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methadone

✓ Approved

Recordati S.p.A. · OPRD1 · 小分子

什么是 methadone?

methadone 是一种小分子,由Recordati S.p.A.研发。该药已获批,用于治疗相关适应症,给药途径:Oral (PO)。

药物档案

公司Recordati S.p.A.
药物类别小分子
分子靶点OPRD1, OPRK1, OPRM1
给药途径Oral (PO)
状态Approved

作用机制

分子靶点

methadone 作用于 3 个分子靶点:

OPRD1opioid receptor delta 1 (DOR, OPRD)
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

methadone 针对 2 个适应症,涉及 2 个治疗领域。

治疗领域疾病/病症分期
Psychiatric disordersDrug dependence✓ Approved
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Cancer pain✓ Approved

相关研究文献

PubMedResearch square2026-10-25

Increase in Methadone Treatment Episodes With Co-occurring Mental Health Disorders between 2013 and 2023.

Kong Yinfei Y, Zhao Kechen K, Leite Alanis Goncalves AG, Howard Daniel D

Objectives To compare US methadone treatment episodes with co-occurring mental health disorders in 2013 and 2023. Methods We analyzed 2013 and 2023 Treatment Episode Data Set-Discharges records for 75,338 episodes with methadone use, a co-occurring mental health disorder, valid sex or gender information, and discharge because treatment was completed, dropped out, or terminated by the facility. We compared demographics, substance use, treatment, and discharge characteristics. Results Eligible episodes increased from 18,935 in 2013 to 56,403 in 2023. Compared with 2013, 2023 episodes involved older clients (mean age, 39.72 vs 36.16 years), fewer female clients (40.2% vs 49.8%), more methamphetamine/speed use (14.7% vs 3.2%), more cocaine/crack use (38.8% vs 29.9%), less injection drug use (37.1% vs 55.3%), more Medicaid payment (22.9% vs 7.7%), and more homelessness (19.3% vs 12.7%). Conclusions The profile of methadone treatment episodes with psychiatric comorbidity changed markedly. Public Health Implications: Treatment systems may need greater capacity for stimulant co-use, aging-related needs, Medicaid-financed integrated care, and housing support.

PMID 42926927
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PubMedAsia-Pacific journal of clinical oncology2026-10-24

Opioid Prescribing Changes in Advanced Cancer Before and After Withdrawal of Hydromorphone Slow-Release Tablets.

Wong Aaron K AK, McManus Helen H, Vogrin Sara S, Dib Youseph Y et al.

Ongoing disruptions to opioid supply in Australia have raised ongoing concerns about their impact on cancer pain management. The withdrawal of hydromorphone slow-release (SR) tablets from the Australian market has presented challenges to advanced cancer pain management. This study aimed to determine how this affected the utilisation of alternative slow-release opioids in patients with advanced cancer. A retrospective cohort study was conducted at a quaternary cancer centre, comparing opioid prescribing patterns across two 12-month periods: before hydromorphone SR tablet discontinuation was announced and after its discontinuation. Inpatient and outpatient prescribing data were analysed for adult patients with incurable advanced or metastatic cancer who first presented to the centre during each study period. A total of 2856 patients were included (n = 1475 pre and n = 1381 post hydromorphone SR discontinuation). Following hydromorphone SR withdrawal, opioid prescribing patterns shifted. Methadone use rose modestly (adjusted odds ratio [aOR] 1.42, p = 0.07), accompanied by a doubling of median dose (45 mg vs. 22.5 mg; p = 0.005). Morphine use declined (aOR 0.69, p < 0.001), yet daily OMEDD increased by ∼20% (95% confidence interval 1.01-1.37). Tapentadol (aOR 1.40, p = 0.01) and buprenorphine (aOR 1.37, p < 0.001) were prescribed more frequently, without corresponding dose escalation. Following hydromorphone SR withdrawal, the frequency of methadone use increased and median doses doubled. Research incorporating national datasets is needed to clarify the broader impact of opioid supply interruptions. These findings indicate a potential need to reframe the place of methadone in practice, and potentially upscale the focus of clinician training on its safe and effective use.

PMID 42920383
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PubMedHarm reduction journal2026-10-24

Jail-based opioid treatment implementation, outcomes, and costs: lessons learned from the Massachusetts Justice Community Opioid Innovation Network (MassJCOIN).

Evans Elizabeth A EA, Stopka Thomas J TJ, Pivovarova Ekaterina E, Ryan Danielle D et al.

