Tiotropium bromide

Anti-cholinergics Tiotropium bromide remains bound to M3-receptors for up to 36 h, and requires only daily intake, whereas other anti-cholinergics (e.g. ipratropium, oxytropium) have to be given up to four-times daily and are often used as maintenance treatment. Possible side-effects are dry mouth, metallic taste after inhalation and very rarely close-angle glaucoma. 

Ipratropium bromide and tiotropium bromide are competitive inhibitors of muscarinic receptors they produce bronchodilation only in cholinergic-mediated bronchoconstriction. Anticholinergics are effective bronchodila-tors but are not as potent as /J2-agonists. They attenuate, but do not block, allergen- or exercise-induced asthma in a dose-dependent fashion. 

The time to reach maximum bronchodilation from aerosolized ipratropium is longer than from aerosolized short-acting / -agonists (30 to 60 minutes vs. 5 to 10 minutes). This is of little clinical consequence because some bronchodilation is seen within 30 seconds and 50% of maximum response occurs within 3 minutes. Ipratropium bromide has a duration of action of 4 to 8 hours tiotropium bromide has a duration of 24 hours. 

Inhaled ipratropium bromide is only indicated as adjunctive therapy in severe acute asthma not completely responsive to / -agonists alone because it does not improve outcomes in chronic asthma. Tiotropium bromide has not been studied in asthma. 

Koumis T, Samuel S. (2005) Tiotropium bromide A new long-acting bron-chodilator for the treatment of chronic obstructive pulmonary disease. Clin... 

Prakash O, Kumar R, Rahman M, Gaur SN. (2006) The clinico-physiological effect of inhaled tiotropium bromide and inhaled ipratropium bromide in severe chronic obstructive pulmonary disease. Ind J Allergy Asthma Immunol 20 105-111 For further information http //www.rxlist.com/spiriva-drug.htm (accessed on 24.12.2010). 

Atropine (1) Tiotropium bromide (26) Tropane alkaloid Chronic obstructive pulmonary disease... 

R=Me Artemether Sodium artesunate (25) Ipratropium bromide (26) Tiotropium bromide... 

Hansel TT, Barnes PJ, Tiotropium bromide A novel once-daily anticholinergic bronchodilator for the treatment of COPD, Drugs Today (Bare) 38 585-600, 2002. 

Saberi F, O Donnell DE. The role of tiotropium bromide, a long-acting anticholinergic bronchodilator, in the management of COPD. Treat Respir Med. 2005 4 275-281. 

Keam SJ, Keating GM. Tiotropium bromide. A review of its use as maintenance therapy in patients with COPD. Treat Respir Med. 2004 3 247-268. 

The crystalline structure of tiotropium bromide monohydrate is provided (2). 

Tiotropium bromide is a long-acting anticholinergic bronchodUator that binds with similar affinity to the three muscarinic receptor subtypes (SEDA-20, 190) (1). However, it dissociates more slowly from Mi and M3 receptors in bronchial smooth muscle than from M2 receptors (1). This results in a long half-hfe of the bound complex, allowing once-daUy administration. 

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