As the number of deaths by overdose climbs, the opioid crisis often hits the headlines in Canada. The addictive nature of opioids is a tragedy with many roots and difficult to address with any single treatment. The crisis has become worse with the widespread availability of fentanyl, a drug about 50 to 100 times more potent than morphine. One acute treatment that can save the lives of individuals who might otherwise die from an opioid overdose is naloxone.
Naloxone is not new: in my graduate training in the late 1970s, I studied the effects of morphine and naloxone (and other drugs) on the behaviour and physiology of rats. I explored the temperature effects of these drugs and probably have the world record for the number of temperature measurements I have made in rats.
But at that time we did not know much about how morphine and naloxone affected the body, except that naloxone was able to reverse the effects of morphine and heroin. Morphine has for years been one of the most helpful drugs in a physician’s arsenal because it blocks pain and is helpful in inducing constipation and supressing coughs, in addition to other effects. But its addictive nature has always been a serious liability.
In the intervening years, a lot of research has revealed that morphine works at the cell level on receptors, which neurotransmitters activate naturally. Researchers discovered this by looking at two forms of the morphine molecule that, like your hands, have a “right” and a “left” shape. Only one shape of morphine works on a receptor into which it fits like the appropriate glove: the µ-opioid receptor. This led to the search for the natural molecules that activated these opioid receptors and three main families of neurotransmitters were discovered: endorphins, enkephalins and dynorphins.
Receptors are complex molecules found on the surface of cells; when a drug or neurotransmitter fits into them (like a key in a lock), they change how the cell acts. Morphine is a drug that binds with (fits into) the µ-opioid receptor, like the body’s endorphins doing what they normally do, for example blocking pain, so morphine is called an agonist. Naloxone also fits in the µ-opioid receptor, but prevents it from being activated (like a tooth-pick stuck in a lock) and thus is called an antagonist (an anti-agonist).
When naloxone is administered by itself in a normal person, it has little effect except to render the person more pain-sensitive. It is a great drug because it is strong enough to replace morphine and other opioids at the µ-opioid receptor, blocking their action, but in itself does very little harm. This strong blocking action reverses the effects of an overdose of morphine, heroin or fentanyl.
There are many factors that determine how effective a drug is in the body. Sometimes the ability of the drug to physically get to its receptor is important. Heroin and fentanyl are more potent than morphine; they get into the brain much more easily. How the body breaks down these drugs is also important. Relative to morphine, naloxone breaks down much more quickly, so in the case of an opioid overdose, it may have to be administered multiple times. Naloxone kits are now being given to Emergency Health Services in Nova Scotia, and may be available in pharmacies soon, as CBC reported in early August.
It is clear from this very simplified discussion that our bodies are complex, and the biochemistry of drugs has many differing aspects. But the pharmacology of opioids is only one small part of the complex societal issues that lead people to become addicted to these drugs. Thus the best treatment programs take multiple approaches to help the addict. As Christians we know that ultimately we can be made fully whole only in the new creation through the action of our Lord. On this side of the grave or before his return, addicts need to learn to live with their cravings, which can be long lasting, and we must offer our love, support and hope to those who have to fight this deadly brokenness.
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