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glycopyrrolate (Robinul Forte / Robinul / Cuvposa)

✓ Approved

Merz · CHRM1 · 小分子

什么是 glycopyrrolate？

glycopyrrolate 是一种小分子，由Merz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Robinul Forte, Robinul, Cuvposa
公司Merz
药物类别小分子
分子靶点CHRM1, CHRM3
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Merz

作用机制

分子靶点

glycopyrrolate 作用于 2 个分子靶点：

CHRM1cholinergic receptor muscarinic 1 (M1, HM1)
CHRM3cholinergic receptor muscarinic 3 (HM3, PBS)
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

glycopyrrolate 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 disordersSalivary hypersecretion✓ Approved

相关研究文献

PubMedEuropean journal of internal medicine2026-08-02

Particle engineering, aerosol physics, and pulmonary deposition of single-inhaler triple ICS/LABA/LAMA therapies in obstructive airway diseases.

Sorino Claudio C, Virchow Johann Christian JC, Spanevello Antonio A, Buscemi Agata A et al.

Single-inhaler triple therapy (SITT) combining an inhaled corticosteroid, long-acting β2-agonist, and long-acting muscarinic antagonist (ICS/LABA/LAMA) represents the current ceiling of inhaled pharmacotherapy for moderate-to-very-severe chronic obstructive pulmonary disease and severe uncontrolled asthma. Five device platforms are currently approved: two extrafine formulations delivering beclomethasone dipropionate/formoterol/glycopyrronium (the Modulite solution pressurised metered-dose inhaler [pMDI] and the NEXThaler breath-actuated dry powder inhaler [DPI]); the co-suspension pMDI Aerosphere platform (budesonide/glycopyrrolate/formoterol); the standard-particle Ellipta DPI (fluticasone furoate/umeclidinium/vilanterol); and the low-resistance, single-dose capsule-based DPI Breezhaler (mometasone furoate/indacaterol/glycopyrronium). Despite a shared pharmacological class, these systems differ in aerosol physics, particle engineering, intrapulmonary deposition patterns, and device-patient interaction. Furthermore, some of them are authorized only for COPD or asthma. This narrative review examines the technology and in vivo deposition evidence for each SITT platform, discusses real-world performance determinants (particle size, flow dependency, technique robustness), and proposes an expert-informed framework for patient-level device selection. Methodological limitations include reliance on in silico Functional Respiratory Imaging data when in vivo scintigraphy is unavailable, and inconsistent dose denominators across studies (emitted vs. metered dose). Cross-platform comparisons are limited by heterogeneous methodologies, and no SITT platform has demonstrated universal superiority. In platform-specific studies, NEXThaler shows relatively high lung deposition (∼55% of emitted dose) though flow-dependent; Aerosphere is robust to inhalation technique variations; Modulite provides extrafine, peripheral delivery; Ellipta and Breezhaler offer once-daily convenience with moderate deposition. Rational device selection requires structured assessment of patient inspiratory capacity, disease phenotype, coordination, and adherence. Head-to-head scintigraphy and prospective imaging-outcome studies represent major evidence gaps.

PMID 42542404
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PubMedJournal of clinical anesthesia2026-07-31

Sugammadex aliquot pilot project in adults having elective surgical procedures - A pharmacoeconomic retrospective deidentified chart review to improve quality and cost of anesthesia care.

Labadie Michael M, Verdonck Michaël M, Sanders Jen J, Brull Sorin J SJ

Sugammadex is highly effective in reversing neuromuscular block, but costly and not without known complications. Subjectively determined empiric dosing of sugammadex for routine antagonism of neuromuscular block risks over- or under-dosing patients and leads to increases in drug acquisition costs, especially in markets where generics remain unavailable. We hypothesized that our recently implemented sugammadex aliquoting policy and its administration guided by quantitative neuromuscular monitoring would lower the cost of empirically dosed sugammadex antagonism. This retrospective analysis of 524 patients evaluated the pharmacoeconomic impact of sugammadex aliquoting and administration guided by quantitative neuromuscular monitoring versus subjectively determined routine antagonism of neuromuscular block in adults having elective surgical procedures. This single-center retrospective deidentified chart review included adult patients having elective surgical procedures requiring general anesthesia. Cost of sugammadex ($129.05/200-mg vial) antagonism was based on the assumed routine administration of 1 vial. When using sugammadex aliquots (50 mg/0.5 mL), the dose saved was calculated as 200 mg minus total aliquots used. Gross cost savings per patient were determined by subtracting cost (labor, supplies, drug acquisition) of individual aliquots from actual sugammadex vials acquisition cost. Using neostigmine ($1.99/10 mg vial) and glycopyrrolate ($1.74/0.4 mg vial), the total per-case cost was determined by the number of full vials administered. Actual net cost savings/case included sensor cost ($20.00) and hardware cost ($1995/monitor amortized over 7 years) from gross savings per surgical case. In patients receiving sugammadex aliquots (n = 258), the mean gross cost was $51.50 (mean gross savings, $77.55/case vs. full-vial). Neostigmine/glycopyrrolate (n = 111) mean gross cost, $4.39/case. Patients managed without pharmacological reversal (n = 63) incurred no drug costs (savings of 200-mg sugammadex vial, $129.05). For all patients, mean gross (drugs only) and net (including monitoring) costs per case were markedly lower with aliquoting ($51.50 and $71.66, respectively) compared with full-vial use ($129.05 and $149.21, respectively). Aliquoting yielded total hospital net savings (including quantitative monitoring) of $20,008. Aliquoting and dosing sugammadex guided by quantitative neuromuscular monitoring in this single center reduces annual drug acquisition costs and produces consistent savings across dose ranges.

