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The Pharmacological Properties of Tiotropium*

Peter J. Barnes, MA, DM, DSc
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*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@ic.ac.uk



Chest. 2000;117(2_suppl):63S-66S. doi:10.1378/chest.117.2_suppl.63S
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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.

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