Volume 95 Issue 24 | p. 24
Issue Date: June 12, 2017 | Web Date: June 6, 2017

Periodic graphics: The opioid epidemic

Chemical educator and Compound Interest blogger Andy Brunning explains the drugs behind the public health crisis
By Andy Brunning
Department: Science & Technology
Keywords: neuroscience, opioid epidemic, heroin, fentanyl, naloxone, methadone
 

To download a pdf of this article, visit http://cenm.ag/opioidpdf.


References used to create this graphic:

Increases in Drug and Opioid-Involved Overdose Deaths — United States, 2010–2015

Opioid overdose (CDC)

Management of opioid analgesic overdose

Turning the tide or riptide? The changing opioid epidemic


To see more of Brunning’s work, go to compoundchem.com. To see all of C&EN’s Periodic Graphics, visit cenm.ag/periodicgraphics.


 
Chemical & Engineering News
ISSN 0009-2347
Copyright © American Chemical Society
Comments
David Grierson (June 8, 2017 6:17 PM)
Interesting diagram, but to my knowledge heroin is a pro drug of morphine with rapid BBB entry, and that it does not itself turn on the opioid receptors (i.e. Its not an agonist). To be an opioid receptor binding agent (agonist/antagoinist) the phenolic OH group needs to be free (unprotected). Same goes for oxycodone and codeine.

Correct me if I’m wrong (with literature references)

Sincerely,

David Grierson
Professor
Faculty of Pharmaxeutical Sciences
UBC
Vancouver, Canada
Shankar (June 9, 2017 8:12 AM)
That is correct and is a prodrug. But in vivo it would be difficult to judge if it behaves like pro-drug or that Heroin itself is active? The interesting I that when you free these molecules of their shackles to arrive at simpler structures, these are even more active!
Michael Torrice (June 12, 2017 5:35 PM)
Thank you for your comment, David. I'm one of the editors who worked on this graphic.

You are correct: Heroin is a prodrug. Deacetylation of heroin yields morphine, which then binds to opioid receptors.

In a graphic like this, space is limited and so we have to make decisions about what to include and what not to include. The goal of that first sentence in the first box was to set up the idea that when people take opioids, including heroin, they are turning on opioid receptors on their nerve cells, which leads to pain relief and feelings of euphoria. So we didn't have space to go into the prodrug mechanism specific to heroin.

But thank you for pointing out that mechanism. There is a lot of interesting chemistry involving the development of opioids and drugs used to treat the side effects of opioid use.
Paul Comet (June 8, 2017 9:19 PM)
Could it be that social anthropology might be the "cure" for this epidemic? "Being the best you can be" (all the time), implies endless comparison of oneself with others "who are doing better, economically, socially (having more fun/better relationships etc.),& more "toys". Meanwhile one looks at ones own meager achievements & mutters "roll on death"! Maybe our culture based on competitive rights should be better balanced by cooperative social obligations "being the best WE can be" (not communism). Being the most beautiful, the most perfect, the cleverest, the "coolest", the most moral paragon, is terribly hard on our kids & maybe adults also. Those without a good job, drifting relationships are at risk. Opiates are excellent "social pain killers. Value change could be the answer.Unstable nuclear families don't help much either.
Wallace Fu (June 8, 2017 9:52 PM)
Imagine the two lone electron pairs on the dihydrofuran oxygen atom as the mandible of an arthropod, the two acetate groups are the claws and the aminomethyl group the stinger hook; heroin is deadly like a scorpion. So stay away. The antidote naloxone is still a scorpion without the claws. Stay away from that too.
Kurt Levy (June 9, 2017 12:05 AM)
I agree with Wallace Fu 1000%
Istvan Ujvary (June 9, 2017 12:49 AM)
It has become popular to characterize the risks of addiction and overdose by using the vague term "potency". However, the often quoted 100x or 10,000x figures refer to relevan ED50 values originating from pain models using specific tests with mice or rats; Not humans. Few, if any, addiction liability studies have been conducted with fentanyl analogs, the fentanils. Virtually no study addressed the toxicity (such as LD50) of these recently emerged fentanils. Importantly, overdose is not due to the more or less characterized analgesic effect but respiratory depression, which could be fatal if not treated properly (see naloxone above). Antinociceptive potency, as estimated in rodents in vivo or receptor studies in vitro, does not necessarily reflect acute toxicity!
Saganuwan Alhaji Saganuwan (June 9, 2017 5:14 AM)
The solution to opioid epidemic is to ban the drugs across the globe.Addiction, tolerance, Physical and psychological dependence are some of the adverse effects of opioids.The opioid addicts are also vulnerable to prostitution,robbery and other forms of criminal acts.
Shankar (June 9, 2017 8:14 AM)
There is a role for these medications but people abuse it. Banning it is a knee jerk reaction.
James Cunnion (June 9, 2017 8:26 AM)
There are laws that already forbid the manufacture and distribution of many of these opioids. They don't work. Many of these drugs have very legitimate uses for treating pain and are preferred to NSADS. An example is the prescribing guidelines for cancer patients who can receive unrestricted amounts of opioids. There is a significant difference between addicted and dependent.
Tim Mason (June 9, 2017 9:11 AM)
These drugs are useful. Banning them would be like banning gasoline to stop drunk driving. The pain management physicians have programs in place to weed out would be abusers. The program is working.This is done via drug screens, etc. There is no "opioid epidemic" by definition. What the FDA means to say is that prescribing these drugs has reached epidemic like proportions.
As Paul eludes to above: The biggest risk to addiction is YOUTH. One must suffer chronic pain themselves to understand the value of these drugs (fentanyl, morphine). Otherwise, your comment sound like the comment made by an embalmer: "I know what it is like to be dead, I work at a funeral home".
Michael Olah (June 9, 2017 9:20 AM)
While I do believe that drug companies need to be held responsible for flooding the world with more opioids than are needed for valid medical purposes, banning these drugs would likely not have much of an effect. Heroin is illegal after all, and it's still widely available. If we really want to do something about this "epidemic", we need much more money for drug treatment clinics and mental health services (many people turn to drugs because of untreated anxiety, depression, or other mental illnesses). Opioid users also need access to safe needles to stop the spread of HIV and other bloodborne illnesses, and they need ready access to naloxone for when overdoses do occur. The United State's treatment of the drug crisis as if it was a war or a issue of criminal law has only fueled deadly gangs and filled our prisons with otherwise non-violent offenders. The science is clear, we are wasting our dollars on prisons when we should be spending them on clinics.
 (June 9, 2017 12:12 PM)
Heroin is not found in the poppy, it is a derivative of Morphine, so it is not a "natural" opioid. The use of opium and opium type compounds is an age old problem. One of the many reasons the government banned the use of opium around the turn of the twentieth century.

