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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

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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PubMedIndian journal of anaesthesia2026-06-29

Effect of sugammadex versus neostigmine/glycopyrrolate combination on peak expiratory flow rates in adult patients undergoing laparoscopic surgery.

Srihitha Penna P, Saini Vikas V, Samra Tanvir T, Ganesh Venkata V et al.

Residual neuromuscular blockade impacts peak expiratory flow rate (PEFR). The primary aim of this study was to compare post-extubation PEFR in adults undergoing laparoscopic cholecystectomy when neuromuscular blockade was reversed by either neostigmine or sugammadex. Patients aged 18-60 years were randomised into two equal groups of 43 each based on the reversal agent used - sugammadex versus neostigmine. Pre- and post-operative PEFRs were recorded using a handheld flow-type spirometer. Percentage reduction in forced expiratory volume in first second (FEV1), forced vital capacity (FVC), and FEV1/FVC were calculated. Adverse events and recovery scores were compared between the two groups. The post-operative PEFR with sugammadex was 336.88 ± 65.94 L/min, compared to 293.93 ± 43.76 L/min with neostigmine. The mean difference was statistically significant {42.95 L/min [95% confidence interval (CI): 18.95-66.95 L/min], P = 0.001}. The mean percentage reduction in PEFR from baseline was significantly lower with sugammadex (9.66 ± 6.11%) compared to neostigmine (16.33 ± 10.9%). The median time to extubation with sugammadex was 3 min [interquartile range (IQR): 3-4)], and 7 min (IQR: 6-8) with neostigmine (P = 0.001). The time to achieve modified Aldrete score >8 with sugammadex was shorter by an absolute difference of 8.814 (CI = 10.28-7.35) min. No incidence of post-operative pulmonary complication (PPC) was reported in either group. Reversal of neuromuscular blockade with sugammadex is associated with higher post-operative values of PEFR when compared with neostigmine. Higher values of PEFR and FEV1, FVC, and FEV1/FVC ratio after surgery shorten the time to extubation, minimise PPC, and facilitate early post-operative recovery.

PMID 42369978
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PubMedFASEB journal : official publication of the Federation of American Societies for Experimental Biology2026-06-15

Don't Sweat It: Cannabinoid CB1 Receptors Reduce Sweating in a Mouse Model.

Murataeva Natalia N, Youkilis Joseph J, Rao Yogith Y, Straiker Alex A

Numerous exocrine glands play key physiological roles in the body that include tearing, salivation, and lactation, as well as the control of body temperature via sweating. Malfunction of sweat glands can be deeply problematic or-in the case of anhidrosis-life-threatening. The prevalence of sweating disorders is high, affecting millions. The few available therapies are generally of limited effectiveness. Several lines of evidence point to regulation of sweating by the cannabinoid signaling system, an arrangement that would mirror cannabinoid regulation of tearing and salivation. Mice sweat in their paws via glands that closely resemble human eccrine sweat glands, including regulation by muscarinic signaling and by temperature. We applied a galvanic skin response-based assay to investigate cannabinoid regulation of sweating in awake, unanesthetized mice. The muscarinic agonist pilocarpine increased conductance while the antagonist glycopyrrolate reduced conductance, validating the model as a measure of sweating. The cannabinoid receptor agonist CP55940 substantially reduced conductance in wild-type and CB2 but not CB1 receptor knockout mice. The phytocannabinoid tetrahydrocannabinol (THC) also reduced conductance, while the non-psychoactive cannabidiol (CBD) did not. Using immunohistochemistry, we detected CB1 receptors in periglandular cholinergic axons, the anandamide-synthesizing enzyme NAPE-PLD in myoepithelial cells, and the anandamide metabolizing enzyme FAAH in acinar cells. This indicates that a local CB1/anandamide-based circuit is present in mouse walking pads. In summary, we employed a novel galvanic skin response-based assay to determine that cannabinoid CB1 receptors reduce sweating in a mouse model. This may point to a previously unappreciated effect on sweating in cannabis users.

PMID 42287607
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PubMedMedicine2026-06-09

Adverse event mining for Breztri and Trelegy Ellipta based on the three international pharmacovigilance databases.

