Drug Database
BU

buprenorphine

✓ Approved

Roche · OPRK1 · 小分子

什么是 buprenorphine?

buprenorphine 是一种小分子,由Roche研发。该药已获批,用于治疗相关适应症,给药途径:Oral (PO)、Sublingual (SL)/Oral Transmucosal。

药物档案

公司Roche
药物类别小分子
分子靶点OPRK1, OPRM1
给药途径Oral (PO), Sublingual (SL)/Oral Transmucosal
状态Approved

作用机制

分子靶点

buprenorphine 作用于 2 个分子靶点:

OPRK1opioid receptor kappa 1 (KOR1, OPRK)
OPRM1opioid receptor mu 1 (MOR1, LMOR)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

buprenorphine 针对 1 个适应症,涉及 1 个治疗领域。

治疗领域疾病/病症分期
Gastrointestinal disordersAbdominal pain✓ Approved

相关研究文献

PubMedClinical case reports2026-09-10

Sublingual Epidermoid Cyst in a Neonate-A Rare Case Report on Early Detection and Intervention.

Ararso Gelana Garoma GG, Dana Demerew Dejene DD, Fikire Matewos Amare MA, Bonger Mulugeta Temesgen MT et al.

Epidermoid cysts are rare benign developmental lesions that occur infrequently in the oral cavity, accounting for less than 0.01% of oral cysts. Congenital sublingual epidermoid cysts in neonates are extremely uncommon but may interfere with feeding and tongue movement. This report presents a rare case of a congenital sublingual epidermoid cyst in an 11-day-old neonate managed successfully with early surgical excision to restore normal feeding function. An 11-day-old male neonate from Ethiopia presented with a congenital swelling on the floor of the mouth beneath the left side of the tongue, which was noticed immediately after birth. The swelling, measuring 4 × 3 cm, was noticed immediately after birth. The initial fine needle aspiration cytology (FNAC) revealed a sublingual keratin cyst. Clinically, epidermoid cysts are characterized by a rubbery consistency on palpation, well-defined borders, and varying sizes. They are usually asymptomatic and slow-growing. The final diagnosis is usually confirmed by histopathological examination. Surgical excision, with the goal of complete removal including the cyst wall, is the definitive treatment option to prevent recurrence. If left untreated, the lesion may grow significantly and lead to complications such as dysphagia, breathing difficulties, pain, and reduced tongue movement.

PMID 42719121
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PubMedPediatrics international : official journal of the Japan Pediatric Society2026-09-10

A Pediatric Case of Reversible Eosinophilic Duodenitis Associated With Sublingual Immunotherapy.

Yabe Kiyoaki K, Shida Masaki M, Inagi Yoshihide Y, Shibusawa Hiroshi H et al.

PMID 42717621
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PubMedSpecial care in dentistry : official publication of the American Association of Hospital Dentists, the Academy of Dentistry for the Handicapped, and the American Society for Geriatric Dentistry2026-09-10

Adverse Oral Mucosal Reaction to Sublingual Captopril: A Case Report With Exploratory Insights Into AI-Assisted Clinical Reasoning.

Júnior Antônio Roberto Garcia ARG, Velane Catarina Melquiades CM, Silva Larissa Araújo LA, Magario Caroline Akemi Mendes CAM et al.

PMID 42720001
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PubMedAdvances in therapy2026-09-10

Brixadi for Stimulant Use Disorder: Evolving Pharmacologic Considerations and Clinical Implications.

Sawaya M Farris MF, McNulty Molly E ME, Germain Collin J St CJS, Hachem Ibraheem A IA et al.

Substance use disorders are an increasing concern globally, causing a tremendous uptick in public health burden in recent years. Despite the growing attention these disorders receive, there remain no approved pharmacotherapies for stimulant use disorder, thereby contributing a major portion of this burden. This review examines the potential use of Brixadi, an extended-release injectable formulation of the widely used pharmacotherapy buprenorphine, indicated for opioid use disorder, in the treatment of stimulant use disorder. Psychostimulants, including cocaine, methamphetamine, and designer stimulants, all exert their effects by inhibiting or reversing the directionality of the monoamine transporters in the synaptic cleft. Inhibition or reversal of these transporters in the synaptic cleft allows dopamine, serotonin, and norepinephrine to remain in the synapse, which ultimately enhances their activity and contributes to the reinforcement of substance use. The reinforcement loop driven by excess neurotransmitters, particularly dopamine, provides a pharmacotherapeutic target via receptor interactions. Brixadi is an injectable extended-release buprenorphine primarily used to treat opioid use disorder. The extended-release mechanism enables sustained drug-receptor interaction, resulting in stable plasma drug concentrations. Buprenorphine is as a dual-acting agent, a partial μ-opioid receptor (MOR) agonist and a κ-opioid receptor (KOR) antagonist. KOR antagonism modulates symptoms of withdrawal in OUD, including dysphoria, stress, and drug cravings. Therefore, Brixadi's KOR antagonism may offer a promising pharmacologic target for stimulant use disorder recovery by mitigating these negative affective states. Additionally, the bimodal mechanism suggests that Brixadi may be a beneficial pharmacologic candidate for people who suffer from polysubstance use involving opioids and psychostimulants. While there is promise behind these developments, current studies are limited to preclinical trials and have not yet advanced toward clinical trials. However, Brixadi's extended-release profile and potential capability to minimize withdrawal-related dysphoria and stress-induced drug seeking present promise for further clinical investigation.

