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 [email protected].

Alcohol’s Effects on Your Sleep Pattern

Many people hold the notion that alcohol can act as a sedative. Therefore, leading them to the belief that drinking before bed will lead to a better night’s sleep. However, modern science has proven for this to be anything but true.

For one, alcohol is actually a stimulant – to some regards – even though it’s classified as a depressant. If it didn’t wake us up and feel good, millions wouldn’t be going out every Friday night and having their drinks as a means of socializing. Alcohol makes us feel good and it does so in the essence of filling the brain with endorphins. These are the chemicals responsible for us becoming talkative, confident, and less socially ashamed.

These chemicals do eventually wear off and leave us feeling rather sluggish. Ending our drunkenness with a drowsiness. Sometimes, instances appear where an individual has drunk too much to the point of sending themselves into a loss of consciousness. But it should be noted that this is simply the body’s reaction the lack of consumption in terms of blood alcohol levels.

Interestingly, scientific research has led to the conclusion that alcohol, in fact, reduces the amount of time it takes to fall asleep. Yet, it increases the amount of time the brain spends within deep sleep.

To top this off, the second half of the sleep cycle is very much disturbed. Causing abusers to not get as good of a night’s sleep and more susceptible to waking up from minor annoyances. With this data, it’s highly suggested that people with insomnia do not use alcohol as a sedative. Though it may help an insomniac fall asleep quicker, there is a very likely chance one will be awakened before they’ve received a full night’s rest.

Some may be asking the question as to whether alcohol is always bad for sleep. There are instances where – in an example – a glass of wine has sedative qualities that will help an individual fall asleep and stay in sleep for a longer period of time. However, it’s highly noted that the body builds a tolerance to alcohol very quickly. And soon enough, the individual would have to increase the amount of alcohol consumption in order to recreate the same effects. With this, they will not only be doing harm to their body but also great damage to their sleep schedule.

Understanding the Sleep Structure with Alcohol

There’s usually a time in everyone’s school career where they learn about the sleep cycle. To those unaware, the average adult begins their night in a stage called NREM (defined non-rapid eye movement). To put it simply, this is when the brain slowly goes from consciousness to unconsciousness.

Following NREM is REM (defined rapid eye movement). During this period is when a sleeper will experience dreams as they are very deep into unconsciousness. Throughout the night, we experience the sleep cycle around four to five times.

When an individual brings the toxification of alcohol into this they are disturbing much of what the brain is used to. In essence, throwing it off the steady course of the cycle and almost creating an entirely new one.

As mentioned, alcohol will make you fall asleep faster as well as cause you to stay within deeper sleep for a longer period of time. With this knowledge, we can understand that the third and fourth stages of the sleep cycle are heightened to some degree. This also causes the SWS (defined slow wave sleep) to increase during the first half of a night’s sleep. For those unaware, SWS is responsible for refurbishing the body and immune system for the following day.

At this point, it does seem as though alcohol may help an individual find sleep. However, it’s during the second half of one’s sleep cycle that a person will experience the disturbance caused by inebriation. REM is greatly reduced during this time, therefore, leaving the user in a very fragile state of mind before a full refreshment of the body is complete.

How Alcohol Affects Everyone’s Sleep Differently

People are likely to have a versatile amount of experiences while attempting to sleep with alcohol in their system. For alcoholics, these experiences may happen more frequently than to that of a non-alcoholic having their fun with a night of drinking. And vice versa.

Being that alcohol also affects us all differently, the number of possibilities in which an individual sleeps – or wakes up – to remain inconsistent.

  1. Waking Up Too EarlyAs mentioned, the second half of the sleep cycle is very much disturbed by alcohol flowing through the blood. Being this, people will often find themselves waking up in the early morning – before their intended wake up time – and unable to fall back asleep. This is commonly known as the rebound effect.
  2. Combining Pills with AlcoholPreferably, we’re going to quickly discuss sleeping pills as many believe it’s a way to counteract any disturbance brought on by alcohol. Though some may find themselves getting full night’s rest – or even more – there is much danger in sleeping pills combined with alcohol. For one, the body is not receiving proper refurbishing as it would in a healthy body. But also, there are chances of accidents that could lead to fatal situations.
  3. Night SweatsAlcohol has the ability to open up blood vessels which, in essence, heat up the body to temperatures all too warm. With this, individuals will have the tendency to sweat throughout the night.
  4. Increased SnoringPeople who are affected by snoring are likely to worsen their symptoms. Being that alcohol relaxes the muscles in the throat and airway. If you’re not affected by snoring, there’s still the chance of gaining these symptoms through alcohol.
  5. Increased UrinationThis one may be obvious, but the more alcohol an individual is going to consume, the more they’re going have to use the bathroom. With this, it can be assumed that a night’s sleep will often be disturbed by the constant necessity of urination.
  6. Increased Chance of SleepwalkingBeing that alcohol increases our SWS, there are likely chances of people suffering from somnambulism increasing their suffering through drinking. The occurrence of sleepwalking happens more frequently in the SWS. Therefore, with alcohol only heightening the condition, people may find themselves in the position of sleepwalking more frequently.

