05/11/21

In Search of Functional Heroin Use

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In the midst of the so-called “opioid epidemic,” there are a couple of notable examples of individuals who “came out” as recreational heroin users. Both insisted personal relief that they could now live honestly after their admission. And both emphasized that their drug-use was not a problem. One individual is an author and artist, the other person is a tenured neuroscientist and professor of psychology. Both say they practice functional heroin use.

M. L. Lanzillotta is a twenty-something author and artist who first identified herself as a functional heroin user in, “I Chose Functional Heroin Use.” She said that abstinence from heroin didn’t work for her. She didn’t connect with 12 Step groups, saying that she argued with her sponsor and was “too scientifically-minded to believe in a Higher Power.” Maintenance drugs like methadone and buprenorphine didn’t work for her. She then realized she would be happier and healthier if she used, so she stopped trying to force herself to be sober.

That’s why, at age 19 and after more than a year of trying to quit, I stopped trying to force myself to be sober. Instead, I decided to focus on staying as healthy and stable as possible whilst continuing to inject heroin. I’m now 20. So far my plan has worked. People may choose to dismiss my story because of my age, but most drug use, of any kind, is non-problematic. In my case, I don’t just use heroin for fun. It serves a purpose.

She felt free when using. It made her tired in a cheerful way, and took away worry. In hindsight, she sees that she was physically dependent after two months. “And if I hadn’t used on a daily basis for that initial period, I might not’ve gotten stuck.” Initially she smoked heroin and found it protected her from toxic “friends” and other problems. But she also stopped having meltdowns and no longer wanted to die.

Lanzillotta said you can’t let heroin become your wife, life and everything. “Letting your life revolve around any one thing isn’t healthy.” She admitted she is dependent on diacetylmorphine, but doesn’t let it run her life. She doesn’t recommend unprescribed opioid use to anyone, but she’s learned to live with using heroin in a way that makes sense to her.

Nineteen months later, on December 28, 2020, she wrote, “What It’s Like to Be ‘Out’ as a Person Who Uses Heroin.” She wrote about her heroin use because she figured being totally honest about her drug use might help other functional addicts. In defying the stereotypes by working for her drug money and telling the truth, she hoped to make it harder for others to shun or mock her. “I wanted to be living proof that drug users can be good, caring, moral, responsible people.” Her vlogs on YouTube about her heroin use slowly garnered a few hundred views.

The worst thing that happened in connection with my being open about my drug use in my general life was in a work situation, when an older man in a position of power harassed me, exploited me and ultimately sexually assaulted me. He used the offer of giving me drugs (fake drugs, it turned out) to manipulate me, and demeaned me as a “junkie,” among other things. I am certain that knowing I was a drug user made him feel empowered to do those things to me. When I tried to tell HR about what had happened, they refused to believe me—because, I’m sure, I was a known, “out” drug user.

She has roughly ten or 12 YouTube videos on drug use, like “Why I Believe All Drugs Should Be Legal and Regulated, Part 1,” where she said: Opioids aren’t the problem! … prohibition is!” Or “Drugs Don’t Make Celebrities Racist/Sexist/Etc.,” where she said drugs don’t make you a bad person. Interestingly, in “Drug Use Isn’t Inherently Problematic,” she commented that she wasn’t using heroin right then, but may return to using it. Something seems to have changed with her since stating, “Opioids made me truly happy for the first time in my life,” in “I Chose Functional Heroin Use.” I wonder if it had started to become her wife, life and everything.

The Pursuit of Happiness?

Carl Hart is a professor of Psychology at Columbia University. His general area of research is in the behavioral and neuropharmacological effects of psychoactive drugs in humans. Currently his lab is trying to understand factors that mediate drug self-administration and then develop effective treatment methods from that knowledge. His recently published book, Drug Use for Grown Ups, hoped to present a more realistic image of the typical drug user as “a responsible professional who happens to use drugs in his pursuit of happiness.”

In an article for The Guardian, he said he can now live more honestly. “I can look in the mirror. My children can have an example of what courage looks like in real time, not in history.” He admitted he could catch some flack from his employers at Columbia. But “such is life.” He thought the evidence and his public record in the book would exonerate him. He thinks the harm that drugs do has been wildly overstated. In the Prologue to Drug Use for Grown Ups, he said:

I am an unapologetic drug user. I take drugs as part of my pursuit of happiness, and they work. I am a happier and better person because of them. I am also a scientist and a professor of psychology specializing in neuroscience at Columbia University, known for my work on drug abuse and addiction.  It has taken me more than two decades to come out of the closet about my personal drug use. Simply put, I have been a coward.

Hart then cited the philosopher John Locke, who once noted that pursuing happiness was “the foundation of liberty.” He said this idea was at the core of the Declaration of Independence, which asserts that we are endowed with certain unalienable rights, including “Life, Liberty and the pursuit of Happiness.” As an aside, the Declaration of Independence actually reads, “We hold these truths to be self-evident, that all men are created equal, that they are endowed by their Creator with certain unalienable Rights, that among these are Life, Liberty and the pursuit of Happiness.”

For Hart, the freedom to use drugs is a civil liberty issue. He thought the use of drugs in the pursuit of happiness was an act the government was obliged to safeguard. He believes he has the right to take drugs, which he contends is not harmful if done responsibly. Bizarrely, he speculated that the government could develop a competency requirement in order to legally take certain drugs. “You may have to take a test or an exam in order to get the license for permission to purchase individual drugs such as heroin, MDMA, cocaine.”

But Locke did not say exactly what Hart says he did. Locke did not equate happiness with pleasure or the satisfaction of desire. He distinguished between “imaginary happiness” and “true happiness” and thought the pursuit of real, true happiness was the foundation of human liberty. On page 348 of Essay concerning Human Understanding, Lock said:

As therefore the highest perfection of intellectual nature lies in a careful and constant pursuit of true and solid happiness; so the care of ourselves, that we mistake not imaginary for real happiness, is the necessary foundation of our liberty. The stronger ties we have to an unalterable pursuit of happiness in general, which is our greatest good, and which, as such, our desires always follow, the more are we free from any necessary determination of our will to any particular action. . . Therefore, till we are as much informed upon this inquiry as the weight of the matter, and the nature of the case demands, we are, by necessity of preferring and pursuing true happiness as our greatest good, obliged to suspend the satisfaction of our desires in particular cases.

The “pursuit of happiness” envisaged by John Locke and Thomas Jefferson was not merely the pursuit of pleasure, property or self-interest. It is the freedom to be able to make decisions that result in the best life possible for a person, which includes intellectual and moral effort. Happiness is the foundation of liberty when it enables us to use our reason to make decisions that are in our long-term best-interest, as opposed to simply afford us immediate gratification. So, we are able to abstain from drinking a glass of wine, or decide to help a friend when we’d rather not. “As such, the pursuit of happiness is the foundation of morality and civilization.”

Hart seems to me to have gone too far in his assertion that the government was obliged to safeguard the use of drugs for its citizens as they pursue life, liberty and happiness. Where should you set the limit with permitting the so-called functional, recreational use of heroin? According to Addiction Center, an estimated 494,000 Americans over the age of 12 are regular heroin users and about 25% of those individuals are projected to become addicted to heroin. I seriously doubt whether either he or M. L. Lanzillotta will be able to sustain functional, regular heroin use. Might they be confusing imaginary happiness for true happiness as they attempt it?

