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Neostigmine with glycopyrrolate
Neostigmine inhibits acetylcholinesterase to increase acetylcholine levels, while glycopyrrolate blocks muscarinic receptors to counteract cholinergic side effects.
Neostigmine inhibits acetylcholinesterase to increase acetylcholine levels, while glycopyrrolate blocks muscarinic receptors to counteract cholinergic side effects. Used for Reversal of neuromuscular blockade after anesthesia, Myasthenia gravis.
At a glance
| Generic name | Neostigmine with glycopyrrolate |
|---|---|
| Sponsor | The Cleveland Clinic |
| Drug class | Acetylcholinesterase inhibitor with anticholinergic agent |
| Target | Acetylcholinesterase; muscarinic acetylcholine receptors |
| Modality | Small molecule |
| Therapeutic area | Neurology |
| Phase | FDA-approved |
Mechanism of action
Neostigmine is a reversible acetylcholinesterase inhibitor that increases acetylcholine concentration at the neuromuscular junction and in the central nervous system. Glycopyrrolate is an anticholinergic agent added to this combination to prevent excessive muscarinic stimulation (salivation, bronchospasm, bradycardia) that would otherwise result from neostigmine monotherapy. Together, they enhance nicotinic effects while minimizing unwanted muscarinic effects.
Approved indications
- Reversal of neuromuscular blockade after anesthesia
- Myasthenia gravis
Common side effects
- Bradycardia
- Muscle fasciculations
- Increased salivation (despite glycopyrrolate)
- Bronchospasm
- Nausea
Key clinical trials
- Neostigmine and Glycopyrrolate for the Treatment of Headache After Dural Puncture (PHASE2)
- NMBA Reversal and Postoperative Urinary Retention
- Neuromuscular Blockade Comparison for GI-2 Recovery After Bowel Resection (PHASE4)
- The Impact of Sugammadex on Ileus After Abdominal Wall Reconstruction (PHASE4)
- Sugammadex v.s. Neostigmine/Glycopyrrolate (NA)
- Sugammadex vs Neostigmine/Glycopyrrolate on Urinary Retention After Spine Surgery (PHASE4)
- Neostigmine/Glyco-pyrrolate 50 Mikrogram/kg or Sugammadex 2 mg/kg for Reversal of Neuromuscular Blockade in Elderly Patients (PHASE4)
- Efficacy, Safety, and Pharmacokinetics of Sugammadex (MK-8616) for Reversal of Neuromuscular Blockade in Pediatric Participants Aged Birth to <2 Years (MK-8616-169) (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Neostigmine with glycopyrrolate CI brief — competitive landscape report
- Neostigmine with glycopyrrolate updates RSS · CI watch RSS
- The Cleveland Clinic portfolio CI