Chronic drooling (sialorrhea) is a common dysfunction in children with neurologic disorders such as cerebral palsy. Glycopyrrolate oral solution, an anticholinergic agent, is the first drug treatment approved in the US for drooling in children with neurologic conditions. This article reviews the clinical efficacy and tolerability of glycopyrrolate oral solution in pediatric patients with neurologic conditions and provides an overview of the pharmacological properties of the drug. In a phase III, randomized, double-blind, multicenter trial, children (aged 3-16 years; n = 36) with problem drooling associated with neurologic conditions and receiving glycopyrrolate oral solution had a significantly (p < 0.01) greater modified Teacher's Drooling Scale (mTDS) response rate at 8 weeks (primary endpoint) than those receiving placebo (73.7% vs 17.6%). At 24 weeks in an additional, noncomparative, phase III study, 52.3% of glycopyrrolate oral solution recipients (aged 3-18 years; n = 137) had an mTDS response (primary endpoint); the response rate was consistently above 50% at all 4-weekly timepoints, aside from the first assessment at week 4 (40.3%). In general, glycopyrrolate oral solution was well tolerated in clinical trials. The majority of adverse events were within expectations as characteristic anticholinergic outcomes.