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Neostigmine w/ Glycopyrrolate

University of Texas Southwestern Medical Center · FDA-approved active Small molecule

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.

At a glance

Generic nameNeostigmine w/ Glycopyrrolate
SponsorUniversity of Texas Southwestern Medical Center
Drug classAcetylcholinesterase inhibitor with anticholinergic agent
TargetAcetylcholinesterase (neostigmine); muscarinic acetylcholine receptors (glycopyrrolate)
ModalitySmall molecule
Therapeutic areaNeurology
PhaseFDA-approved

Mechanism of action

Neostigmine is a reversible acetylcholinesterase inhibitor that increases acetylcholine concentration at the neuromuscular junction and in the central and peripheral nervous systems. 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

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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