Prince's death this April intensified the spotlight on an already-centerstage public health concern: opioid dependence, abuse, and addiction.
The Centers for Disease Control and Prevention issued a new, no-nonsense set of guidelines for prescribing opioid pain relievers directed at primary care doctors this past March, just one month before Prince's passing, and Hillary Clinton has spoken publicly about including efforts to combat opioid abuse in her presidential platform. The situation is so dire that the trend in overdose deaths has been compared to the HIV/AIDS crisis of the late 1980s and early 1990s.
OxyContin is one of the most name-recognizable prescription painkillers, falling under a whole class of drugs called opioids, also known as opiates. Opiates are usually given to patients to alleviate chronic pain, but are arguably over-prescribed and often with little physician oversight or understanding of the risks, opening the door to abuse. That abuse is getting out of hand, too: nearly 2 million people in the US over the age of 12 have a painkiller use disorder, so it's no wonder why many -- from politicians to government agencies to media to some pharmaceutical companies -- have labeled opioid abuse an epidemic.
Why do opioids and opiates work so well?
It all starts with the poppy, somewhat ironically known as both a symbol of medicinal power and death. As psychiatrist Anna Fels has noted, prescribed uses of the poppy plant (especially opium) and its descendents have been around for millennia -- opiates can refer to "close relatives of opium," like codeine, morphine, and heroin, while opioids include synthetic opiates like OxyContin, Percocet, Vicodin, and Dilaudid. Heroin is the only drug among those that's whole-hog illicit in the United States. That's a particularly odd medical quirk, especially since, when abused, OxyContin and Percocet function very similarly to heroin on brain chemistry.
But why do these drugs feel so damn good?
The human brain is essentially wired to respond to opioids, holding a concentrated collection of mu-opioid receptors ready to make you feel better at a moment's notice. Receptors send and receive messages in the brain, allowing neurons to communicate with one another; opioids send the message, "You are relieving your pain now."
These receptors are present in several areas of the brain, namely the regions that manage perception of pain AND the regions that fire off feel-good sensations. Yup, the latter are the parts of your brain that tell you: "Whoa, you're high, buddy!" Opioid medications don't treat the source of the pain, though, which means they don't target muscular injuries, nerve distress, or bone disease. Instead, opioids funnel straight to the brain, the place where we process what the heck's going on elsewhere in the body, in a sense tricking the brain into not recognizing the source of discomfort. This is important.
But here's another thing that mu-opioid receptors do: control respiration and blood pressure. "Opiates hit many different receptors [in the brain], and different receptors respond in different ways," says psychiatrist Dr. John Tsuang, director of the Dual Diagnosis Treatment Program at Harbor-UCLA Medical Center. Some opioid receptors elicit euphoria by eliminating or dampening pain perception and giving users a baseline high. Triggering the others stops breathing. The nasty, unforgiving aspect of opioids, though, is that the receptors for euphoria develop tolerance, so that high feeling wears off, and the patient (or recreational user) needs more OxyContin than before to chase that initial high.
The ones that trigger breathing, though, don't develop tolerance. Put another way: the brain can demand more when the good feelings go away, but that same opioided brain can't tell itself that it's in danger. This phenomenon is true for any opioid, but the one-two punch of its long half-life and high concentration of oxycodone makes OxyContin particularly unpredictable.
OxyContin upped the ante in the painkiller game
Opioids are some of the oldest drugs still used in the modern age. Fels cites the American Civil War as a key historical example of opium's medicinal value, as well as China and Britain's two Opium Wars as an indicator of the plant's economic allure. The staple crop made way for synthetic pills, she writes, adding, "Beginning in the 19th century, chemists derived ever more potent forms of this class of drugs: morphine, oxycodone, heroin, and codeine, to name just a few."
Today, synthetic opioids retain that time-honored combination of medical import and dollar signs once enjoyed by their plant ancestors. But OxyContin stands out in a crowded economic field, netting $3.1 billion in profits and accounting for 30% of painkiller sales in 2010, even as it endured widespread criticism and massive lawsuits. That market share is pretty incredible, given its newcomer status in a class of drugs more than a century old in America.
OxyContin, which is brand-name oxycodone, first appeared in 1996, manufactured and marketed by Purdue Pharma. The press release announcing the drug's entry into the marketplace ran with the headline "New Hope for Millions of Americans Suffering from Persistent Pain." That sounds... hopeful!
The press release went on to extol OxyContin's revolutionary long-lasting, 12-hour formula. "Dosing with OxyContin Tablets on a regular schedule spares patients from anxious 'clock-watching' when pain must be controlled over long periods." In retrospect, the fact that people were anxiously "clock-watching" for the moment they could take another pain pill should've tipped doctors off to the fact that these drugs might be problematic, but hey, hindsight is 20/20.
On top of that longer half-life, OxyContin is known for its potency.
"OxyContin is a very strong opioid medication," says Dr. Tsuang. "It's one of the more potent opioid medications, and it doesn't have other stuff, like acetaminophen, in it." By contrast, Percocet touts the same active ingredient as OxyContin (oxycodone) but is notably milder, containing acetaminophen as well as a much smaller amount of oxycodone. Says Canada's Centre for Addiction and Mental Health, "Just one OxyContin pill can have the same amount of oxycodone as 16 Percocet pills." OxyContin contains a few inactive ingredients, but a single pill contains 90% oxycodone. It's high-octane stuff, in other words.