Brain & Drugs 

Opiate Epidemic

The narcotics that are considered to have the greatest addiction potential include codeine, methadone, hydromorphone, demerol (meperidine), fentanyl, and morphine. In the US opioid dependence is increasing, affects 5 million people and leads to approximately 17,000 deaths annually. Narcotic drugs have always been associated with addiction; however, narcotic drugs remain the best agents to relieve pain. Pain management is the reason people are most likely to seek medical attention. Opioids bind to opioid receptors on neurons distributed throughout the nervous and immune systems. Four major types of opioid receptors have been identified: mu, kappa and delta. These receptors are the binding sites for several families of endogenous peptides, including enkephalins, dynorphins, and endorphins.

Physicians try to balance their desire to elevate suffering against concerns that the patient in pain just wants a drug prescription. Physicians remain constrained by problems of drug dependence and addiction and are reluctant to prescribe narcotics or prescribe weak, inferior narcotics such as codeine and demerol. Weintstein et al polled 386 physicians in Texas and found that a significant number of physicians had prejudice against the use of opioid analgesics displayed lack of knowledge about pain and its treatment, and had negative views about patients with chronic pain. They suggested that new educational strategies are needed to improve pain treatment in medical practice. [i] In Canada and the US opioid dependence is increasing, affects 5 million people and leads to approximately 17,000 deaths annually.[ii]

The World Health Organization (WHO) suggested a progressive treatment of pain. For mild pain: aspirin, acetaminophen, nonsteroidal anti-inflammatory drugs and adjuvants. For moderate pain: mild opioids. For severe pain: traditional opioids. Physician concerns are justified. Narcotic-dependent people routinely solicit prescriptions from a number of physicians and become good at feigning painful conditions. Every primary care physician will have patients who tend to demand prescriptions for pain relievers and other psychotropic drugs and will become chronic users, unless the physician steadfastly resists their demands and limits prescriptions to short term use.

Prescribed narcotics are always available for sale on the street. Most originate with doctors who are lenient prescribers. Drug traffickers have lists of lenient Doctors who write narcotic prescriptions on demand or for a fee. For example, about two million Americans have admitted taking OxyContin (oxycodone) illegitimately. The US Drug Enforcement Administration reported that it is one of the most abused prescription drugs. Another narcotic, hydrocodone also has a high potential for abuse. Hydrocodone, as a narcotic cough medicine, is one of the favorite drugs sought by recreational users when they visit emergency departments. Both drugs act on the opioid mu receptor which blocks the transmission of pain in the spinal cord. In the USA OxyContin is a $1.5 billion per year prescription drug. A report in the New York times from rural Kentucky ( July 2004) provides a perspective on narcotic drug use: “Ever since prescription painkillers like OxyContin became the drugs of choice among dealers and addicts in Appalachia, the days of small-town pharmacists' dispensing medicines from behind an ordinary counter have become a quaint memory. Now many pharmacies have turned into virtual fortresses. Some have bars over the windows. The most sought-after drugs are stored in vaults. The pharmacists often work behind safety glass, and some have even armed themselves. Surveillance cameras and alarm systems monitor every spot. Dan Smoot, chief detective for Operation Unite, an anti-drug task force said that prescription drugs remained the top problem for police agencies in the mountains. Mr. Smoot recently led the largest drug raid in Kentucky history, arresting over 200 people on charges of buying or selling prescription drugs on the black market.” [iii]

