Drug Database
BU

buprenorphine

✓ Approved

Roche · OPRK1 · Small Molecule

What is buprenorphine?

buprenorphine is a small molecule developed by Roche. It is approved for therapeutic indications via oral (po) or sublingual (sl)/oral transmucosal.

Drug Profile

CompanyRoche
Drug ClassSmall Molecule
Molecular TargetOPRK1, OPRM1
RouteOral (PO), Sublingual (SL)/Oral Transmucosal
StatusApproved
Sources: ClinicalTrials.gov, Roche

Mechanism of Action

Molecular Targets

buprenorphine acts on 2 molecular targets:

OPRK1opioid receptor kappa 1 (KOR1, OPRK)
OPRM1opioid receptor mu 1 (MOR1, LMOR)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

buprenorphine is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Gastrointestinal disordersAbdominal pain✓ Approved

Related Research Articles

PubMedAmerican journal of preventive medicine2026-07-17

State X-waiver Statutes and Buprenorphine Prescriber Rates Following Federal X-waiver Elimination, 2021-2023.

Wolde Filmon F, Martin Bradley C BC, Acharya Mahip M, Gressler Laura L et al.

This study examined whether U.S. jurisdictions that retained elements of the X-waiver in their statutes after federal elimination had lower buprenorphine prescriber rates than jurisdictions that did not retain such elements. Using a 25% random sample from IQVIA PharMetrics® Plus for Academics, data from January 2021-October 2023 (analyzed from 2025-2026) were modeled using Comparative Interrupted Time Series (CITS) models of monthly rates of unique buprenorphine prescribers per 10,000 eligible prescribers and jurisdiction fixed-effects generalized estimating equations (GEE). Jurisdictions were classified by whether they incorporated X-waiver language into their statutes, at the jurisdiction-month level, per the Center for Public Health Law Research at Temple University. Models were adjusted for three-month rolling opioid use disorder (OUD) diagnosis rates and annual age-adjusted opioid overdose mortality rates. Analyses were stratified by provider type. Three sensitivity analyses tested an alternative specification and excluded jurisdictions with unstable buprenorphine prescribing rates and enrollment. Forty-nine jurisdictions and 1,558 jurisdiction-months were included. Mean buprenorphine prescriber rates were higher in jurisdictions with X-waiver references than without (96.84 vs 47.01 buprenorphine prescribers/10,000 eligible prescribers). No differences in either level (-8.69 per 10,000 [95% CI: -19.96 to 2.59; p=0.131]) or trend (+0.74 per month [95% CI: -0.92 to 2.40; p=0.380]) of buprenorphine prescribers were found between jurisdiction-months with and without references to the X-waiver following X-waiver elimination. Findings were consistent across strata and sensitivity analyses. Findings suggest that removing jurisdiction-level statutory X-waiver references is unlikely to expand access, as structural barriers persist.

PMID 42462886
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PubMedJournal of dental research2026-07-17

Sublingual Caruncle Taste Buds Drive Taste Perception and Salivary Reflexes.

Liu J J, Xi R R, Han M M, Xu X X et al.

Taste buds (TBs) are the fundamental units of taste perception and are distributed throughout the oral cavity, including the tongue, soft palate, epiglottis, pharynx, and retromolar pad. Despite their widespread presence, a complete and systematic understanding of TB distribution and functional organization remains incomplete. In this study, we focus on a small population of TBs located in the mandibular sublingual caruncle of mice, adjacent to the openings of the Wharton's ducts, a site previously noted in anatomical and physiological studies that has not been comprehensively characterized. TBs of the sublingual caruncle exhibit canonical morphology and cellular composition, comprising type I (NTPDase2 +), type II (Trpm5 +), and type III (Car4 +) cells, as confirmed by transgenic reporter lines and immunofluorescence staining. Molecular analysis revealed the expression of key taste transduction components, including Gnat3, Trpm5, and Plcb2, as well as 26 of 35 bitter taste receptors. Immunofluorescence confirmed TB innervation by βIII-tubulin-positive nerve fibers, including P2X3-positive sensory afferents, Synapsin-1-positive presynaptic terminals, and CGRP-positive peptidergic endings, indicating integration into the peripheral gustatory circuitry. Retrograde neuronal tracing (Dil/DiO) further demonstrated that nerve fibers associated with sublingual caruncle TBs project specifically to the geniculate but not the petrosal ganglion, supporting their attribution to the facial gustatory pathway. Functionally, localized sucrose stimulation of the sublingual caruncle elicited cFos activation in the nucleus of the solitary tract, indicating central connectivity. Furthermore, tastants representing all 5 basic taste qualities (sweet, sour, bitter, umami, and salty) elicited measurable saliva secretion, with bitter-, sweet-, and umami-induced salivation reduced in transgenic mouse models with impaired gustatory function. Together, these findings establish the sublingual caruncle as a functional gustatory site involved in taste-evoked salivary reflexes, expanding current understanding of taste system organization and its coordination with salivary function.

