In the U.S. just over 5,000 people died from opioid overdose in 1968 and this had increased to just over 8,400 people by 1990. Fast forward to 2016 and this number had increased dramatically to over 64,000 – approx.. 175 people per day. Drug overdose is now the single most common cause of death for people under 50 years old in the U.S.
Opioids is a class of drugs which includes prescription pain killers and illegal drugs such as heroin. In the 1990’s opioids became actively promoted for the treatment of pain in the belief they were non-addictive and prescriptions reached record numbers. In 2016, twelve states had more painkiller prescriptions than they had people.
We now know these painkillers are addictive and around 25% of people who are prescribed them will end up misusing the drug. This class of drug creates pathological levels of cravings to obtain and use the drug, and once the body has adapted to their presence, stopping using creates extremely unpleasant withdrawal symptoms. Once “hooked” it is extremely difficult to quit, often resulting in the use of illegal sources of the drug. Furthermore, the availability of more powerful, synthetic opioids, such as fentanyl, has significantly contributed to the current epidemic.
Fentanyl is about 50X more potent than heroin making it very dangerous when used recreationally and without controls – 3 mgs (less than a grain of sand) can kill an average sized adult male. Then there’s Carfentanyl, about 5,000X more potent than heroin. These drugs have been widely available on the street and often “cut” into other drugs to increase profit as they’ve been relatively cheap and easily obtained.
In 2016 the R.C.M.P. seized a 1 kg shipment of Carfentanyl coming into Canada in a box labelled “printer accessories”. That one box contained the equivalent of 50 million lethal doses.
Opiates are natural ingredients found in the dried latex of the opium poppy and are primarily morphine and codeine. Opioids have biological effects similar to natural opiates i.e. heroin is similar to morphine but about 3X more potent. Vicodin and Percocets are considered opioids as the have the same biological effect but as neither are natural ingredients from opium they are not considered to be opiates.
All opioid drugs interact with the same receptors in the brain and body – the opioid receptors. When opioid receptors in the brain’s pain pathways are activated, pain signals are blocked from reaching the brain and there is significant pain relief.
Activation of opioid receptors in the digestive system can lead to constipation and nausea.
The deadly effects of opioids are when the opioid drug reacts with, and activates, opioid receptors in the brain stem, which controls breathing. When these receptors are activated breathing is significantly suppressed, and if activated too much the user can suffocate and die.
Naloxone is what’s called an opioid receptor antagonist – a substance that binds itself to the opioid receptor but DOESN’T activate the receptor. In effect it blocks the opioid receptor to being activated by other opioids and also replaces other opioid drug molecules already bound to the receptor.
It is this ability to replace opioids already bound to receptors and prevent further activation of those receptors in the brain stem that helps restore breathing in individuals suffering an opioid overdose, providing the appropriate dose is administered in time.
Furthermore, some of the synthetic opioid drugs are so strong that repeated applications are necessary, and while Naloxone’s effects last for 60 – 90 minutes, the opioid drug may be present for a longer time period leading to another overdose situation. While Naloxone often helps with an overdose situation, it doesn’t treat any underlying addiction issue.
There are also numerous opioid receptors in the brain’s reward circuit and activation of these not only produces an intense feeling of peaceful euphoria but also leads to unusually large bursts of the neurotransmitter dopamine, now considered to be the addiction drug.
Polk, T. (Presenter). (2018). The Opioid Epidemic [Video]. Viewed at The Great Courses Plus (The Teaching Company, 4840 Westfields Blvd, Suite 500, Chantilly, VA 20151): https://www.thegreatcoursesplus.com
William Stokeld, M.A., R.P.
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