04/14/17

An Opioid Shell Game

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Heroin sales and overdoses get a significant mount of attention, but we need to also remember that since 2002, the number of deaths related to controlled prescription drugs (CPD) have outpaced those for cocaine and heroin COMBINED. And the number of individuals who report current use of CPDs is more than those reporting use of cocaine, heroin, methamphetamine, MDMD and PCP (phencyclidine) combined. Each day, 129 individuals die from a drug overdose in the U.S. And yes, five of the seven most prescribed CPDs are opioids. The other two are amphetamine (i.e., Adderall) and methylphenidate (i.e., Ritalin and Concerta).

This information was taken from a yearly statistical summary published by the DEA called the National Drug Threat Assessment (NDTA). The 2016 NDTA Summary covers a wide range of data and classes of drugs. There’s even information on the various drug cartels operating in the U.S. This article will focus on CPDs.

The first figure (Figure 26) gives a comparison of the drug poisoning deaths for prescription drugs, cocaine and heroin from 2007 to 2014. Then Figure 29 shows the top five CPDs distributed nationwide in the BILLIONS of dosage units. Far and away from all the other CPDs, hydrocodone and oxycodone are the most prescribed drugs in the U.S. Both of these figures were taken from the 2016 NDTA Summary.

Not surprisingly, the number of admissions to publically funded treatment facilities for non-heroin opiate/synthetic abuse was 24% higher in 2013 than in 2008. The number of admissions has declined since 2011, but that has been offset by an increase in heroin use between 2011 and 2013.

Recently there has been an increase in the abuse of stimulant medications, specifically amphetamine. Between 2006 and 2011 the nonmedical use of Adderall increased by 67%.  Emergency department visits related to Adderall almost tripled between 2005 and 2010. Misuse of ADHD medications as a class resulted in a 76% increase in poison control interventions from 2005 to 2010.

Young adults 18-25 years old represent the majority of the increase in Emergency Department visits, despite children comprising the largest subset of ADHD diagnoses. Many high school and college age students display limited knowledge of either the side effects or the addictive nature of Adderall. This coincides with the popular reputation of the drug on college campuses as a study-aid to improve concentration, and not something harmful or addictive. This contributes to the increased rate of non-medical use among adults.

Looking at concerns with prescription drug use and misuse from another perspective, a report by Quest Diagnostics suggested many Americans are misusing their prescription drugs. In their 2016 Prescription Drug Monitoring Report, Quest Diagnostics found that 54% of patient specimens showed signs of prescription drug misuse. For the purposes of their analysis, a consistent result was when a patient was taking a prescribed drug appropriately. An inconsistent result meant the patient was either not taking their prescribed drug, was taking drugs in addition to those that were prescribed, or was taking drugs that hadn’t been prescribed to them. These three combined causes of “inconsistent test results” indicated potential drug misuse in the Quest report.

About 45% of the inconsistent specimens showed evidence of patients taking drugs in addition to what was prescribed to them, “suggesting the potential for dangerous drug combinations in a sizeable number of patients.” This 2015 finding was considerably higher than other years. STAT News quoted Quest’s medical affairs director as saying, ““The discovery that a growing percentage of people are combining drugs without their physician’s knowledge is deeply troubling, given the dangers.” Of particular concern is the combination of opioids and sedatives, which can lead to respiratory depression, coma and death. The following graphic was taken from the Quest Diagnostics report.

Quest also examined the drug groups associated with the highest number of inconsistencies, by age groups. Unfortunately, given their composite sense of “inconsistent test results,” it is not clear what caused the top inconsistent drug classes. For example, we can speculate that in the under age 10 category, the top two drug inconsistent classes (amphetamine and methylphenidate) were likely due to no drug found, meaning those children were prescribed, but not taking their ADHD medications. The same can be said for the various places that “marijuana metabolite” appeared. However, the inconsistent classes for benzodiazepines, opiates and oxycodone are not distinguished by cause. So while benzodiazepines are noted as the top inconsistent drug class for every age group over 25, it is not clear if that meant they were taken in addition to what was prescribed or not.

One exception to this was with heroin and benzodiazepines. Quest found 1.56% of their tests were positive for heroin. Among adults who tested positive for heroin, 28.6% were also positive for benzodiazepines. Among those who combined these two drugs, 92.3% of the benzodiazepines were not prescribed.

The Fix, an addiction and recovery website, enlisted Peter Grinspoon, the author of Free Refills: A Doctor Confronts His Addiction, to look at the study. Dr. Grinspoon observed that Quest Diagnostics is in the business of doing urine drug testing, so they are interested in promoting drug testing. He went on to say:

Drug tests simply aren’t that accurate. They’re subject to human and lab error, and are rife with both false positives and false negatives. Savvy drug users can outsmart these tests. Any drug testing needs to be interpreted in the context of who is using the drug and why they are using it.

It is true that Quest Diagnostics makes money by increasing the amount of urine testing it does; that it is interested in promoting and highlighting drug-testing. But this was the fifth Prescription Drug Monitoring Report done by Quest. Additionally, Quest provides testing services to about half of all physicians and hospitals in the U.S. So the claim in the report, that it is “well positioned to identify trends in prescription drug monitoring and misuse” is legitimate.

Further, Dr. Grinspoon’s comments on the inaccuracy of urine testing seem overstated. Yes, there are false positives and negatives; and labs can make mistakes. But he gave the impression these errors happen so often that drug testing was a questionable, unreliable procedure. The FDA, among other sources, considers laboratory testing of urine samples to be the most reliable way to confirm drugs of abuse.

He also seems to assume the testing in the Quest report included drug users given urines as part of their treatment within drug treatment programs, which is not the case. Quest specifically stated that drug rehabilitation clinics and addiction specialists were excluded from the analysis “given the higher rates of testing and potentially higher rates of inconsistency.” There is no reason for a drug user to want to outsmart a urine test done in conjunction with their ongoing medical treatment that I can imagine.

The bottom line is that I think the Quest Prescription Drug Monitoring Report still provides helpful and valuable information on the dangerous practice of combining prescription medications. But prescription drug misuse is just one third of a kind if opioid shell game. Along with heroin and fentanyl, it keeps us trying to guess where the next opioid crisis will be.

02/10/17

Guns and Needles

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Reporting for The Washington Post, Christopher Ingraham gleaned some grim facts from the recent CDC data on drug and opioid deaths in the U.S. Opioid deaths surpassed 30,000 in 2015; an increase of 5,000 from 2014. Deaths from synthetic opioids like fentanyl rose by over 70% from 2014 to 2015. For the first time since the late 1990s, heroin deaths surpassed traditional opioid painkillers like hydrocodone and oxycodone. The grimmest reality is that more people died in 2015 from heroin-related causes than gun violence. “As recently as 2007, gun homicides outnumbered heroin deaths by more than 5 to 1.”

The above linked Washington Post article graphs and discusses CDC data showing the surge in opioid deaths from 8,280 in 1999 to 33,092 in 2015. You will also find graphs of the death rate increases by three classes of opioids. And there is a graph showing the rapid increase in heroin deaths over the last five years or so to 12,989 in 2015, surpassing gun homicide deaths in 2015 by 10 (12,979).

The CDC MMWR—Morbidity and Mortality Weekly Report—indicated that the rate of drug overdose deaths increased in 30 states and DC; and remained stable in 19 others. Opioid death rates increased by 15.6% from 2014 to 2015. The report suggested the increase was most likely driven by illicitly manufactured fentanyl. These increases were also concentrated in eight states. According to another CDC MMWR from August 26, 2016, those states were: Massachusetts, Maine, New Hampshire, Ohio, Florida, Kentucky, Maryland and North Carolina.

During 2014 to 2015 death rates increased overall, as well as for both males and females in the three different classes of opioids. The following chart gives the CDC death rates by class of opioid, year, sex and overall population. The opioid classes are: natural and semi-synthetic opioids (codeine, morphine, hydrocodone, hydromorphone, oxycodone, oxymorphone and buprenorphine), synthetic opioids (meperidine and fentanyl) and heroin. Heroin is a semi-synthetic opioid, but was assessed separately by the CDC. Methadone is a synthetic opioid but was also assessed separately. See the CDC MMWR for data on methadone deaths.  The “rate” in the chart is the death rate per 100,000 people.

