Since the mid 1800’s scientists have struggled to find effective pain killers that did not create addiction in their patients. Heroin was one of the first synthetic opiates that claimed to be more effective at reducing pain without addiction. Oxycodone is one the most recent compounds to make the same claim. Unfortunately, neither were valid.

Both of these compounds were attempting to separate the pain relieving (analgesic) from the pleasure inducing (euphoric) effects. Through heroin there was an attempt to make a chemical modification to the morphine molecule. Through oxycodone, there was an attempt to use a time release mechanism to make the drug therapeutic over a longer period of time.

This separation is very complicated. The abundance and variety of opioid receptors in the body and their functions make it difficult to separate analgesia from euphoria. There are basically four types (and some sub-types) of opioid receptors in the body. Opiates bind to one of those types (mu) and activates them. This mode of action is known as agonism, and most common opiates are agonists. They bind to a receptor and activate it.

Naloxone is also an opiate, however, it has the opposite effect. It is an antagonist. It occupies an opioid receptor, but it does not activate it. This is why it is useful in overdose situations. It effectively kicks other opiates out of the receptor, and inactivates it while it is bound.

The complicated chemistry and neurobiology of the situation is a big part of the problem, and it is something that we have very little control over. The other part of the problem is much more human.

Chronic pain management is a burden for many people, and the appropriate use of drugs like these can bring some relief. It is, however, a slippery slope to addiction. As Sam Quinones pointed out in his book Dreamland, many addiction cases started out with a prescription. Over time, many patients developed tolerance for opioids and became dependent.

When their options for prescriptions became fewer they would get unused pills from friends and family. Many people used the internet to find mail order options, which gave them a more reliable stream of medication. Even heroin started becoming an option. Unfortunately, opioids don’t leave a lot of room for error, and accidental overdoses started to skyrocket.

The opioid crisis we currently live in, is largely built on three related trends, as pointed out by the Surgeon General’s report. Since 1999, there has been in an increase in prescription opioid deaths. The rate of deaths due to heroin overdoses increase by a factor of 4 since 2010. Finally, the rate of death from synthetic opioids such as fentanyl has tripled since 2013. The Center for Disease Control has compiled statistics on this for the United States where the problem is so large, it led to a decrease in average life expectancy.

Treatment for addiction has been is being addressed globally. France decreased overdose rates by removing barriers for doctors to administer antagonists like buprenorphine. Dual diagnosis facilities have been combining physical and behavioral therapy with drug treatment to address depression and mental health issues that often accompany opioid dependence.

Help is available. The department of Health and Human Services maintains a database of more than 14,000 substance abuse centers in the United States. To keep drugs from being diverted, Google has added drug disposal sites to Google Maps. It is possible to avoid opioid addiction with more informed choices on pain management. Finally, it is possible to overcome opioid addiction with effective substance abuse programs and the support of family and friends.

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