PMID 42531960
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PubMedCOPD2026-07-29

A Real-World Prospective Observational Study to Describe the Safety Profile and Clinical Outcomes of Budesonide/Glycopyrrolate/Formoterol Fumarate (BGF) In Chinese Patients with Chronic Obstructive Pulmonary Disease (COPD).

Sun Yongchang Y, Chen Yunfeng Y, Zhang Xiuwei X, Guo Ruibin R et al.

This observational, multicenter, prospective, single-arm study (NCT04536402) aimed to describe the safety profile and clinical outcomes of Budesonide/Glycopyrrolate/Formoterol Fumarate metered dose inhaler (BGF MDI) for Chinese patients with COPD in clinical practice. COPD patients who had been prescribed and had planned to take at least one inhalation of BGF MDI were followed-up for 12 weeks at 4-week intervals. The primary endpoints were incidences of adverse events (AEs) and serious adverse events (SAEs). Secondary endpoints included changes from baseline in COPD Assessment Test (CAT) score and St George's Respiratory Questionnaire (SGRQ) score and patient global impression of change (PGIC) scale at week 4. Patients were also stratified into subgroups according to the asthma history, exacerbation history, and baseline treatment and assessed. Of the enrolled 3,317 patients, 2,137 completed and 1,180 discontinued the study. No unexpected safety signals were observed; most AEs were mild (13.2%) or moderate (7.2%). SAEs occurred in 4.9% of patients. BGF MDI was associated with decreased CAT and SGRQ total scores (mean [SD] changes from baseline: -6.7 [7.27], -14.5 [18.19]) and increased FEV1 (189 mL, n = 241) at week 12. Similar trend of improvement was also observed in the subgroups. At week 4, 84.8% rated overall PGIC status as "improved," and 87.6% were satisfied with the MDI device. In real-world practice, BGF MDI demonstrated good tolerability consistent with previous RCTs, and associated with a trend toward improvement in patients' symptoms, quality of life, and lung function, regardless of asthma history, exacerbation history, or baseline treatment. NCT04536402 (ClinicalTrials.gov), registered on 28 August 2020.

PMID 42522405
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PubMedJournal of clinical medicine2026-07-28

Comparative Real-World Effectiveness of Fixed-Dose Triple Therapy Regimens in COPD: A Retrospective Cohort Study.

Patel Rushi R, Thompson Jacob J, Patel Namra N, Lohana Abhi C AC et al.

Background/Objectives: Fixed-dose triple therapy is recommended for patients with chronic obstructive pulmonary disease (COPD) at high risk of exacerbations; however, direct comparative effectiveness data between available triple therapy regimens remain limited. We compared real-world clinical outcomes among adults with COPD receiving fluticasone furoate/vilanterol/umeclidinium (FF/VI/UMEC) or budesonide/glycopyrrolate/formoterol (BUD/GLY/FOR). Methods: We conducted a retrospective propensity score-matched cohort study using the TriNetX Research Network. Adults with a spirometrically confirmed diagnosis of COPD who received fluticasone furoate/vilanterol/umeclidinium (FF/VI/UMEC) or budesonide/glycopyrrolate/formoterol (BUD/GLY/FOR) between July 2020 and August 2024 were included in the analysis. A 365-day landmark period was applied to establish maintenance therapy, with outcome follow-up beginning 1 year after treatment initiation. Patients were followed for outcomes through August 2025, the date of database analysis. After 1:1 propensity score matching, treatment groups were compared for COPD exacerbations, acute respiratory failure (ARF), hospitalization, and all-cause mortality using RR and Cox proportional hazards analyses. Results: In matched cohorts, FF/VI/UMEC was associated with a significantly higher risk of COPD exacerbations (5.6% vs. 3.9%; RR 1.44; 95% CI 1.30-1.59; p < 0.001) and ARF (2.5% vs. 1.9%; RR 1.28; 95% CI 1.11-1.46; p < 0.001) compared with BUD/GLY/FOR. Time-to-event analyses demonstrated lower event-free probability for exacerbations (HR 1.35; (95% CI 1.21-1.50) and ARF (HR 1.15; (95% CI 1.00-1.32))). All-cause mortality was numerically higher in the FF/VI/UMEC cohort (5.2% vs. 4.7%; RR 1.09; 95% CI 1.00-1.19; p = 0.050); however, time-to-event analysis did not demonstrate a statistically significant difference. Hospitalization rates were similar between groups. Conclusions: In this large propensity score-matched real-world cohort study, patients receiving BUD/GLY/FOR experienced lower rates of COPD exacerbations and acute respiratory failure than those receiving FF/VI/UMEC. Because of the retrospective observational nature of the analysis, these findings should be considered hypothesis-generating and require confirmation in prospective comparative effectiveness studies.