Wang Junyu J, Chen Kexu K, Yun Lu L, Xu Dexiang D

This study aimed to identify adverse drug reaction (ADR) risk signals associated with budesonide/glycopyrrolate/formoterol (Breztri) and fluticasone furoate/umeclidinium/vilanterol (Trelegy Ellipta) to support clinical decision-making and risk management. ADR reports related to Breztri and Trelegy Ellipta from the FDA Adverse Event Reporting System (FAERS) database, Japanese Adverse Drug Event Report (JADER) database and Canada Vigilance Adverse Reaction database (Q3 2004 to Q2 2024) were analyzed. After deduplication, reports were categorized using Medical Dictionary for Regulatory Activities (MedDRA) to obtain System Organ Class (SOC) and preferred terms (PTs). Disproportionality analysis was conducted using reporting odds ratio (ROR) and proportional reporting ratio methods. Analysis of 394 Breztri and 18,866 Trelegy Ellipta FAERS reports (predominantly consumer-submitted, U.S.-originated) identified 47 signals across 11 SOCs for Breztri (e.g., "Drug delivery system issue" ROR = 411.16, "Intentional device misuse" ROR = 410.69) and 160 signals across 15 SOCs for Trelegy (e.g., "Chronic eosinophilic rhinosinusitis" ROR = 187.65, "Foreign body in mouth" ROR = 107.67), revealing unlabeled risks like administration errors and packaging confusion. JADER data reinforced respiratory risks (Breztri: Chronic obstructive pulmonary disease (COPD) ROR = 516.8; Trelegy: gastrointestinal fungal infection ROR = 413.11) and device-independent safety signals (e.g., Trelegy urinary retention ROR = 28.81), while CVARD highlighted region-specific concerns including Trelegy-associated vasculitis (pulmonary vasculitis n = 29) and Breztri hypertension (ROR = 7.82). Cross-database convergence confirmed core anticholinergic/cardiopulmonary risks, yet divergent signals, FAERS' device errors, JADER's infection prominence, and CVARD's immunological events, underscore geographic heterogeneity in adverse reaction profiles, necessitating tailored risk management strategies for inhaler therapies. Inhalation device-related ADRs were observed, with Breztri showing higher incidence than Trelegy Ellipta, likely due to its more complex device usage. These findings highlight the need for enhanced patient education by healthcare providers to ensure proper device use in COPD treatment. Although core respiratory and anticholinergic risks are globally relevant, infection profiles, device complications, and rare immunological events exhibit significant geographic heterogeneity, necessitating tailored risk mitigation strategies aligned with regional pharmacovigilance patterns.

PMID 42260824
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PubMedCureus2026-05-25

Survival and Closure by Secondary Intention of a Pharyngocutaneous Fistula After Fulminant Descending Necrotizing Mediastinitis.

Zhang Vanessa J VJ, Maxfield Mark W MW, Ito Christopher J CJ

Descending necrotizing mediastinitis is a rare, life-threatening extension of deep neck infection. We report the case of a 51-year-old woman who initially presented with a sore throat and was treated as uncomplicated pharyngitis before rapidly developing neck swelling, chest pain, dyspnea, septic shock, pneumomediastinum, and bilateral pleural empyemas. Combined cervicothoracic exploration showed dishwater fluid in the neck and mediastinum without esophageal perforation, and cultures grew Streptococcus anginosus and mixed oral flora with Actinomyces odontolyticus bacteremia. Her course was complicated by stress-induced cardiomyopathy, acute kidney injury requiring continuous renal replacement therapy, and vasopressor-associated digital ischemia. On hospital day 17, repeat exploration identified a large left hypopharyngeal pharyngocutaneous fistula communicating with the open neck wound. Because of critical illness and poor peripheral perfusion, flap reconstruction was deferred. The fistula was managed with repeated antiseptic packing, strict gastrostomy feeding, salivary suctioning, glycopyrrolate, scopolamine, and later botulinum toxin injections to the parotid and submandibular glands. The defect gradually contracted and closed by secondary intention over approximately 10 weeks. This case highlights that, in carefully selected high-risk patients, structured conservative management with salivary suppression may allow closure of a large pharyngocutaneous fistula after fulminant descending necrotizing mediastinitis.

PMID 42181439
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