glycopyrrolate (inhaled)
Brand: Seebri Neohaler, Lonhala Magnair, Bevespi Aerosphere (with formoterol)
Prototype: tiotropium
Drug Class: muscarinic receptor antagonist (LAMA)
Drug Family: bronchodilator
Subclass: long-acting quaternary ammonium anticholinergic
Organ Systems: respiratory
Mechanism of Action
Competitive muscarinic antagonist; the quaternary ammonium structure confers minimal systemic absorption and CNS penetration; M3 receptor blockade in bronchial smooth muscle prevents acetylcholine-mediated bronchoconstriction; M1 and M2 blockade reduces secretions and reflexive bronchoconstriction.
M1, M2, M3 muscarinic receptors (airway smooth muscle and glands)
Indications
- COPD maintenance bronchodilator therapy
Contraindications
- hypersensitivity to glycopyrrolate or any excipient
Adverse Effects
Common
- upper respiratory tract infection
- urinary tract infection
- hypertension
- dry mouth
Serious
- acute urinary retention
- narrow-angle glaucoma exacerbation
- paradoxical bronchospasm
Pharmacokinetics (ADME)
| Absorption | inhaled; Cmax within 5 minutes; low systemic absorption due to quaternary structure |
| Distribution | low volume of distribution systemically; quaternary structure prevents CNS penetration |
| Metabolism | hydrolysis and limited hepatic CYP3A4; primarily excreted unchanged |
| Excretion | renal (as unchanged drug) |
| Half-life | approximately 33-53 hours (pulmonary elimination slower than systemic) |
| Onset | within 5 minutes |
| Peak | 5-15 minutes |
| Duration | 12-24 hours depending on formulation |
| Protein Binding | 38-41% |
| Vd | low systemic Vd due to quaternary structure |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| other anticholinergic agents | additive anticholinergic systemic effects | moderate |
| inhaled glycopyrrolate is distinct from oral/IV glycopyrrolate | different pharmacokinetic profiles; do not substitute formulations | minor |
Nursing Considerations
- Seebri Neohaler requires capsule puncturing and inhalation via device; Lonhala Magnair is a nebulized solution — verify which formulation is prescribed and ensure patient has the appropriate device.
- The quaternary ammonium structure of inhaled glycopyrrolate results in minimal systemic anticholinergic effects compared with tertiary amines like ipratropium; however, urinary retention remains a risk in susceptible patients.
- Screen patients for BPH, narrow-angle glaucoma, or other anticholinergic contraindications before initiating; instruct patients to avoid allowing inhaled solution to contact eyes.
- This is a maintenance medication only; a SABA must be prescribed for acute symptom relief — reinforce the distinction between maintenance and rescue inhaler therapy at every visit.
Clinical Pearls
- Inhaled glycopyrrolate's minimal systemic absorption (quaternary structure) and minimal CNS penetration make it preferable over some other anticholinergics in elderly patients where CNS anticholinergic effects (confusion, delirium) are a concern.
- In combination with formoterol (Bevespi Aerosphere), inhaled glycopyrrolate provides dual bronchodilation comparable to tiotropium-based combinations while offering the convenience of a metered-dose inhaler platform.
Safety Profile
Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Required
Hepatic Adjustment Not required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.