What are the indications, dosing, and potential side effects of Glycopyrrolate?

From the Guidelines

Glycopyrrolate is an anticholinergic medication that should be used at a dose of 0.1-0.2 mg IV/IM 30-60 minutes before anesthesia for preoperative use, with potential side effects including dry mouth, blurred vision, urinary retention, constipation, and tachycardia due to its anticholinergic mechanism. The indications for glycopyrrolate include reducing secretions before surgery, managing peptic ulcer disease, controlling excessive drooling (sialorrhea), and treating certain types of bowel and bladder disorders.

• For chronic conditions like sialorrhea, oral dosing ranges from 1-2 mg two to three times daily, with pediatric dosing based on weight (typically 40-100 mcg/kg/dose) 1.
• For hyperhidrosis, topical formulations are available.
• Common side effects include dry mouth, blurred vision, urinary retention, constipation, and tachycardia due to its anticholinergic mechanism.
• More severe side effects can include confusion, especially in elderly patients, heat intolerance, and exacerbation of narrow-angle glaucoma. Glycopyrrolate works by blocking muscarinic acetylcholine receptors, thereby inhibiting parasympathetic nervous system activity and reducing secretions from glands.
• It has limited blood-brain barrier penetration compared to other anticholinergics, potentially resulting in fewer central nervous system effects 1. The medication is contraindicated in patients with myasthenia gravis, narrow-angle glaucoma, and certain gastrointestinal obstructive disorders, and should be used cautiously in patients with cardiovascular disease, prostatic hypertrophy, and in geriatric populations 1. Some studies suggest that glycopyrrolate can be used to reduce excessive secretions associated with dyspnea, with a dose of 0.2-0.4 mg IV or subcut q 4 hr prn 1. However, the most recent and highest quality study recommends using glycopyrrolate at a dose of 0.1-0.2 mg IV/IM 30-60 minutes before anesthesia for preoperative use 1.

From the FDA Drug Label

GLYCOPYRROLATE ORAL SOLUTION is an anticholinergic indicated to reduce chronic severe drooling in patients aged 3-16 years with neurologic conditions associated with problem drooling (e.g., cerebral palsy). Initiate dosing at 0.02 mg/kg three times daily and titrate in increments of 0.02 mg/kg every 5-7 days, based on therapeutic response and adverse reactions. The maximum recommended dose is 0.1 mg/kg three times daily, not to exceed 1.5-3 mg per dose based upon weight. The most common adverse reactions (incidence ≥30%) are dry mouth, vomiting, constipation, flushing, and nasal congestion.

The indications of Glycopyrrolate are to reduce chronic severe drooling in patients aged 3-16 years with neurologic conditions associated with problem drooling. The dosing of Glycopyrrolate should be initiated at 0.02 mg/kg three times daily and titrated in increments of 0.02 mg/kg every 5-7 days, based on therapeutic response and adverse reactions. The potential side effects of Glycopyrrolate include constipation, diarrhea and intestinal blockage, problems with control of body temperature, dry mouth, vomiting, flushing of the face or skin, nasal congestion, headache, swollen sinuses, upper respiratory tract infection, and problems urinating. 2

From the Research

Indications of Glycopyrrolate

• Glycopyrrolate is used for the treatment of chronic drooling in children with neurodevelopmental disabilities, such as cerebral palsy 3.
• It is also used to treat clozapine-induced sialorrhea in adults 4.
• Additionally, glycopyrrolate is used to inhibit drooling and excessive secretions of the respiratory tract in various medical conditions 5.
• It has been approved by the US Food and Drug Administration for the treatment of hyperhidrosis (excessive sweating) in topical formulations 5.
• Glycopyrrolate is also used in children with medical complexity under three years of age to decrease drooling 6.

Dosing of Glycopyrrolate

• The dosing of glycopyrrolate varies depending on the indication and patient population. For children with chronic drooling, the initial dose is 0.02 mg/kg per dose orally three times a day, with a maximum dose of 3 mg 3.
• In adults with clozapine-induced sialorrhea, the dose of glycopyrrolate is not specified in the available studies 4.
• For children under three years of age with medical complexity, the median starting daily dose of glycopyrrolate is 0.065 mg/kg/day, divided into three doses 6.

Potential Side Effects of Glycopyrrolate

• Common side effects of glycopyrrolate include dry mouth, constipation, and behavioral changes 3.
• Other potential side effects include arrhythmias, nausea, and vomiting 7.
• In children under three years of age, no major side effects were observed with the use of glycopyrrolate 6.
• The use of glycopyrrolate has been associated with a more stable cardiovascular system and fewer arrhythmias compared to atropine 7.