularly cancer, with approximately 50% of active cancer patients receiving opioids long term. They are also routinely used for short-term pain control following surgeries; some common opioid medications include hydrocodone, oxycodone, morphine and fentanyl. While excellent at controlling pain, their effectiveness comes at a cost – placing the patient at high risk for addiction and opioid misuse, even in those with no history of substance abuse. It is believed that roughly 80% of heroin users’ addiction started with the misuse of prescribed opioids initiated for legitimate, medically necessary reasons.

Statistics

The statistics on opioids in the United states are unsettling. The National Institute on Drug Abuse estimates that in 2018, 3.4% of 12th graders in the United States had tried a narcotic other than heroin.3 The Centers for Disease Control and Prevention (CDC) estimates that from 1999 – 2017, opioid overdoses have been responsible for more than 700,000 deaths in the United States, with fentanyl being responsible for the most drug overdoses doses of any drug in 2016. People who begin abusing opioids may have originally been prescribed opioids legitimately for pain or obtained them illegally. Regardless of the origin of addiction, opioid drugs and their addictive potential pose a significant threat to any user’s physical and mental health, as opiate addicts will often resort to extreme measures to chase the “high” associated with their use.

The “Opioid High”

You may have heard of or even experienced “runner’s high,” the euphoric feeling many runners get while going for a long jog. The feeling is due to the release of endorphins, our body’s natural painkillers – one runner describes the feeling as follows:

“It’s that euphoric feeling where my mind is all of a sudden significantly clearer. I feel a lot lighter emotionally — all of my worries and anxieties start to subside — and I feel instantly lighter on a physical level.”

Now, imagine feeling that same blissful state of euphoria where all your worries melt away, except you didn’t need to run 10 miles – you just had to take a pill. That is precisely what happens with opioids. Opioids mimic our body’s endorphins to both effectively treat pain, but also create that feeling of euphoria that leaves people wanting more.

Tolerance & Dependence

After prolonged use, the body develops tolerance to opioids, whereby more of the drug is required to exert the same effect. This often leads to people taking more of the drug to achieve the same feeling. Tolerance is unavoidable and will always develop following long-term opioid use; it is our body’s way of “adjusting” to the opioid.

As might be expected, once our body becomes adjusted to the opioid, abruptly stopping it can cause undesirable effects – this is called withdrawal. Withdrawal is the constellation of symptoms that occur when someone taking an opioid for a long period of time suddenly stops taking it. Withdrawal symptoms include severe diarrhea, sweating, muscle aches and intense cravings for the drug.

Side Effects

In addition to the feeling of euphoria, opioids can cause side effects such as:

  • Nausea
  • Constipation
  • Respiratory depression

The constipation associated with high-dose opioid use is not typical constipation that can be relieved with an over-the-counter laxative. This constipation can be so extreme that it is impossible to remove without a licensed professional to physically dislodge the fecal matter. In more severe cases surgery may be required. The most fatal side effect of opioids is respiratory depression, characterized by slow, shallow, and ineffective breathing. In many cases, respiratory depression is ultimately what kills individuals who overdose on opioids. The individual’s breathing becomes so slow and shallow that death results due to oxygen deprivation.

Narcan – The Opioid Antidote

Luckily, respiratory depression can be stopped if action is taken quickly. The drug Narcan® (naloxone) can be used to reverse the deadly effects of an opioid and is available in most states without a prescription, including California. It is most commonly used as a nasal spray that works within minutes to restore normal breathing function. While naloxone is effective at reversing the deadly respiratory depression associated with an opioid overdose, it reverses all the effects of an opioid, immediately throwing the individual into a state of painful withdrawal.

Addiction Treatment

Drug addiction is a complex disorder that requires the aid of qualified healthcare professionals who specialize in addiction treatment, a strong support system, and often medications that help control both the physical and psychological symptoms of withdrawal. Several options for addiction treatment include methadone, Suboxone and Subutex.

Methadone – The Gold Standard

Historically the drug methadone has been used as the gold standard for the treatment of opioid addiction. Methadone is itself an opioid, which may at first seem counter-intuitive to use for opioid addiction. It is effective because methadone stays in the body significantly longer than other opioids, providing long-lasting prevention of withdrawal. It has also been shown to suppress cravings for opioids in general. Many opioid-addicted individuals treated with methadone remain on methadone indefinitely, sometimes their entire lives. While it can be argued that this strategy is essentially choosing the lesser of two evils (replacing heroin or prescription opioids with methadone), maintenance therapy with methadone allows monitoring of addiction in a controlled environment with a well-studied drug. The major drawback of methadone is that patients can only receive it in a registered methadone treatment facility, which can be costly and inconvenient. Methadone is also associated with significantly more drug interactions than most opioids, including cardiac abnormalities.

Subutex and SuboxoneNewer Options

Newer options for the treatment of opioid addiction include Subutex (buprenorphine) and Suboxone, a combination of the drugs buprenorphine and naloxone. The naloxone in Suboxone is the same drug used to reverse the effects of opioids. Suboxone is available as sublingual films while Subutex is available as sublingual tablets. Both the tablets and films are dissolved under the tongue, where the drug diffuses into the bloodstream though the tissue in the tongue.

Buprenorphine is similar to methadone in that it is an opioid used to suppress withdrawal symptoms, however it doesn’t carry the risk of drug interactions associated with methadone. It also doesn’t require the patient be seen in a clinic; it can be picked up at any retail pharmacy. When Suboxone is taken correctly, by dissolving it under the tongue, the naloxone has essentially no effect. If, however, the drug is injected or snorted, the naloxone component of Suboxone kicks in with full effect, throwing the individual into a painful state of withdrawal. This mechanism deters abuse and ensures the drug is taken correctly.

  Suboxone Subutex
Indication Opioid addiction Opioid addiction
Ingredient(s) Buprenorphine + naloxone Buprenorphine
Formulation Sublingual film Sublingual tablet
A Personalized Approach

There is no “one size fits all” drug for the treatment of opioid addiction, as each treatment has its own advantages and disadvantages. Your healthcare provider will help determine which option is best for you

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