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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

Mechanism of Action

Molecular Targets

buprenorphine acts on 2 molecular targets:

OPRK1opioid receptor kappa 1 (KOR1, OPRK)
OPRM1opioid receptor mu 1 (MOR1, LMOR)
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Therapeutic Indications

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

Therapeutic AreaConditionPhase
Gastrointestinal disordersAbdominal pain✓ Approved

Related Research Articles

PubMedJournal of substance use and addiction treatment2026-09-18

Association between medications for opioid use disorder and child removals.

Quast Troy T, Bright Melissa M, Lofwall Michelle R MR, Delcher Chris C

Buprenorphine and methadone are effective medication treatments for opioid use disorder (MOUD), but their population effects on child welfare are unclear. MOUD may help parents in recovery better care for their families and reduce the risk of children being removed from their homes. The rate of child removals by state Child Protective Services was estimated as a function of per-capita purchases of methadone and buprenorphine for OUD using data for U.S. counties from 2010 to 2019. The estimates were estimated for all counties and, to account for baseline differences in OUD prevalence, were also stratified by quintiles of per-capita opioid analgesic purchases in 2010. A one standard deviation increase in milligrams per capita of buprenorphine for OUD treatment predicted a decrease of 4.9% (p = .008) in the removal rate due to parental neglect. A significant association between the per capita amounts for buprenorphine for OUD or methadone and the all-cause removal rate was not observed. Stratifying by the baseline level of per-capita morphine milligram equivalents (MMEs) for pain management, the negative association between buprenorphine for OUD and removals due to parental neglect was present in the first (lowest) and third quintiles. For methadone, there were negative associations between removals due to neglect and removals due to parental drug use in the highest quintile of baseline MMEs for pain management. Our findings suggest an important population-level benefit of MOUD that may vary according to the prevalence of OUD and the medication. Clinicians and policymakers should take steps to ensure that OUD treatment is accessible to parents who may benefit.

PubMedClinical neuropharmacology2026-09-18

Efficacy and Safety of Inhaled and Sublingual Apomorphine for On‑Demand Treatment of OFF Episodes in Parkinson Disease: A Systematic Review and Meta-Analysis With Exploratory Network Comparison.

Pitton Rissardo Jamir J, Vargas Rojas Jorge Luis JL, Aristizabal Marin Juan J, Fornari Caprara Ana Leticia AL

OFF episodes are a major source of disability in Parkinson disease (PD). Noninjectable apomorphine formulations, including inhaled (INH) and sublingual (SL) delivery systems, provide rapid dopaminergic stimulation for on-demand symptom relief. However, their efficacy and safety remain incompletely characterized. We conducted a systematic review and meta-analysis of randomized parallel-group and crossover trials evaluating inhaled or sublingual apomorphine for OFF episodes in PD. The primary outcome was change from baseline in MDS-UPDRS III scores at 30 and 60 minutes post-dose, pooled as mean differences (MD). Safety outcomes were summarized as risk ratios (RR). Random-effects models were applied when substantial heterogeneity was present. PROSPERO (CRD420261440116). Four randomized controlled trials (n=406) were included. At 30 minutes, noninjectable apomorphine significantly improved motor function compared with control interventions (MD: -11.66 points, 95% CI: -17.56 to -5.76; I2= 92%). A similar effect was observed at 60 minutes (MD: -13.03 points, 95% CI: -20.75 to -5.31; I2=87%). Formulation type was not a significant moderator of treatment effect, although subgroup analyses suggested greater persistence of benefit with SL formulations at 60 minutes. Somnolence/fatigue (RR: 2.19, 95% CI: 1.11-4.31) and yawning (RR: 3.90, 95% CI: 1.06-14.00) were more frequent with apomorphine. Certainty of evidence for motor outcomes was moderate according to GRADE. INH and SL apomorphine provide clinically meaningful short-term motor improvement during OFF episodes in PD. Despite substantial heterogeneity, these findings support their use as effective on-demand therapies and highlight the need for individualized treatment strategies and further comparative-effectiveness research.

PubMedFrontiers in allergy2026-09-18

Genes and cells associated with sublingual allergen immunotherapy revealed by integrated transcriptome analysis in allergic rhinitis patients.

Li Zhengqi Z, Hou Yilin Y, Li Hang H, Ji Ding D et al.

Sublingual allergen immunotherapy (SLIT) is known as an effective therapy for allergic rhinitis (AR), although its efficacy varies across different treatment duration and individuals. The factors associated with the duration and response of SLIT need to be explored. Twenty-seven AR patients undergoing SLIT and three healthy volunteers were recruited. Peripheral blood mononuclear cells were isolated for RNA sequencing, and key results were further examined by quantitative PCR (qPCR) in available PBMC samples. Time-correlated and response-associated genes were identified and analyzed using bioinformatic tools. The data were further integrated with single-cell transcriptome. We first identified 164 genes significantly correlated with SLIT duration. The expressions of genes associated with immunoregulation, nitric oxide and serotonin transportation were regulated as the treatment proceeded. qPCR validation further showed a significant positive correlation between SLC6A4 expression and SLIT duration, while SH2D1B and ARG1 showed positive trends. Then, we identified 257 up-regulated and 349 down-regulated genes in SLIT responders. Several pathways were enriched in these genes, including interferon signaling (up-regulated in responders) and granulocytes migration (down-regulated in responders). Single-cell and deconvolution analyses suggested that natural killer cell-associated signals may associate with SLIT efficacy, potentially in relation to T-cell-regulatory and eosinophil-migration-related transcriptional programs. This study revealed potential genes and cells associated with SLIT duration and response. Regulation of T cells and NK cells may play a crucial role in the successful treatment responses. Further studies are required to validate these findings and assess their clinical relevance.