Limited access to medications for opioid use disorder (MOUD) is a major driver of the opioid overdose crisis. Jails have been slow to implement MOUD treatment, especially agonist medications (methadone, buprenorphine). Massachusetts mandated certain county jails pilot-test delivery of all FDA-approved MOUD treatments, stipulating jails continue MOUD, or initiate it prior to release, and facilitate MOUD continuation in the community post-release. The Massachusetts Justice Community Opioid Innovation Network (MassJCOIN) partnered with seven pilot jails, the Massachusetts Department of Public Health, and community treatment providers to conduct a Type 1 hybrid effectiveness-implementation study of this carceral MOUD program. Drawing from selected MassJCOIN evidence on MOUD treatment program implementation, outcomes, and costs, we consider how findings can inform more effective, humane public health and clinical responses to treating incarcerated individuals. MOUD treatment in jail improves treatment engagement, reduces recidivism, and saves lives. MOUD program implementation facilitators included: policies and processes to offer universal MOUD access; transformative and adaptive leadership; appropriate staffing capacity and capabilities; proactive prevention of MOUD diversion; and consideration of patient preferences for MOUD treatment and co-occurring mental health conditions. MOUD program success was influenced by the legislative mandate and other major statewide changes and a community-based treatment system conducive to MOUD implementation. MOUD treatment continuity post-release was facilitated by re-entry planning and preparing individuals for post-release risk environments. Site-specific costs of implementing and sustaining MOUD programming provide information for decisions about program design, budgetary needs, and resource allocation. Carceral MOUD programming is a compelling strategy to advance public safety and public health. Lessons learned provide a playbook for broader diffusion of carceral MOUD programs and can help carceral leadership, healthcare providers, and policymakers make carceral healthcare improvements. Within a harm reduction framework, carceral MOUD treatment can provide substantial opportunities to fill gaps in public health prevention efforts and clinical care to reduce opioid overdose and other concomitant risks. Carceral MOUD programming offers ways for carceral systems to work for the common good, garner trust in public institutions, and increase their legitimacy and value as public institutions.

PMID 42920115
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PubMedDrug discovery today2026-10-23

Methadone: Historical success, modern challenges and lessons for opioid drug discovery.

Li Ennian E, Shah Preet P, Zhang Yan Y

Methadone is a long-standing synthetic opioid that remains clinically important for pain management and opioid use disorder, yet it exemplifies the dual nature of opioid drug discovery. Despite its therapeutic success, methadone exhibits complex pharmacokinetics, polypharmacology and safety liabilities that have limited its broader clinical application. This review examines methadone as a case study to illustrate how chemical structure, stereochemistry, receptor pharmacology and pharmacokinetic properties collectively shape therapeutic outcomes and risk. We summarize key advances in methadone synthesis, structure-activity relationships, pharmacology and clinical limitations and discuss how lessons learned from methadone continue to inform modern opioid drug discovery. Particular emphasis is placed on balancing efficacy, duration of action and safety in the design of next-generation opioid therapeutics.

PMID 42918487
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PubMedRegional anesthesia and pain medicine2026-10-23

Comparison of oral and intravenous methadone for postoperative analgesia after cardiac surgery: a pilot randomized clinical trial.

Ramanujan Krishnan S KS, Grate Jeremy C JC, Khan Fazal F, Paul Johar J et al.

PMID 42919629
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PubMedVeterinary anaesthesia and analgesia2026-10-23

Evaluation of opioid consumption using the quadratus lumborum block or intraperitoneal instillation with bupivacaine in dogs undergoing ovariohysterectomy in a teaching institution.

Quesada Nuria N, Mallea M Julieta MJ, Miccio Mercedes M, Martínez Jaiden J et al.

To compare postoperative opioid consumption between ultrasound-guided quadratus lumborum block (QLB) with bupivacaine and intraperitoneal bupivacaine instillation. Prospective, randomized, single-blinded, cross-sectional, clinical study. A total of 74 owned female dogs undergoing elective ovariohysterectomy. Dogs were premedicated with dexmedetomidine (5 μg kg-1) and methadone (0.3 mg kg-1) intramuscularly. Anesthesia was induced with intravenous propofol and maintained with isoflurane in oxygen. Carprofen (4 mg kg-1) was given subcutaneously after orotracheal intubation. Dogs underwent either a QLB with 0.3 mL kg-1 (1.5 mg kg-1) per side of 0.5% bupivacaine (group QLB) or intraoperative intraperitoneal instillation (group IP) of 0.5% bupivacaine (3 mg kg-1) as part of a multimodal analgesic protocol. Ovariohysterectomies were performed by undergraduate students under instructor supervision. Postoperative pain was assessed at 1, 2, 3, 4, 6, and 8 hours after extubation, using the short form of the Glasgow Composite Measure Pain Scale, and methadone (0.2 mg kg-1) was given as rescue analgesia if the pain score was ≥ 6/24. Opioid consumption was quantified by the number of rescue boluses required, using Poisson regression models. Methadone boluses were given at least once to 9/37 dogs (24%) in group QLB and 15/37 dogs (41%) in group IP. Dogs in group QLB were given 0-2 (range) methadone boluses, whereas those in group IP were given 0-3 boluses, with a total of 11 and 21 boluses, respectively. Methadone consumption was significantly reduced in group QLB versus group IP with a rate ratio of 0.42 (95% confidence interval = 0.19-0.92, p = 0.023). As part of a multimodal analgesic protocol, the QLB reduced postoperative opioid consumption compared with intraperitoneal instillation of bupivacaine in dogs undergoing ovariohysterectomy performed by veterinary students. The QLB can be an alternative to the IP instillation of bupivacaine in dogs undergoing OVH, particularly in teaching settings where surgical procedures may be longer and more stimulating.

PMID 42914770
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