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  • Writer's pictureDr. Harold Pierre

Buprenorphine for Chronic Pain Management: A Systematic Review

Updated: Jan 11


Buprenorphine for Chronic Pain Management: A Systematic Review of Treatment Options

Chronic pain impacts millions globally. Finding effective solutions is vital. This review examines using buprenorphine for chronic pain management. Various formulations like buprenorphine buccal film, sublingual, and transdermal systems are analyzed. The article dives deep into the action and mechanisms of buprenorphine. It is worth reading for anyone seeking comprehensive information on opioid options for chronic pain, focusing on buprenorphine.


What is Chronic Pain?


3D rendering illustration of the human anatomy showing chronic pain

Chronic pain persists over 3-6 months, unlike acute pain resolving with injury healing. Nearly 1 in 5 U.S. adults have chronic pain from causes like arthritis (i.e. patients with chronic low back pain), nerve damage, and unknown origins. It impairs quality of life and requires complex treatment addressing physical, mental, and emotional aspects. Left untreated, it negatively impacts physical and mental health. Chronic pain places major economic burdens through healthcare costs and lost productivity. Treatment focuses on reducing pain and improving function through medications, therapy, lifestyle changes, and more. With proper management, quality of life can improve significantly.


Coping with chronic pain is an important part of treatment. This can involve changing negative thoughts, setting achievable goals, and finding meaningful activities. Support groups and therapy can provide needed understanding and tools for coping. While chronic pain may not be completely curable, treatment can significantly improve quality of life.

Patients often see me after failing other treatments. They present on high doses of opioids. Over time, these high opioid doses worsen function. I believe buprenorphine is the best chronic pain medication. Formulated in buccal films, sublingual tablets, and topical patches makes it adaptable. Buprenorphine activates opioid receptors to reduce pain signals as a partial agonist. Unlike morphine and oxycodone, it may be safer at higher doses.


Buprenorphine in the Treatment of Chronic Pain


Buprenorphine is a powerful medication. It's used commonly used for opioid addiction. However, I believe it is the best medication for chronic pain. It comes in different forms making it very versatile and adaptable to patient's needs.


What is Buprenorphine?


Buprenorphine is an opioid medication used to treat moderate to severe chronic pain. It works by activating the opioid receptors in the brain and nervous system to reduce pain signals. Buprenorphine is considered a partial opioid agonist. This means it activates the opioid receptors enough to relieve pain, but does not suppress breathing as strongly as full agonists like morphine or oxycodone.


It comes in various forms. Sublingual buprenorphine tablets are common. Transdermal buprenorphine is another option. Buprenorphine buccal film is also available. These options offer different ways to treat chronic pain.


Buprenorphine tablets spilled on a bluish white background

What Makes Buprenorphine Unique?


Buprenorphine has unique properties that distinguish it from other opioid medications used for pain management. Several factors make buprenorphine a safer alternative to opioids like morphine, oxycodone, and fentanyl.


First, buprenorphine is a partial rather than full opioid agonist. It binds to and activates the brain's opioid receptors, but not to the same degree as full agonists. This “ceiling effect” reduces risks of respiratory depression and overdose death at higher doses.


Second, buprenorphine dissociates slowly from opioid receptors in the brain. This prolongs its pain-relieving effects and allows for less frequent dosing. The long-acting property also minimizes withdrawal symptoms when stopping the medication.


Third, buprenorphine has lower intrinsic activity at opioid receptors. This results in less euphoria compared to other opioid agonists, making it less likely to be misused or abused. The lower abuse potential makes buprenorphine more readily accessible than other controlled substances.


Fourth, buprenorphine is available in formulations like transdermal patches and long-acting injections. These options provide steady delivery of the drug over days or weeks. This is unlike short-acting opioids that require dosing every few hours.


Finally, buprenorphine seems to cause fewer hormonal and immune system changes compared to other opioids. This may result in fewer long-term side effects with prolonged use.


Detailed Mechanism of Action of Buprenorphine


As mentioned earlier, the clinical pharmacology of buprenorphine is unique among opioids. It has a unique receptor binding profile that differentiates it from other opioid medications used for pain relief. Lets look at the details. It binds to all three major opioid receptor types in the brain and spinal cord: mu, kappa, and delta. Buprenorphine also attaches to the orphanin receptor but with much lower affinity.


