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neostigmine/glycopyrolate
Neostigmine inhibits acetylcholinesterase to increase acetylcholine levels, while glycopyrolate blocks muscarinic receptors to counteract parasympathomimetic side effects.
Neostigmine inhibits acetylcholinesterase to increase acetylcholine levels, while glycopyrolate blocks muscarinic receptors to counteract parasympathomimetic side effects. Used for Reversal of neuromuscular blockade following anesthesia, Myasthenia gravis (neostigmine component).
At a glance
| Generic name | neostigmine/glycopyrolate |
|---|---|
| Sponsor | Henry Ford Health System |
| Drug class | Cholinesterase inhibitor with anticholinergic agent |
| Target | Acetylcholinesterase (neostigmine); muscarinic acetylcholine receptors (glycopyrolate) |
| Modality | Small molecule |
| Therapeutic area | Neurology / Anesthesia |
| Phase | FDA-approved |
Mechanism of action
Neostigmine is a cholinesterase inhibitor that prevents the breakdown of acetylcholine, thereby enhancing cholinergic neurotransmission. Glycopyrolate is an anticholinergic agent added to this combination to block unwanted muscarinic effects (such as excessive salivation, bronchospasm, and bradycardia) that would otherwise result from neostigmine monotherapy. Together, they provide enhanced nicotinic effects while minimizing parasympathomimetic adverse effects.
Approved indications
- Reversal of neuromuscular blockade following anesthesia
- Myasthenia gravis (neostigmine component)
Common side effects
- Bradycardia
- Muscle fasciculations
- Increased salivation (if glycopyrolate inadequate)
- Bronchospasm
- Nausea
Key clinical trials
- Comparison of Reversal of Neuromuscular Blockade With Sugammadex Versus Neostigmine Plus Glycopyrolate in Patients Undergoing Burn Surgery (PHASE3)
- Residual Neuromuscular Blockade in Cardiac Surgery Patients (PHASE4)
- Deep NMB in Ambulatory Gynecological Laparoscopy (PHASE4)
- Deep vs Moderate Neuromuscular Blockade in Day Case Laparoscopic Cholecystectomy. (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/glycopyrolate CI brief — competitive landscape report
- neostigmine/glycopyrolate updates RSS · CI watch RSS
- Henry Ford Health System portfolio CI