Extended-Release Opioids: Dangers, Differences, Precautions

Extended-release or sustained-release opioids tend to contain higher doses. They’re formulated to gradually release into the patient’s body over an extended time, typically either a 12-hour or 24-hour period.

However, this time-release mechanism can be bypassed depending on the technology used. Crushing, snorting, and injecting extended-release tablets greatly increases the risk of life-threatening overdose.

The Current Opioid Overdose Crisis

As of 2015, an estimated 1 6 million people worldwide have been affected by opioid use disorders. A majority of heroin users begin taking opioids as legally prescribed pain-relieving tablets. In 2016, the United States recorded over 42,000 deaths due to opioid overdose.

This number grows every year. Many of the deaths are attributed to recreational use. The illegal manufacturing of the potent synthetic opioids like fentanyl are largely to blame. Fentanyl is 80 to 100 times more potent than morphine. It is commonly mixed in illegally pressed pills and sold as Xanax or various other street drugs.

However, many of the deaths are due to recreational users who take legally manufactured synthetic opioids in ways that are not recommended by physicians.

A Safer Extended-Release Oxycodone

Efforts are being made through the coordinated efforts of pharmaceutical companies and the FDA to reformulate extended-release tablets to reduce the likelihood of overdose. Collegium Pharmaceutical’s Xtampza ER is a sustained-release version of oxycodone. Xtampza ER is used to treat moderate to severe chronic pain in opioid-tolerant patients. It’s made in sustained-release capsules of 9 mg, 13.5 mg, 18 mg, 27 mg, and 36 mg. The pills are designed to release a percentage of the drug immediately upon ingestion, with the majority of the drug being released gradually over a 12-hour period.

The patient takes two pills a day for around-the-clock pain relief. Taking more than 36 mg in a single dose or exceeding 72 mg in a 24-hour period dramatically increases the risk of overdose.

According to a recent study presented at PAINWeek 2017 in Las Vegas, Nevada, Xtampza ER’s new formulation has a lower abuse potential than immediate-release oxycodone. Typically, extended-release opioids have a higher abuse potential due to their higher drug content. When crushed, the total drug content is released into the system all at once, increasing the risk of overdose.

The opposite proved to be the case with Xtampza ER. Researchers evaluated the pharmacokinetics of crushed and intact extended-release oxycodone compared to crushed immediate-release oxycodone.

Participants were asked to rank the euphoria of the high along with its pain-relieving effects. Researchers used various metrics, including pupil constriction to determine the strength of the drug’s effects. In general, the smaller the patient’s pupils, the higher the intensity of the effects. When all the numbers were crunched, immediate-release oxycodone had an overall higher risk of drug abuse and overdose.

This is a great accomplishment, considering that sustained-release opioids tend to have a significantly higher abuse potential, especially when crushed.

A Safer Version of Opana ER

In similar fashion, Endo Pharmaceuticals came out with a reformulation of their extended-release oxymorphone hydrochloride tablets in 2012. Opana is derived from morphine but is significantly more potent. Opana ER was first approved in 2006. Just like Xtampza ER, it’s intended for the management of moderate to severe chronic pain that requires 24-hour pain relief.

In 2012, Endo Pharmaceuticals changed the formulation of Opana ER to make it more difficult to manipulate for snorting or injecting. The new formulation met the FDA’s regulatory standards for approval. Following the drug’s release, the FDA determined that the new formulation did not meaningfully reduce Opana ER’s abuse potential.

Endo suggested adding additional warnings to the Opana ER’s label to highlight the potential of drug abuse. However, since the drug’s 2012 release, more evidence has surfaced indicating additional risk factors.

FDA Requests Removal of Opana ER

The 2012 reformulation of Opana ER is significantly more difficult to take via injection. However, taking it through this route is still possible, and severely opioid-dependent users continue to crush, dissolve, and inject the substance.

Common side effects of Opana ER include nausea, vomiting, heart palpitations, sedation, drowsiness, and respiratory depression. When Opana ER is taken intravenously, these adverse effects can become intensified.

Clinically significant respiratory depression is more likely to occur when Opana ER is injected. This can lead to carbon dioxide toxicity, oxygen-deprivation, coma, critical organ failure, irreversible paralysis, brain damage, and death.

In 2015, state officials in Indiana to emergency action following an epidemic of HIV in Austin, Indiana. The epidemic was spread primarily by drug users who were injecting oxymorphone intravenously. This event was one of the final strikes against extended-release oxymorphone tablets like Opana ER. Following this event, the FDA formally recommended the removal of Opana ER from the market.

In 2017, Endo Pharmaceuticals voluntarily removed Opana ER from the market due to the high rates of overdose and risk factors associated with recreational drug use.

How to Take Opioids Safely

All opioids carry with them a high potential for misuse, addiction, and overdose. Substances like oxycodone, oxymorphone, morphine, codeine, and fentanyl are classified as Schedule II controlled substances by the FDA. The manufacturing and distribution of these drugs are tightly regulated. Most have limits as to how much can be produced each year.