Its distinctive mechanism of action gives buprenorphine both analgesic and safety advantages. At mu opioid receptors, buprenorphine acts as a partial agonist. This means it does not fully activate the receptor like opioids such as morphine or fentanyl. As a result, buprenorphine displays a ceiling effect on dangerous side effects like respiratory depression.


Research shows the pain relieving effects of buprenorphine depend on a newly discovered mu receptor subtype called the arylepoxamide receptor. Mice without this receptor target did not experience analgesia from buprenorphine. Other opioids that require this receptor include nalbuphine and butorphanol, which also have ceiling effects.


In contrast, most potent opioids work through traditional mu opioid receptors to produce both analgesia and serious adverse effects. The unique arylepoxamide receptor interaction contributes to buprenorphine's improved safety profile.


At kappa opioid receptors, buprenorphine acts as an inverse agonist. Blocking kappa receptor overactivity is linked to reducing pain hypersensitivity and lessening side effects like sedation and dysphoria. The kappa antagonism may also contribute to buprenorphine's antidepressant effects.


Buprenorphine displays biased signaling at mu opioid receptors. It activates beneficial pain relieving pathways without recruiting beta-arrestin. Avoiding beta-arrestin interactions prevents mu receptor downregulation on neuron surfaces. Traditional opioids trigger beta-arrestin, which amplifies side effects like tolerance, constipation and respiratory depression.

The distinctive structure of buprenorphine causes a high mu receptor binding affinity and slow dissociation off the receptor. This long receptor occupancy time determines its prolonged analgesic effects. Buprenorphine also blocks voltage-gated sodium channels, which provides additional pain relief.


In summary, buprenorphine has a one-of-a-kind receptor binding and signaling profile compared to other opioid medications. Its unique mechanism produces potent pain relief with a ceiling on life-threatening respiratory effects and less tolerance. These advantages lead to an improved therapeutic window that differentiates buprenorphine for treating chronic pain.


Different Formulations of Buprenorphine


Buprenorphine written on a sticky note isolated on a wooden table copy

Buprenorphine is available in several different formulations and brand-name products for treating opioid addiction and chronic pain. The dose of buprenorphine is dependent on the bioavailability (absorption into the bloodstream).

  • Suboxone (buprenorphine and naloxone) is a brand used for opioid addiction. This contains buprenorphine combined with the opioid antagonist naloxone. The addition of naloxone lowers the potential for abuse if injected. Suboxone comes as a sublingual film or tablet taken daily.

  • Zubsolv (buprenorphine and naloxone) is another brand that provides sublingual tablets of buprenorphine with naloxone. It contains a higher ratio of buprenorphine to naloxone compared to traditional Suboxone.

  • Bunavail (buccal buprenorphine and naloxone) and Cassipa are buccal film formulations of buprenorphine/naloxone. They adhere to the inside of the cheek and dissolve to release the medication.

  • For pain management, common brand names for buprenorphine without naloxone include Belbuca, Buprenex, and Butrans.

  • Belbuca (buccal buprenorphine) provides weekly buccal films that stick to the cheek. It is available in varying strengths.

  • Buprenex comes as an injectable solution given intravenously or intramuscularly. It is often used for acute pain relief.

  • Butrans (buprenorphine transdermal system) is a transdermal patch applied to the skin weekly. It continually releases buprenorphine through the skin over 7 days.

Some newer long-acting buprenorphine products for chronic pain include Buvidal and Sublocade. Buvidal is a monthly subcutaneous injection while Sublocade is given as a monthly intramuscular shot.


Research is also looking at implanted drug delivery systems and other extended-release formulations of buprenorphine for pain management. Having more options allows the medication to be tailored to each patient's needs.


Systematic Review of Buprenorphine Effectiveness


A recent systematic review examined the effectiveness of buprenorphine in managing chronic pain. The review looked at multiple clinical studies on using buprenorphine patches, tablets, and injections for pain relief.


