Common Opioid and Morphine Derivatives: Effects and Community Impact

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When considering drugs that depress the nervous system, or “downers”, substances like alcohol and heroin might come to mind; for some, the age-old stereotype of an intravenous heroin user might complete the mental image. However, due to the availability of prescription opioid analgesics, thoughts of “downers” might currently bring prescription drugs to mind, rather than heroin.

A Global Crisis

Since the 1970s, deaths related to opioid analgesics have been on the rise, resulting a national crisis throughout the United States, Canada, and globally [1, 2].

In fact, various states and provinces have made reference to an epidemic sweeping through their communities, with the Centers for Disease Control and Prevention (CDC) first categorizing deaths related to opioid prescription drugs as an epidemic in 2012 [2,3].

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More recently, in 2014 the CDC estimated that approximately 19,000 deaths in the United States were related to prescription opioid overdose [4]. In Canada, in 2015, several provinces reported more than double the amount of overdoses of the year prior [5].

This article is intended to introduce commonly abused prescription analgesics, with the term opioid being used to encompass both opioid and morphine-derivatives, exploring the short- and long-term effects, and finally, explore come of the strategies communities are using to mitigate some of the potentially deadly effects. Heroin will not be discussed.

Common Misused Opioid Analgesics

Due to their pain-relieving properties, opioid analgesics are commonly used to manage acute and chronic pain, with a variety of options for prescription. The following are examples of commonly misused or abused opioid analgesics [6]:

  • Morphine (MSIR, Roxanol®, MS Contin®, Kadian®, Avniza®)
  • Hydromorphone (Dilaudid®)
  • Methadone (Dolophine®, Methodose®)
  • Oxycodone (Roxicodone®, OxyIR®, OxyContin®
  • Oxymorphone (Opana®, Opana ER®)
  • Fentanyl (Sublimaze®, Duragesic®, Actiq®, Fentora®)

Group of three medicine bottles filled with various pillsOf course, whether these substances are prescribed in the form of immediate, controlled, or extended release matters [6]. For instance, controlled release oxycodone comes in the form of OxyContin®, while immediate release might come in the form of Roxicodone® [6].

Of note, these derivatives are not of equal strength to one another and vary in terms of potency, while the route of administration impacts the onset, duration, and dosing of each opioid analgesic [6].

Several equianalgesic tables exist comparing the approximate potency of each, and sources agree that, for instance, when considering 10 mg of intravenous morphine, the equivalent dose of fentanyl is estimated to be 0.1 mg, approximately a hundred times the potency of morphine [6].

As you can see, the differences in potency can be extreme, with high potential for overdose. For instance, an alarming trend has seen fentanyl packaged in OxyContin® casings, resulting in un-intentional overdoses.

Opioid Analgesic Combinations

Furthermore, combination opioid analgesics exist encompassing hydrocodone, oxycodone, and codeine combinations with differing levels of opioid, aspirin, ibuprofen, and acetaminophen content, the following is a list of combinations and brand names [6]:

  • Hydrocodone combinations include Lortab®, Lorcet®, Maxidone®, Norco®, Vicodin®, Xodol®, Zydone®, Ibudone®, Reprexain®, and Vicoprofen®.
  • Oxycodone combination brands include Percocet®, Roxicet®, Roxilox®, Tylox®, Percodan®, and Roxipirin®.
  • Combination codeine includes Tylenol® from No.1 to No.4, Aspirin with codeine and Empirin® with Codeine No.3 and No.4.

The Side Effects

Despite their pain-relieving properties, a variety of short and long term effects result from opioid use; with potentially deadly side effects, some of the risks outweigh potential benefits, making opioid analgesics potentially deadly when abused.

Female having terrible headache taking painkillersFor instance, the opioid AH-7921 was synthesized in the 1970s for medical purposes, however, its potential use as a medical analgesic was abandoned as a result of the high risks associated with its use [7]. Opioid analgesics function by binding to specific receptors throughout the body to modulate pain perception, side effects including drowsiness, confusion, nausea and constipation [8].

Constipation is reported to be one of the most common side effects of opioid use and significantly decreases individual quality of life, due to the extreme levels of pain reported [8]. If too much of an opioid is taken, the person will experience difficulty breathing and maybe death, as a result of an opioid’s function as a respiratory depressant.

Regular opioid use quickly results in physical and psychological dependency, with both extreme physical and psychological withdrawal symptoms when one stops taking the drug. Symptoms of withdrawal include nausea, flu-like symptoms, anxiety, hot/cold flashes, vomiting, diarrhea, dilated pupils, muscle aches, crawling skin, to name a few.

Deterring Abuse

Some abuse-deterrent formulations have slowed down the abuse of some prescription opioids, however, the trends associated with these formulations made it clear that decreasing access will not decrease use.

Specifically, considering the abuse-deterrent forms of OxyContin® – an outer coating that makes the pill difficult to crush – the decrease in OxyContin® abuse appears correlated with an increase in the use of narcotic analgesics, like heroin, with individuals citing that heroin is easier to obtain and cheaper to use [9].

