New Forms of Buprenorphine for Opioid Addiction Treatment

depot injection of buprenorphine

depot injection of buprenorphine

At this year’s American Society of Addiction Medicine conference, researchers talked about innovative ways to dose buprenorphine (formerly known as Suboxone) that may be available in the future.

One of the new products doesn’t yet have a trade name. Researchers call it “CAM 2038.” It’s made by Camurus Pharmaceuticals, a small Swedish company that invented a nanoscale drug delivery system, as they say on their website. This “Fluidcrystal” injection containing buprenorphine comes in preparations of varying doses, and can be dosed once per week or once per month, depending on the preparation.

The liquid substance containing buprenorphine is injected subcutaneously (under the skin), where it forms a gel. Then a capsule-type substance surrounds it, allowing buprenorphine to be into the body over time. The capsulized gel makes the medication time release. Started weekly, the dose can be adjusted to meet patient needs. Eventually, the patient can move to once-monthly injections. The matrix of material is biodegradable, and eventually completely absorbed by the body.

This subcutaneous injection of medication has a very low viscosity, meaning it can be given with small needles that cause less pain to the patient. The medication is already pre-mixed, making it convenient for medical providers, and it is stable at room temperature for up to three years.

This form of buprenorphine is in Phase II trials in Germany now, so it will be some time before it’s even considered in the U.S. for FDA approval. Per the Drug Addiction Treatment Act of 2000, without this FDA approval, it can’t be used to treat opioid addiction. As we know, the buprenorphine implant (Probuphine) was turned down for approval by the FDA earlier this year, likely because the implants didn’t deliver a high enough dose of buprenorphine to patients.

Initial trials with CAM 2038 don’t appear to have this problem. The company’s initial studies show a fast delivery of medication, giving rapid onset and a steady blood level over one week or one month, depending on the preparation given. Safety data was pretty good; other than some headache and a low rate of inflammation at the injection site, it was well-tolerated. Because of the Fluidcrystal technology, if an addict attempts to inject into the vein, it will form a deposit at the injection site, blocking the vein.

Reckitt-Benckiser, the company who makes sublingual brand name Suboxone and Subutex, is developing a medication using a depot technology called Atrigel. Buprenorphine is put into the Atrigel preparation, a precipitation polymer that must be mixed before being injected. This delivery form of buprenorphine is also in Phase II trials now. RB apparently bought exclusive rights to use the Atrigel technology about four years ago.

These injectable depot forms of buprenorphine may be superior to sublingual forms of buprenorphine in the treatment of opioid addiction for several reasons:

First, with daily buprenorphine dosed sublingually, some patients relapse. They may decide to stop taking the buprenorphine for a few days so that they can use their opioid of choice and get high again. True, they have to do a little more planning to relapse than if they were not on buprenorphine, but relapse rates are still too high. The depot forms make relapse less likely, I think, because compliance is assured once the medication is injected.

Second, with the depot forms of buprenorphine, the patients don’t have to think about taking something to treat their addiction. They don’t have to think about their medication at all, and their addiction doesn’t have the chance to urge them to take more of their medication than prescribed. Thankfully with buprenorphine there is a ceiling to its opioid effect, so that patients already on a blocking dose of sublingual buprenorphine won’t usually feel any intoxication from taking more of their medication. But the disease of addiction is always telling the addict, “More!” so injectable forms thwart that urge completely.

Third, we’ve seen recent increases in the numbers of emergency department visits due to buprenorphine. Pediatric exposure remains a huge concern. Unlike pills which must be swallowed to have an effect, children who put the sublingual forms in their mouths will absorb the medication. Any pediatric exposure to buprenorphine is too much; unfortunately there have been a few pediatric deaths as well. With depot forms of buprenorphine, I don’t see how pediatric exposure would be possible.

Fourth, and probably politically most important, diversion of buprenorphine into the black market is getting much attention from press and law enforcement officials. More people are being arrested with illicit buprenorphine tablets and films, and law enforcement personnel believe buprenorphine is a desirable street drug. Of course, research shows most people using it illicitly are trying to prevent withdrawal and not trying to get high. The actual proportion of this medication getting into the black market hasn’t really risen; it’s being prescribed much more, so there’s more buprenorphine to be diverted. But diversion makes buprenorphine look like a desired street drug, and puts the DATA 2000 program at risk. I don’t see how a depot injection can be diverted, though I don’t doubt someone will try.

According to the Drug Addiction Treatment Act of 2000, the FDA must give approval to any form of buprenorphine that’s to be used to treat opioid addiction. At present, only the sublingual form of buprenorphine has that FDA approval. Other forms of buprenorphine in patch (Butrans) or injectable form are illegal for a doctor to prescribe to treat opioid addiction. If these new preparations of buprenorphine get approved, there will be a second delivery form that can be used in patients with addiction.