Characteristic

Natural and semi-synthetic opioids

2014

2015

% change in rate, 2014 to 2015

No. (rate)

No. (rate)

Overall

12,159 (3.8)

12,727 (3.9)

2.6%

Sex

Male

6,732 (4.2)

7,117 (4.4)

4.8%

Female

5,427 (3.3)

5,610 (3.4)

3.0%

Characteristic

Synthetic opioids other than methadone

2014

2015

% change in rate, 2014 to 2015

No. (rate)

No. (rate)

Overall

5,544 (1.8)

9,580 (3.1)

72.2%

Sex

Male

3,465 (2.2)

6,560 (4.2)

90.9%

Female

2,079 (1.3)

3,020 (1.9)

46.2%

Characteristic

Heroin

2014

2015

% change in rate, 2014 to 2015

No. (rate)

No. (rate)

Overall

10,574 (3.4)

12,989 (4.1)

20.6%

Sex

Male

8,160 (5.2)

9,881 (6.3)

21.2%

Female

2,414 (1.6)

3,108 (2.0)

25%

From 2014 to 2015, the combined opioid death rates increased by 15.6%. The most radical increases were with synthetic opioids, overwhelmingly from fentanyl. The overall increase was 72.2%, driven primarily by a 90.9% increase in male deaths. Overall heroin deaths in 2015 were higher than the number of deaths from natural and semi-synthetic opioids in 2015. Death rates from natural and semi-synthetic opioids increased as well, but at a more leisurely rate.

Another Washington Post article by Christopher Ingraham, “Where opiates killed the most people in 2015,” again used CDC data to compose a series of maps. These maps illustrated which states in 2016 had the most opioid deaths overall and also by classes of opioids: heroin, synthetic and natural (natural and semi-synthetic). Nationally, there were roughly 10.4 opioid overdose deaths per 100,000 people. But New England, and the Ohio/Kentucky/West Virginia had the highest rates. Ohio, West Virginia and Connecticut had the highest death rates from heroin overdoses, between 20 and 36.

Synthetic opioid deaths were primarily located along the East Coast. The national death rate from synthetic opioids is 3.1 per 100,000. In Rhode Island it’s 13.2; in Massachusetts it’s 14.4; and in New Hampshire it’s 24.1. Ohio and West Virginia weren’t far behind. Deaths from natural and semi-synthetic opioids were concentrated in West Virginia and Utah. There is also a table of raw data by state in the article.  The following map, taken from the article, is for overall opioid deaths in the U.S. for 2015.

The following chart, taken from the 2016 National Drug Threat Assessment Summary, combines CDC data for deaths by drug poisoning, homicide, firearms and motor vehicle crashes between 1999 and 2014. You can clearly see how overdose deaths have risen, outpacing the other causes of death. The 2016 NDTA Summary said drug overdose deaths are at the highest level ever recorded. “In 2014, approximately 129 people died every day as a result of drug poisoning.” Since 2010, there has been a 248% increase in heroin overdose deaths.

The U.S. has seen a dramatic increase in the availability of heroin in the last ten years, allowing the heroin threat to expand exponentially.  The increases with heroin production in Mexico have guaranteed a steady supply of low-cost heroin, despite the increases in the number of users over the past decade. While heroin from four source areas (Mexico, South America, Southwest Asia, and Southeast Asia) can be found somewhere in the U.S., Mexico is the main source of heroin. South America is the second most common source. Mexican heroin accounted for 79% of the total weight of heroin analyzed by the Heroin Signature Program.

The domestic supply of Mexico-sourced heroin is more than sufficient to satisfy current U.S. market demand. Moreover, Mexican heroin traffickers are able to keep the supply steady and reliable. This is evidenced by high availability levels in U.S. heroin markets and low retail-level prices.

The number of individuals who used heroin in the month prior to a National Survey on Drug Use and Health (NSDUH) increased by 154% between 2007 and 2014. There was a 51% increase in just the last year of the survey; 27% reported lifetime heroin use. “The estimated number of new heroin initiates doubled between 2007 (106,000) and 2014 (212,000).” See the following graph for more information on current heroin users between 2007 and 2014 from the 2016 NDTA Summary.

So far we’ve looked at the opioid epidemic from the perspective of national statistics and surveys. But I want to close with a more up-close-and-personal look at the issue. During the summer of 2016, I read Gun, Needle, Spoon by Patrick O’Neil. Gun is a compelling look at the life of a “current heroin user.” Patrick has over fifteen years clean now, but gives you a clear-eyed, non-blinking look into the abyss of heroin addiction in his memoir. What follows are a couple of paragraphs of life in that nightmare. Read Gun, Needle, Spoon for more.

Technically, kicking heroin takes three days. Every junkie’s kick is slightly different, yet the symptoms are the same. For me it starts out with an unpleasant familiar taste in the back of my throat. My nose begins to run, I sneeze a lot, and my eyes water. Then the aches arrive, followed by vomiting and diarrhea. There’s no sleeping. I’m either cold and shivering or hot and continually sweating. My muscles cramp, my head feels thick, and all I think about is doing more dope in order to not be in such misery. . . .The digital clock on the desk in the living room read 11:55 PM. I light a cigarette and stare at the gun. Before I can really think about it, I pull on a pair of jeans and get dressed. Digging through a pile of dirty clothes, I find a black bandana and tie it loosely around my neck. I slip the gun into my waistband, button my overcoat, and quickly open the front door.

P.S. There is good new here. Patrick just wrote that he received a pardon from the governor of California for his past crimes. You can read about the day he received his pardon here. And take the time to congratulate him, will you?

10/28/16

Fluctuations in the Heroin Market

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© 4designersart | stcokfresh.com

The 2016 World Drug Report (2016 WDR) is a good-news bad-news source of information on global opiate statistics. The good news is that global opium production fell by 38% in 2015. The decrease was primarily the result of a decline in opium production in Afghanistan, which fell 48% compared to 2014. This was mainly because of poor yields in the country’s southern provinces. Despite this, Afghanistan was still the world’s largest opium producer, accounting for 70% of global opium production.

The bad news is that despite the drop in production, the global number of opiate users has remained relatively stable. And opium production in Latin America, mostly in Mexico, Columbia and Guatemala, more than doubled from 1998-2014. Central and South American production accounts for 11% of the estimated global opium production. Also, in North America, heroin use and heroin-related deaths have continued to rise. In both cases, the increases were roughly three times the 1999 levels. See the following chart from the 2016 WDR.

heroin-deathsIn 2014, the largest seizures of opiates were in South-West Asia, with Europe next in line. The Islamic Republic of Iran reported the largest opiate seizures worldwide, accounting for 75% of global opium seizures and 17% of global heroin seizures. The next largest heroin seizures were from Turkey (16% of global heroin seizures), China (12%), Pakistan (9%), Kenya (7%), the U.S. (7%), Afghanistan (5%), and the Russian Federation (3%). Iran is the first stop on the so-called “Balkan route” of opiate distribution. From there the route travels into Turkey, and onto South-Eastern Europe, where it is distributed throughout Western and Central Europe. “Seizure data suggest that the Balkan route, which accounts for almost half of all heroin and morphine seizures worldwide, continues to be the world’s most important opiate trafficking route.”

