Buprenorphine Overdose After Naltrexone Treatment

Naltrexone induces mu-receptor hypersensitivity.  Buprenorphine’s protective ‘ceiling effect’ may not prevent overdose in patients with this ‘reverse tolerance’.

A new patient described his recent history of respiratory failure several days into buprenorphine treatment.  He was told by his doctors that he experienced an allergic reaction to Suboxone. The rarity of buprenorphine or naloxone allergy led me to look deeper into his history, and my conclusion differs from what he was told by his last treatment team.

The patient, a man in his mid-50s, has a history of significant opioid use over the past 20 years.  He used a variety of opioid agonists over the past year, mostly prescription opioids, with an average daily dose greater than 200 mg of oxycodone per day.

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Cannabinoid Hyperemesis: How Rare?

Marijuana might cause pain and vomiting in the people who value the drug the most. Doctors should learn more about cannabinoid hyperemesis syndrome.

I recently read a CBS news story about CHS, or Cannabinoid Hyperemesis Syndrome, describing a 100% increase in cases in Colorado since the legalization of marijuana there.  A search for ‘THC’ and ‘CHS’ pulls stories from a range of sources including High Times, Wikipedia, Fusion.net, and Current Psychiatry.  A broader search reveals articles calling the disorder ‘fake news‘.

Most articles about CHS describe the condition as rare, but becoming less rare as the legalization movement takes root and grows.  The syndrome occurs in heavy, long-time users of marijuana who first notice reduced appetite, mild nausea, and sometimes weight loss.  Those symptoms, and the symptoms that follow, are relieved by smoking marijuana, leading those with the condition to become heavier users who come to see marijuana as beneficial to their health.

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Post-op Pain on Suboxone

Many patients on Suboxone or buprenorphine eventually require pain treatment, just like people who aren’t on buprenorphine products.  I’ve written about post-op pain control several times, but I continue to get emails from patients who haven’t seen my comments and who view an upcoming surgery with the same fear experienced by patients before the early 1900’s, when the OR was correctly seen as a horror-chamber.

These patients are often torn between following the treatment plan vs. doing what they have learned may work better.  In all cases, I tell patients that they cannot act in ways counter to what their physician prescribes.  But I often support their intent to ask their doctors to clarify or modify their treatment plans.

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Media Bias Against Suboxone

First Posted 2.8.2014

After Philip Seymour Hoffman’s death, I anticipated a flood of articles describing the ineffectiveness of non-medication treatments for opioid dependence.  I assumed the media would finally report on the need for long-term treatment of a long-term illness.  Instead we read more articles describing Suboxone (i.e. buprenorphine) as a ‘bad drug’, since Hoffman may have used the drug to reduce withdrawal between heroin binges.

Taking buprenorphine within a few days of using heroin blocks most of heroin’s effects and makes overdose much less likely– a fact rarely reported.  Out of about 400,000 overdose deaths over the past ten years, only 400 deaths included buprenorphine as one drug in the fatal mix– a stunning statistic that calls out for more life-sustaining buprenorphine treatment, not less.  In most of those cases, death would not occurred had there been more buprenorphine in the victim’s bloodstream.

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Does Suboxone Stop Working Over Time?

First Posted 12/31/2013

Buprenorphine is relatively unique among opioids in having a ‘ceiling’ to mu opioid effects.  There are other known molecules that act as partial agonists at mu opioid receptors, but buprenorphine is the most useful, at this point, because of other traits of the molecule– such as having few side effects from actions at non-mu receptors.

As most opioid users soon realize, opioid agonists increase tolerance over time to what appears to be an infinite degree.  The mechanisms of tolerance are complicated. I often describe tolerance as a process where receptors become less and less sensitive to opioids with stimulation, to the point where native opioids (endorphins and enkephalins) no longer activate opioid pathways.  Some of the change in sensitivity is caused by the binding of phosphate molecules to the intracellular portion of receptors, causing changes in conformation. Tolerance development is likely far more complicated, though, and includes other changes in synaptic transmission through different mechanisms.

Opioid Effect vs. Dose of Drug
Opioid Effect vs. Dose of Drug

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