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glycopyrrolate (Robinul Forte / Robinul / Cuvposa)

✓ Approved

Merz · CHRM1 · Small Molecule

What is glycopyrrolate?

glycopyrrolate is a small molecule developed by Merz. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesRobinul Forte, Robinul, Cuvposa
CompanyMerz
Drug ClassSmall Molecule
Molecular TargetCHRM1, CHRM3
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Merz

Mechanism of Action

Molecular Targets

glycopyrrolate acts on 2 molecular targets:

CHRM1cholinergic receptor muscarinic 1 (M1, HM1)
CHRM3cholinergic receptor muscarinic 3 (HM3, PBS)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

glycopyrrolate is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Gastrointestinal disordersSalivary hypersecretion✓ Approved

Related Research Articles

PubMedAnaesthesia, critical care & pain medicine2026-11-10

Sugammadex versus Neostigmine-Glycopyrrolate for Reducing the Risk of Postoperative Urinary Retention in High-Risk Patients Undergoing Otolaryngologic Surgery: A Randomised Controlled Trial.

Lin Yueh-Juh YJ, Chan Kuang-Cheng KC, Lin Pei-Lin PL

Postoperative urinary retention (POUR) is a clinically important postoperative complication, particularly in patients at high risk for voiding dysfunction. Sugammadex reverses aminosteroid neuromuscular blockade without requiring concomitant antimuscarinic administration and may therefore reduce the risk of POUR compared with neostigmine-glycopyrrolate. In this prospective randomised trial, 124 adults at high risk for POUR undergoing elective otolaryngologic surgery were randomly assigned (1:1) to receive neostigmine-glycopyrrolate or sugammadex for neuromuscular block reversal. The primary outcome was confirmed POUR, defined as inability to void requiring urinary catheterisation with an ultrasound-confirmed bladder volume ≥400 mL. Secondary outcomes included postoperative nausea and vomiting, haemodynamic events, patient-reported thirst intensity, and hospital length of stay. Confirmed POUR occurred in 12 of 62 patients (19.4%) in the neostigmine-glycopyrrolate group and in none of the 62 patients (0%) in the sugammadex group (risk difference, 19.4%; 95% CI, 9.5%-30.9%; P <  0.001; NNT = 6). Exploratory analysis showed that symptomatic urinary retention was also more frequent with neostigmine-glycopyrrolate than with sugammadex (40.3% vs. 4.8%; P <  0.001). No statistically significant between-group differences were observed in postoperative nausea and vomiting, haemodynamic events, thirst intensity, or hospital length of stay; secondary-outcome comparisons were not powered to detect between-group differences. Among patients at high risk for POUR undergoing elective otolaryngologic surgery, sugammadex reduced the risk of confirmed POUR compared with neostigmine-glycopyrrolate. Comparisons of secondary outcomes were underpowered and should be interpreted cautiously. ClinicalTrials.gov (NCT06398899; principal investigator: Pei-Lin Lin; registered on 5 March 2024).

PMID 43009017
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PubMedChronic obstructive pulmonary diseases (Miami, Fla.)2026-10-29

Pharmacodynamic Equivalence and Safety of Budesonide/Glycopyrrolate/Formoterol Fumarate With a Next-Generation Propellant Versus Hydrofluoroalkane-134a Propellant: A Randomized Phase 3 Study in Chronic Obstructive Pulmonary Disease.

Camiolo Matthew M, Pandya Hitesh H, Jassal Mandeep M, Bednarczyk Artur A et al.