I like the idea of these depot injections. I’ve decided I don’t want to learn to do the minor surgery required to place Probuphine implants, but I can already do intramuscular and subcutaneous injections. Plus, I’d be seeing the patients once a week or once a month, rather than every six months with the implants. That’s more opportunity to keep track of what is happening with the patient’s addiction treatment counseling, a key component of recovery from addiction.

I’m looking forward to more research on these new forms of treatment.

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11 responses to this post.

  1. Posted by Heather on July 30, 2013 at 12:38 pm

    As always “Janaburson” I thank you for this information. I’m addicted to your blog, no pun intended lol **wink wink**. As if you’re not already busy enough, I wish I could read a DAILY blog entry because your entries are not only relevant to my life, but they are relevant to the most important piece of my life & survival; God willing, I will celebrate 5 years being clean from opiates such as Percocet, methadone, OxyContin, MS Contin & heroin;) I’ve been in Suboxone program since September 8, 2008 and if it WEREN’T for buprenorphine, God only knows where I would be today. I’m famous for teasing almost everyday that I’d love to be featured in a Suboxone commercial (if they ever DID have T.V. commercials because it is, without any question, a life-saver!
    So before I continue to ramble on & on (SORRY!!), I’ll just sum up my comment with: On behalf of ALL addicts that while certainly not ‘cured’, are blessed with a new life and a whole new way of thinking, THANK YOU for dedicating your life in medicine to “helping our cause”. In my eyes, the number of physicians that actually UNDERSTAND the minds & bodies of us addicts is unfairly and extremely small, so whether wrong or right, I can’t help but think that those of you M.D.’s in the addiction field are viewed as “unpopular” by some of your peers, sadly. But you still fight the good fight & it’s doctors such as YOU that I give my most gracious thanks. God Bless.
    H A Reid

    Reply

  2. Posted by kevin on July 31, 2013 at 1:04 am

    I wish they would come up with other ways for methadone….what ever happened to the 30 day box that was being developed with little doors that would only open at there pre-set time. I heard something about this. It was kinda similar to a 7 day pill box like u can buy and most any store except it is electronic and will only open at its set time for each dose or doses depending on the amount. I heard it was gonna be used with all narcotics not just for us that are in addiction treatment

    Reply

  3. This is a most fascinating blog. I am so glad I found it. We introduced suboxone maintenance into all of our treatment programs years ago. My specific focus is on how to use families as a part of the recovery solution rather than as a part of the problem. We were able to dramatically increase engagement rates through “meta” family programs that worked continuously with both family and individual.

    http://www.recoverymaps.com

    Reply

    • I just looked at your website and found it very interesting! I agree with you on family being a huge part of the solution. It’s sad though when a lot of people don’t have family to turn to.
      For example my husband is black and white fella- with NO grey in between.
      He tells me my addiction is sin (which I agree) but he doesn’t believe it’s a disease 🙂 so that makes conversation between us two a little difficult to say the least.
      And my parents are both on opioids themselves and have no plans of getting off, so that makes that a little harder for a recovering person.

      I had no where else to turn but to put my life in a psychiatrists hands 🙂 but I know many who get their main support from family and think that is awesome and the way to go!!!

      Awesome site! Thanks for sharing!

      Reply

  4. The use of buprenorphine for detoxification from opioids is a Best Practice in addiction treatment.The Treatment Improvement Protocol (TIP) series promotes resilience and facilitates recovery from substance use disorders.The effects of buprenorphine last longer than heroin so it is usually prescribed as a once-daily dose. If you begin, you will usually be asked to take it under the supervision of the medical persons who dispenses the buprenorphine to you. This means there can be no doubt about how much buprenorphine you take at each dose. This supervision may be relaxed after a few months of your taking a regular maintenance dose.

    Reply

  5. Posted by Glow on March 20, 2014 at 2:19 pm

    Hi, Jana,
    you write about CAM2038: “This form of buprenorphine is in Phase II trials in Germany now”. Do you mean the Phase I/II trial completed in 2011? I can’t find any other, and Camurus won’t say…
    Thanks,
    Glow

    Reply

  6. Posted by Martin on November 28, 2015 at 1:11 pm

    Cam2038 is now entering stage III in the end of 2015. The Swedish Company camarus is soon to be introduced on the stock market. And your blog explaining the use of cam 2038 better than the prospect for the Investors can do! Well written, thank you. Martin from sweden

    Reply

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