PMID 42466736
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PubMedResearch square2026-07-17

Blunted modulation of hierarchical brain organization in opioid use disorder.

Tomasi Dardo D, Manza Peter P, Demiral Sukru S, Giddens Natasha N et al.

Opioid use disorder (OUD) is associated with persistent catecholaminergic dysfunction, but its impact on large-scale cortical organization remains unclear. We used pharmacological resting-state fMRI and functional gradient mapping to test whether OUD alters catecholaminergic modulation of cortical hierarchy. Fifty-three individuals with OUD and 40 healthy controls underwent resting-state fMRI after placebo and methylphenidate. Under placebo, principal and secondary cortical gradients showed canonical organization with no group differences. In controls, methylphenidate compressed the dynamic range of the principal gradient while preserving its spatial topology, indicating state-dependent modulation of the unimodal-transmodal hierarchy. This response was attenuated in OUD and further reduced among participants receiving methadone or buprenorphine. Methylphenidate improved visual attention in controls but not OUD, and gradient modulation predicted attentional benefit only in controls. Gradient features also predicted years of opioid use. These findings identify blunted catecholaminergic modulation of cortical hierarchy as a clinically relevant systems-level feature of OUD.

PMID 42466414
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PubMedThe American journal on addictions2026-07-16

Extended-release buprenorphine in adults with opioid use disorder involving poppy seed tea: An 18-month retrospective case series.

McMaster John J, Seshakumaran Saumiya S, Abeysundera Hesitha H, Tipirneni Isha I et al.

Poppy seed tea (PST) contains unpredictable opioid concentrations, destabilising tolerance and increasing overdose risk. Extended-release buprenorphine (BUP-XR) provides sustained coverage without daily dosing. Eighteen-month follow-up of adults (N = 3) with opioid use disorder (OUD) involving PST in Australia. All had polysubstance use and transitioned to BUP-XR after 2 days to 6 months of sublingual buprenorphine. Posttransition urine drug screens were morphine-negative; one patient was intermittently tramadol-positive. All remained in treatment at 18 months. BUP-XR assisted stability within multidisciplinary care. This series adds longer-term follow-up on PST-related OUD and suggests BUP-XR feasibility.

PMID 42458627
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PubMedClinical practice and cases in emergency medicine2026-07-16

Intravenous Low-dose Buprenorphine for Acute Pain Management in the Emergency Department: A Case Series.

Lee Jonathan J, Ashenburg Nicholas N, Park Joshua J, Ahern Terence T

Buprenorphine is used for treating opioid use disorder, but its role as an analgesic in the emergency department (ED) is frequently overlooked. Emerging evidence indicates that, at low doses, it can be used safely and advantageously as an alternative to full-agonist opioids for treating acute pain. This case series examines the novel use of intravenous (IV) low-dose buprenorphine for acute pain management in the ED for five patients presenting with diverse past medical history and varied painful indications. Intravenous low-dose buprenorphine may represent an important new tool in our ED armamentarium, and research into its role in emergency pain management is warranted. Further work is needed to determine optimal dosing strategies and identify which patients will be most likely to benefit from IV low-dosebuprenorphine in the ED.

PMID 42456306
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PubMedJournal of addiction medicine2026-07-16

An Institutional Provider Survey Evaluating Access and Implementation of Opioid Use Disorder Treatment in the Intensive Care Unit.

Quaye Aurora N AN, Richard Janelle M JM, Craig Wendy Y WY, Scharnetzki Elizabeth E et al.

Patients with opioid use disorder (OUD) are increasingly admitted to intensive care units (ICUs) due to complications stemming from undertreated OUD. Rural hospitals are disproportionately affected. Hospitalization represents a critical opportunity to initiate OUD treatment; however, no ICU-specific guidance exists. We conducted a survey to assess the knowledge and practices of providers caring for patients with OUD in critical care settings, focusing on differences between rural and urban hospitals. We conducted a survey of providers in 9 ICU and acute care units at MaineHealth, the largest integrated health system in northern New England, from April to December 2024. Survey domains included access to addiction services, medications for OUD (MOUD) utilization, buprenorphine prescribing knowledge, and naloxone prescribing. Differences were assessed using the χ2 or Fisher exact tests. Fewer than half of respondents (46.2%) felt adequately supported to manage OUD. Methadone and buprenorphine were always continued in only 10% and 8.6% cases, respectively. A total of 30.0% of respondents correctly identified that any provider with Schedule III authority can prescribe buprenorphine. Fewer rural providers reported access to consultative OUD teams (39.3% vs. 70.0%, P=0.023) but were more likely to prescribe naloxone (71.4% vs. 35.9%, P=0.013). Overall, 69.2% indicated that naloxone was rarely or never prescribed to patients at the time of self-directed discharge. Our survey identified that both rural and urban hospitals reported low rates of MOUD utilization and knowledge gaps regarding buprenorphine prescribing. These findings reinforce the need for system-level efforts to expand access to MOUD and improve provider education across intensive care settings.

PMID 42460618
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