The North American opioid overdose epidemic began in the late-1990s and has been growing exponentially ever since. In response, hospitals and physicians have taken the initiative to reduce the rate at which opioids are prescribed.

Patients should only be prescribed opioids when milder, non-opioid pain-relievers are ineffective. The minimum effective dose of opioids should always be prescribed. Doses can be gradually increased every few days until the minimum effective dose is achieved. In general, only opioid-tolerant individuals should be prescribed extended-release versions of opioids.

When it’s time to stop taking opioids, doses should be reduced gradually to minimize symptoms of opioid withdrawal. Discontinuation of opioid use should always be conducted under medical supervision for the best possible outcome.


If you or someone you love is struggling with opioid dependency, Stonewall Institute Treatment Center is more than happy to answer any questions you may have. Call us today at 602-535 6468 or email us at info@stonewallinstitute.com.

Symptoms of Opioid Withdrawal

Symptoms of Opioid Withdrawal

 

If you or anyone you love has made the strong decision to enter drug rehabilitation, it’s key to be mentally prepared of the experience. Everyone who enters drug treatment must start with a professionally supervised drug detox. This is to ensure that the body is safely cleaned out in preparation for mental changes that will follow.

 

When it comes to opioids, it’s important to remember that we are talking about some of the most overwhelming drugs one can take. In essence, their introduction to the medical world was precisely for extreme pain. Pain so devastating, only a substance of power can truly take it away.

 

And though opioids have done some wonders in the medical world, they’ve only done harm to the streets. For people who end up experimenting with these substances almost always end up hooked being the power of the high.

 

It’s important to be aware of this due to the fact that the withdrawal symptoms are just as overwhelming. Your body is going to experience a change so impactful, it’s not going to understand how to properly handle the metamorphosis immediately. It’s going to take lots of time and effort in order for the body to return to its normal, functioning state.

 

This is what you or your loved one should be mentally prepared for. If you are unaware of the types of substances that are considered opioids, refer to the following list:

 

  • Oxycontin (Oxycodone)
  • Dilaudid (hydromorphone)
  • Vicodin (hydrocodone or acetaminophen)
  • Fentanyl
  • Morphine
  • Heroin

 

The Causes of Opioid Withdrawals

 

Just as with any other substance, over a period of time, your body becomes more and more immune to its effects. Therefore, you’ll need more of the substance in order to feel a high. This increases your risk at death and is one of the prime reasons for overdose. To put this into picture, the National Institute on Drug Abuse claims that 90 Americans die daily from an opioid overdose.

 

As your tolerance constantly builds, your brain and body come to need opioids. This is due to the fact that the chemicals become apart of your regular functioning. Your body expects to intake the drug on a regular basis and if it doesn’t, your mind comes to only desire the next intake. During withdrawals, it should be expected that your conduct will be an experience out of this normal.

 

Withdrawal symptoms have been comparable to an extreme flu. With this, there are many users out there who don’t even realize they’ve become dependent. In fact, even after the first couple uses of opioids, the body has already begun to miscomprehend the drugs as something normal. When this happens, the dependence slowly builds upon itself – to an extent where the user truly isn’t aware of the dependence they’re creating.

 

This is especially true for those who’re prescribed certain opiates. Often, individuals are overprescribed a particular substance and, inevitably, start taking more than necessary. People who find themselves in this position will build tolerances that cause dependence. According to the National Institute on Drug Abuse, around 24% of people who’re prescribed opioids for chronic pain will end up misusing them.

 

The withdrawal symptoms that will be experienced vary from one individual to the next. Tolerances are built at different rates. Therefore, not everyone has the same dependence. With that, it can be expected that the withdrawal symptoms will, likewise, vary.

 

However, there’s one condition that’s pretty common amongst opioid addicted individuals. This is called acute opiate withdrawal. It is a condition that occurs when the body starts losing that normality it had felt from the opioid drugs. It’s also when the brain experiences a major deficiency of dopamine – a happy hormone opioids trigger.

 

This should be something you need to mentally prepare for. The journey that follows after will be that of replacing the void opioids always filled. And in order to that, your body and mind must be completely taken off the chemical.

 

The Five Most Common Withdrawal Symptoms

 

Typically, when it comes to opioid addiction, individual’s experience five common symptoms. It should be noted that there are many factors which go into these symptoms, but the following are something to be expected;

 

  • Insomnia
  • Agitation and anxiety
  • Excessive sweating
  • Symptoms similar to the flu
  • Depressive/dysphoric state

 

Let’s look into these symptoms a little deeper in order to properly understand them for the benefit of your expectations.

 

Insomnia

 

Being that your body is going through an overwhelming amount of pain during withdrawals, it’s going to be difficult to sleep at night. The withdrawal caused by opioids is traumatizing for the body to experience. Insomnia only worsens these symptoms because it leaves the body continuously feeling worse as the mind lays in bed wide awake.

