Is there literature to support the use of buprenorphine sublingual tablets for chronic pain?

Comment by InpharmD Researcher

The 2022 CDC guidelines for prescribing opioids in chronic pain acknowledge the use of buprenorphine in general for pain management, but primarily make recommendations for buprenorphine in patients with opioid use disorder who are experiencing acute pain. Data on the use of sublingual buprenorphine for chronic pain is summarized in Table 1, but high quality prospective studies are lacking to extrapolate efficacy and safety.

Background

The 2022 Centers for Disease Control and Prevention (CDC) guidelines for prescribing opioids in chronic pain acknowledge the use of buprenorphine in pain management, but primarily makes recommendations for buprenorphine in patients with opioid use disorder who are experiencing acute pain. Buprenorphine dosage forms and use in chronic pain are not discussed. [1]

According to a 2018 systematic review, buprenorphine may exhibit lower rates of constipation and discontinuation versus morphine with comparable chronic pain analgesia. Despite being oral, sublingual buprenorphine tablets demonstrate a bioavailability rate of ~50% relative to parenteral buprenorphine. Peak plasma concentrations occur at 90 mg for sublingual tablets. Newer buprenorphine/naloxone tablets approved by the US in 2013 also deliver greater sublingual bioavailability and faster dissolving rates, but how this translates to pain control is not yet certain. While the buccal formulation has not yet been compared to other opioids, studies have demonstrated pain reduction in opioid tolerant and naïve patients. In general, the studies reviewed suffered from heterogeneity from various qualities of randomized and non-randomized trials as the authors expressed difficulty finding high-quality RCTs. [2], [3]

A 2014 systematic review of 10 studies between 1979-2012 evaluated the efficacy of sublingual buprenorphine (with or without naloxone) for the treatment of chronic pain in 1,190 cancer and noncancer patients. Four studies were general chronic pain while other studies assessed osteoarthritis, sickle-cell disease, nociceptive chronic pain, chronic pain in the elderly, pediatric chronic cancer pain, and cancer chronic pain. Four studies included patients on prior opioid therapy (morphine equivalent daily dose up to 840 mg/day) using SL buprenorphine >400 mcg/dose (high dose). The other 6 studies used SL buprenorphine <400 mcg/dose (low-dose). All studies reported some effectiveness for analgesia in chronic pain. Due to the heterogeneity of the studies, data could not be pooled and findings were described through qualitative syntheses. These outcomes varied in methods to include a decrease in mean pain score using visual analog or numeric rating scales, a narrative description method, and degrees of pain relief including “acceptable”, “Moderate to very good”, and “good to excellent”. For those that reported statistical significance, they demonstrated a decrease in mean pain score by 2.3/10 (p <0.001), 6.6/10 to 2.1/10 (p <0.01), and 2.1/3 to 1.1/3 (p <0.01). Low-dose studies reported a dosing range of 0.1-3.2 mg/day in adults. One RCT of low-dose SL buprenorphine described mean morning pain score decreased from 5.9/10 to 3.1/10 and equivalence of SL buprenorphine 0.2-0.4 mg every 6-8 hours to transdermal buprenorphine 5-20 mcg/h although a higher incidence of nausea, dizziness, and vomiting noted (p <0.05). Various protocols were used in the high-dose SL buprenorphine studies regarding concurrent opioid therapy, all reporting improved pain scores. While SL buprenorphine appeared effective as a chronic pain analgesic, the studies were observational (exception of 1 RCT) with low level of evidence concluding the quality of evidence was not sufficient to provide consensus. [4]

Another 2018 systematic review investigated the efficacy of various buprenorphine formulations, including sublingual buprenorphine tablets. Three included studies investigated the efficacy of SL buprenorphine, generally finding no significant improvement in pain when comparing SL buprenorphine to comparators (memantine, transdermal buprenorphine, and tramadol). None of the included studies compared buprenorphine to placebo, which may hinder true assessment of efficacy. [5]

