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baclofen (Fleqsuvy)

✓ Approved

Azurity Pharmaceuticals, Inc. · GABBR1 · 小分子

什么是 baclofen？

baclofen 是一种小分子，由Azurity Pharmaceuticals, Inc.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

商品名Fleqsuvy
公司Azurity Pharmaceuticals, Inc.
药物类别小分子
分子靶点GABBR1
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Azurity Pharmaceuticals, Inc.

作用机制

分子靶点

baclofen 作用于 1 个分子靶点：

GABBR1gamma-aminobutyric acid type B receptor subunit 1 (GABABR1, GB1)
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

baclofen 针对 3 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Nervous system disordersMultiple sclerosis✓ Approved
Nervous system disordersMuscle spasticity✓ Approved
Injury, poisoning and procedural complicationsSpinal cord injury✓ Approved

相关研究文献

PubMedNeuromodulation : journal of the International Neuromodulation Society2026-09-10

Management of Intrathecal Baclofen Pump System Malfunction and the Value of the Radio-Opaque Catheter Dye Study: A Retrospective Data Analysis of 49 Pump System Investigations Over a Seven-Year Period.

Lee Heesook H, Betteridge Nicola N, Keenan Elizabeth E, Farrell Rachel R et al.

Timely and thorough investigation of intrathecal baclofen (ITB) pump system malfunction is essential for optimal spasticity management. We reviewed seven years of investigation data to determine the value of the radio-opaque catheter dye study (RCDS) in confirming suspected ITB pump system malfunctions. A retrospective review of electronic medical records was conducted for patients admitted under the author's spasticity service for ITB pump system investigation or catheter revision surgery from January 2018 to December 2024 (a seven-year period). Demographic data, investigation results, and ITB dose at various stages were collected and compared. In the ITB cohort of 188 patients, 41 patients experienced at least one suspected ITB system malfunction (49 admissions). There were five admissions where investigations were not performed, all of which proceeded to catheter revision based on a strong clinical suspicion of catheter malfunction. Catheter access port (CAP) procedures were completed in 44 admissions; in nine of these, it was not possible to aspirate, and all nine proceeded directly to catheter revision. Of the 35 successful CAP procedures, 22 proceeded to RCDS; only one was positive and went directly to catheter revision surgery. Thirteen of the 21 admissions with a negative RCDS underwent lumbar puncture (LP) boluses; eight of these demonstrated a superior effect to pump boluses, suggesting catheter malfunction. Of the eight admissions with negative RCDS without LP, four went on to have catheter revision due to a clear history of fluctuating spasticity. In total, 31 of the 49 admissions investigated showed evidence of catheter malfunction; 27 proceeded to operating theatre for revision surgery. The RCDS showed a high false-negative rate and provided a low value in identifying ITB pump system malfunction. Instead, careful clinical assessment, early CAP procedure, and consideration of a pump ITB bolus with or without a comparison LP bolus are more valuable and effective.

PMID 42720639
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PubMedLegal medicine (Tokyo, Japan)2026-09-09

Ultrafiltration for baclofen measurement in blood using liquid chromatography-tandem mass spectrometry.

Takeuchi Akiko A, Matoba Kotaro K, Uozumi Ryo R, Murakami Manabu M et al.

The accurate measurement of baclofen concentrations in blood is essential for diagnosing baclofen-related fatalities, which have increased in recent years. This study presents a simple, rapid, and highly sensitive method for the quantitative analysis of baclofen in whole blood and serum using liquid chromatography-tandem mass spectrometry following ultrafiltration. This method is based on multiple reaction monitoring in positive-ion mode and has high sensitivity with a lower limit of quantification of 0.2 ng/mL. The precision and accuracy of this method satisfy the basic requirements for quantitative analysis (intra- and inter-day assays yielded relative standard deviation of ≤9.0%; the matrix effect ranged from 99.7%-105.4%). Using our method, baclofen concentrations of 442-493 ng/mL in blood samples and 62 mg/mL in urine were detected in cases of prolonged baclofen poisoning. No differences were observed between baclofen concentrations in whole blood and serum.

