is an antagonist of M1, M2 and M3 muscarinic receptors - however it dissociates more slowly from the M1 and M3 subtypes than from the M2 subtype
has a long duration of action (terminal elimination half-life is 5-6 days), which allows it to be taken once daily
with regular once-daily dosing, the maximum effect of tiotropium on forced vital capacity (FVC) may take more than a week to develop fully
seems to be more effective than ipratropium bromide (40µg four times daily) in terms of reduction in exacerbations, but whether it is more effective in improving trough FEV1 is unclear
the most common side effect is a dry mouth
other common adverse effects of tiotropium (affecting 1-10% of patients) include constipation, candidiasis, sinusitis and pharyngitis
uncommon adverse effects (0.1-1.0% of patients) include allergic reactions, urinary difficulty, urinary retention and tachycardia
there have also been isolated reports of atrial fibrillation and supraventricular tachycardia
care should be taken to avoid co-prescription of preparations containing anticholinergics
no consistent difference in health outcomes has been found between long-acting b2-agonists and tiotropium. Therefore, drug choice depends on individual factors and cost
Results of short- and long-term randomized, controlled clinical trials of tiotropium in patients with COPD indicated tiotropium was safe and significantly improved lung function, health-related quality of life, and exercise endurance, and reduced dyspnoea, lung hyperinflation, exacerbations, and use of rescue medication compared with placebo or active comparators.
Tiotropium is safe and efficacious as a long-term, once-daily LAMA for the maintenance treatment of COPD and for reducing COPD exacerbations. The soft mist inhaler (SMI) generates a low-velocity, long-duration aerosol spray with a high fine-particle fraction, which results in marked lung drug deposition.
Reference:
Global Initiative for Chronic Obstructive Lung Disease (GOLD). Global strategy for the diagnosis, management, and prevention of chronic obstructive pulmonary disease: 2025 report. 2025 [internet publication].
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