Suboxone Side Effects pt. 2

We can now leave naloxone out of the discussion, and focus on the side effects of Suboxone that are caused by buprenorphine. Side effects are symptoms caused by a given medication that are not part of the therapeutic benefit of that medication.  Whether a symptom is a side effect depends on the reason for taking […]

Additional Programming

Last post about the odds and ends of blogging…. today I spent some time reading over the intent of the people behind Twitter. I read that a billion tweets are sent every…. well, every something-or-other, and the number was astouding. I can see all sorts of benefits, once I figure out how to get it […]

Publicize me please!

While I’m on the topic of ‘content’, I’ll take a moment to ask readers to share a post if you find it interesting.  Social media is THE way to increase readership these days.  I realize that the content matter– addiction– is less likely to end up on Facebook than a picture of puppies (maybe I […]

It Might Not Be Me– Suboxone Talk Zone Impersonators

Just a quick note that I’ve been meaning to write for several weeks…  Over the past few months I’ve come across more and more web sites that have copied my web sites, copied my material, used my name, reposted my videos, resold my ‘user’s guide’… Someone once said that imitation is the sincerest form of […]

New Mobile App

I have created a mobile app for Suboxone Talk Zone, SuboxForum, my YouTube videos about buprenorphine, SubocDocs doc finder… a one-stop app for information about buprenorphine, Suboxone, and opioid dependence.  If the app is accepted by Apple, it will eventually appear among their i-Tunes application downloads.  But for now, if everything is working correctly, you can get […]

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Withdrawal Symptoms on Suboxone

I struggle with the length of my posts.   I shoot for 1000 words—an amount of reading that most people can knock off in a typical trip to the bathroom— but I find it difficult to limit posts to that size.  So as I have done in the past, I will break this post into a […]

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Codeine Never Works For Me…

The FDA recently released a Drug Safety Announcement about the use of codeine in young children after tonsillectomy/adenoidectomy surgery for obstructive sleep apnea.  I was somewhat surprised to see a safety announcement on a medication that has been in use for decades, but the release underscores our improved knowledge of drug metabolism, and the broadening demographics […]

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Dear CEO

I’m going to start by paraphrasing John Le Carre’s comments in his book The Constant Gardener: “Nobody in the letter below is based upon an actual person or outfit in the real world. But I can tell you this; as my knowledge of the pharmaceutical world increases, I come to realize that, by comparison with […]

Post-op Pain on Suboxone

I often receive emails from patients on buprenorphine (or Suboxone) who are preparing for surgery or other painful medical procedures. Ideally in such cases, the surgeon would have a discussion with the person prescribing buprenorphine, in order to coordinate the plan for treating postoperative pain. In practice such discussions don’t seem to take place, leaving patients to scramble for effective pain control after surgery– when it is too late to take the steps necessary for a smooth perioperative course.

I am familiar with an NIH article that describes pain control in people who take buprenorphine. I’ve also prepared a handbook that describes the issues that must be considered in such patients; the handbook can be found easily-enough by searching for the User’s Guide to Suboxone.

Even with those descriptions ‘out there,’ I’ll get requests for a short, ‘just-the-facts’ note that patients can give to their surgeons. I realize that unfortunately, the average surgeon will not sit down for an in-depth discussion of post-op pain control, so I have prepared a few paragraphs that lay out the issues. People on buprenorphine who are having surgery are welcome to copy the paragraphs below and give them to their surgeons, in order to facilitate discussion.

Surgery in Patients on Buprenorphine

Buprenorphine is a partial opioid agonist that is used for several indications. In low doses—less than 1 mg—buprenorphine is used to treat pain (e.g. Butrans transdermal buprenorphine). In higher doses i.e. 4 – 24 mg per day, buprenorphine is used as a long-term treatment for opioid dependence and less often for pain management. At those doses, Buprenorphine has a unique ‘ceiling effect’ that reduces cravings and prevents dose escalation. Patients taking higher dose of buprenorphine, trade name Suboxone or Subutex, become tolerant to the effects of opioids, and require special consideration during surgical procedures or when treated for painful medical conditions.