PMID 42715732
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PubMedFrontiers in pharmacology2026-09-09

Sex-specific pharmacovigilance signals and time-to-onset patterns of drug-related myoclonus and epileptic seizures: a real-world pharmacovigilance analysis.

Zhang Fu F, Yuan Wenjun W, Yao Jingxi J, Wei Yushu Y et al.

Drug-related myoclonus and epileptic seizures are neurological adverse events that may cause trauma, impaired consciousness, hospitalization, treatment interruption, and life-threatening outcomes. In practice, these events may be difficult to distinguish from neurological diseases, metabolic abnormalities, disease progression, or complications of comorbidities and polypharmacy. Research has focused on individual drugs, case reports, or specific populations, leaving the risk-drug spectrum, sex-related reporting patterns, and onset characteristics insufficiently characterized. Systematic evaluation of these features is important for early identification, optimized monitoring, and individualized risk management. FAERS reports from 2004Q1 to 2025Q4 were analyzed. Drug names were standardized using RxNorm, and adverse events were identified using MedDRA 27.1 preferred terms. Primary suspect drugs were evaluated by reporting odds ratio (ROR)-based disproportionality analysis. Sex-stratified analysis, ATC classification, time-to-onset (TTO) analysis, Weibull modeling, and cross-database validation using CVARD were performed. Reports were concentrated in North America, Europe, and East Asia, with female predominance and most patients aged 18-65 years. A total of 165 myoclonus-related and 235 epileptic seizure-related risk drugs were identified. Nervous system agents predominated, while antiinfectives, antineoplastic and immunomodulating agents, metabolic drugs, and cardiovascular agents also contributed. Bupropion had the highest report count (1,412; 265 myoclonus and 1,147 epileptic seizure reports), followed by tramadol (829). For myoclonus, gabapentin showed strong signals in males (ROR = 23.31, 95% CI: 20.95-25.95) and females (ROR = 18.06, 95% CI: 16.24-20.08), whereas tranexamic acid showed the strongest male signal (ROR = 128.41, 95% CI: 98.29-167.75). For epileptic seizures, bupropion showed signals in males (ROR = 18.08, 95% CI: 16.21-20.17) and females (ROR = 20.21, 95% CI: 18.70-21.85), with tramadol signals in both sexes. Drugs exhibited early-failure Weibull patterns (β < 1). Median TTOs were 16.5 days for pregabalin-related myoclonus and 31.0 days for tramadol-related seizures, but 214.0 days for lamotrigine and 387.0 days for interferon beta-1a. CVARD identified 498 myoclonus-related and 940 seizure-related drugs and reproduced core signals, including clozapine, gabapentin, baclofen, pregabalin, sertraline, bupropion, quetiapine, and olanzapine. Integrating signal detection, sex-stratified analysis, TTO modeling, and cross-database validation identified core risk drugs and monitoring windows, supporting earlier recognition and individualized management of drug-related neurological adverse events.

PMID 42712776
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PubMedFrontiers in pharmacology2026-09-08

Comparative pharmacotherapeutic efficacy and dose-related safety profiles of intrathecal baclofen: a systematic review and meta-analysis in neurological spasticity.

Chen Haoyuan H, Lei Honghui H, Yu Yang Y, Ma Caizhi C et al.

Intrathecal baclofen (ITB) acts as a selective GABAB receptor agonist to modulate spinal inhibitory pathways. While effective for severe spasticity, the pharmacotherapeutic efficacy and safety profile across distinct neurological etiologies-cerebral palsy (CP), spinal cord injury (SCI), and brain injury (BI)-remain poorly characterized from a comparative pharmacological perspective. We systematically searched five global databases (up to August 2025) for trials evaluating ITB therapy. Random-effects models were employed to synthesize efficacy data, focusing on dose-response relationships and clinical outcomes. 15 studies (6 RCTs, 9 observational) were analyzed. Our results demonstrate that ITB significantly reduced Ashworth Scale scores across all subgroups, but with marked etiology-specific variations in effective dosage requirements. Specifically, SCI patients exhibited the most significant reduction in spasm frequency. Safety pharmacology analysis revealed that pharmacological adverse events (AEs), such as somnolence and respiratory depression, were dose-dependent and more prevalent in BI populations. In contrast, hardware-related complications (e.g., catheter malfunction) were idiosyncratic but clinically severe. ITB therapy provides robust anti-spasticity effects mediated through its targeted action on spinal inhibitory circuits. However, the heterogeneity in dosage efficacy suggests etiology-driven differences in GABAB receptor sensitivity or drug distribution. These findings underscore the necessity for precision titration strategies based on patient-specific pathophysiology and highlight the importance of differentiating between pharmacodynamic side effects and mechanical complications to optimize the therapeutic index of ITB. https://www.crd.york.ac.uk/PROSPERO/view/CRD420251112388, identifier CRD420251112388.

