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Recovery Bulletin
March 7, 2017  |  Blog

Dr. A’s Blog – How Do I Know What Formulation of Buprenorphine is Best For Me?

A Blog By Dr. Gregory Acampora, Addiction Psychiatrist & MD

Today I want to answer the question: How can you be a Lion in recovery and not a Lamb when it comes to addressing the complex subject of when is a medication a bridge versus an impediment to building durable sustained recovery?

I’m going to use this as the stepping stone to address the newest formulations of buprenorphine being offered up on the market.

The slang words “bupe” and “subs” are often used interchangeably for a specific medication that is used to help folks recuperate from a dependence on opioids associated with problem misuse patterns.  This medication is buprenorphine initially marketed as SUBOXONE ® and SUBUTEX ® and recently other formulations.

Before I discuss what formulation is “best,” I’ll review what buprenorphine is, where it came from and why we use it.

Opioid dependence is an age old problem.

NIH biologist recently provided a good timeline identifying several interesting milestones

Sumerians who lived before 3000 BC, in what is known today as Iraq, collected seeds to grow the poppy plant that produced a liquid that generated joy (gil).  Apparently the intended use of this elixir was to produce euphoria, that is, improvement in mood.  The Greeks eventually gave us two words used often in opioid vernacular: “Euphoria” means happy (eu) feeling (phoria) and “Opioid” comes from opos meaning fluid, used to describe the liquid gotten by notching a poppy pod (think of Maple syrup that come from putting a tap into a maple tree). As world trade increased in the 800’s AD (globalization?), more population was exposed to opium’s “medicinal qualities.”

First records of tolerance and dependence appear in the 1600’s when opium was significantly marketed for profit.  In 1806, Sertürmer identified the active ingredient and named it morphine after the God of Dreams Morpheus. Soon morphine was discovered to help in surgery and applied post-operatively for pain.

 

Thereafter pain reducing derivatives of morphine were developed generating three major groups of opioids in use today: 

 

  1. naturally occurring (distilled from the opium producing poppy)
  2. semi-synthetics which, are pharmacologically modified versions of that natural product
  3. synthetics, which are entirely man-made in a laboratory (no plant)

Semi synthetics included heroin, oxycodone and buprenorphine.  Synthetics include methadone, fentanyl and tramadol.

Why are opioids such a problem?

 

Words are powerful and some of the answer lies in the early descriptive words used to speak about this “liquid (opos) of the Gods” that generated joy (gil).  One hallmark of opioids is they can be euphorigenic – they generate good feeling or wellbeing.  Wellbeing can be associated with sense of calm, pleasure and joy – the opposites of anxious, pain and sadness. Again, the first records of the effects of this product address mood and joy.  Pain applications of opioids for are comparatively new; the overwhelming sense of comfort often generated in some people helps explain the seductive aspect of the opioids.

Interestingly the scientific name for the opium poppy is Papaver somniferum – this last word translates as hypnotic or sleep-inducing. History tells the tale of how this seductive substance was associated with dependence and tolerance leading to both historic and present day opioid crises.

In an attempt to “control” opioid epidemics, pharmacological variants of naturally occurring opioids were created generating heroin and methadone as remedies. Heroin proved riskier than the cure.  Methadone, another pure opioid, has become one accepted control approach, but substitutes one pure opioid for another and must be highly regulated.

Buprenorphine is a thoroughly modern treatment approach to addressing opioid dependence. It is a complex molecule that resembles the naturally occurring opioids but it has a unique feature – it is a partial agonist, meaning it turns “on” opioid receptors only 40%.

Opioids fit into the opioid receptor and turn the key 100% – a partial agonist fits into the lock and only turns it part way but “blocks the lock” while doing that.

 

So buprenorphine both activates AND blocks at the same time.

The result is we “satisfy” the opioid receptor thereby reducing or stopping craving or withdrawal.  It’s the partial agonist effect that gives that “I feel normal without a high” with chronic administration.  An added benefit to buprenorphine is it stays in the opioid receptor better and longer (stays in the lock) than most other opioids, so it can protect against illicit opioid use.

Burprenorphine IS a potent analgesic (pain reliever) like ANY drug that works at the opioid receptor.

 

I don’t want to get lost on the three kinds of opoid receptors but buprenorphine has a unique blend that seems to help uniquely with cancer pain and chronic pain, but not always.

Now let’s bring this home by talking about formulations.

 

All opioids (natural, semi-synthetic and synthetic) are absorbed poorly by the stomach.  Thus, in hospital, we often administer opioids intramuscularly (IM) or intravenously (IV).  One way to bypass the stomach is let the opioid get absorbed through the mouth – that works well (but it tastes bad!). This is why buprenorphine is typically given sublingual (“park it” under your tongue).

Remember, buprenorphine does give some “high” (40% remember?) so in order to satisfy the FDA for safety so that it wouldn’t be crushed and injected, a pharmaceutical company made SUBOXONE ® which has the opioid 100% blocking agent naloxone in it to discourage crush-and-snort or crush-and-shoot. It turns out naloxone is very poorly absorbed through the mouth.  SUBUTEX ® is designed for situations where naloxone needs to be avoided like pregnancy.

In all registered® formulations of buprenorphine, it is only the dose and delivery that are different. There is no magic or perfect “one.”

 

THE AVAILABLE PRODUCTS INCLUDE:

ORAL TABLETS

  • SUBOXONE®
  • SUBUTEX®

FILMS

  • SUBOXONE®
  • BUNAVAIL®
  • ZUBSOLV®

SLOW RELEASE ORAL PATCH

  • BELBUCA® (but it’s really very similar to the oral formulations).

INJECTION

  • BUPRENEX® (IM or IV administration so will only be available in hospital).
  • The “newest kid on the block” will be depot (slow) release over periods from one week to three months. This can help with adherence but introduces a risk; like depot naltrexone (VIVITROL®), the injection can allow for the belief of “Once I’ve got my shot – that’s all I need to stay sober.”

 

Focus more on how a medication is being used to help you achieve your recovery goals, rather that how that medication itself will sustain recovery.

Remember, some medications may help specifically against a specific type of drug (nicotine, opioids, alcohol) but they do not replace the hard work of recovery that is the “inside job” – that is to build a wide-ranging and durable program with as many pillars as possible to fashion a virtual “Fort Knox” against relapse.

 

– Dr. Acampora

 

Dr. A’s blog is meant to generate recovery momentum, to encourage anyone fighting addiction to get, give & keep stability. At the Recovery Research Institute, we oppose stigma, shame & present authenticated approaches to healthy living. We seek practices to deliver permanent change for a durable, sustained recovery.

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