The massive decline in opium production of almost 40 per cent in 2015 is unlikely, however, to result in a decline of the same magnitude within a year in either the global number of opiate users or the average per capita consumption of opiates. It seems more likely that inventories of opiates, built up in previous years, will be used to guarantee the manufacture of heroin (some 450 tons of heroin per year would be needed to cater for annual consumption) and that only a period of sustained decline in opium production could have any real effect on the global heroin market.

In 2015 Bloomberg published an article with three maps of global drug smuggling routes. The major opiate producers are: Afghanistan, Myanmar, Laos, Mexico and Columbia. The opiate map illustrates the vast reach of the so-called Balkan route. The Americas are primarily supplied with opiates grown in Mexico and Columbia. More than 70% of all heroin and morphine seizures in the Americas were in the U.S. between 2009 and 2014. Seizures more than doubled from around 2 tons per year from 1998-2008 to 5 tons per year from 2009-2014. Heroin trafficking and use was seen in 2015 as the main national drug-related threat in the US, according to the 2015 National Drug Threat Assessment (NDTA).

The 2015 NDTA reported that heroin was available in larger quantities, used by larger numbers of people, and caused more overdose deaths than 2007. The increased demand and use of heroin is driven by greater availability and controlled prescription drug (CPD) abusers switching to heroin. Cheaper prices for heroin contribute to the switch as well.

Increases in overdose deaths are driven by several factors. The purity of heroin has increased in some areas. New heroin users switching from prescription opioids are used to the set dosage amounts potency of prescription drugs. Illicitly–manufactured drugs can vary widely in their purity, dosage and adulterants. Over the past few years the use of highly toxic adulterants like fentanyl (20 to 40 times stronger than heroin) in certain markets has also added to the increase in overdose deaths. Then there are heroin users who stopped using for a while (from treatment or incarceration) whose tolerance has decreased because of their abstinence.

Most of the heroin in the US today comes from Mexico and Columbia. Columbian heroin is still the predominant type available in the Eastern US. While Southeast Asian heroin, largely from Afghanistan dominates the global market, very little makes its way to the US. Southeast Asian heroin was the dominant supplier of heroin in the US at one time. But it no longer can compete with the transportation and distribution networks of the Mexican and Columbian drug cartels. Se the following chart from the 2015 NDTA.

heroin-seizuresThe Mississippi River has been a dividing line in the US heroin market for the past 30 years, with Mexican black tar and brown powder heroin west of the Mississippi and white powder heroin from South America in the East. There is increasing evidence that Mexican drug cartels are processing their own white powder heroin and mixing white heroin with Mexican brown powder heroin to create a more appealing product to the Eastern US markets. See charts 12 and 13 in the 2015 NDTA for further information on the availability of heroin types purchased in Eastern and Western cities.

The suspected production of white powder heroin in Mexico is important because it indicates that Mexican traffickers are positioning themselves to take even greater control of the US heroin market. It also indicates that Mexican traffickers may rely less on relationships with South American heroin sources-of-supply, primarily in Colombia, in the future. If Mexican TCOs [transnational criminal organizations] can produce their own white powder heroin, there will be no need to purchase white powder heroin from South America to meet demand in the United States. This would also reinforce Mexican TCOs’ poly-drug trafficking model and ensure their domination of all major illicit drug markets (heroin, cocaine, methamphetamine, and marijuana) in the United States.

Mexican TCOs have been increasing their cultivation of opium poppies, to an estimated 17,000 hectares in 2014. This can potentially produce up to 42 metric tons of heroin. Switching to opium cultivation from marijuana cultivation may be at least partly due to the lowered demand for illicit marijuana in the US because of the legalization movement. See “The Economics of Heroin” for more information.

The number of heroin users reporting they used heroin over the past month increased 80% between 2007 and 2012. Of the total number of heroin-related treatment admissions in 2012, 67.4% reported daily use and 70.6% reported their preferred route of use was by injection. Heroin treatment admissions were consistently highest in the New England and Mid-Atlantic states. There are also high rates of repeated treatment among heroin users. Eighty percent of the primary heroin users admitted to treatment in 2012 reported previous treatment; 27% had been in treatment five or more times.

Most opioid users in the 1960s began by using heroin. But that steadily changed until 75% of heroin-users in the early 2000s reported they began by using prescription opioids. The number of people using illicit prescription opioids who switched to heroin was a relatively small percentage of the total number of prescription drug abusers at 3.6%. But it represented 79.5% of new heroin users. Heroin use was 19 times higher among individuals who had previously used pain relievers non-medically.

The reformulation of OxyContin in 2011 is seen as helping to curb the abuse of the drug. In 2011 emergency department visits involving oxycodone declined for the first time since 2004. Overdose deaths from opioid analgesics also began to decrease in 2011. But remember, CPD abusers have been switching to heroin and seem to be contributing to the dramatic increase in overdose deaths from heroin.

The number of heroin overdose deaths increased 244% between 2007 and 2013. Keep in mind that heroin deaths are undercounted. This occurs because of the differences in state reporting procedures for reporting drug-related deaths; and because heroin metabolizes very quickly into morphine. A metabolite unique to heroin, 6-monoaceytlmorphine (6-MAM), quickly metabolizes into morphine erasing the biochemical evidence for heroin use. So many heroin deaths get reported as morphine-related deaths. So what does the future hold for heroin use in the US? The 2015 NDTA concluded the current outlook for the near future is more of the same.

Heroin use and overdose deaths are likely to continue to increase in the near term. Mexican traffickers are making a concerted effort to increase heroin availability in the US market. The drug’s increased availability and relatively low cost make it attractive to the large number of opioid abusers (both prescription opioid and heroin) in the United States.

The United Nations Office on Drugs and Crime (UNODC) publishes a yearly report giving a global overview of the supply and demand of various drugs and their impact on health.

09/9/16

The Dragon Threat

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© Linda Bucklin | 123rf.com

The DEA released its updated “National Heroin Threat Assessment Summary” on June 27, 2016 and the news is not good. Chuck Rosenberg of the DEA called the death and destruction from heroin and opioids “unprecedented and horrific.” The number of users, treatment admissions, overdose deaths, seizures from heroin traffickers all increased since the 2015 Summary. The increased demand and use of heroin is being driven by greater availability of heroin in the U.S. and prescription opioid users switching to heroin because it’s cheaper. “The problem is enormous and growing, and all of our citizens need to wake up to these facts.”

There were three big takeaways in the 2016 Summary: 1) the number of people currently using heroin almost tripled between 2007 and 2014. 2) Deaths due to heroin more than tripled between 2010 and 2014. 3) Deaths due to synthetic opioids, like fentanyl, increased 79% between 2013 and 2014. You can access a pdf of the full report here.

In 2014, 10,574 American died from heroin-related overdoses. Geographic areas of the country particularly hard hit are in the Northeast and the Midwest. See Map 2 in the 2016 DEA Summary. Not surprisingly, availability levels are the highest in these areas as well. Possible reasons for the increase in overdoses and deaths include: more heroin users, especially those who are new to heroin, who are young and inexperienced; the higher purity of heroin found in certain areas and the use of adulterants like fentanyl.

Twenty to thirty years ago, the average retail-level purity of heroin available in the U.S. was about 10%. By 1999, the average purity was 40%. While the purity increased, the price decreased. The average price per gram in 1981 was $3,260 in 2012 US dollars. By 1999, the price for a gram of heroin had dropped to $622. Heroin prices have remained low since then. With an increase in purity, heroin can be snorted or smoked, which broadens its appeal. “Many people who would never consider injecting a drug were introduced to heroin by inhalation.”

