Anticholinergics are the bronchodilators of choice in the management of chronic obstructive pulmonary disease (COPD). They work by blocking muscarinic receptors in airway smooth muscle. Cholinergic tone appears to be the only reversible component of COPD. With the discovery of different muscarinic receptor subtypes, the development of more selective anticholinergics is possible. A major advance in this therapeutic area has been the discovery of tiotropium bromide, which has kinetic selectivity for M3 receptors as well as a duration of action of >24 hours. Once-daily administration of tiotropium is well tolerated and has shown significant advantages over ipratropium bromide, given 4 times daily, in the control of COPD.