There are two hurdles to providing effective analgesia for patients taking buprenorphine: 1. the high opioid tolerance of these individuals, and 2. The opioid-blocking actions of buprenorphine. The first can be overcome by using a sufficient dose of opioid agonist, on the order of 60 mg per day of oxycodone equivalents or more. The second can be handled by either stopping the buprenorphine a couple weeks before agonists are required—something that most patients on the medication find very difficult to do—or by reducing the dose of buprenorphine to 4-8 mg per day, starting the day before surgery and continuing post-operatively. Given the long half-life of buprenorphine, it is difficult to know exactly how much remains in the body after ‘holding’ the medication. That fact, along with the difficulty patients have in stopping the medication, leads some physicians to use the latter approach- i.e. to continue 4 mg of buprenorphine per day throughout the postoperative period. People taking 4-8 mg of daily buprenorphine report that opioid agonists relieve pain if taken in sufficient dosage, but the subjective experience is different, in that there is no feeling of euphoria.

Quick Notes:

Patients taking maintenance doses of buprenorphine do NOT receive surgical analgesia from the medication, as they are completely tolerant to the mu-opioid effects of buprenorphine after the first week or so on the medication.

Discontinuation of high dose buprenorphine or Suboxone treatment results in significant opioid withdrawal symptoms within 24-48 hours.

Normal amounts of opioid pain medication are NOT sufficient for treating pain in people on buprenorphine maintenance.

Opioid agonists will NOT cause withdrawal in people on buprenorphine. Initiating buprenorphine WILL cause withdrawal in someone who is tolerant to opioid agonists, unless the person is in physical withdrawal before initiating buprenorphine.

Non-narcotic pain relievers CAN and should be used for pain whenever possible in people on buprenorphine to reduce need for opioids.

Ceilings

A question was asked about the last post that warrants top billing:

“Buprenorphine acts similar to opioid agonists in lower doses, with the same addictive potential as oxycodone or heroin. In higher doses—doses above 8 mg or 8000 micrograms per day—the ‘ceiling effect’ eliminates interest and cravings for the drug.”

Buprenorphine Ceiling Effect

Ceiling Effect

I’m not sure I followed this. Can you explain more? What would you think about someone who is taking 1-2mg of Suboxone twice a day without a prescription, and says they want to stay on that dose once they find a prescriber? Are they better off on 8mg or more per day, or would it be ok for a prescriber to keep them at the lower dose? Is the answer the same if they hope to taper off the medication completely within a year (they don’t feel able to do this on their own right now, but hope to be able to when some life circumstances change). Thanks!

This gets a bit complicated, but I’ll do my best. A couple background issues; buprenorphine has a ‘ceiling’ to its effect, meaning that beyond a certain dose, increases in dose do not cause greater opioid effect. That is the mechanism for how buprenorphine blocks cravings.

If the blood level of buprenorphine is ABOVE that ceiling, the opioid receptors are maximally, 100% stimulated. If the person takes more buprenorphine, and the blood level increases, the opioid receptors don’t feel the increase, as they cannot be stimulated more than 100%. But more importantly: when the person takes less, and the blood level of buprenorphine goes DOWN, the receptors also sense nothing– as long as the level stays above the ‘ceiling’ level.

Read the above paragraph, and think on it until you grasp it– as it explains buprenorphine and Suboxone. If you understand that paragraph, you will know more about Suboxone than most doctors!

Below that ceiling level, the opioid effect from buprenorphine varies directly with dose—just as with oxycodone, hydrocodone, heroin, etc. Medications that have effects that increase with dose are called ‘agonists’. Buprenorphine is a ‘partial agonist;’ it acts like an agonist up to point, the ceiling effect, beyond which increases in blood level have no greater effect.