References: [1] Dowell D, Ragan KR, Jones CM, Baldwin GT, Chou R. CDC Clinical Practice Guideline for Prescribing Opioids for Pain — United States, 2022. MMWR Recomm Rep 2022;71(No. RR-3):1–95. DOI: http://dx.doi.org/10.15585/mmwr.rr7103a1
[2] Davis MP, Pasternak G, Behm B. Treating Chronic Pain: An Overview of Clinical Studies Centered on the Buprenorphine Option. Drugs. 2018;78(12):1211-1228.
[3] Fishman MA, Kim PS. Buprenorphine for Chronic Pain: a Systemic Review. Curr Pain Headache Rep. 2018;22(12):83.
[4] Cote J, Montgomery L. Sublingual buprenorphine as an analgesic in chronic pain: a systematic review. Pain Med. 2014;15(7):1171-1178. doi:10.1111/pme.12386
[5] Aiyer R, Gulati A, Gungor S, Bhatia A, Mehta N. Treatment of Chronic Pain With Various Buprenorphine Formulations: A Systematic Review of Clinical Studies. Anesth Analg. 2018;127(2):529-538. doi:10.1213/ANE.0000000000002718
Literature Review

A search of the published medical literature revealed 1 study investigating the researchable question:

Is there literature to support the use of buprenorphine sublingual tablets for chronic pain?

Level of evidence

C - Multiple studies with limitations or conflicting results  Read more→



Please see Table 1 for your response.


 

Studies Using Sublingual Buprenorphine for Chronic Pain

Study

N

Duration Population Prior Opioid Therapy

Buprenorphine SL Dose

Analgesic Outcome

Adriaensen et al. 1985

70

Few days to over 4 weeks Chronic pain None 0.4-3.2 mg/day, in divided doses Mean degree of pain relief moderate to very good in majority of patients

Bach et al. 1991

453

Median 39 days Chronic pain; nociceptive NR Median 0.6 mg/day compared to 60 mg/day SR morphine SL buprenorphine: Acceptable pain relief if 77.6% vs 80% with SR morphine

Brema et al. 1996

131

Up to 6 mo Cancer pain N/A 0.2 mg every 6-8 h compared to tramadol 100mg every 8-12 h VAS posttreatment scores: tramadol 6.09 ± 2.78; buprenorphine 4.74 ± 2.6 (p < 0.05)

Daitch et al. 2012

104

> 60 days Chronic pain Mean MEDD 180 mg/day 8-32 mg/day Mean pain score decreased by 2.3/10 (p < 0.001)

Daitch et al. 2014

35 At least 2 months Chronic pain Mean MEDD 550 mg/day 28.11 ± 5.94 mg 51% decrease in pain score after conversion to SL buprenorphine, from 7.2 to 3.5 (p < 0.001)

Jain et al. 2011

45 6 days Treatment seeking heroin-dependent males N/A 2 mg compared to oral memantine 20 mg/day

VAS score: buprenorphine +10 (-50 to +50); memantine +10 (30-50)

(p > 0.05)

James et al. 2010

 

 

246 7 weeks Osteoarthritis pain hip(s) and/or knee(s) None 0.2 to 0.4 mg tablets every 6-8 h compared to TDS buprenorphine 5, 10, and 20 mcg/h Mean morning pain score decreased from 5.9/10 to 3.1/10, with equivalence to TDS

Malinoff et al. 2005

95 Mean 8.8 months Chronic pain Long-term opioid therapy 2-20 mg/day in divided doses Mean pain score decreased from 3.9 to 2.2

Mandell et al. 2010

5 NR Chronic pain; sickle-cell disease Patient 1: numerous opioids; 2 & 3: low-dose methadone; 4 & 5: high-dose methadone NR Patients 1 & 3: NR; 2: complete resolution of daily pains; 4 & 5: initial improvement in pain, but reverted back to chronic opioids

Massimo et al. 1985

13 NR Chronic pain; pediatric cancer NR 2.5-10 mcg/kg every 12 h Relief of pain good to excellent in 11/13 patients

Nasar et al. 1986

51 14 days Chronic pain; elderly None 0.1 mg 3-4 times daily Pain severity decreased from 2.1/3 to 1.1/3 (p < 0.01)

Robbie 1979

141 Average 12 weeks Chronic pain; cancer None 0.15-0.8 mg/dose, as often as every 12 h Good analgesia with dull aching head and neck pains

Rosenblum et al. 2012

12 3-6 months Chronic pain MEDD 15-450 mg/day 8-24 mg/day, in divided doses Mean pain score decreased from 6.6/10 to 2.1/10 (p< 0.01)