Beginning in late 2013, several states started reporting overdose death due to fentanyl and acetyl-fentanyl. There were 5,544 reported synthetic-opioid-related deaths in 2014. But the DEA speculated it was much higher because of a lack of standardization in reporting; and because coroners and state crime labs don’t initially test for fentanyl or its analogs unless they have a reason to do so. The eastern U.S. is the area most effected by this, because white powder heroin from South America predominates. Fentanyl, also a white powder, is mixed with heroin or sold disguised as white powder heroin. The following chart is from the 2016 DEA Summary.

Heroin deathsThe Mississippi River has historically been a geographic dividing line with Mexican, “black tar” and brown powder heroin more common west of the Mississippi and white powder heroin, now supplied from South America, common east of the Mississippi. But that is changing. Mexican traffickers are making inroads into major eastern cities. Mexican organizations are now the most prominent wholesale-level traffickers of heroin in Chicago, New Jersey, Philadelphia, and Washington DC. Increased trafficking of Mexican heroin means more heroin is entering the U.S. across the Southwest border from Mexico. Black tar heroin is popping up more frequently in the Northeast, although it still comprises a small percentage of the heroin seized.

Mexican traffickers have taken a larger role in the U.S. heroin market, increasing their heroin production and pushing into eastern U.S. markets that for the past two decades were supplied by Colombian traffickers. This is notable because Mexican traffickers control established transportation and distribution infrastructures that allow them to reliably supply markets throughout the United States

The DEA also noted the increase in counterfeit prescription pills, many which contain deadly amounts of fentanyl. Small-scale local drug entrepreneurs can buy the materials and equipment to produce the counterfeit drugs online and set up their own operation, ala Breaking Bad. “Fentanyl pill press operations have been identified in the United States, Canada, and Mexico, indicating a vast expansion of the traditional illicit fentanyl market.” Oxycodone and other opioid painkillers are the main counterfeited medications, but traffickers are also packaging fentanyl as Xanax and other benzodiazepines. See “Buyer Beware Drugs” for more information.

When comparing heroin use to other drugs in the U.S., we find that the population of heroin users is slightly smaller than the estimated population of methamphetamine users and significantly smaller than individuals reporting current cocaine use. However, the number of individuals reporting current use of prescription pain relievers non-medically was about TEN TIMES the size of heroin users. So although a rather small percentage of prescription drug abusers (4%) will try heroin, this represents a significant increase in the number of heroin users because the size of the prescription drug abuse population is so much larger. See the following chart taken from the 2016 DEA Summary.

chart 7Behind all these statistics are real people, some living and some now dead. And despite all the law enforcement efforts over the past several decades, the problem seems to be getting worse. So two federal law enforcement agencies decided to combine their efforts and try a different tactic. They thought they’d try to address the problem from the demand side instead of the supply side.

Back in February the FBI and DEA released a documentary film addressing the growing epidemic of prescription drug and heroin abuse. “Chasing the Dragon: The Life of an Opiate Addict” is intended as an educational film for high school and above. Educational materials have had mixed effectiveness with decreasing drug usage. But the value of this film is in its portrayal of the real people who chased the dragon and became part of the above statistics. You can watch the film here.

08/30/16

The Devil in Ohio

© Olena Yakobchuk | 123rf.com

© Olena Yakobchuk | 123rf.com

Around the beginning of July 2016, there were a series of overdoses and deaths in Akron Ohio. The ABC News affiliate in Cleveland reported there had been 173 overdoses in Akron by July 22; 16 of which were fatal.  Some of the first people to overdose had not shot up—they were snorting what they thought was heroin. “As soon as I sniffed it, I knew something was up because it got me feeling super intense,” he said. When I woke up, I was on a stretcher. I was freaking out because I didn’t know what happened. I was tied down.”

The overdoses are being attributed to a street mixture of heroin and carfentanil, an opioid considered to be 4,000 times as potent as heroin. There were some misleading news reports at the time suggesting that heroin users themselves were mixing heroin and carfentanil (carfentanyl). Reporting for Cincinnati.com, Terry DeMio said that the Hamilton County Heroin Coalition warned carfentanil had been found in the local heroin of Cincinnati, Akron and Columbus. Dr. Marc Fishman said: “Carfentanil is one of the most potent opioids known, as an anesthetic agent by veterinarians for large animals, not used for humans.” Veterinarians who are licensed to use it cover up hands, arms and faces when they use it … and they keep naloxone handy.

Then the overdoses started happening again in the Cincinnati area. The Washington Post reported there were 78 overdoses and at least three deaths during a 48-hour period. By the end of the week, the overdose total has reached 174. Some of the overdose victims required multiple doses of naloxone to reverse the effects. Although they are still awaiting the lab results, the police believe this is another batch of heroin mixed with carfentanil. So far law enforcement has not been able to identify the source of the mixture. Newtown Police Chief Tom Synan said:

These people are intentionally putting in drugs they know can kill someone. . . . The benefit for them is if the user survives, it is such a powerful high for them, they tend to come back. … If one or two people die, they could care less. They know the supply is so big right now that if you lose some customers, in their eyes, there’s always more in line.

WKRC in Cincinnati reported thirty overdoses in the course of just one day—Tuesday August 23rd. One man overdosed while driving through an intersection. Another man overdosed at a gas station; with his child in the car. Three other people overdosed in the same house. “It was too early to tell if the spike in overdoses Tuesday night, August 23, had anything to do with carfentanil. But, it was found in several places throughout the city of Cincinnati in early August 2016.”

carfentanil molecule

carfentanil molecule

So what exactly is carfentanil? According to PubChem, carfentanil is an analog drug of fentanyl that was first synthesized in 1974 by a team of chemists working for Janssen Pharmaceuticals. It’s marketed under the trade name of Wildnil as a general anesthetic for large animals, like elephants and rhinoceros. Its extreme potency makes it an inappropriate agent for human use, unless you happen to be a Walter White-type of entrepreneur with heroin. It is classified as a Schedule II controlled substance.

A 2012 study found evidence that the Russian military used an aerosol form of carfentanil and remifentil in the 2002 Moscow theatre incident to subdue Chechen hostage takers. The Washington Post reported the death toll was 170 people; only 40 of the dead were attackers. Because of the lack of information provided to emergency workers, they didn’t bring enough naloxone or naltrexone to prevent the complications experienced by the gassed victims “from both respiratory failure and aerosol inhalation during the incident.” A 10 mg dose of carfentanil could sedate or kill a 15,000-pound elephant or take down a musk ox, bull moose or full grown buffalo. The same amount could kill 500 human beings.

Heroin cut with carfentanil offers a harder-hitting, longer-lasting high and allows dealers a shortcut to increase their supplies. But users often don’t know what they’re getting. In recent months, authorities have linked carfentanil to a spike in overdoses in several states, and have warned that it could spread to others.

On August 9, 2016 Canadian border officials reported they had intercepted a one-kilogram package of carfentanil heading to Calgary from China. The package was shipped to a 24 year-old man at his home address and labeled as “printer accessories.” A kilogram of carfentanil is equivalent to four metric tons of pure heroin. The package could have produced 50 million doses. Roslyn MacVicar of the Canadian Border Services Agency said: “It is hard to imagine what the impact could have been if even the smallest amounts of this drug were to have made its way to the street.”

In a DEA report Donald Cooper presciently thought that analogs of fentanyl would become a future drug of abuse He indicated that the already published synthesis schemes for fentanyl compounds allow for a variety of precursor chemicals to be used in synthesizing the drugs. The DEA became aware of this potentiality from the confiscated notes from an anonymous clandestine laboratory. Two formulas for synthesizing carfentanil have been extracted from separate volumes of the Journal of Organic Chemistry and made available for any enterprising chemist in “Synthesis of Carfentanil” on Erowid. The DEA indicated that over 12 different analogues of fentanyl have been clandestinely produced and identified in the U.S. drug traffic.