PubMedFrontiers in psychiatry2026-09-18

Novel pharmacotherapies for opioid use disorder and opioid withdrawal.

Shen Mary R MR, Owusu-Boaitey Kwadwo K, Murphy Zackari D ZD, Rains Alex N AN et al.

Opioid use disorder (OUD) remains a major public health crisis despite evidence-based medications, including methadone, buprenorphine, and naltrexone. Persistent challenges with treatment retention, access, stigma, and incomplete response highlight the need for adjunctive pharmacotherapies targeting neurobiological systems beyond the mu-opioid receptor. We conducted a narrative review of emerging pharmacologic approaches for OUD and opioid withdrawal syndrome, focusing on ketamine and NMDA receptor antagonists, cannabinoids, psychedelics, and incretin-based therapies, including glucagon-like peptide-1 receptor agonists and dual glucose-dependent insulinotropic polypeptide/glucagon-like peptide-1 receptor agonists. Ketamine has preliminary randomized evidence suggesting potential effects on abstinence, withdrawal, craving, and psychotherapy augmentation. Cannabidiol may reduce cue-induced craving and anxiety, whereas dronabinol may modestly suppress opioid withdrawal symptoms. Psychedelic research, particularly involving ibogaine, shows observational signals for withdrawal reduction and abstinence but is limited by safety concerns, regulatory barriers, and sparse controlled evidence. Incretin-based therapies have generated strong observational signals linking GLP-1-based treatment to reduced overdose and OUD-related outcomes, though prospective trials remain limited. Across these therapeutic classes, convergent mechanisms include modulation of mesolimbic reward circuitry, cue-reactivity, stress responsivity, neuroplasticity, and cognitive flexibility. Future studies should prioritize rigorous blinding assessment, active comparators, objective endpoints, standardized cue-reactivity measures, diverse samples, and careful safety monitoring. Regulatory policies should facilitate the development and implementation of future research in novel therapies for OUD.

PubMedEuropean addiction research2026-09-18

AI-Enabled Prescribing in Opioid Use Disorder Care: Decision Support, Risk Scores, Large Language Model Copilots, and Digital Therapeutics (2024-2025).

Zack Mike M, Skryabin Valentin V

This narrative, practice-oriented review maps the 2024-2025 landscape of AI-enabled prescribing in opioid use disorder (OUD) care, where the evidence base is most developed, while noting cautious extension to other substance use disorders (SUDs). We link concrete clinical decisions to fit-for-purpose tools across four domains: EHR-embedded prediction and safety nudges; PDMP-derived analytics and risk scores; clinician-facing large language model (LLM) copilots; and prescription digital therapeutics, just-in-time adaptive interventions (JITAIs), and personal sensing systems. The regulatory analysis uses U.S. frameworks as worked examples and translates the same governance questions to European settings through the EU AI Act, MDR/IVDR medical software requirements, GDPR, the European Health Data Space, and the HMA-EMA data and AI workplan. Evidence maturity is uneven. EHR-based clinical decision support for naloxone co-prescribing and protocolized buprenorphine initiation has the most established implementation base. PDMP risk scores are clinically visible but incompletely validated and should remain advisory. Digital therapeutics and JITAI approaches may support engagement and retention, but they should not automate dosing. LLM copilots are most defensible as audited, citation-first conformance checkers rather than autonomous prescribers; patient-facing agents should be restricted to education, skills support, navigation, and escalation. Across settings, the highest-yield systems are transparent, narrowly scoped, workflow-native, and evaluated with prescribing-centered outcomes such as dose optimization, 28/90/180-day retention, naloxone co-prescribing and fills, and overdose-related safety. We propose safeguards that keep AI explainable, equitable, transferable across health systems, and subordinate to clinical judgment.

PubMedBMJ open2026-09-18

In situ exploration of endothelial function in vasoplegic syndrome after cardiac surgery with cardiopulmonary bypass: protocol for a single-centre prospective cohort study - the Vasoshock study.

Ferry Nicolas N, Renard Domitille D, Gillibert André A, Clavier Thomas T et al.

Vasoplegic syndrome (VS) is a severe complication after cardiac surgery with cardiopulmonary bypass (CPB), characterised by vasodilation, hypotension and vasopressor dependence. Endothelial dysfunction, dysregulated nitric oxide signalling, inflammation and glycocalyx injury may contribute. Combining flow-mediated dilation (FMD), sublingual side-stream dark-field (SDF) imaging and biomarkers may improve postoperative vascular phenotyping. The primary objective is to compare allometrically corrected brachial artery FMD between patients with VS and patients without VS 48 hours after CPB weaning. This prospective, single-centre observational cohort study will enrol 124 adults aged 18-80 years undergoing cardiac surgery with CPB (62 VS and 62 non-VS). VS is defined clinically as norepinephrine bitartrate ≥0.05 µg/kg/min for at least 4 hours to maintain mean arterial pressure ≥65 mm Hg after CPB weaning, following haemodynamic optimisation and exclusion of a predominant low-cardiac-output phenotype or another cause of shock. FMD, SDF imaging and biomarkers will be assessed at 4-8 and 48 hours after CPB weaning. The primary comparison will use multiple linear regression for corrected FMD at 48 hours with prespecified covariate adjustment. Secondary and exploratory analyses will assess SDF-derived parameters, biomarkers and associations across modalities. The protocol was approved by the Comité de Protection des Personnes Sud-Méditerranée III (CPP Sud-Méditerranée III; 2023-A02079-36). For this non-interventional routine-care study, French law requires prior oral and written information and absence of opposition rather than written consent; absence of opposition will be documented. Results will be published in peer-reviewed journals and presented at scientific conferences. NCT06318689.

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