The first drug made specifically to treat addiction in America, or at least marketed for this purpose, was “Hero-In”, which came out the same year as “Asper-In” from that first of pharmaceutical giants, Bayer.
Heroin was a modified form of morphine. Morphine is of course an opiate, readily purified from raw opium. The Bayer chemists acetylated the morphine, ending up with diacetylmorphine, which was much more lipophilic and could cross the blood brain barrier faster than morphine, and was also cleared out faster.
There was a long-standing theory that the longer a medication’s actions, the longer the withdrawals, and that such a fast-acting medication would treat the terrible withdrawals of morphine and opium addiction without, itself, being addictive.
As you can imagine, the implementation of this theory proved less than effective.
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Heroin, while extremely effective at treating severe acute pain, a purpose for which it is still used in the United Kingdom, turned out to be more addictive than morphine, giving rise to a new theory.
The faster and stronger a substance causes a euphoric or anxiolytic response, the more addictive it is.
Heroin was declared to have “no medical purpose” by Congress, and its production, sale, and possession banned in the United States.
Then the treatment of addiction itself was criminalized in 1914 by the Harrison Act, and during the first decade of its enactment about 25,000 doctors were indicted and over 3,000 sent to prison, though accurate statistics are hard to find.
Despite the fact that anything used in medicine, even software, is supposed to undergo post-market analysis, no one tracks the true effect of a political intervention when Congress decides to play doctor.
"The faster and stronger a substance causes a euphoric or anxiolytic response, the more addictive it is."
The next big thing to come along to help patients with addiction was methadone.
In 1969, this medication had been recognized by medical scientists for its potential use as an addiction treatment, and the FDA approved it for this purpose in 1972.
This might seem strange since the Supreme Court had already said that addiction was not a medical disease and could not be treated, but remember, coequal branches, Congress passed the Narcotic Treatment Act of 1974 authorizing the use of methadone in addiction, and it was all we had, until 2002, so almost half a century.
During that time the use of methadone was severely restricted, and patients had to go to federally approved treatment centers for daily dosing.
Methadone is a full opioid agonist, like morphine or even fentanyl, but its uniquely long half-life compared to its euphoric effects; 59 hours vs about 8 hours, make it useful for addiction.
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Methadone’s long half-life and respiratory suppression effects also give it one of the most dangerous overdose profiles of any opiate, which might make it an odd choice, but with daily dosing,
I see it as a “controlled addiction”.
Preventing death but making the patient’s life revolve around that daily dose, without which, withdrawals from methadone are some of the worst of any opiate.
This did not go unnoticed by organized crime, and its influence has been uncovered in some investigations, notably the Gambino crime family in the Eastern District of California.
But that would be true of any major business operation, especially those that deal with lots of cash, as it’s an easy way to launder money from other operations and still appear to be helping society.
But even though buprenorphine was available in 2002, it was not adopted by most primary care doctors or even addiction specialists at first.
“Methadone’s long half-life and respiratory suppression effects also give it one of the most dangerous overdose profiles of any opiate, which might make it an odd choice, but with daily dosing, I see it as a “controlled addiction.”
Buprenorphine had been patented in 1965 and approved for medical use in the United States in 1981. But it was not immediately very popular. Buprenorphine is not a particularly strong agonist, meaning that it only activates the mu opiate receptors about 60%, unlike morphine and fentanyl at 100%.
But it does have a very high binding affinity, higher even than naloxone (Narcan), meaning it will shove other molecules off the mu opiate receptor.
Since this receptor mediates most of an opiate’s analgesic effects, you end up with a weak pain medicine that will displace any stronger one that is still around.
That is why starting buprenorphine induction too soon after other opioid use can cause severe precipitated withdrawals.
Doctors and other prescribing healthcare specialists learned to avoid this complication by waiting longer or using much smaller starting doses more frequently.
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Despite not being initially very successful as a pain medication, it has now been embraced as THE treatment, for addiction and now by some, for almost all chronic pain.
This is because as doctors are currently being targeted for increasing the “risk of diversion, addiction, and overdose”, sometimes being sentenced to life behind bars if a patient dies while on opiates, they seem to believe that buprenorphine’s respiratory depression ceiling will protect them.
I disagree.
Current prosecutions of physicians are not based on reason, logic, or real medical science at all.
They are based on the manipulation of a jury’s emotions and the singular opinions of opioid prohibitionists whose medical opinions do NOT reflect the generally accepted standard of care.
These juries, exposed to a media blast of anti-pharmaceutical films and news, are now extremely biased against any accused physician.
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No deference whatsoever is given to medical expertise.
Prosecutors blaming doctors for the deaths of patients proceed full steam, even when coroners and medical examiners find that prescribed medication did NOT cause the death.
The worst case I’ve seen is that of a physician accused of an “opiate related death” because a patient on opiates for chronic pain shot herself in the head.
In a just world, the argument could be made that the patient had been undertreated, and that the severe unremitting pain she suffered had contributed to her death.
"The worst case I’ve seen is that of a physician accused of an “opiate related death” because a patient on opiates for chronic pain shot herself in the head."
But we do not live in a fair and just world today when it comes to medical practice.
We live in one where any excuse to prosecute a doctor will be amplified by an eager media and propagated to the jury as vengeance, inflicted on the doctor in lieu of the true culprit.
The federal government’s absolute failure to stop fentanyl from flooding our country.
