SAFETY ALERT FOR ORAL BUPRENORPHINE
In January 2022, the Food and Drug Administration (FDA) issued a
More than ever, patients have easy access to information once read only by scientists and medical professionals. And at the same time, doctors have reduced the time spent with patients during appointments. The result has been an increase in internet-educated patients, who come to appointments armed with data from package inserts, information from internet health forums, and stacks of questions from net-savvy relatives.
There is a good side to this process, of course. Patients are wise to take greater interest in their personal health, and to be knowledgeable of medications that they are taking. And whether good or bad, the situation is necessary, given the abdication by many physicians of their roles as educators.
But there are downsides to the situation as well. Package inserts provide studies and odds ratios for the risks from medications, but interpreting the studies and odds ratios requires education and experience. Some data is reported in a way that a person without considerable education in statistics would have a hard time deciphering what is or isnt relevant. Some patients struggle under the burden of calculating and weighing risks, and prefer to have a careful, caring doctor provide his/her opinion whether a medications is safe or not. Speaking from my role as physician, I am frustrated when patients choose to follow advice from an online forum over a recommendation based on medical knowledge or a careful literature search..
Doctors sometimes add to the problem. I am frustrated when doctors make claims that are not supported by best medical practice or by medical science. Distinctions between sources of information are blurred, so that some facts are based on nothing but rumor. The process is like the old telephone line game; a doctor reads a question about a medication or illness, and responds with his/her opinion. Another doctor then hears or reads that answer, adopts it as fact, and shares it with other doctorswho then reinforce the factual nature of the information.
People tend to take information from physician educators/writers verbatim, as if the act of putting information online, in writing, guarantees that it to be true. People are confused when they read conflicting facts or recommendations from people with comparable credentials.
I try, when writing here, to differentiate between facts, best medical practice, and personal opinion. If someone asks how long should I stay on Suboxone?, Ill reply that several studies show high relapse rates in people who stay on Suboxone for less than 6 months (fact), that more and more physicians are keeping patients on the medication long-term (medical practice), and that in my opinion, many people are best off staying on the medication for an extended period of time. You get the idea.
I think it is because of my PhD training that I tend to take a closer look at things that everyone knows and ask, says who? History has given us many examples of things that everyone knew that turned out to be wrongfrom the connection between autoimmune disease and breast implants that wasnt, to global cooling, the impending disaster when I was a kid (read the Newsweek story on this page)and we all know how THAT turned out!
The treatment of opioid dependence with buprenorphine/Suboxone appears to be particularly vulnerable to misinformation. Some examples:
The naloxone in Suboxone prevents the person from getting high: Naloxone is not active orally or sublingually, and is added to Suboxone to prevent intravenous injection of the medication. Confusion comes in part from mistaking naloxone, an IV medication, with naltrexone, an orally-active medication that is NOT part of Suboxone.
People will abuse Subutex because it doesnt have the opioid blocker in it:Subutex or the generic equivalentbuprenorphineworks just like Suboxone when taken correctly. Doctors and pharmacists are mistaken when they believe that buprenorphine is more addictive if naloxone is not included. In reality, the subjective effects of Suboxone and Subutex are identical. There IS a relatively low incidence of intravenous abuse of buprenorphine; Suboxone in theory causes withdrawal if injected because of the presence of naloxone. Realize, though, that the effects of buprenorphine or Suboxone are similar, whether injected or taken correctly. Injected buprenorphine has the same ceiling effect as does sublingual buprenorphine, and so people on buprenorphine maintenance would NOT experience an opioid high after injecting their medicationany more than they do when taking it sublingually.
The tablet should not be crushed or chewed: The package insert recommends that Suboxone tablets should be taken sublingually, without crushing the tablet. I am guessing that the recommendation comes out of an attempt to standardize the bio-availability of buprenorphine. Studies show that as little as 15% of a dose of buprenorphine is absorbed, and in my opinion, the high cost of the medication warrants efforts to reduce the amount that gets wasted. The bio-availability is affected by the concentration of buprenorphine in saliva, the surface area available for absorption, and the time that the medication is in contact with absorptive surfaces. Passage of buprenorphine through mucous membranes is the rate-limiting step for absorption–NOT dissolution of the tablet. In other words, crushing or chewing the tablet does NOT cause a high, and is NOT a sign of drug-seeking behavior. Neither does crushing or chewing hasten the onset time of a dose of Suboxone.
Discussions about chewing or crushing buprenorphine provide examples of the doublespeak that only confuses people. My own recent discussion with another Suboxone prescriber went like this: I dont want patients to crush or chew the tablet because that will make it get absorbed too quickly. In fact, I usually recommend the film, because it dissolves much more quickly than the tablet. Say what? Do we want it to dissolve more quickly or not? The truth is that it really does not matter. The dissolving of buprenorphine— or the film– is the LONG part of the process.
The veins under the tongue absorb the drug in Suboxone. Actually, buprenorphine passes through all of the surfaces in the mouth, eventually entering capillaries under the surface. The veins under the tongue absorb little or no buprenorphine.
You must stop smoking cigarettes if you are on Suboxone: I have searched the literature and I have talked to folks at Reckitt Benckiser, and I can find no evidence to back up this claim. Scientifically, I cannot think of a reason that cigarette smoking would affect the absorption of buprenorphine, except perhaps to increase production of saliva, diluting the buprenorphine in solution and reducing diffusion into tissues. I doubt this would have any significant effect on the bio-availability of buprenorphine, and my clinical experiences backs that up. Patients in my practice who smoke have had normal responses to buprenorphine or Suboxone.
You cant take pain pills if you are on Suboxone: Actually you can, but they will only reduce pain if the dose is sufficient. I often use this approach to treat people on buprenorphine who undergo surgery. But problems ARE caused if a person does things in the opposite order. In that caseif someone taking opioid agonists then takes buprenorphine– there is risk that the person will develope precipitated withdrawal, depending on the amount of opioid agonist that was being used.
The longer you are on Suboxone, the harder it is to stop: I have read no studies supporting this oft-read comment, and I can think of NO reason that it would be true. The tolerance to buprenorphine is set by the ceiling effect of the drug, and once tolerance develops, typically by several weeks on the medication, longer periods of time do not push tolerance higher.
The film formulation is safer than the tablet. Says who? If we are worrying about kids getting their hands on Suboxone, yesthe little orange tablets look like candy to a toddler. But little red strips of flavored material appear appetizing as well. ALL medications should be kept away from children. If the safety concerns are directed toward patientsfor example one doctor told me he prescribes the film because it cannot be crushedremember that crushing Suboxone is not a problem. I SUSPECT (only my opinion) that the change in formulation was a marketing ploy aimed toward preventing acceptance of generic buprenorphine tablets. Reckitt Benckiser apparently convinced the state of Wisconsin to cover the film exclusively, rather than allow addicts the choice of taking generic buprenorphinea medication that works exactly the same as Suboxone, at about half the cost.
I think you get the idea. Whether thinking about Suboxone or another medication, I urge readers to always ask the question, says who? There are MANY experts out there on the internetand some exhibit more restraint in their comments than others. Ask yourself, what is the mechanism for what is being described? And if it doesnt seem to make sense, consider that just perhaps, youre the right one.
Photo by Kevin Clauson, available under a Creative Commons attribution license.