In other words, abuse-deterrent formulations decreased OxyContin® abuse, but there have been increased levels of residual abuse, making the conclusion that decreasing supply will not end the opioid abuse epidemic [9].
More radical harm reduction strategies have taken flight throughout Canada and the United States, in an effort to reduce the amount of unintentional overdoses resulting from opioid use [10]. Naloxone is a prescription medication without potential for abuse, which is used to reverse opioid induced respiratory depression [10].

In other words, Naloxone (sold under brand name Narcan®) has been found to be effective in reversing the effects of an opioid overdose. Since June 2014, approximately 644 programs have been established throughout the United States with the purpose of community education and Naloxone distribution [10].

Negative Effects of Alcohol Abuse on DiabetesBy June 2015, approximately 32 states passed legislation to allow prescriptions to be provided for care-givers of individuals at risk for accidental opioid overdose [10] Interestingly, Rhode Island implemented opioid specific harm reduction strategies that included utilizing a variety of naloxone interventions to help mitigate overdose risks; such as providing police with Naloxone kits [10].

In 2014, unlike neighbouring states which saw significant increases in opioid related overdose, Rhode Island reported experiencing only 7 more deaths than the previous year [10]. In Canada, a review of Naloxone’s prescription status has been proposed to address the increasing number of overdoses in Canada, while several provinces already provide take home Naloxone kits to individuals at risk for opioid overdose [5].

Due to the enormous variety of opioids available to consumers, it is important to be informed on the potential for harm. Consumers, family members and communities should inform themselves on the opioids being abused within their communities and begin conversations around preventative measures, treatment options, and available community resources.

Because harm reduction strategies utilizing Naloxone have the potential to reduce the deaths related to opioid abuse, it is potentially lifesaving to be aware of state regulations regarding naloxone and any other harm reduction strategies available.

While more research needs to be completed on the topic, gaining awareness of community services available to provide support around addiction and mental health is an important first step for family members and those battling opioid dependency.

Community Discussion – Share your thoughts here!

What steps should be taken in the addiction recovery community to bring awareness to the growing crisis of opioid abuse?


References:

[1] Cicero, T. J., & Ellis, M. S. (2015). Abuse-deterrent formulations and the prescription opioid abuse epidemic in the United States: lessons learned from OxyContin. JAMA psychiatry, 72(5), 424-430. doi: 10.1001/jamapsychiatry.2014.3043
[2] Doyon, S., Aks, S. E., & Schaeffer, S. (2014). Expanding access to naloxone in the United States. Clinical Toxicology, 52(10), 989-992. doi: 10.1007/s13181-014-04321-1
[3] Centers for Disease Control and Prevention (2012). CDC grand rounds: prescription drug overdoses-a US epidemic. MMWR. Morbidity and mortality weekly report, 61(1), 10.
[4] Centers for Disease Control and Prevention (2014). Vital signs: opioid painkiller prescribing. July 2014 (http://www.cdc.gov/vital/signs/opiod-precribing).
[5] Alberta Health Services. (2016). Alberta’s fentanyl response. Retrieved from www.health.alberta.ca/health-info/AMH-Naloxone-Take-home.html
[6] Department of Pharmacy Services and the Pain Management Service. (2011). Medical University of South Carolina: Opioid analgesic comparison chart. Retrieved from MUSC website: http://academicdepartments.musc.edu/pharmacy_services/medusepol/pdf/OpioidAnalgesicConversionChart.pdf
[7] Coppola, M., & Mondola, R. (2015). AH-7921: A new synthetic opioid of abuse. Drug & Alcohol Review, 34(1), 109-110. doi:10.1111/dar.12216
[8] Anantharamu, T., Sharma, S., Kumar Gupta, A., Dahiya, N., Singh Brashier, D. B., & Kumar Sharma, A. (2015). Naloxegol: First oral peripherally acting mu opioid receptor antagonists for opioid-induced constipation. Journal of Pharmacology & Pharmacotherapeutics, 6(3), 188-192. doi:10.4103/0976-500X.162015
[9] Cicero, T. J., Ellis, M. S., & Surratt, H. L. (2012). Effect of abuse-deterrent formulation of OxyContin. New England Journal of Medicine, 367(2), 187-189.
[10] Green, T. C., Dauria, E. F., Bratberg, J., Davis, C. S., & Walley, A. Y. (2015). Orienting patients to greater opioid safety: models of community pharmacy-based naloxone. Harm reduction journal, 12(1), 1-9. doi: 10.1186/s12954-015-0058-x
[11] Health Canada. (2016). Health Canada statement on change in federal prescription status of naloxone. Retrieved from Canada News Centre website: http://news.gc.ca/web/article-en.do?nid=1027679


About the Author:

Gabrielle CebuliakGabrielle Cebuliak is currently undertaking her Master of Arts in Counselling Psychology from Yorkville University in New Brunswick, Canada. She previously completed a B.A. in Psychology, which provided her the foundation to pursue her Master’s degree. She has been working in the field of mental health and addiction for 7 years.


The opinions and views of our guest contributors are shared to provide a broad perspective of addictions. These are not necessarily the views of Addiction Hope, but an effort to offer discussion of various issues by different concerned individuals.

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Last Updated & Reviewed By: Jacquelyn Ekern, MS, LPC on March 14, 2016
Published on AddictionHope.com

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Baxter Ekern is the Vice President of Ekern Enterprises, Inc. He contributed and helped write a major portion of Addiction Hope and is responsible for the operations of the website.