The level of this ‘ceiling’ varies from one person to the next, depending on efficiency of absorption (on average, only a third of a dose is absorbed from under the tongue), body size, liver function, differences in regional blood flow, and the presence of other medications that affect buprenorphine metabolism. In order for buprenorphine to have the unique, craving-blocking effects, the blood level of buprenorphine must stay above the ceiling level, for the reasons described above.

Lower levels (blood levels of buprenorphine below the ceiling level) still have SOME effects on cravings. Buprenorphine has a long half-life, an that alone reduces the desire to take more—especially if the medication is taken more than once per day– since the blood level drops very little between doses. For agonists or for buprenorphine below the ceiling level, drop in blood level equals drop in opioid effect, equals sense of things wearing off, equals cravings.

But the classic method for treating with Suboxone, as described in the certification course, is for it to be given at a high enough dose to stay above the ceiling level… and dosed only ONCE per day. If the blood level stays above the ceiling level, once-per-day dosing covers cravings completely. Yes, people still want to take more, especially initially, but that desire is not driven by chemical effects; the desire is instead based on psychological factors, like habit, or from being accustomed to feeling better after a dose, and getting a placebo ‘lift’ from taking a second dose.

A person can eliminate that second dose fairly easily, providing that the morning dose is high enough, i.e. usually 8-16 mg. To eliminate the second dose, the person should distract him/herself as soon as the thought about taking the second dose comes to mind. Immediately, do anything else—the dishes, call a friend, wrestle with the dogs… and the thought will pass. If the person does the distraction method for a few days, the need to take the second dose will go away—a psychological process called ‘extinguishment.’

Dosing every other day, and even every third day, has been studied; people cannot tell the difference, if the dose is raised enough to keep the blood level above the ‘ceiling’ (providing the person is given a placebo that tastes the same).

As for as the writer’s friend… I’m not a fan of any illicit use, but I am aware of the shortage of physicians. When the person has a physician, in my opinion the person should be prescribed a dose that allows for once per day dosing. Realize that buprenorphine wears off VERY slowly; it takes over three days for half of a dose to leave the body! So that ‘need’ to take more is almost always entirely learned or ‘conditioned.’ The medication does not wear off in that short period of time.

Even if the person has withdrawal symptoms, the sensations are almost surely imagined. How to tell? Use the distraction method, and note that a couple hours later, when the person remembers that the dose was skipped, note that the withdrawal went away. That doesn’t happen with ‘real’ withdrawal!

The sense of withdrawal that drives the second dose is simply a memory; a conditioned response that the body has that triggers the person to take more opioid. We become conditioned by drug use, just like the salivating dogs from science books! In the case of opioids, whenever we feel down, we think that an opioid will lift us up, as it has hundreds of times before. And even if what is taken is not a real opioid, the mind ‘feels’ a boost, just from expecting what has always happened in the past.

As for tapering, I look at many factors in order to recommend, or not recommend, stopping buprenorphine—things like age, presence/absence of using friends or contacts, physical health, mood, support network, personal motivation to stop buprenorphine, ability or lack thereof to dose once per day, consistently, number of relapses and personal ‘recovery’ plan, etc.

Realize that EVERYONE looks forward to a day when life circumstances will change for the better—but most of the time, life becomes more, not less challenging. Yes, it is nice to have a reliable job… but it is much more stressful being the sole breadwinner for a family with children, than working to pay for one’s self! Marriages settle down in some ways over time, but they also lose the intense infatuation that can gloss over personal differences.

As I have often written, it is VERY hard to stop opioids. It is a little easier to stop buprenorphine; I am convinced of that fact because I have seen opioid addicts taper off buprenorphine, but I know of no opioid addict who tapered off an agonist. But SOME people cannot taper of ANY opioids—including buprenorphine. I do not consider those people ‘addicted’ to buprenorphine, because they lack the constant obsession for opioids that is so destructive to the mind of an active addict. But they ARE physically dependent on buprenorphine— a fair trade, in my opinion, for a life of chaos, broken relationships, legal problems, and death.