To understand the efficacy, safety, and tolerability of the budesonide/glycopyrrolate/formoterol fumarate (BGF) pressurized metered-dose inhaler (pMDI) with the next-generation propellant hydrofluoroolefin-1234ze (HFO-1234ze), a propellant with substantially lower global warming potential, versus hydrofluoroalkane-134a (HFA-134a). This randomized, 3-way crossover study (NCT06075095) assessed pharmacodynamic equivalence and safety of BGF HFO-1234ze versus BGF HFA-134a in participants with chronic obstructive pulmonary disease. Participants received twice-daily doses for 4 weeks in 3 consecutive treatment periods: A) BGF HFO-1234ze 320/18/9.6 μg, B) BGF HFA-134a 320/18/9.6 μg, and C) placebo HFA-134a in 1 of 6 randomized sequences. Two lung function endpoints (change from baseline in post-dose FEV1 area under the curve 0-4h [FEV1 AUC0-4h; primary] and morning pre-dose trough FEV1 [secondary] at Day 29) were assessed. Superiority of BGF HFA-134a versus placebo HFA-134a was assessed to demonstrate assay sensitivity. Propellant equivalence was demonstrated if 2-sided 90% CIs for ratios of BGF HFO-1234ze/BGF HFA-134a for both lung function endpoints were within 0.8-1.25 and 0.7-1.43, respectively. Safety was also assessed. 296 participants were randomized and started treatment. Superiority of BGF HFA-134a versus placebo HFA-134a, and thus, assay sensitivity for the effect of BGF was confirmed for both lung function endpoints (p<0.001). Change from baseline in post-dose FEV1 AUC0-4 and morning pre-dose trough FEV1 at Day 29 were equivalent between BGF HFO-1234ze and BGF HFA-134a (Ratio [90% CI]: 0.94 [0.88, 1.00]; 0.95 [0.84, 1.08], respectively). Adverse events were balanced across treatments. Findings support the switch from HFA-134a to HFO-1234ze in BGF pMDIs.

PMID 42954429
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PubMedThe Journal of asthma : official journal of the Association for the Care of Asthma2026-10-18

A prospective observational real-world study to assess the effectiveness and safety of single-inhaler triple therapy with glycopyrrolate/formoterol fumarate/budesonide in patients with uncontrolled asthma.

Thekkinkattil Mohankumar M, Katiyar Subodh S, Gopal Bharat B, Saha Arnab A et al.

Individuals with asthma remain inadequately controlled despite treatment with inhaled corticosteroid and long-acting β2-agonist (ICS/LABA) therapy. Single-inhaler triple therapy (SITT) combining ICS, LABA, and long-acting muscarinic antagonist (LAMA) offers a practical treatment escalation option. This study aims to assess the real-world effectiveness, safety, and adherence of SITT with budesonide/glycopyrrolate/formoterol fumarate in adults with uncontrolled asthma. This multicentric, prospective, observational study was conducted across five centers in India. Adults with uncontrolled asthma on stable ICS/LABA therapy who were prescribed SITT as part of routine care were followed for 12 weeks. Changes in lung function, asthma control (ACT), and quality of life (Mini-AQLQ) were assessed. Medication adherence, adverse events, and asthma exacerbations were recorded. Of 258 enrolled patients, 231 were included in the final analysis. Spirometry measurements showed notable improvements before and after bronchodilator use (all p < 0.012). These included higher MMEF values, suggesting improved small-airway function. Mean ACT scores improved from 14.29 at baseline to 18.49 at follow-up. Mini-AQLQ scores also improved over 12 weeks, indicating better patient-reported quality of life. Medication adherence was high, and no asthma exacerbations, adverse events, or serious adverse events were reported during follow-up. In routine practice, SITT BGF was associated with short-term improvements in lung function, asthma control, and QoL in adults with uncontrolled asthma. The mean ACT improved to partially controlled range at 12 weeks. Results suggest short-term effectiveness and tolerability, but longer-term and comparative studies are needed.

PMID 42892309
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PubMedCureus2026-10-17

Comparison of Sugammadex and Neostigmine for Reversal of Vecuronium-Induced Neuromuscular Blockade in Pediatric Patients: A Prospective Randomized Study.

Tiwari Neha N, Agarwal Aarti A, Verma Shilpi S, Goyal Puneet P et al.

Background and objective Neuromuscular blocking agents (NMBAs) used during general anesthesia require effective reversal to prevent residual paralysis. Neostigmine, the conventional reversal agent, is associated with slower recovery and muscarinic side effects. Sugammadex selectively encapsulates amino-steroidal NMBAs, providing rapid and predictable reversal. This study compared the efficacy, safety, and recovery profile of sugammadex and neostigmine for reversal of vecuronium-induced neuromuscular blockade in children. Methods In this prospective, randomized, double-blind trial, 100 children aged two to 12 years (American Society of Anesthesiologists (ASA) I-III) undergoing elective surgery requiring general anesthesia were randomized to receive sugammadex (2 mg/kg) or neostigmine (50 mcg/kg) with glycopyrrolate (10 mcg/kg). Neuromuscular function was monitored using train-of-four (TOF) stimulation. The primary outcome was time to achieve TOF ratios of ≥0.9 and 1.0 after reversal. Secondary outcomes included residual neuromuscular blockade, functional respiratory recovery assessed by tidal volume, hemodynamic adverse events, and respiratory complications. Results Demographic and intraoperative characteristics were comparable between groups. The median time (±IQR) to achieve TOF ≥0.9 and 1.0 was significantly shorter with Sugammadex than with Neostigmine [70(65-108) vs 252(240-280) and 85.5(75-142) vs 272(255-304) seconds, respectively, p = 0.001]. Heart rate was significantly higher following reversal with neostigmine and glycopyrrolate than with sugammadex, with the difference peaking at five minutes and progressively narrowing thereafter, but remaining significant for up to 1.5 hours after arrival in the post-anesthesia care unit. Tidal volume increased more rapidly with sugammadex than neostigmine after reversal, although this exploratory secondary outcome does not establish a causal relationship. Conclusions Sugammadex provided significantly faster and more reliable reversal of vecuronium-induced neuromuscular blockade in children aged two to 12 years, compared to neostigmine (as shown by neuromuscular monitoring), with less tachycardia following reversal.

