The Abuse Potential Difference Between Immediate-Acting and Extended-Release Opioids

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Depending upon the injury or condition, physicians routinely prescribe either immediate-acting or extended-release opioids for pain relief. But patients who don’t know the difference between the two will often take these very different medications in the same manner. And that little mistake can have big consequences.

What Is an Immediate-Acting Opioid?

“If we know that pain and suffering can be alleviated and we do nothing about it, we, ourselves, are tormentors.”

~Primo Levi, concentration camp survivor

Immediate-release opioids are prescription painkillers typically dispensed for episodic or “breakthrough” pain. It is persistent pain that can unpredictably flare up and “break through” most round-the-clock opioid medications. Breakthrough pain is identified by:

  • Rapid onset – usually peaking within 3 minutes
  • Short duration – 30-60 minutes
  • High severity
  • Pain-related functional impairment
  • Anxiety
  • Depression
  • Reduced quality of life

Immediate-release opioids are specifically necessary for the treatment of breakthrough pain because they take effect quickly, they last just long enough to get patients through the episode and then wear off, and they are easy to take.

Immediate-release opioids are also called IR, short-acting, or rapid-onset opioids. Because they relieve episodic pain flare-ups, they are also referred to as “rescue medications”.

Conditions That Cause Breakthrough Pain

Breakthrough pain is most-frequently associated with cancer:

  • 96% of cancer patients experience breakthrough pain at least once per month.
  • 71% have an episode at least once per week.
  • 20% suffer several episodes daily.
  • 73% awaken at night at least once a month with breakthrough pain.
  • Based on a 10-point scale – with 10 being the worst pain available – the average patient with breakthrough pain rates it at a 7.4.
  • Over half rate their pain level as an 8 or 9.

Other conditions that linked through breakthrough pain include:

  • Arthritis
  • Back Pain
  • Diabetic Neuropathy
  • Fibromyalgia
  • Shingles

Examples of Immediate-Acting Opioids

  • Codeine (generic, contained in many medications)
  • Fentanyl (Actiq)
  • Hydrocodone (Lortab, Vicodin)
  • Hydromorphone (Dilaudid)
  • Morphine Sulfate (MSIR, Roxanol)
  • Oxycodone (Oxy IR, Percocet, Percodan,Roxicodone, Tylox)
  • Oxymorphone (Numorphan)

What Is an Extended-Release Opioid?

“OxyContin changed the face of addiction in this region. It made addicts out of people who otherwise weren’t. It drove this region crazy.”

~ Dan Smoot, President of the Eastern Kentucky anti-drug organization Operation UNITE

Extended-release opioids are given for the relief of moderate-to-severe pain that requires daily, around-the-clock, long-term treatment. They are typically only prescribed when other pain management options have proven to be inadequate.

Compared to IR painkillers, ER opioids – also referred to as controlled-release or long-acting opioids – typically contain higher doses of medication. And because they deliver the opioid medication over a longer period of time, there is an increased risk of overdose and death.

Examples of Extended-Release Opioids

  • Buprenorphine transdermal patch (Butrans)
  • Fentanyl transdermal patch (Duragesic)
  • Hydromorphone Extended-Release (Exalgo ER)
  • Morphine Controlled-Release Tablet (MS Contin, Oramorph SR)
  • Morphine Controlled-Release Capsule (Kadian)
  • Morphine Extended-Release Capsule (Avinza)
  • Oxycodone Controlled-Release (OxyContin)

Which Is Most Likely to Be Abused – IR or ER Opioids?

“We know that there is persistent abuse, addiction, overdose mortality and risk of NOWS (neonatal opioid withdrawal syndrome) associated with IR opioid products. Today, we have taken an important next step in clarifying and making more prominent the known risks of IR opioid medications.”

~ Dr. Douglas Throckmorton, M.D., Deputy Center Director of Regulatory Programs, Center for Drug Evaluation and Research, US Food and Drug Administration

Between 2011 and 2015, researchers at Washington University in St. Louis conducted a survey of over 8300 people entering a drug rehab for opioid abuse. Their goal was to determine if opioid addicts had a preference to immediate-release or extended-release painkillers.

They concluded that BOTH IR and ER opioids were very often abused by individuals who met the criteria for an opioid use disorder:

  • Lifetime abuse prevalence – ER – 91%, IR – 98.7%
  • Past-month abuse prevalence – ER – 46.1%, IR – 67.4%

But when it came to which formulation opioid addicts prefer to use, the disparity was striking. An overwhelming 66.1% of survey respondents had a preference for IR opioids, compared to just 4% preferring ER formulations.

For comparison purposes, 29.9% had no preference.

Why the Difference?

There were two major reasons self-reported by survey respondents as to why they preferred IR opioids. 73% mentioned the rapid onset and quality of the high experienced. Also, 31.2% indicated that IR medications are easier to divert for misuse than ER opioids.

For example, an IR medication, such as Vicodin, has an onset of action as brief as 10 minutes, reaching peak effect in as little as 30 minutes. On the other hand, an ER opioid like controlled-release OxyContin has an onset of effects at about an hour, and reaches peak effect in around 3 hours.