Sturgeon et al. 2020

Buprenorphine taper group (45)

At least 1 month after completion of intervention Chronic pain Median MED 265  NR Median follow-up MED 120; no significant difference in median pain intensity from baseline to follow-up of those transitioned to buprenorphine (p= 0.66)

Abbreviations: BS-11= Box scale-11; CI= confidence intervals; MED= morphine equianalgesic dose; MEDD= morphine equivalent daily; NR= not reported; SL= sublingual; SR= sustained release; TDS: transdermal delivery system; VAS= visual analog scale

References:
[1] [1] Adriaensen H, Mattelaer B, Vanmeenen H. A long-term open, clinical and pharmacokinetic assessment of sublingual buprenorphine in patients suffering from chronic pain. Acta Anaesthesiol Belg. 1985;36(1):33-40.
[2] [2] Bach V, Kamp-Jensen M, Jensen N-H, Eriksen J. Buprenorphine and sustained release morphine— Effect and side-effects in chronic use. Pain Clin 1991;4(2):87–93.
[3] [3] Brema F, Pastorino G, Martini MC, et al. Oral tramadol and buprenorphine in tumour pain. An Italian multicentre trial. Int J Clin Pharmacol Res. 1996;16(4-5):109-116.
[4] [4] Daitch J, Frey ME, Silver D, Mitnick C, Daitch D, Pergolizzi J Jr. Conversion of chronic pain patients from full-opioid agonists to sublingual buprenorphine. Pain Physician. 2012;15(3 Suppl):ES59-ES66.
[5] [5] Daitch D, Daitch J, Novinson D, Frey M, Mitnick C, Pergolizzi J Jr. Conversion from high-dose full-opioid agonists to sublingual buprenorphine reduces pain scores and improves quality of life for chronic pain patients. Pain Med. 2014;15(12):2087-2094. doi:10.1111/pme.12520
[6] [6] Jain K, Jain R, Dhawan A. A double-blind, double-dummy, randomized controlled study of memantine versus buprenorphine in naloxone-precipitated acute withdrawal in heroin addicts. J Opioid Manag. 2011;7(1):11-20. doi:10.5055/jom.2011.0044
[7] [7] James IG, O'Brien CM, McDonald CJ. A randomized, double-blind, double-dummy comparison of the efficacy and tolerability of low-dose transdermal buprenorphine (BuTrans seven-day patches) with buprenorphine sublingual tablets (Temgesic) in patients with osteoarthritis pain. J Pain Symptom Manage. 2010;40(2):266-278. doi:10.1016/j.jpainsymman.2010.01.013
[8] [8] Malinoff HL, Barkin RL, Wilson G. Sublingual buprenorphine is effective in the treatment of chronic pain syndrome. Am J Ther. 2005;12(5):379-384. doi:10.1097/01.mjt.0000160935.62883.ff
[9] [9] Mandell EB, Okam M. The use of suboxone to manage chronic pain in sickle cell disease. Am J Hematol 2010;85(8):E30.
[10] [10] Massimo L, Haupt R, Zamorani ME. Control of pain with sublingual buprenorphine in children with cancer. Eur Paediatr Haematol Oncol 1985;2:224.
[11] [11] Nasar MA, McLeavy MA, Knox J. An open study of sub-lingual buprenorphine in the treatment of chronic pain in the elderly. Curr Med Res Opin. 1986;10(4):251-255. doi:10.1185/03007998609110446
[12] [12] Robbie DS. A trial of sublingual buprenorphine in cancer pain. Br J Clin Pharmacol. 1979;7 Suppl 3(Suppl 3):315S-317S. doi:10.1111/j.1365-2125.1979.tb04706.x
[13] [13] Rosenblum A, Cruciani RA, Strain EC, et al. Sublingual buprenorphine/naloxone for chronic pain in at-risk patients: development and pilot test of a clinical protocol. J Opioid Manag. 2012;8(6):369-382. doi:10.5055/jom.2012.0137
[14] [14] Sturgeon JA, Sullivan MD, Parker-Shames S, Tauben D, Coelho P. Outcomes in Long-term Opioid Tapering and Buprenorphine Transition: A Retrospective Clinical Data Analysis. Pain Med. 2020;21(12):3635-3644. doi:10.1093/pm/pnaa029
[15]