Fentanyl Deaths

Fentanyl has become the most potent narcotic with the greatest danger, causing sudden death. Gatehouse and Nancy reported on the tragic rise in Fentanyl deaths in Canada. They described:" Over the past few months, fentanyl has been making headlines across North America, as police discover more and more of it on the streets, and overdose deaths surge. Authorities in Alberta linked the drug to 120 fatalities in 2014, and 50 more in just the first two months of this year. In British Columbia, it killed almost 80 people in 2014, and was responsible for a quarter of all drug deaths, up from just five percent in 2012. In Ontario, where 625 people died of opioid overdoses in 2013, fentanyl was involved in 133 of those cases and, each year, it now kills twice as many people as heroin. First developed by pharmaceutical trailblazer Paul Janssen in 1959, it was originally used as an anesthetic under the brand name Sublimaze. The slow-release transdermal patches for chronic pain relief were introduced in the mid-1990s. Its dangers have also long been recognized. There have been a number of scholarly studies about all the doctors and nurses, especially anesthesiologists, who have become addicted to it, and notable victims such as Jay Bennett, the late guitarist for Wilco, who died of an accidental fentanyl overdose in 2009 after being prescribed the patch for an old hip injury. And the drug’s illicit analogs—there are at least a dozen variations—have been killing people on the streets since the late 1970s, most infamously under the name “China White.” But the deeper story of the drug and its abuse is even more worrying. Police and health workers now face an unprecedented situation, with a burgeoning street trade in both the legitimate prescription patches and illicitly manufactured fentanyl—often sold in pill form and made to look like OxyContin, a far less powerful narcotic. The drug, also available in liquid and powder form, is increasingly being used to cut cocaine and heroin, dramatically boosting their potency, often with fatal consequences. Indeed, fentanyl seems to turning up almost everywhere you look. And it’s killing both inexperienced newbies and hardened addicts. The illicit fentanyl that’s currently flooding Canadian markets in pill form has more benign nicknames: greenies, green beans and green monsters (all references to its emerald hue). But that doesn’t make it any less deadly. Stamped as OxyContin, the fentanyl has been retailing for as little as $10 a pill—an indication of how cheap it is to manufacture, and how easy it is to obtain the raw material. The big B.C. investigation in March turned up two industrial pill presses that were used to make the 29,000 tablets. Two of the 14 people arrested in associated raids in Alberta and Saskatchewan are “full-patch” members of the Hells Angels. A third man is the president of an affiliated motorcycle gang, the Fallen Saints. Then there’s the other problem: the growing abuse of the legitimate pharmaceutical version of the drug. Prescriptions for high-dose painkillers have skyrocketed over the last 15 years. A study by a group of Ontario researchers, published last fall in Canadian Family Physician, determined that Canadians are now the world’s biggest per capita consumers of legal opioids, with more than 30 million high-dose tablets and patches distributed every year. Such widespread availability of opioids inevitably leads to widespread abuse.

A recent meta-analysis by an American Scientist, published in the journal Pain, found that the average rate of misuse of prescribed painkillers is around 25 per cent and that one in 10 medical users ends up addicted. In recent years, it was OxyContin that was driving that trend, because it could easily be crushed and snorted. But, once governments forced the manufacturer to introduce a tamper-resistant formulation, called OxyNeo, to the Canadian market in early 2012, the preferred drug became fentanyl. Dr. Karen Woodall, a toxicologist with the Ontario Centre of Forensic Sciences in Toronto, regularly testifies as an expert in fentanyl cases. She first noticed the drug in 2005 in the autopsy files that cross her desk. She later traced deaths as far back as 2002, mostly via people overdosing after chewing cut-up bits of patches—a particularly dangerous practice, since there’s no way to predict the quantity of the drug in each piece. “The big problem with fentanyl is that a lot of people who aren’t tolerant to the drug are taking it. And if you’re not tolerant, it’s a lot more likely to cause serious toxicity and even death,” she says. “It severely depresses breathing and the heart rate. Combined with alcohol or other drugs that slow the central nervous system, it becomes even more dangerous. It’s a serious issue, we’re seeing more and more deaths.” [v]

Naloxone, the antidote for opioid overdose, is a competitive mu opioid–receptor antagonist that reverses all signs of opioid intoxication. It is active when the parenteral, intranasal, or pulmonary route of administration is used but has negligible bioavailability after oral administration. The initial dose of naloxone for adults is 0.04 mg; if there is no response, the dose is increased every 2 minutes to a maximum of 15 mg. Reversal of opioid analgesic toxicity after the administration of single doses of naloxone is transient; recurrent respiratory depression is an indication for a continuous infusion.[vi]

[i] Winsetin et al. South Med J 93(5):479-487, 2000. © 2000 South Med Ass’n

[ii] David W Dixon, Glen L Xiong. Opioid Abuse. Medscape May 03, 2017

[iii] Associated Press. Pill Thefts Alter the Look of Rural Drugstores. N.Y. Times July 6, 2004

[iv] Roscoe, M.S, The Drug-Seeking Patient. Undertreated Pain or Underhanded Motives? Clinician Reviews 14(2):51-58, 2004. © 2004 Clinicians Group. Posted 03/29/2004 http://www.medscape.com/viewarticle/470779

[v] Jonathon Gatehouse and Nancy Macdonald. Fentanyl: The king of all opiates, and a killer drug crisis. It’s stronger than heroin and more potent than OxyContin. It’s also cheap, ubiquitous, and incredibly deadly. Inside the rise of fentanyl. Macleans. June 22, 2015

[vi] Boyer EW. Management of Opioid Analgesic Overdose. The New England journal of medicine. 2012;367(2):146-155. doi:10.1056/NEJMra1202561.


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