Recent research published in the December 2013 issue of PAIN reported that:

  • 75% of opioid-dependent individual show a preference for hydrocodone or oxycodone as their abused drug of choice.
  • Oxycodone – found in OxyContin, Percocet, and Percodan – is more popular than hydrocodone – found in Lortab and Vicodin45% to 29%, due to the subjective quality of the high.
  • 9 out of 10 opioid abusers self-report that “mood alteration” is the reason for their preference.
  • 6 out of 10 say pain management is another important factor.
  • Hydrocodone medications often contain acetaminophen, and this may act as a deterrent that influences preference. For example, non-medical misuse of oxycodone dropped significantly when an abuse-deterrent formulation was introduced.

Demographic Differences Opioid Abuse

“Most of what we currently know about…treatment is based on studies that included few or no women at all. Our results show that men and women who are addicted to opioids have very different demographics and health needs, and we need to better reflect this in the treatment options that are available.

~Dr. Monica Bawor, PhD, McMaster University

There are differences in the people who “typically” choose to abuse certain opioids. For example:

Hydrocodone abusers are more likely to:

  • Be female or elderly
  • Be more cautious, avoiding unnecessary risk
  • Obtain their abused opioids from physicians, friends, or family members

On the other hand, oxycodone abusers are more likely to:

  • Be young and male
  • Be tolerant of risk
  • Misuse their opioid medication by crushing it and then either snorting or injecting it
  • Pay DOUBLE the price for their illicit opioids than hydrocodone abusers

Dr. Bawor also says, “We found men and women who are addicted to opioids have very different demographics and health needs, and we need to better reflect this in the treatment options that are available…A rising number of women are seeing treatment for opioid addiction…yet, in many cases, treatment is still geared towards a patient profile that is decades out of date…”

Signs of Opioid Abuse

Generally, the warning signs of opioid painkiller misuse can be divided into two categories – physical and behavioral.

Physical Signs –

  • Noticeable intoxication – euphoria/elation
  • Extreme drowsiness or sedation
  • “Nodding off” or unconsciousness
  • Mental confusion
  • Inability to focus or concentrate
  • Constricted or “pinpoint” pupils
  • Shallow or slowed breathing
  • Extreme constipation

Behavioral signs –

  • Dramatic mood changes
  • Social isolation or withdrawal
  • Loss of interest in hobbies or outside activities
  • Secretive behavior
  • Taking more of a medication than has been prescribed
  • Running out of medication early
  • “Shopping” for prescriptions from multiple doctors
  • Money problems
  • Issues at work or school – poor performance, absenteeism, disciplinary actions

In addition, opioid painkillers are extremely habit-forming, even when taken exactly as prescribed. This means that when a person who is physically dependent on opioids runs out of their medication, they can suffer harshly-unpleasant symptoms of withdrawal. The discomfort experienced is often what drives the person to seek more drugs.

Opioid withdrawal symptoms –

  • Uncontrollable drug cravings
  • Headache
  • Nausea
  • Vomiting
  • Diarrhea
  • Profuse sweating
  • Nonstop yawning
  • Extreme fatigue
  • Heightened anxiety
  • Irritability
  • Depression
  • Insomnia
  • Tremors
  • Muscular spasms
  • Chills
  • Fever
  • Muscle and joint pain
  • Goosebumps – the origin of the term “cold turkey”

Opioid withdrawal is not particularly dangerous, but it is both psychologically and physically painful. Most experts recommend the use of anti-craving medications to ease withdrawal and to help prevent relapse.

Dangers of Opioid Painkiller Addiction

ANY problematic substance use can result in serious consequences to every area of the abuser’s life. But addiction to opioid painkillers has very specific dangers.

  • Cross-addiction – As new guidelines and regulations make it increasingly-difficult to obtain fraudulent prescriptions, many desperately-addicted painkiller abusers switch to heroin, which is both widely available and much cheaper.

In fact, 80% of heroin abusers started out by misusing opioid pain medications.

  • Fatal overdose – All opioids slow down normal breathing, even at therapeutic doses. At abuse levels, respiratory depression can be fatal. This is especially true when opioids are taking other depressants such as alcohol or benzodiazepines. 95% of overdose deaths involve more than one substance.

The Bottom Line about Opioid Pain Medications

“It is clear that not all drug abusers share the same characteristics. The decision to use one drug over another is a complex one, largely attributable to individual differences such as personality, gender, age, and other factors. Prevention and treatment approaches should benefit from this because it may help prescribing physicians determine which drug to prescribe and monitor for abuse.”

~Dr. Theodore Cicero, PhD, Washington University, Department of Psychiatry

These findings clearly demonstrate that there is no single “one-size-fits-all” drug rehab program that will work for 100% of the people, 100% of the time. On the contrary, to be truly effective, opioid rehab must be both individualized and specialized. In other words, any prescribed treatment plan needs to be tailored to the individual after a thorough assessment by a qualified medical professional.

For nearly 40 years, Chapman House has been providing comprehensive treatment services to anyone struggling with an addictive disorder. If you need help, contact Chapman House today.

by Albert Fontenot