 

Agitation and Anxiety

 

Being that your brain experiences a lack of dopamine, there’s this constant urge to find an instant kick of the chemical to balance out the mind. Previously, opioids were what brought the brain to this balance. Yet, as you go through withdrawal, you’re going to realize that dopamine won’t come so easily anymore.

 

The agitation and anxiety that follow will be out of a loss of focus as to how to receive dopamine without a substance. What you’ll learn in drug treatment is that there are many ways to find this dopamine within your average day-to-day life. It’s important you focus on these ways.

 

The amount of agitation and anxiety one feels all depends on how big of a dependence you have to opioids. It’s said by professionals that the more one intakes, the harder and longer they will fall during withdrawals.

 

Excessive Sweating

 

Due to the large amount of chemical changes the body will be going through, it’s going to react in a natural sense to the stress it bears. One of these ways is through excessive sweating. Just as with agitation and anxiety, the amount of sweat one experiences has lots to do with the level of their opioid dependence.

 

Excessive sweating can, likewise, cause much of the insomnia experienced at night. Just remember that it’s nothing more than the body trying to find a way to feel normal again. And it will ease off just as the other withdrawal symptoms with time.

 

Symptoms Similar to the Flu

 

Just like excessive sweating, the flu-like symptoms are simply out of the body trying to rebalance to its natural chemicals. The symptoms that can be expected are diarrhea, runny nose, body aches, and puking. This is a primary reaction of the immune system, for most it’s the part of the body that’s most affected by withdrawal.

 

Depressive/Dysphoric State

 

Just as with agitation and suicide, the depressive state of withdrawal is due to a lack of dopamine. Your mood is going to be greatly weighted once the body no longer feels a normal amount of the chemical. Depending on the individual, each will experiences different senses and levels of depression. However, extreme sadness and dissatisfaction should be expected.

 

On top of everything mentioned above, you may also experience the following;

 

  • Pupil dilation
  • Restlessness
  • Goosebumps
  • Increased heart rate/blood pressure

 

Treating Opioid Addiction

 

As mentioned above, the body’s detox of chemicals comes before any kind of therapy. Depending on the individual and their circumstance, the timeframe for withdrawal symptoms vary. Generally speaking, the symptoms mentioned in the section above hold possibility for around twelve to thirty hours after the last intake of the drug.

 

However, in order to truly clean the body out of the chemical, these symptoms should be expected to last for anywhere between 4 to 10 days. There are instances known as “extended release opioid” in which recovering individuals will experience the symptoms for up to 21 days.

 

To further the withdrawal period, there’s also the situation known as post-acute withdrawal symptoms (PAWS). This takes place after the acute symptoms are no longer apparent and can be defined as similar symptoms to those mentioned above, but at minor levels of pain. Depending on the individual and their mentality throughout treatment, these symptoms can last up to months. They mostly include; depression, anxiety, insomnia, fatigue, and mood swings.

 

Being the overall state of the opioid epidemic happening in America, there are numerous treatments being offered to the public. One example is known as medication-assisted withdrawal. This is when a person eases off opioids by taking smaller and smaller doses over a period of time.

 

There are also a few behavioral therapies to look into that focus on treating the mentality of opioid addiction rather than the body.

 

The first is cognitive-behavior therapy. A treatment that centers its focus on the effects opioids have had over the individual. You can expect to explore your thoughts, beliefs, and experiences on the drug and what you desire out of a life without it.  This also includes Intensive Outpatient therapy.  Stonewall Institute Treatment Center provides services for drug and alcohol dependency and co-occurring issues. Our program allows for clients to sustain life responsibilities while providing an intensive treatment environment 3 evenings per week for 10 weeks. Clients in our Drug and Alcohol Treatment program will learn about underlying issues that contribute to substance dependence and obtain the vital skills necessary to sustain long-term sobriety and recovery.

 

The second is contingency management. This is a reward based treatment in which individuals who remain drug-free will receive prizes for their productive behavior.

 

The third is motivational interviewing. Just as the title intends, this is when individuals are interviewed for the sake of discovering what motivations will help them through their recovery. And to discover their true desires in such a major life change.

 

Lastly, there’s family therapy. Depending on your family and friend’s situation in terms of your drug use, you may want to consider this option. It’s meant to inform any loved ones of what the experience of substance abuse is truly like. It’s also meant to build relationships through recovery.

 

If you or anyone you love is interested in an opioid treatment or looking for more information on the topic, Stonewall Institute Treatment Center is glad to help. Please, give us a call today at (602) 535 6468 or email us at info@stonewallinstitute.com.

Drug Treatment in Phoenix, Arizona

Stonewall Institute in Phoenix provides drug treatment for any and all drugs of choice.  If that drug is cocaine, methamphetamine, alcohol, marijuana, opioids or prescription medications, you can find help at Stonewall Institute’s Intensive Outpatient Program.  You know it is time to get help.  At Stonewall Institute, we offer an Intensive Outpatient Rehab Program that utilizes chemical dependency counselors who are trained to help you with compassion and respect.  Read about our program at www.stonewallinstitute.com or call us today at 602-535-6468.