Glycopyrrolate
ROBINUL
What it isQuaternary antimuscarinic with minimal CNS entry; secretion control, bradycardia, and sialorrhea.
Why this oneMinimal CNS entry lets it dry secretions with less confusion than atropine.
What limits itPeripheral anticholinergic effects remain: urinary retention, constipation, blurred vision, and impaired sweating.
FDA-approved for
- secretions/ulcers (~1961)
Off-label
- clozapine-induced sialorrhea
- hyperhidrosis
- secretion control at end of life
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Reduction of GI symptoms (anticholinergic) | Adults | 1 mg TID (AM, early PM, bedtime) | 1 mg BID (maintenance) | 8 mg/day |
Renal Substantially renally excreted; monitor for anticholinergic reactions and discontinue if they occur
Hepatic Undefined
Instructions
- Use lowest effective dose; some patients need 2 mg at bedtime
- 2 mg tablets not recommended when a 1 mg strength is appropriate for initial/maintenance dosing
Contraindications
- Glaucoma
- Obstructive uropathies (e.g., prostatic hypertrophy)
- Mechanical GI obstruction (pyloroduodenal stenosis, strictures)
- GI motility disorders (achalasia, paralytic ileus, intestinal atony)
- Bleeding GI ulcer
- Active inflammatory or infectious colitis (risk of toxic megacolon)
- History of or current toxic megacolon
- Myasthenia gravis
Cautions
- May precipitate acute angle-closure glaucoma
- Mechanical intestinal obstruction (diarrhea may be early sign)
- Decreased GI motility → ileus/toxic megacolon
- Cognitive/visual impairment (drowsiness, blurred vision)
- Heat prostration in hot environments
- Increased anticholinergic risk in geriatric patients (not recommended)
Adverse reactions
- Blurred vision
- Drowsiness
- Decreased sweating
- Flushing
- Vomiting, constipation
- Dry mouth
- Tachycardia
- Urinary retention
Pregnancy No published human data; no adverse developmental effects in animal studies
Lactation No data; may cause suppression of lactation (anticholinergic)
NO BOXED WARNINGS
Principal riskPeripheral anticholinergic effects; impaired sweating
Cost, est. cash$5–$150/month
Generic entry1983
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.
Mechanism of action: Glycopyrrolate ballicule
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