Interviewed by CBS News, Kevin McCutheon of Akron Ohio is a long-time addict. He believes when he overdosed he ingested carfentanil. He said he had used fentanyl and has been “doin’ dope,” but this wasn’t the same. The interviewer commented that he had tears in his eyes. He said it was because he was here and knew he shouldn’t be. “It’s the devil.”

05/4/15

The Opioid-Heroin Cycle

© Ouroboros tattoo by Sahua | Stockfresh.com

© Ouroboros tattoo by Sahua | Stockfresh.com

Since the death of Philip Seymour Hoffman on February 2, 2014, there has been a series of calls for the distribution of naloxone or Narcan, which is a prescription medication that reverses an opioid overdose. But it seems that the price of Narcan has doubled over the past year. The Fix and others report that the price of naloxone has recently gone from $51.50 per kit, to nearly $100 per kit. These are the Luer-Jet™ kits sold by Amphastar Pharmaceuticals, the only US company currently selling nasal kits. There is a cheaper injectable form of narcan, but it is supposed to be less user friendly.

Within four days of Hoffman’s death, The New York Times published an article by an emergency physician, noting how greater availability of Naloxone could prevent deaths. He referred to a report in the Annals of Internal Medicine that suggested up to 85 percent of users overdose in the presence of others, providing the opportunity for others to intervene. In Forbes Magazine David Kroll said the CDC reported that naloxone was used in over 10,000 opioid-overdose reversals between 1996 and mid-2010. He also expressed his concerns over potential shortages of naloxone.

Victoria Kim for The Fix reported that Amphastar’s president blamed the price increase of their naloxone product on “steadily increasing” manufacturing costs. But Matt Curtis, the policy director for a New York advocacy group said there had been a fairly steady price for several years. “Then these big government programs come in and now all of a sudden we’re seeing a big price spike. . . . The timing is pretty noticeable.” The Hill reported that Senator Bernie Sanders and Representative Elijah Cummings sent a letter to Amphastar complaining about the price increase and how it is “an obstacle in efforts by police departments to equip officers with the drug.”

Areille Pardes of Vice said that after the CDC said there was an opioid epidemic in 2008, the manufacturer of naloxone, Hospira, increased the price of a dose of naloxone from $3 to a little more than $30. Pardes also reported that the supposed difficulty of a lay-friendly delivery system has also been used to justify the high costs of epipens (around $400) and the naloxone auto-injector, EVIZO (Over $600 for a kit of 2 auto-injectors at Walmart, Sams Club, Target and other retail outlets). However a study found few differences between trained and untrained overdose rescuers in their abilities to use the syringes in a naloxone rescue kit. “Anyone with common sense could figure it out, even without training.”

It does seem that the timing of the price increases for naloxone (a generic drug) and its delivery systems occurred just as the epidemic of overdoses took place. The CDC reported in a March 2015 NCHS Data Brief that from 2000 to 2013 the rate of drug overdoses quadrupled, from .7 deaths per 100,000 to 2.7 deaths per 100,000. Overdoses are now the number one cause of injury-related death in the US. While the overdose deaths involving (prescription) opioid analgesics have leveled off in recent years, those from heroin have almost tripled. See Figure 1 of the NCHS Data Brief. While the heroin overdose rates increased among all age brackets, the highest rate of increase was among 25-44 year olds. Geographically, while there were increases in all regions of the country, the greatest increase took place in the Northeast and the Midwest. See figure 5 of the NCHS Data Brief.

There is some sense that effort to curb problems with overprescribing pain medications has inadvertently led to a boom in the misuse of heroin. Richard Juman reported for The Fix that while some treatment providers suggest that is the case, others note that there is evidence that heroin use was increasing before any state or federal interventions with prescribed opioids were implemented. According to Andrew Kolodny, MD:

The idea that efforts to curb prescription drug misuse have led to a spike in heroin use or overdose has become a common media narrative, but the facts don’t support it. It is the overprescribing of opioids itself that has caused increases in opioid addiction of all kinds, not the efforts to control the prescribing. The transition from prescribed opioids to heroin has been happening since the beginning of the epidemic, and there is no evidence that the interventions brought forth to reduce the overprescribing have been fueling the increase in heroin use or overdoses. Because of the epidemic of opioid addiction, you now have markets for heroin that you didn’t have in the past. So there has been an increase in heroin overdose deaths, but that increase was prior to states’ implementation of Prescription Monitoring Programs or any of the changes from the FDA.

I tend to agree with Dr. Kolodny’s assessment. There is a price factor in the shift for many opioid users switching to heroin. And there has been a global market increase in heroin production that paralleled the rise of prescription opioid use. Increased heroin use in the US is market driven. What does seem to be related to increased heroin availability in the US is the diversification of Mexican drug cartels into growing opium poppies, as their market for marijuana dries up. See “The Economics of Heroin.”

There is something very wrong with the cycle of Pharma marketing for increased use of opioids, leading to overprescribing opioids, leading to increased heroin use and increased overdoses, leading to an increased need for narcan, leading back to increased profits with drug companies, where the cycle began. The ouroboros pictured above is a symbol in Greek mythology of a dragon eating its own tail. It symbolizes something that constantly re-creates itself, which seems to be happening here with the opioid-heroin cycle.

04/13/15

The Economics of Heroin

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© Berna Namoglu | 123RF.com

I live in the suburbs of Pittsburgh. At least nine times each week I drive past a retail store where someone I know once told me they shot up heroin in the store’s parking lot. The store sits on a busy street. This incident was a few years ago, but I’m pretty sure that wasn’t the only time someone used heroin in my neighborhood, because it’s happening all around me.

A teacher from the Montour School District was recently charged with two counts of possession with intent to deliver. Police said he was selling heroin out of his home. The school district suspended him immediately. The school district’s solicitor said there was no evidence that the man possessed or sold drugs on school property. The accused has been a math teacher for at least a decade. The ironic twist is that he rented his home from the Robinson Township police chief, who said he’s never had any problems with the accused … until now.

The Pittsburgh Post-Gazette reported at the end of February 2015 that three people from Armstrong County were charged in connection with an overdose death linked to fentanyl-laced heroin known as “theraflu.” I work part time at an outpatient treatment center in Pittsburgh and remember when the theraflu scare was going on in January last year. Seventeen people from around Pittsburgh died of overdoses in a week. A local medical examiner at the time said it was  “major public health crisis.”

An ongoing investigation of drug trafficking in Homewood and other communities in the Pittsburgh metro area recently added 14 new defendants to the 40 who were originally indicted in October of 2014. US Attorney David Hickton said they were “important cogs” in a multi-state drug distribution ring. “They would be the Pittsburgh connection to this organization that has reach far beyond out state.” The trafficking involved heroin, cocaine and crack cocaine coming from Los Angles to Homewood via Cleveland. Harold Hayes of KDKA said: “The FBI says the long-term investigation has led to the indictment of more than 100 people and the seizure of more than $1 million.”

The 2014 National Drug Threat Assessment Summary (NDTS) published by the DEA stated that the threat posed by heroin in the US has been increasing across the country, particularly in the Northeast and North Central regions. The two major geographic areas for heroin supply in the US are Mexico and South America. Together they account for 96% of the heroin analyzed by the DEA in 2012. The NDTS reported that heroin seizures increased 87 percent in five years, from 2009 to 2013.

The observed increase in demand for and abuse of heroin is said to be the result of individuals who used to abuse prescription opioids switching to heroin. Reasons given for the switch include: the relatively lower cost of heroin than prescription opioids; the decreasing availability of prescription opioids versus the increasing availability of heroin; the reformulation of OxyContin, making it more difficult to abuse. My own experience with people abusing heroin is that the switch is mostly market driven, by the cost differential and the availability of heroin.