PMID 42707787
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PubMedRegional anesthesia and pain medicine2026-09-08

Implanted intrathecal drug delivery systems: a narrative review for the perioperative, obstetric, and intensive care anesthesiologist.

Jenkinson Robert R, Jergensen Tyson T, Sivanesan Eellan E, Leffert Lisa L et al.

Patients with implanted intrathecal drug delivery systems (IDDS) present unique challenges for anesthesiologists in the perioperative, peripartum, and intensive care settings. A comprehensive and practical review on this topic is needed. This narrative review highlights essential knowledge required for safe management of this patient population, including familiarity with: (1) IDDS technology and therapeutics; (2) the appropriateness of neuraxial procedures in IDDS patients; and (3) IDDS-related complications in the operating room and intensive care unit. A literature search was conducted using PubMed/MEDLINE and Google Scholar with the following keywords: intrathecal pump, intrathecal drug delivery, intrathecal morphine, perioperative medicine, labor anesthesia, regional anesthesia, and intrathecal baclofen. Reference lists of relevant articles were manually screened to identify additional pertinent studies, case series, and case reports. Intrathecal pump device manuals were also reviewed to obtain technical details. Based on the available evidence, we provide background medical knowledge and guidance regarding IDDS across five main sections: intrathecal pharmacology, considerations related to IDDS implantation, perioperative care of patients with IDDS, neuraxial anesthesia, and device-related safety concerns. In each section, we summarize available literature and provide contextual interpretation informed by expert opinion when evidence is limited. This review provides a comprehensive overview of current best practices for the perioperative management of patients with IDDS, emphasizing evidence-based approaches to optimize clinical outcomes and ensure patient safety. Key topics covered include intrathecal medications, their performance under MRI, and precautions prior to attempting any neuraxial access in patients with IDDS.

PMID 42710951
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PubMedThe Journal of neuroscience nursing : journal of the American Association of Neuroscience Nurses2026-09-08

Expressions of Pain and Spasticity in People With Stroke.

Bhimani Rozina R, Charania Kaif K, Xiong Jiayue J, Anderson Lisa L

Pain and spasticity are prevalent poststroke symptoms that frequently co-occur. The coexistence of spasticity and pain in patients with neurological injury can be attributed to maladaptive neuronal changes within the central nervous system. This secondary analysis aimed to explore the patterns, descriptors, and temporal trajectories of pain as they relate to spasticity experiences in people with stroke. A secondary analysis was conducted on data acquired from a sample of 22 people with stroke. Data included longitudinal numerical ratings and expressions of pain and spasticity from admission to the rehabilitation unit to 1-month follow-up, alongside qualitative descriptors of these sensations. Graphical analysis revealed that spasticity scores generally remained higher than or equal to pain scores, acting as the primary physical driver. Pain trajectories exhibited an overall upward linear trend despite daily fluctuations. Participants used distinct descriptors for each symptom, though "heaviness" and "numbness" emerged as common overlapping terms, indicating sensory blurring. The intensity of pain reported on the evening of the first admission day appears to set the subsequent pain trajectory; participants with lower initial evening pain maintained consistently lower levels throughout the study period. Notably, while 100% of participants were prescribed acetaminophen, only 30% received antispasticity medication baclofen, despite high spasticity ratings (levels 8-10). Poststroke pain is inextricably linked to spasticity, with the latter serving as a foundational trigger. The commingling nature of these symptoms and the identified temporal surges suggest that clinical management should prioritize early antispasticity interventions. Neuroscience nurses play a vital role in identifying these trajectories early to prevent chronic symptom escalation.

PMID 42709934
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