The Veterans Administration recently released guidelines for chronic pain that recommend using buprenorphine if opioids are indicated. That idea has some validity, but the VA, and commenters, get much of the issue wrong.

Buprenorphine is a very potent opioid, a partial agonist, with a ‘ceiling effect.’ That means that buprenorphine activates mu-opioid receptors — the same receptors activated by oxycodone, heroin, or fentanyl — and also tightly blocks those same receptors with an action similar to Narcan (naloxone), the overdose medication.

Available in the US?

Those actions make buprenorphine a complicated medication. When administered for the first time to a person who has other opioid pain meds in his/her system, it will precipitate severe withdrawal symptoms similar to what occurs when a person suffering overdose is given naloxone.

And if administered in the dosage used to treat addiction found in Suboxone, buprenorphine can easily cause severe respiratory depression and death – especially if the person takes a second respiratory depressant like clonazepam (which is often prescribed for PTSD symptoms). I’ve testified in two cases of healthy people who died from taking tiny amounts of Suboxone after drinking alcohol or taking clonazepam. The naloxone in Suboxone is irrelevant to this issue. In both cases where I testified, the people who died took Suboxone, not plain buprenorphine. One took one tab, and the other took a half tab (before Suboxone film was invented).

The ‘ceiling effect’ is a related issue. As the blood level of buprenorphine rises, it eventually reaches a threshold where higher blood levels have no greater effect. When used to treat addiction, a dose of Suboxone or buprenorphine is given that yields a buprenorphine blood level higher than that threshold. If that patient takes a boatload of more Suboxone or buprenorphine, there is no effect.

Patients in addiction treatment quickly become tolerant to that amount of buprenorphine (usually, the person’s tolerance is already higher than that level of opioid stimulation), and as result, the patient feels completely normal. I have had patients who are lawyers, doctors, pharmacists, and truck drivers. There is no impairment after that tolerance forms — and as long as the blood level is maintained above the ceiling threshold, the person feels no opioid effect and no withdrawal.

Congratulations — you now know more about buprenorphine and Suboxone than most pharmacists in northern Wisconsin!

There are many misperceptions out there. Some pharmacists won’t dispense buprenorphine without the naloxone added — even though every information pamphlet you will read explains that naloxone does not affect anything when the medication is taken the usual way, dissolved in the mouth. Even when buprenorphine or Suboxone is dissolved and injected, naloxone does nothing beyond slightly lowering the ‘liking score’ of the drug for about 10 minutes.

Few opioid users would inject buprenorphine, though, because if there is any other opioid in their system, the injection will precipitate severe withdrawal.

Mu opioid receptors are strongly blocked by buprenorphine, so other opioids like heroin and fentanyl won’t produce a ‘high’ when addiction-treatment-doses are on board. Buprenorphine is an amazing medication for treating addiction.

Buprenorphine is approved to treat pain in doses much lower than those used to treat addiction. A standard addiction dose is 16 mg/day, and the highest amount of the transdermal patch indicated for pain contains about 0.5 mg daily. Will VA docs know the difference and the reason for that dose range? I have concerns since articles about the VA decision discuss ‘Suboxone,’ and some even show pictures of that product. One article shows pictures of 0.4 mg buprenorphine tablets, but I don’t believe that formulation is sold in the US. There IS a microgram-dosed buccal film; will docs know to use that expensive drug? Or will they prescribe 8 mg buprenorphine tabs, #60, from Walgreens for $20 (with coupon)?

Many of my addiction patients started opioids when doctors prescribed them for chronic pain. Some patients believe they get some measure of pain relief from their buprenorphine. I typically respond, ‘I doubt it.’ Opioid effects are subject to tolerance. A continuous dose of any opioid will quickly form a tolerance that removes the opioid effect of the drug. Because of the ‘ceiling effect,’ the opioid tone from buprenorphine is ‘perfectly level,’ unlike the tolerance produced by pills. Using buprenorphine for chronic (long-term) pain creates dependency. It will help prevent overdose from other opioids. But it won’t do much for pain.

Even the low-dose pain preparation isn’t that useful for chronic pain. It doesn’t suffer from the ‘ceiling effect’ because it doesn’t create blood levels that high. But it is a skin patch that creates constant blood levels of buprenorphine, which creates almost perfect tolerance.

My other concern is that the VA puts out guidelines for handling surgery in patients on buprenorphine. For elective surgery, those guidelines recommend tapering off ‘high-dose buprenorphine’ before surgery. As a former anesthesiologist, I know that buprenorphine does not have to interfere with an anesthetic in any way. I also see the danger of doing elective surgery on a person who has experienced two weeks of opioid withdrawal and comes to the OR depressed, malnourished, dehydrated, and exhausted.

Buprenorphine can interfere with post-op pain control, but only if the person providing pain control doesn’t understand buprenorphine. The NIH consensus paper on pain control in buprenorphine patients lists three options for post-op pain: increase the buprenorphine, use higher than regular doses of lipid-soluble opioid agonists, or stop the buprenorphine ahead of time. That last option is the worst and the one recommended by the VA. It takes weeks to get buprenorphine out of the body, and the patient will still have a high opioid tolerance. That last recommendation should never have been a part of anyone’s treatment plan.

The benefit of using buprenorphine is that opioid overdose will be largely avoided, providing that buprenorphine isn’t started at full dose in opioid-naive individuals. The downside is that addiction-dose buprenorphine requires patients having elective surgery to suffer through withdrawal, makes pain control after emergency and elective surgery more complex, and prevents short-term use of opioids for acute pain (such as a broken hip). I treat such pain in my patients using 15 mg of oxycodone. Still, I’ve worked in a VA, and I know that few VA docs will provide analgesic doses of opioids necessary to treat post-op or emergency pain in patients on buprenorphine.


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