tiotropium
Brand: Spiriva
Prototype Drug
Drug Class: bronchodilator
Drug Family: bronchodilator
Subclass: long-acting muscarinic antagonist (LAMA)
Organ Systems: respiratory
Mechanism of Action
Once-daily LAMA with prolonged M3 receptor binding dissociation; reduces bronchoconstriction, mucus secretion, and mucociliary dysfunction; kinetically selective for airway M3.
muscarinic M3 receptor (bronchial smooth muscle and mucus glands)
Indications
- COPD (first-line)
- asthma (adjunct in uncontrolled disease)
Contraindications
- urinary retention
- narrow-angle glaucoma
Adverse Effects
Common
- dry mouth (most common)
- urinary retention
- constipation
- blurred vision (if drug contacts eyes)
Serious
- paradoxical bronchospasm
- severe urinary retention
- acute angle-closure glaucoma
Pharmacokinetics (ADME)
| Absorption | inhaled (Handihaler powder or Respimat mist) |
| Distribution | local lungs; some systemic |
| Metabolism | CYP3A4 minor |
| Excretion | renal 14% unchanged |
| Half-life | 5-6 days (accumulation to steady state) |
| Onset | 5 min (bronchodilation) |
| Peak | 1-3 hours |
| Duration | 24 hours |
| Protein Binding | 72% (locally) |
| Vd | low systemic |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| other anticholinergics | additive anticholinergic side effects | major |
Nursing Considerations
- Once-daily dosing — same time each day
- Rinse mouth after use to reduce dry mouth
- Advise patient NOT to exhale into Handihaler device (moisture damages capsule)
- Monitor for urinary retention (prostatic hyperplasia patients)
- Screen for narrow-angle glaucoma before use — avoid contact with eyes (mist inhaler)
Clinical Pearls
- UPLIFT trial: tiotropium reduced COPD exacerbations, improved QoL, slowed FEV1 decline
- Kinetically selective: long dissociation from M3 (slow-off) while fast dissociation from cardiac M2 (safety)
Safety Profile
Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Required
Hepatic Adjustment Not required
TDM Not required
Guideline Update pending
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.