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

PubMedJournal of psychopharmacology (Oxford, England)2026-08-30

A randomized crossover trial comparing the acute physiological and psychological effects of botanical formulations of oral psilocybin, oral psilocin, and sublingual psilocin.

Tai Marlene L ML, Szigeti Balázs B, Downey Amanda E AE, Aday Jacob S JS et al.

Psilocybin, a serotonergic psychedelic found in hallucinogenic mushrooms, is metabolized to psilocin, the compound responsible for its psychoactive effects. Psilocybin has demonstrated therapeutic potential for neuropsychiatric conditions. While recent trials have primarily used orally administered synthetic psilocybin, alternative formulations and delivery methods may offer therapeutic advantages, yet the effects of these approaches remain poorly characterized. To compare the pharmacodynamic profiles and tolerability of oral psilocybin, oral psilocin, and sublingual psilocin derived from whole-mushroom extracts in healthy adults. In this randomized, within-subject, crossover trial, 20 healthy adults (10 men, 10 women; mean age 40.1 ± 5.9 years) completed up to four drug administration sessions involving botanical oral psilocybin (25 mg), oral psilocin (17.5 mg), or sublingual psilocin (2.18, 4.36, or 8 mg). All sessions included therapeutic support and pre- and post-dose psychotherapy. Acute effects were assessed using vital signs and subjective ratings of drug intensity and psychedelic experience. Oral psilocin produced a similar temporal and subjective profile to oral psilocybin, with a lower burden of adverse effects. Sublingual psilocin was well tolerated, though the apparently lower achieved drug exposure limited comparability to oral administration. Oral psilocin may offer tolerability advantages over oral psilocybin. Sublingual psilocin was well tolerated at the dosages tested. Further studies are needed to evaluate botanical formulations and optimize delivery approaches.Clinical trial registration: https://clinicaltrials.gov/study/NCT05317689.

PMID 42668404
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PubMedPublic health reports (Washington, D.C. : 1974)2026-08-30

Framework for the Opioid Use Disorder Cascade of Care: Adaptation and Application for a Large Municipal Health System.

Kalmin Mariah M MM, Crowley Christina C, Pak Lia L, McCullough Colleen M CM et al.

Most people with opioid use disorder (OUD) do not receive effective treatments despite their existence. The OUD cascade of care framework can be used to inform quality improvement efforts to address this gap, but data access and linkage requirements may limit its use. We sought to adapt the framework under the constraints of electronic health record data and identify patient populations at risk for OUD treatment discontinuity. We extracted data on patients with OUD from the Los Angeles County Department of Health Services from July 2022 through June 2023. We adapted the cascade of care to include probable OUD diagnosis, receipt of naloxone prescription, and receipt of ≥1 and ≥2 buprenorphine prescriptions. We then stratified and conducted statistical analyses for associations by sex, race and ethnicity, and facility type (inpatient, primary care, emergency, or urgent care). Of 3881 patients identified with probable OUD, 49% received a naloxone prescription and 30% and 17% had ≥1 and ≥2 buprenorphine prescriptions, respectively, in 1 year. Non-Hispanic Black and Hispanic patients were less likely to receive buprenorphine prescriptions than were non-Hispanic White patients and patients of other or unknown race and ethnicity. We observed larger gaps in care between receipt of ≥1 and ≥2 buprenorphine prescriptions for patients using urgent care and emergency departments compared with patients in other settings. This study illustrates substantial gaps between OUD diagnosis and treatment. This adapted framework for the OUD cascade of care can serve as a quality-monitoring tool to aid clinicians and health care administrators in narrowing the treatment gap for people with OUD.

PMID 42669155
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PubMedCurrent medical research and opinion2026-08-30

Antidepressant initiation after sublingual immunotherapy in Japanese cedar pollinosis: a real-world propensity score-matched cohort study.

Matsushita Rie R, Tanaka-Mizuno Sachiko S, Kawakami Koji K

To evaluate whether sublingual immunotherapy (SLIT) for Japanese cedar pollinosis is associated with subsequent initiation of antidepressants, and to assess its clinical implications for mental health management in real-world clinical practice. We conducted a retrospective real-world cohort study using a large nationwide administrative claims database in Japan from 2014 to 2021. Adult patients diagnosed with Japanese cedar pollinosis were identified and classified as SLIT users or non-users using a new-user design. Propensity score matching was performed to balance patients' baseline characteristics, including age, sex, insurance type, and medical history. The primary outcome was initiation of antidepressant prescriptions. Hazard ratios were estimated using matched cohorts. A total of 4,126 SLIT users and 88,455 non-users were identified, with 3,991 propensity-matched patients in each group. Before matching, mental disorders were more prevalent among SLIT users than among non-users, whereas allergic rhinitis severity was similar between groups. Crude initiation rates of antidepressants were 5.0 and 2.9 per 1,000 person-years among SLIT users and non-users, respectively. After matching, no statistically significant association was observed between SLIT use and antidepressant initiation (hazard ratio = 1.11, 95% confidence interval = 0.73-1.69). Kaplan-Meier analysis also showed no significant between-group differences. No statistically significant association was observed between SLIT for Japanese cedar pollinosis and antidepressant initiation. These findings suggest that mental health outcomes should continue to be monitored independently of immunotherapy use in routine clinical practice. Further adequately powered studies with longer follow-up periods are warranted to better characterize depressive outcomes in this population.

PMID 42669179
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PubMedCurrent pain and headache reports2026-08-29

Adjunct Medications for Single-Injection Pediatric Regional Blocks: Implications for Peripheral Nerve Blocks.