PMID 42889689
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PubMedThe journal of ECT2026-10-13

Percussion Pacing as a Rescue for Peri-Stimulus Asystole During Electroconvulsive Therapy.

Arora Vivek V, Kataria Sandeep S

Electroconvulsive therapy (ECT) can provoke a brief parasympathetic surge, commonly causing transient sinus bradycardia or a short sinus pause. Most events last only seconds and resolve without intervention. Rarely, however, bradyarrhythmia or asystole may persist long enough to threaten cerebral perfusion, requiring anesthesia teams to respond immediately. We report the case of a male patient with treatment-resistant major depressive disorder who underwent bilateral ECT under methohexital and succinylcholine. Baseline sinus bradycardia was present at 47 beats per minute. Immediately after the ECT stimulus, the monitor demonstrated high-grade atrioventricular block that progressed to ventricular asystole with a flat plethysmographic waveform. Within 10 to 15 seconds, while glycopyrrolate and epinephrine were being prepared, percussion pacing was delivered using the ulnar aspect of a closed fist over the left lower sternal edge at ∼ the fourth-to-fifth intercostal space. Each blow produced a QRS complex on electrocardiography and a pulsatile deflection on the plethysmogram. An organized intrinsic rhythm returned after 3 impulses. The patient recovered uneventfully, and subsequent ECT sessions were preceded by prophylactic intravenous glycopyrrolate without recurrence. This case describes percussion pacing as an immediately deployable, equipment-free bridge within the cardiovascular rescue strategy for ECT services, with a low threshold to escalate to chest compressions and advanced cardiac life support.

PMID 42864698
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PubMedAmerican journal of veterinary research2026-10-07

Cardiovascular effects of increasing doses of glycopyrrolate in anesthetized New Zealand white rabbits.

Marchiori Jocelyn J M JJM, Sanchez Andrea A, Beaufrère Hugues H, Hawker William W et al.

To characterize the cardiovascular effects of 3 increasing doses of glycopyrrolate in healthy rabbits anesthetized with isoflurane. 9 healthy 1-year-old female New Zealand white rabbits were anesthetized with isoflurane and received increasing doses of glycopyrrolate at low dose (LD; 0.025 mg/kg), medium dose (MD; 0.05 mg/kg), and high dose (HD; 0.1 mg/kg) IV. Heart rate was recorded at baseline and 3, 5, 10, 20, and 30 minutes after administration of each dose. An arterial blood sample was collected to measure plasma glycopyrrolate concentrations at baseline and 3 and 30 minutes after administration of each dose. Analysis of plasma glycopyrrolate concentrations was performed using LC-MS-MS. The HD led to a significantly higher heart rate δ value than LD and MD only at 3 minutes (all P < .003). The HD caused significantly higher systolic arterial pressure and mean arterial pressure δ values at 3, 5, 20, and 30 minutes (P < .05) and diastolic arterial pressure at 3, 20, and 30 minutes (P < .05) than LD. The MD caused a significantly higher diastolic arterial pressure δ value at 20 and 30 minutes (P < .05) and mean arterial pressure at 5, 20, and 30 minutes (P < .05) than LD. The mean plasma concentration that elicited a significant increase in heart rate was 62 ± 16.11 ng/mL. A brief increase (< 5 minutes) in HR in nonbradycardic rabbits was observed with 0.1 mg/kg of glycopyrrolate during isoflurane anesthesia. Even at HDs, clinical effects of glycopyrrolate in rabbits appear very short lived.

PMID 42843405
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