The researchers found 14 randomized trials comparing buprenorphine to morphine and fentanyl. Buprenorphine reduced pain more than morphine and had fewer side effects like constipation. Patients on morphine also stopped treatment more often. Transdermal buprenorphine caused less nausea than fentanyl patches. However, the wide confidence intervals in the data made the results less conclusive.


Additional studies showed mixed findings on side effects of transdermal buprenorphine versus fentanyl. Fentanyl caused more constipation but rates of other side effects were similar between the two medications. The researchers concluded buprenorphine likely has a better safety profile than morphine and fentanyl. But more research is needed, especially in elderly, sick, or kidney disease patients.


The review also examined trials of sublingual buprenorphine tablets for cancer and chronic pain. These were lower quality observational studies with a high risk of bias. On average, the tablets reduced pain scores by 2-3 points on a 10-point scale. Side effects like nausea were worse with the tablets compared to the patches.


Eight studies looked at transdermal buprenorphine for cancer pain. Buprenorphine improved pain relief compared to placebo. Side effects were less frequent than morphine and similar to placebo. But most studies were small with fewer than 100 patients. There was insufficient evidence for the sublingual tablets in treating cancer pain.


No randomized trials have properly assessed buprenorphine for neuropathic pain. More research is needed to demonstrate its benefits for nerve pain conditions.


Overall, the review concluded there is moderate evidence for buprenorphine's effectiveness in chronic pain management. More high quality head-to-head comparisons with other potent opioids are necessary. Buprenorphine appears to have a better safety profile and less tolerance over time. This makes it a reasonable option when standard pain medications have failed or caused side effects.


The review discussed important practical issues with using buprenorphine. For post-surgery pain, combining buprenorphine with short-acting opioids can provide adequate relief. Rotating from high doses of opioids like morphine to buprenorphine requires careful timing to prevent withdrawal symptoms. While licensed for addiction treatment, buprenorphine tablets can also be prescribed off-label for pain when specified on the prescription.


Long Term Efficacy and Safety of Buprenorphine for Moderate to Severe Pain


Multiple clinical trials studied buprenorphine for over 6 months. They assessed general, back, osteoarthritis and cancer pain patients. Buprenorphine provided significant pain relief in all these long term studies. Patients also needed less breakthrough medication over time on buprenorphine.


In a 5.7 year study, most patients reported buprenorphine was effective long term. Sleep quality, duration and mood also improved over years of treatment. Another 3 year study found consistent pain reduction with buprenorphine.

12 week studies in osteoarthritis and back pain patients showed sustained pain relief and improved sleep and daily function on buprenorphine. Benefits increased over the length of the trials.


A 3 year post-marketing study also found buprenorphine safe long term. Side effects were consistent with short term studies. Respiratory depression was extremely rare in over 13,000 patients.


I am Here to Help


When you searched “Chronic Pain Doctor Near Me” or “Suboxone Doctor Near Me” and found me, I believe you found the best clinic for buprenorphine services in the Tulsa area. I lead a team with decades of experience, and a commitment to providing you with comfort, care, and respect as you navigate this challenging time in your life. We also make treatment super convenient with hours of operation that extend from 0800 AM to 0900 PM, 7 days a week through scheduled appointments, accept most insurances, making addiction treatment accessible to practically all who call. I am waiting for your call.


Conclusion


Buprenorphine is a key player in chronic pain management. Here are some important things to remember:

  • Chronic Pain: A serious and lasting problem.

  • Buprenorphine: An opioid used for pain relief.

  • Formulations: Includes sublingual, transdermal, and buccal forms.

  • Action: Unique action on multiple receptors.

  • Efficacy: Proven effective for chronic pain.

  • Safety: Generally considered safe and tolerable.

This systematic review sheds light on buprenorphine. It's a must-read for understanding pain management options. It offers hope to those struggling with chronic pain.


About the author:

Dr. Harold Pierre is a board-certified anesthesiologist and addiction medicine specialist with over 20 years of experience. He is board-certified by the American Board of Anesthesiology and the American Board of Preventive Medicine.


This website is provided for educational and informational purposes only and does not constitute providing medical advice or professional services. The information provided should not be used for diagnosing or treating a health problem or disease, and those seeking personal medical advice should consult with a licensed physician or another qualified medical professional. Never disregard professional medical advice or delay in seeking it because of something you have read on this website.




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