|Trade names||Spiriva, Braltus|
|Inhalation by mouth|
|Elimination half-life||5–6 days|
|Chemical and physical data|
|Molar mass||472.416 g/mol g·mol−1|
|3D model (JSmol)|
Tiotropium bromide, sold under the brandname Spiriva among others, is a long-acting bronchodilator used in the management of chronic obstructive pulmonary disease (COPD) and asthma. Specifically it is used to try to prevent periods of worsening rather than for those periods themselves. It is used by inhalation through the mouth. Onset typically begins within half an hour and lasts for 24 hours.
Common side effects include a dry mouth, runny nose, upper respiratory tract infection, shortness of breath and headache. Severe side effects may include angioedema, worsening bronchospasm, and QT prolongation. Tentative evidence has not found harm during pregnancy, however, such use has not been well studied. It is an anticholinergic medication and works by blocking acetylcholine action on smooth muscle.
Tiotropium was patented in 1989 and approved for medical use in 2002. It is on the World Health Organization's List of Essential Medicines, the safest and most effective medicines needed in a health system. In the United States the wholesale cost was about US$13.75 per dose as of 2019. In the United Kingdom a dose costs the NHS about 0.86 pounds as of 2019. In 2016 it was the 95th most prescribed medication in the United States with more than 8 million prescriptions. There is no generic version available in the United States as of 2019.
Adverse effects are mainly related to its antimuscarinic effects. Common adverse drug reactions (≥1% of patients) associated with tiotropium therapy include: dry mouth and/or throat irritation. Rarely (<0.1% of patients) treatment is associated with: urinary retention, constipation, acute angle closure glaucoma, palpitations (notably supraventricular tachycardia and atrial fibrillation) and/or allergy (rash, angioedema, anaphylaxis).
Tiotropium and another member of its class ipratropium were linked to increased risk of heart attacks, stroke and cardiovascular death. The FDA requested further trials; these are now complete, and adequately resolve the previous safety concerns.
Mechanism of action
Tiotropium is a muscarinic receptor antagonist, often referred to as an antimuscarinic or anticholinergic agent. Although it does not display selectivity for specific muscarinic receptors, when topically applied it acts mainly on M3 muscarinic receptors located on smooth muscle cells and submucosal glands. This leads to a reduction in smooth muscle contraction and mucus secretion and thus produces a bronchodilatory effect.
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