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The Pharmacological Properties of Tiotropium^*

^* From the Department of Thoracic Medicine, National Heart and Lung Institute, London, UK.

Correspondence to: Peter J. Barnes MA, DM, DSc, Department of Thoracic Medicine, National Heart and Lung Institute, Dovehouse St, London SW3 6LY, UK; email: p.j.barnes{at}ic.ac.uk

Tiotropium is a long-acting anticholinergic drug. Studies with cloned human muscarinic receptors show that tiotropium binds equally well to M₁, M₂, and M₃ receptors. However, it dissociates very slowly from M₁ and M₃ receptors compared with ipratropium, and more rapidly from M₂ receptors. Binding studies with [³H]tiotropium in human lung show that it is approximately 10-fold more potent than ipratropium. In vitro, tiotropium has a potent inhibitory effect against cholinergic nerve-induced contraction of airways. It dissociates extremely slowly, compared with the dissociation of atropine and ipratropium. Clinical studies with single doses of inhaled tiotropium confirm that it is a potent and long-lasting bronchodilator. Furthermore, it protects against cholinergic bronchoconstriction for > 24 h. Pharmacokinetic studies show that little of the inhaled drug is absorbed, thus predicting a high margin of safety.

Key Words: acetylcholine • anticholinergic • cholinergic nerve • ipratropium bromide • M₁ receptor • M₂ receptor • M₃ receptor • muscarinic receptor • tiotropium bromide

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