 

If you or anyone you love is looking for alcohol abuse treatment or desire more information on how alcohol affects a person’s sleep patterns, please, give us a call at 602-535-6468 or email us at [email protected].

How to Recognize a Heroin Addiction

A recent epidemic has been escalating in the United States involving many young teenagers and adults. For some time, heroin seemed to only be a problem revolving around lower class neighborhoods. However, in recent years, we’ve seen it shift to middle and upper-class areas.

Every day, we are seeing heroin creep into the lives of our families and friends. The problem isn’t just with teenagers and young adults. Men and women with children are just as susceptible to becoming addicted.

And with this escalation in opiate use, it’s important we make ourselves aware of what addiction looks like before it overcomes our loved ones. With the right knowledge, you might be able to stop an addiction before it’s too late.

The Birth of the Epidemic

Though opiate addiction isn’t a new epidemic, there are some ideas to how all this addiction grew in recent years. The United States is known to prescribe millions of medications annually to help with a variety of pains. But there’s one little pill that has caused more trouble than help.

OxyContin hit the market in the early 2000s and was labeled as the perfect pain medication. Before long, people were realizing how highly addictive the substance is. Besides OxyContin, a number of other opiate-based pain medication was being released to the public.

  • Lortab
  • Percocet
  • Vicodin
  • Hydrocodone

With the recent heroin epidemic, we are noticing that many of the individual’s addicted started using these sorts of substances.

Usually, an individual addicted to the above-mentioned drugs will search for something more powerful in order to get the feelings of opiate euphoria again. Either that or they can no longer obtain a prescription medication and turn to the streets for their fix.

The Signs of Heroin Addiction

In places like Arizona, there’s been not only a noticeable rise in those becoming addicted but also a threatening escalation in those overdosing. However, this epidemic is popping up all over the country. Specifically, the Northeast United States is getting it the worst.

Another apparent sign of the epidemic is that every year, less and less are being treated in rehabilitation facilities for alcohol and prescription medication. Rather, we are noticing an increase in those needing treatment for heroin addiction.

These statistics gives us a peek into what is happening with the drug epidemic in the United States. More and more seem to be jumping straight to heroin, especially in the younger generations. The concern lies in these young people’s education on not only the fatality of such a substance, but it’s highly addictive nature.

The clues to whether a loved one is using or not are fairly straightforward. If you’re curious as to whether your loved one is using heroin, answer the following questions.

  • Did he/she undergo a sudden and drastic change in behavior that’s led him/her to seem withdrawn from society and/or family and friends?
  • Has he/she spent more time alone recently rather than going out?
  • Does he/she avoid seeking out new crowds to hang out with?
  • Has there been a sudden loss of weight and/or appetite in him/her?

There’s also the question of whether marks are appearing on their skin (preferably, in places where veins are easily accessible). However, it cannot be forgotten that heroin can be snorted and smoked.

If you have concern over a loved one and would like more information on heroin addiction, Stonewall Institute Treatment Center is always here to answer your questions. If you are led to believe that a loved one is using and are seeking out help, please give us a call at 602-535-6468 or email us at [email protected].

Best Drug Rehab Arizona

Stonewall Institute is the best drug rehab in Arizona.  We offer treatment for any and all issues that arise from abuse of drugs and/or alcohol.  Our well-qualified drug and alcohol counselors work with the client to address individual needs.  We offer the intimacy of small groups in an upscale environment.  We accept major insurance plans and also provider financial hardship payment plans.  Find out about our Intensive Outpatient Program by calling us today at 602-535-6468 or check out our website at www.stonewallinstitute.com.