Jha Sachin Sunny SS

Single-injection peripheral nerve blocks (PNBs) provide excellent perioperative analgesia in children but are limited by finite duration. Pediatric populations were excluded from the major adult adjunct reviews. This narrative review synthesizes the evidence for adjuncts added to local anesthetics for single-injection PNBs and caudal blocks in patients aged 0 to 18 years, including dexamethasone, dexmedetomidine, clonidine, conventional opioids, buprenorphine, magnesium sulfate, midazolam, ketamine, neostigmine, tramadol, nalbuphine, and epinephrine. Across 58 studies, dexmedetomidine (0.5 to 1 mcg/kg) and dexamethasone (0.1 mg/kg perineural) were the best-supported agents, each roughly doubling analgesic duration with acceptable safety. Two network meta-analyses ranked neostigmine highest for caudal duration, but its postoperative nausea and vomiting burden limits use. Clonidine has the longest safety record. Ketamine and midazolam show robust caudal efficacy but unresolved neurotoxicity concerns. Nalbuphine and buprenorphine are promising but under-studied. Tramadol carries pediatric regulatory restrictions, while epinephrine and conventional opioids add little. Dexmedetomidine and dexamethasone are the preferred adjuncts in pediatric regional anesthesia. Adult evidence should not be extrapolated directly given developmental pharmacology and pediatric-specific safety considerations. Prospective trials in true pediatric PNBs and pediatric rebound-pain studies remain the critical evidence gaps.

PMID 42667510
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PubMedJournal of cardiothoracic and vascular anesthesia2026-08-29

Blood Glucose Variability and Postoperative Organ Function in Coronary Artery Bypass Grafting: A Prospective Cohort Study of Microcirculatory Perfusion and Oxygenation.

Mansjoer Arif A, Alwi Idrus I, Yunir Em E, Aditianingsih Dita D et al.

Coronary heart disease remains the leading cause of cardiovascular morbidity and mortality. The relationship between perioperative blood glucose variability (BGV), microcirculatory changes, and subsequent organ dysfunction after coronary artery bypass grafting (CABG) remains poorly defined. Associations among BGV, sublingual microcirculation, and organ dysfunction, as measured by the Cardiac Surgery Score (CASUS) were evaluated. Prospective cohort study. A tertiary academic cardiac hospital and a secondary cardiac hospital. 51 adult patients undergoing elective on-pump CABG. None. Perioperative BGV was quantified using standard deviation (SD), coefficient of variation (CV), and mean amplitude of glycemic excursions. Sublingual microcirculation, including the proportion of perfused vessels (PPV) and perfused vessel density, was assessed. The primary outcome was organ dysfunction on postoperative day 1, defined by a CASUS >6.5. Higher perioperative BGV correlated significantly with impaired microcirculation and metabolic stress. CV was negatively associated with PPV (r = -0.309, p < 0.05) and positively with lactate (r = 0.280, p < 0.05). Postoperative BGV metrics were significant indicators of organ dysfunction, demonstrating high discrimination for SD (area under the curve [AUC] 0.952), CV (AUC 0.931), and mean amplitude of glycemic excursions (AUC 0.936). An optimal SD cutoff of 56.98 mg/dL identified at-risk patients with 100% sensitivity and 91.5% specificity. Furthermore, impaired admission microcirculation was strongly associated with subsequent organ failure. Lower admission PPV (AUC 0.963) and perfused vessel density (AUC 0.918) were significantly associated with high CASUS scores on postoperative day 1. Postoperative BGV and early microcirculatory impairment are associated with high risk for organ dysfunction in CABG patients. Integrating BGV control with bedside microcirculatory and lactate monitoring may strengthen early risk stratification and management.

PMID 42668244
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PubMedCureus2026-08-28

Unusual Cause of Sublingual Hematoma Compromising Upper Airway: Acquired Hemophilia A.

Miyake Saho S, Okazaki Yuji Y, Ichiba Toshihisa T

Sublingual hematoma is an uncommon but potentially life-threatening cause of upper airway obstruction. While most cases result from trauma, surgery, or anticoagulant use, acquired hemophilia A (AHA) is a rare autoimmune bleeding disorder caused by factor VIII inhibitors that may, in rare cases, present with spontaneous sublingual mucosal bleeding. We report a rare case of sublingual hematoma due to AHA that narrowed the upper airway. A 90-year-old woman without a history of spontaneous bleeding presented to the emergency department (ED) with acute sublingual swelling and dysphagia. She had no history of trauma, recent dental procedures, or anticoagulant use. Physical examination revealed hoarseness and purplish swelling of the sublingual and submandibular regions. Laboratory examinations showed isolated prolongation of activated partial thromboplastin time (aPTT). Contrast-enhanced computed tomography revealed a sublingual hematoma with airway narrowing. Given the risk of airway obstruction, we prepared for awake nasotracheal intubation. A mixing study demonstrated failure of aPTT correction, and factor VIII activity was undetectable, strongly suggesting AHA. Because the hematoma enlarged during the first 12 hours after ED admission, we initiated intravenous administration of activated prothrombin complex concentrate. The hematoma subsequently improved. A positive factor VIII inhibitor confirmed the diagnosis of AHA, and immunosuppressive therapy with glucocorticoids was started. The aPTT normalized within two weeks, and the inhibitor became undetectable after three weeks. She was discharged on day 41 without additional bleeding events. AHA should be considered in cases of spontaneous sublingual hematoma, particularly when accompanied by isolated aPTT prolongation. In such cases, because the hematoma may rapidly progress to cause upper airway obstruction, clinicians should initiate hemostatic therapy promptly when AHA is strongly suspected, even before a definitive diagnosis is established.

PMID 42662534
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