Side Effects of Topical Glycopyrrolate 2%
Topical glycopyrrolate 2% can cause several anticholinergic side effects including dry mouth, blurred vision, urinary retention, and local skin reactions, with most side effects being mild and localized due to limited systemic absorption compared to oral anticholinergic medications. 1
Common Side Effects
Topical glycopyrrolate, as an anticholinergic medication, produces side effects that are primarily extensions of its pharmacological actions. These include:
Local Effects:
- Skin dryness at application site
- Burning or stinging sensation
- Skin irritation
- Pruritus (itching)
Systemic Effects (Less Common with Topical Application):
- Xerostomia (dry mouth) 1, 2
- Sore throat 3
- Headache 3, 4
- Decreased sweating in non-target areas
- Blurred vision
- Urinary hesitancy and retention
- Tachycardia and palpitations
- Pupil dilation
- Loss of taste
Incidence and Severity
Research studies have demonstrated that side effects from topical glycopyrrolate 2% are generally mild and well-tolerated:
In a study of patients with gustatory hyperhidrosis, adverse effects included mild dry mouth and sore throat in 2 patients using 2% glycopyrrolate, and light headache in 1 patient using 1.5% glycopyrrolate 3
In a comparative study between topical 2% glycopyrrolate and botulinum toxin A for facial hyperhidrosis, side effects were reported as "minor and temporary" 5
In a study of patients with craniofacial hyperhidrosis, topical glycopyrrolate 0.5% was associated with "few adverse effects" even after two years of continued use 4
Pharmacokinetic Considerations
The limited systemic absorption of topical glycopyrrolate contributes to its favorable side effect profile:
- Glycopyrrolate is a quaternary ammonium compound, which limits its passage across lipid membranes like the blood-brain barrier 1
- This results in fewer CNS-related side effects compared to tertiary amine anticholinergics like atropine and scopolamine 1
- A pharmacokinetic study demonstrated limited systemic absorption of topical glycopyrronium tosylate compared to oral glycopyrrolate, with no evidence of drug accumulation 6
Risk Factors for Side Effects
Certain factors may increase the risk of experiencing side effects:
- Higher concentrations (2% vs. lower concentrations)
- Application to larger surface areas
- Occlusion of the treated area
- Concurrent use of other anticholinergic medications
- Pre-existing conditions such as glaucoma, urinary retention, or cardiovascular disease
Management of Side Effects
If side effects occur, the following approaches may be helpful:
- Reducing the concentration of glycopyrrolate
- Decreasing the frequency of application
- Ensuring proper application technique (avoiding occlusion, washing hands after application)
- Discontinuing use if severe side effects occur
Special Considerations
Elderly Patients
Elderly patients may be more sensitive to anticholinergic effects and should be monitored closely for:
- Cognitive impairment
- Urinary retention
- Increased risk of falls
- Exacerbation of glaucoma
Pediatric Patients
Limited data exists on the use of topical glycopyrrolate 2% in pediatric patients, though pharmacokinetic parameters appear similar between adult and pediatric patients 6.
Conclusion
Topical glycopyrrolate 2% is generally well-tolerated with mostly mild and localized side effects. The limited systemic absorption compared to oral anticholinergic medications results in fewer systemic anticholinergic effects. However, patients should be monitored for both local and systemic side effects, particularly those at higher risk for anticholinergic complications.