PMID 42720725
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PubMedScientific reports2026-09-09

Exploring serum sST2 and miR-223 as potential biomarkers of disease activity and clinical response to SLIT in HDM-induced allergic rhinitis.

Mokhtar Ghada A GA, Gebriel Manar G MG, Abdelnour Hanim M HM, Salah Abd El Azeem El Sayed Mohamed M et al.

Soluble suppression of tumorigenicity 2 (sST2), a decoy receptor of interleukin-33 (IL-33), is involved in allergic inflammation and may serve as a biomarker in allergic rhinitis (AR). MicroRNA-223 (miR-223) has also been implicated in allergic inflammation. To investigate serum sST2 and miR-223 as potential biomarkers of disease activity and treatment-associated changes in patients with house dust mite (HDM)-induced moderate-to-severe allergic rhinitis (MSAR) undergoing sublingual immunotherapy (SLIT). This study included 54 patients with moderate-to-severe AR (MSAR) and 54 healthy controls (HC). Serum sST2, total IgE, HDM-specific IgE, and eosinophil counts were measured. Serum miR-223 relative expression was assessed using real-time PCR. Clinical severity was assessed using the total nasal symptom score (TNSS) and visual analogue scale (VAS). MSAR patients received SLIT for 6 months. Treatment response was defined as a ≥ 30% reduction in TNSS from baseline. Serum sST2 and miR-223 were significantly higher in MSAR patients than in healthy controls (p < 0.001). sST2 correlated positively with HDM-specific IgE and eosinophil counts and decreased significantly after six months of treatment (p < 0.001). Post-treatment sST2 was lower in responders, whereas baseline sST2 did not differ significantly between groups. ROC analysis showed good discrimination of MSAR from HC for sST2 (AUC = 0.933) and miR-223 (AUC ≈ 0.96). Serum sST2 and miR-223 show promising potential as candidate biomarkers of HDM-induced MSAR. The decrease in sST2 after treatment suggests its potential value for monitoring treatment-associated changes. Further studies are needed to validate these findings.Trial registration Retrospectively registered on ClinicalTrials.gov, registered at 25/2/ 2026, Identifier (NCT07436208). Registered at: https://clinicaltrials.gov/study/NCT07436208.

PMID 42711401
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PubMedJournal of addiction medicine2026-09-08

Treatment Discontinuation and Barriers and Facilitators to Retention Among Individuals Initiating Buprenorphine for Opioid Use Disorder: A Longitudinal Cohort Study.

Poulsen Melissa N MN, Truong Michelle L ML, Pabla Jasmine K JK, Poissant Amy A et al.

Early discontinuation of medication for opioid use disorder (MOUD) is associated with increased mortality and hinders remission. Combining data from electronic health records (EHRs) and patient questionnaires, we examined buprenorphine discontinuation and barriers and facilitators to retention in outpatient settings. Adults initiating buprenorphine in a Pennsylvania outpatient program (2021-2023) completed 2 questionnaires: at medication initiation (baseline) and 6 months after initiation (follow-up). Among 1189 eligible patients, we evaluated buprenorphine discontinuation (≥30-d gap in medication supply) and compared demographic factors using EHRs. We identified discontinuation reasons among survey participants (baseline n = 374; follow-up n = 197) through medical record review; questionnaires assessed treatment barriers and facilitators. Within 6 months, 629 (53%) patients discontinued buprenorphine, though 15% restarted medication within the 6-month period. Discontinuation was more common among younger patients. Among baseline survey participants, discontinuation was usually unplanned (66%) or against provider advice (19%). Among follow-up participants who discontinued the program during the follow-up period, 54% reported receiving MOUD at 6 months, indicating that many transition to other treatment programs. Those not receiving medication at 6 months cited lack of need (46%). Travel challenges (distance/transportation to clinics), scheduling, and mental health conditions were common barriers to treatment; facilitators centered on improving these factors and clinic processes. Observed patterns reflect dynamic and noncontinuous receipt of medication over time and underscore the early months of treatment as a critical window for supporting buprenorphine engagement. Findings reveal actionable areas to improve retention by reducing logistical burdens, enhancing nonjudgmental therapeutic support, and integrating mental health care.

PMID 42709580
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