Tiotropium

Antimuscarinic, Long-acting muscarinic antagonist (LAMA), Bronchodilator

Tiotropium

Spiriva, Spiriva Respimat

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Titration strategies

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Summary

Classes

Antimuscarinic, Long-acting muscarinic antagonist (LAMA), Bronchodilator

Pharmacy

Starting dose

18 mcg DPI once daily (HandiHaler); 2.5 mcg per actuation × 2 inhalations once daily (Respimat)

Preparations

18 mcg HandiHaler capsules; 2.5 mcg/actuation Respimat solution inhaler (1.25 mcg/actuation for asthma indication)

US FDA Max

One dose per day

Pharmacology

Routes

Inhaled (DPI, soft-mist inhaler)

Onset

Bronchodilation 30 minutes; steady-state at 1-2 weeks

Duration

24 hours (long receptor dissociation half-life from M3)

Half-life

~25-44 hours plasma; receptor kinetics drive the once-daily duration

Bioavailability

Inhaled lung deposition ~20%; systemic absorption from lung ~33%; oral component negligible

Pregnancy

Limited data; LABA/LAMA strategies in pregnancy generally favor agents with the most reassuring data.^{[citation needed]}

Legal status

Rx-only in US

Purported mechanism

Tiotropium is a long-acting muscarinic antagonist binding M1/M2/M3 receptors with markedly slower dissociation from M3 (the airway-relevant subtype) than from M2, producing functional M3 selectivity and 24-hour bronchodilation from once-daily dosing.▲0▼ Class adverse effects are anticholinergic in nature (dry mouth, urinary retention, blurred vision, constipation), though systemic absorption from inhaled administration is low. Use with caution in narrow-angle glaucoma and bladder-outlet obstruction.