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].