In 2013 and 2014, the Northeast and Midwest reported a spike in overdose deaths from fentanyl being sold as heroin. Fentanyl is 30 to 50 times stronger than heroin. The overdoses include both new and experienced users. Thinking they are buying heroin, the users typically don’t realize they are buying fentanyl or a fentanyl-heroin mixture. Between 2005 and 2007 over 1,000 overdose deaths were traced back to a single laboratory in Mexico. The lab was seized and destroyed. The recent outbreak, noted above, covered a wider geographic area than in 2005-2007 and involved both fentanyl and fentanyl analogs.

In Mexican states like Sinaloa and Guerrero, poor farmers living in wood-plank, tin-roofed shacks with no indoor plumbing are growing the poppies that eventually become the heroin sold in American cities like Pittsburgh. Jake Bergman, reporting for the PBS show Frontline, noted how Sinaloa has been the breadbasket for Mexico for decades. Now it a drug-rich area, “the cradle of the biggest traffickers Mexico has ever known.” They even have their own “patron saint”—Jesus Malverde. Malverde’s legend says he robbed from the rich and gave to the poor. Nevertheless, he was hung by the governor of Sinaloa in 1909. His “sainthood” is not recognized by the Roman Catholic church. Father Antonio Ramirez said: “Nobody has become a saint robbing and killing, he was a bandito.”

Nick Miroff reported last year for the Washington Post that the drug trade in Sinaloa has been going through a transition lately. Farmers who used to grow cannabis are now planting opium poppies. Rodrigo Silla, a lifelong cannabis farmer, said it’s not worth it anymore. The wholesale price for a kilogram of cannabis dropped from $100 to less than $25. “I wish the Americans would stop with this legalization. . . . There’s no other way to make a living here.” The Silla family consists of three generations of drug farmers.

A kilo of the raw, sticky opium sap that is used to make heroin sells wholesale for $1,500 in the northern Sierra Madre, nearly double its 2012 price, according to growers. With fertilizer and favorable weather, a well-tended poppy field can yield eight kilos of sap per acre, nearly enough to make a kilo of raw heroin.

David Shirk, a researcher at the University of California at San Diego said that the farmers are simply diversifying because they have a product losing its value. “The wave of opium poppies we’re seeing is at least partly driven by changes we’re making in marijuana drug policy.”

Sinaloa has grown opium poppies since the time of the arrival of Chinese settlers in the last half of the 19th century. But large-scale production did not begin until World War II. Japan controlled the Asian opium market and the US military needed morphine for its soldiers. During this time, many Sinaloans made a fortune. Everyone was growing it. Even some government officials got into the opium export trade. After Japan was defeated, the US no longer wanted the inferior Sinaloan opium. “But many farmers continued to produce opium and heroin; operations became more clandestine, and a smuggling network was set up.”

Writing for the Associated Press, Mark Stevenson reported that farmers in Guerrero don’t like growing opium poppies, but it’s the only thing that will guarantee them a cash income. Humberto Nava Reyna, the head of a group promoting development projects in the region said: “They can’t stop planting poppies as long as there is demand, and the government doesn’t provide any help.” Residents say there are no local users. “It all goes for export, a lucrative business mostly run by the Sinaloa Cartel.”

So it’s sounding like the war on drugs needs to begin changing tactics. Instead of spending so much time and energy on chocking off the supply routes, there should spend more time and energy on drug treatment and prevention to dry up the demand. And there should be some funds given to Humberto Reyna and others like him to help the multi generational drug farmers transition to non-drug crops. And I think I’ll start praying for the Silla family and other drug farmers when I pass by that retail store in my neighborhood.

02/16/15

Legacy of the “Joy Plant”

There is a new, allegedly less addictive painkiller in the pharmaceutical pipeline, CR845, by Cara Therapeutics. Although CR845 is being touted as “non-addictive” (here and here); or a “non-absusable alternative to narcotic opioids” by Cara Therapeutics, that remains to be seen. CR845 is anticipated to be a Schedule 5 controlled substance. This is significantly less addictive than OxyContin and other opioid pain relievers, which are mostly Schedule 2. Even a less addictive pain medication would be great. But the history of opiates is full of similar promises.

The earliest reference to opium was in 3,400 BC where the Sumerians in lower Mesopotamia referred to it as Hul Gil, the “joy plant.” They, in turn, passed the knowledge of the opium poppy to the Assyrians, who gave it to the Babylonians, who passed it on to the Egyptians. The Egyptians were famous for their poppy fields and the opium trade flourished during the eighteenth dynasty (around 1500 to 1300 BC) under the reigns of Thutmose IV, Akhenaton and King Tutankhamen.  Roman gladiators used opium to enhance their fighting … and to die as painlessly as possible if mortally wounded.

Hippocrates, the father of medicine, saw opium as a helpful narcotic for treating disease. The great physician Galen, cautioned that opium should be used sparingly in 158 AD. He said it was better to endure pain than to be bound to the drug. It wasn’t until 400 AD that opium was introduced into China by Arab traders.

A History Channel documentary reported that Alexander the Great used opium to help his soldiers march farther because they couldn’t feel the pain in their feet; and they could sleep through the night because the wounded were sleeping peacefully under the influence of opium. He introduced opium to India, where it’s cultivation flourished. One of the goals of Columbus was to bring back opium from India, as its access had been cut off when the Arabs were expelled from Spain. He didn’t get to India, but he brought back tobacco from the New World and smoking tobacco became common throughout Europe.

Portuguese traders began smoking a tincture of opium with their tobacco around 1500. They also discovered the euphoric effect was instantaneous. In 1680, the English apothecary Thomas Sydenham introduced laudanum, a compound of opium, sherry wine and herbs. Dutch traders introduced the practice of smoking opium to the Chinese around 1700. The Chinese loved the habit and it led to cultural and political ruin. By 1800, 1/3 of the country was addicted to opium.

In 1803, a German chemist named Friedrich Sertuerner synthesized morphine from opium. Sertuerner’s wife overdosed on morphine and died. He then publically warned against its dangers. But morphine was also a great step forward in medicine. It allowed doctors to do true surgery for the first time. Morphine was heralded as “God’s own medicine” for its reliability and long-lasting effects. By 1827, the E. Merck & Company of Darmstadt Germany was commercially manufacturing morphine.

A new technique for administering morphine was developed by Dr. Alexander Wood of Edinburg when he invented the syringe in 1843. Wood believed that if morphine was injected instead of swallowed, “patients would not hunger for it.” He was wrong; and several of his patients became dependent. There is a mythical story that Wood’s wife was among the earliest of these addicts, and died of a morphine overdose. But according to Richard Davenport-Hines, she outlived her husband and survived until 1894.

Needles and morphine were quickly in demand. You could order morphine, opium and syringes through the mail … from Sears and Roebucks. They became a blessing during the Civil War on the battlefield. But their use created a generation of young ex-soldiers as morphine addicts. Morphine addiction became known as “the soldier’s disease” or “the army’s disease.”  This was the first drug epidemic in the United States. Nineteenth century America became “a dope fiend’s paradise.”

Morphine even became part of medical missionary efforts in China. They were selling opium pills and morphine powders, which became known as “Jesus opium.” The Chinese Recorder and Missionary Journal, Vol. 19, published in 1888, had a letter from a concerned person in Foochow: “Missionaries who dabble in this kind of business, probably most of them innocently, should know that their supposed help to suffering humanity is in the majority of the cases an injury to the patient and a positive evil in the church.”