How do you educate people about the dangers of use and abuse? We are still debating it today, see above posts.
Bill (June 9, 2017 12:47 PM)
Why do 'street pushers' go to jail for selling dope, while allopathic doctors (MD's) get paid big bucks, and earn the respect of society? The allopathic doctors and their suppliers paid the tax.
If you haven't done so already, look up the Greek word for sorcery.
Fina Guitart (June 11, 2017 2:07 PM)
Please, could you put the link to download The opioid epidemy? Some times I could'nd find the download option, and it is very useful to use these materials with my students.
Thank you very much.
Adam (June 12, 2017 10:48 PM)
It doesn't make sense to me that to treat a opioid addiction, you prescribe a different opioid with the same high (methadone). Whats stopping the Heroine addicted from abusing the methadone?
Donald Sexton (June 19, 2017 6:52 PM)
Suggest stick with pharma chemistry since still much misinformation & misleading propaganda is evident that fails distinguishing but groups illicit abusers, recreational addicts, pushers, producers, suppliers, & other miscreants with responsible & disciplined people. Such blatant callous disregard has promoted undeserved stigma & worse upon responsible people reliant upon relief without other alternatives for severe injuries & conditions that were caused by others. The undeserved persecution has indulged supposed (often nothing more than fraudulent exploitative corrupt institutions rife with dishonest hypocrites, sociopaths, kleptocrats & worse) medical facilities (Veterans Administration San Diego among others) are indulged to deliberately abuse, neglect, breach therapy agreements, & worse to forsake treatment so wellness deteriorates, injuries exacerbate, & injustice ensues (controlling & reprisal upon a vulnerable person by imposing pain, witholding treatment, & other horrific abuses). More truth to this & media among others must get held accountable by lawsuits when individuals are slandered & harmed. I have been enduring an absurd hell & will take action. Another example of misinformation is in your article; Fentanyl isn't for chronic pain but immediately administered for trauma & alleviate painful procedures. I deserve better than the disparate socio-economic conditions, medican't, & other corruption prevalent across ScAmerika.
Velvet Journigan (August 25, 2017 11:31 AM)
Is there a way to have a higher resolution PDF of this poster? I would like to use this graphic for my CNS class.
Velvet Journigan (August 26, 2017 11:18 AM)
My class is this coming Wednesday, August 30. Please send if available to:
journigan@marshall.edu
Thank you in advance.
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