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Neostigmine and 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 Myasthenia gravis, Reversal of neuromuscular blockade (anesthesia).
At a glance
| Generic name | Neostigmine and Glycopyrrolate |
|---|---|
| Also known as | Glycostigmin. |
| Sponsor | James J. Peters Veterans Affairs Medical Center |
| Drug class | Cholinesterase inhibitor with anticholinergic agent |
| Target | Acetylcholinesterase (neostigmine); Muscarinic acetylcholine receptors (glycopyrrolate) |
| Modality | Small molecule |
| Therapeutic area | Neurology |
| Phase | FDA-approved |
Mechanism of action
Neostigmine is a cholinesterase inhibitor that prevents the breakdown of acetylcholine, thereby enhancing neuromuscular transmission and parasympathetic activity. Glycopyrrolate 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 the therapeutic benefits of cholinergic enhancement while mitigating parasympathomimetic adverse effects.
Approved indications
- Myasthenia gravis
- Reversal of neuromuscular blockade (anesthesia)
Common side effects
- Dry mouth
- Blurred vision
- Tachycardia
- Muscle fasciculations
- Increased intraocular pressure
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 vs Neostigmine Reversal in Pediatric Appendectomy (PHASE4)
- Pharmacokinetics of Neostigmine and Glycopyrrolate (EARLY_PHASE1)
- Transdermal Administration by a Novel Wireless Iontophoresis Device (EARLY_PHASE1)
- Sugammadex v.s. Neostigmine/Glycopyrrolate (NA)
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 |
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