Dr. John Witherspoon warned his fellow doctors in a June 23, 1900 article about their indiscriminant use of morphine. The morphine habit was growing at an alarming rate; and doctors were culpable for “too often giving this seductive siren until the will-power is gone.” Pointing to the Great First Physician, he said doctors should “save our people from the clutches of this hydra-headed monster” which wrecked lives and filled jails and lunatic asylums.

Looking for a non-addictive derivative of opium that could be used as a cough suppressant, the Bayer chemist Felix Hoffman successfully synthesized diacetylmorphine—heroin. When a Bayer executive introduced the drug to the Congress of German Naturalists and Physicians, he said it was 10 times more effective as a cough suppressant than codeine; it was more effective than morphine as a pain reliever and not habit-forming. Bayer began to sell it commercially in 1898 and by 1899 was producing about 1 ton of heroin yearly. The Boston Medical and Surgical Journal said heroin had many advantages over morphine, including: “It’s not hypnotic, and there’s no danger of acquiring a habit.”

Reports of “heroinism” had already surfaced, by 1900, but it took time for the sale and endorsements of heroin to stop. In 1906, the American Medical Association approved heroin for medical use, while cautioning that a “habit” was “readily formed.” In 1913, Bayer stopped making heroin. In 1919 it became illegal for doctors to prescribe heroin to addicts. In 1924, the US banned the use and manufacture of heroin altogether.

02/9/15

Evolution of Synthetic Painkillers

The documentary, “American Addict” (available on Netflix) reported that 106,000 Americans die from prescription drugs each year. In the first six months of 2008, 67% of the oxycodone that was prescribed throughout the U.S. came out of Broward County Florida. What was going on? Mid Eastern states had a prescription drug-monitoring program; Florida didn’t.  Drug seekers from those states went south for their drugs.

By the end of the 1800s, a wide variety of “patent medicines” had come onto the market. They were called “patent” medicines because their formula was a secret; so the ingredients weren’t listed. “Some of the patent medicines were up to 50% morphine by volume. And no matter what ails you, if you take something that is 50% morphine by volume, you’re going to feel better.” And some people began to use opiated “cure-alls” as intoxicants. These cure-alls were popular among women. “The typical opiate user in the nineteenth century was a middle class, middle–aged, white woman living in the middle of the country,” according to Pat Morgan of UCLA.

When Congress passed the Pure Food and Drug Act of 1906, it required the patent medicine industry to label its ingredients. “As a result of these regulations, most of the patent medicines went out of business immediately.” Addiction decreased dramatically; as a result of Americans becoming aware of what these drugs could do, according to historian Cliff Schaffer. But heroin addiction was just coming into its own (See another article, “Legacy of the ‘Joy Plant’”).

By 1913, heroin replaced morphine as the leading cause of hospital admissions for narcotics problems in the US. It was the leading drug of abuse in New York City. In 1914 the federal government passed the Harrison Tax Act. This legislation required an opiate prescriber to get a license and pay a tax; and an opiate user had to be a patient of a licensed prescriber. It created an estimated 100,000 to 200,000 criminals out of users and addicts. Heroin eventually became an illicit substance in 1924 with the Heroin Act, which made it illegal to manufacture, possess or distribute heroin—even for medical use. But the chemists of the world were already working to develop synthetic substitutes.

Oxycodone was first synthesized in 1916 at the University of Frankfurt. It was hoped that it could be a less addictive substitute for morphine and heroin. By the 1920s, there were reports of “euphoric highs” in patients using oxycodone. It was first introduced to the US in 1939. In the early 1960s, the US classified it as a Schedule II drug.  In 1950, Percodan (oxycodone and aspirin), was put on the market by Endo Pharmaceuticals. In 1971, Percocet (oxycodone and acetaminophen) was launched by Endo Pharmaceuticals. In 1996, OxyContin, a time-release form of oxycodone became available from Purdue Pharmaceuticals.

The time-release mechanism that was supposed to make OxyContin more difficult to abuse was quickly and easily neutralized by crushing the tablet before snorting the powder or mixing it with water to inject it. Users compare the high from oxycodone to heroin. In 2010, an abuse-deterrent formulation of OxyContin was introduced. The intent was to make it more difficult to crush. The New England Journal of Medicine published an article, “Effect of Abuse-Deterrent Formulation of OxyContin” in July of 2012 that indicated the new formula did indeed decrease it as a drug of abuse. But 24% of those who had abused OxyContin reported they found a way to defeat the tamper-resistant properties. Sixty-six percent reported switching to another opioid, with heroin being the most common choice. Heroin is easier to use, cheaper and easily available. The article concluded “Abuse-deterrent formulations may not be the “magic bullets” that many hoped they would be.”

Not to be deterred by these conclusions, Purdue Pharmaceuticals recently received approval for Terginiq ER, a combination of oxycodone and naloxone, a drug that is supposed to block the euphoric effects of oxycodone if it is crushed (so it can’t be snorted or dissolved and injected). But if you simply swallow Teriniq ER, the naloxone is not activated. “When the pills are swallowed they are as addictive as pure oxycodone.” Nevertheless, the FDA sees the approval of abuse-deterrent medications like Targiniq ER as a positive step in its fight address the public health crisis of prescription drug abuse in the U.S.

Hydrocodone was first synthesized in 1920, of course, by Germans. In 1924, it was first sold by Knoll Pharmaceuticals in Germany as Dicodid. Knoll was also responsible for the introduction and marketing of oxycodone as Dinarkon in 1917, and Dilaudid (hydromorphone), in 1926. Through a series of mergers, Knoll became a part of Abbott Laboratories in June of 2002.

In 1929, the U.S. Bureau of Social Hygiene gave the National Research Council several million dollars to study various new compounds like hydrocodone, to see if there was a less addictive opioid than morphine or heroin. Nathan Eddy tested the safety, efficacy and side effects of 350 drugs, including morphine, codeine, Dilaudid and hydrocodone. His results showed that hydrocodone was an effective painkiller, with predicable side effects. It also “induced euphoria, and therefore there was a danger of addiction.” Eddy said that tolerance developed more slowly than with morphine or Dilaudid and the occurrence of abstinence syndromes were less severe than with other drugs. This suggested an individual could become dependent on it without knowing it until they are really hooked.

With the Controlled Substances Act of 1971, pure hydrocodone was classified as a Schedule II controlled substance, as was opium and morphine. But in combination with other drugs, it could be regulated as a Schedule III drug. In 1978, Knoll Pharmaceuticals introduced Vicodin, five milligrams of hydrocodone with 500 milligrams of acetaminophen. Generic Vicodin became available in 1983.

Hydrocodone had become the most prescribed medication in the U.S. “Since 2007, more U.S. prescriptions were written for hydrocodone + acteminophen than any other drug.” In 2012 alone, there were over 135 million prescriptions written.

In 2002, emergency room reports involving hydrocodone had increased by 500% since 1990. That same year, the FDA recommended tighter warnings on drugs containing acetaminophen because of the concerns it can cause liver damage. In October of 2014, Vicodin was reclassified as a Schedule II drug. The purpose of the change was to minimize its use as a recreational drug, while ensuring that patients with severe pain still have reasonable access.

A new hydrocodone painkiller called Zohydro, with 5 to 10 times the power of Vicodin, was approved by the FDA in October of 2013. This approval ignored the 11 to 2 vote AGAINST APPROVAL by its own advisory panel. Zohydro is pure hydrocodone. Melanie Haiken, a contributor to Forbes, wondered if we need a new opiate painkiller, given that we don’t seem to be able to prevent the ones we already have from ending up in the wrong hands. She commented: “The U.S., with just 5 percent of the world’s population, now accounts for 84 percent of global oxycodone (OxyContin) consumption and more than 99 percent of hydrocodone (Vicodin, Lortab) consumption. That’s a lot of painkillers.”