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By: Robert G. Bell

Robert G. BellOpioids have the power to heal and the power to hurt. If prior pain management therapies such as physical therapy and nonopioid pharmacotherapies are not effective, opioid treatment may be warranted under medical supervision.

Opium has always been a part of human history. Fossilized poppy seeds suggest that Neanderthal man may have used the opium poppy over thirty thousand years ago, and the first known written reference to the poppy appears in a Sumerian text dated around 4,000 BC. The poppy flower, known as hul gil, “the plant of joy,” was cultivated in ancient Persia, Egypt, and Mesopotamia. Opium is the extract of the latex resin derived from seedpods of the opium poppy, Papaver somniferum, which is the only species of Papaver to produce opium.

shutterstock_429391798Opioids are drug substances that interact with opioid receptors located in the central and peripheral nervous system to reduce pain. Opioids refer to drug products that are derived naturally from opium (e.g., morphine and codeine) as well as those synthesized (e.g., morphine esters such as heroin; semi-synthetic opioids such as hydrocodone and oxycodone; synthetic opioids such as fentanyl) and endogenous opioid peptides (e.g., endorphins, enkephalins, dynorphins, and endomorphins). Tramadol and tapentadol produce analgesia and act as mild and potent agonists (respectively) of the μ-opioid receptor. Opioids exert their pharmacological actions through mu, delta, and kappa opioid receptors. Once bound, the opioid receptors mediate the psychoactive and somatic effects of opioids.

Opioids have varying analgesic potency, and equianalgesic charts can be used to calculate an equivalent dose between analgesics. Codeine is approximately 1/10 the relative strength of morphine; hydrocodone is equivalent (1); oxycodone is 1.5 stronger; fentanyl is about 50 to 100 times stronger; and carfentanyl is greater than 10,000 times stronger than an equivalent dose of morphine.

Opium Image 2Opioid treatment can start with codeine, tramadol, or tapentadol. If relief is not achieved with these modalities, other opioids such as hydrocodone and oxycodone can be introduced. Morphine, buprenorphrine, and fentanyl are usually reserved for the severest of pain such as terminal cancer. Due to the potential for abuse, addiction, and overdose, opioids should only be used for short durations (1–2 weeks). As discussed in a previous post, pain relievers such as oxycodone and hydrocodone are involved in more overdose deaths than any other opioid type—in 2014, there were 28,647 deaths, which accounted for 61% of all drug overdose deaths. The next blog in this series will discuss the pain associated with addiction and death that can’t be healed or alieved by any medication.

Opioids are just one of the many treatment therapies and options associated with effective pain management; however, opioids are not the only or best option. Their use is part of a step-wise approach to pain management, but too often we appear to skip steps and run right for the Percocet. Patients and medical care providers need to identify and address the root cause of the pain and be aware of the step-wise options that include drug free therapies and non-opioid pharmacotherapies prior to the addition of opioids to your pain management regimen.

As stated in the introduction, opioids have the power to heal and the power to hurt. Our next blog discusses how opioids have the power to hurt through abuse, addiction and overdose. Pain and purple rain.

Robert G. Bell, Ph.D., is president and owner of Drug and Biotechnology Development LLC, a consultancy to the pharmaceutical industry and academia for biological, drug, and device development.