PMID 42513564
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PubMedJournal of aerosol medicine and pulmonary drug delivery2026-07-16

Toward Next-Generation Propellants: Assessing Lung Deposition of Beclometasone Dipropionate, Formoterol, and Glycopyrrolate Formulated with HFA-152a Using Functional Respiratory Imaging.

Matturro Angelo A, Monshi Tousi Navid N, Sadafi Hosein H, Cuoghi Erika E et al.

Pressurized metered-dose inhalers (pMDIs) rely on hydrofluoroalkane (HFA) propellants that have a high global warming potential (GWP). Reformulation with next-generation, low-GWP propellants, such as HFA-152a, offers a strategy to reduce climate impact; however, changes in propellant composition can affect aerosol characteristics and potentially alter lung deposition, requiring robust demonstration of therapeutic equivalence. Functional respiratory imaging, combining high-resolution computed tomography and computational fluid dynamics, was used to compare the lung deposition of a fixed triple combination of beclometasone dipropionate, formoterol fumarate, and glycopyrronium bromide (BDP/FF/GB) delivered via a pMDI formulated with either HFA-134a (Reference) or HFA-152a (Test). Ten patients with chronic obstructive pulmonary disease (GOLD stages 2-4) were retrospectively selected. Patient-specific airway geometries, a standardized inhalation profile, and formulation-specific particle size distributions and plume characteristics were applied. Deposition was quantified in the intrathoracic, central + distal, and peripheral lung regions, and the (central + distal)/peripheral ([C + D]/P) deposition ratio was evaluated. Mean intrathoracic deposition was comparable between the Reference and Test formulations, ranging from 45.95% to 46.88% of the delivered dose (DD). Deposition in the central + distal airways accounted for 12% of DD for both formulations, whereas peripheral deposition predominated, with 33.7% of DD for the Test formulation and 34.5% of DD for the Reference formulation. The (C + D)/P ratios were similar across all active components (0.35-0.37), indicating consistent preferential deposition in the peripheral/small airways. Although inter-patient variability was observed, intra-subject comparisons showed close agreement between propellants. Reformulation of the BDP/FF/GB pMDI with the low-GWP propellant HFA-152a preserved total and regional lung deposition characteristics relative to the current HFA-134a formulation. These findings support the maintenance of deposition performance while enabling a substantial reduction in environmental impact, reinforcing the potential of HFA-152a as a next-generation propellant for carbon minimal pMDI therapies.

PMID 42461266
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PubMedJournal of pharmacy practice2026-06-29

Aripiprazole and Unexpected Salivation: A Case of Drug-Induced Sialorrhea Refractory to Anticholinergics.

Yang Charlie C, Eagers Keren K, Kosmisky Desiree D, Nagy Kristen K

Sialorrhea, or excessive drooling, is a distressing side effect of certain antipsychotic medications, including aripiprazole, clozapine, and olanzapine. We present the case of a 53-year-old female with bipolar I disorder who presented with altered mental status, dysphagia, a 2-day history of excessive drooling, and acute hypoxic respiratory failure. Despite being alert and responsive, she required intubation due to the inability to manage oral secretions. At the time, she had been taking aripiprazole 20 mg once daily and lithium 450 mg twice daily for about three months for bipolar 1 disorder, which were continued inpatient. Aripiprazole was discontinued on the third day of hospitalization. Standard treatments for sialorrhea, including anticholinergics such as scopolamine, glycopyrrolate, and sublingual atropine, were ineffective. Substantial improvement only occurred after the initiation of dexmedetomidine, an alpha-2 adrenergic agonist, on day nine, leading to decreased oral secretions and successful extubation. The patient was transitioned to oral clonidine, another alpha-2 adrenergic agonist, and remained extubated for the rest of her hospital stay. Upon further improvement, she was discharged on glycopyrrolate, a 3-day taper of clonidine, and trazodone, with bipolar I disorder management switched to valproic acid monotherapy. This case highlights the potential role of alpha-2 adrenergic agonists in managing refractory aripiprazole-induced sialorrhea, offering a viable alternative when traditional anticholinergic therapies are ineffective.

PMID 42367030
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