Tiotropium bromide

Tiotropium bromide is a muscarinic receptor antagonist (parasympatholytic), a substance with a quaternary nitrogen group, the molecular formula: C19H22NO4S2Br and a molar mass of 472.422 g/mol. Tiotropium bromide is structurally derived from N-butylscopolamine. As a quaternary ammonium salt, its action (in contrast to muscarinic receptor antagonists with a tertiary nitrogen group such as atropine and its derivatives) is limited to the periphery. The two thiophene rings increase lipophilicity.

The pharmacon belongs to the group of long-acting muscarinic receptor antagonists (anticholinergics), which bind to the muscarinic receptors M1 - M5. In the bronchial musculature, the active substance reversibly and competitively occupies the receptor subtype M3 and thus blocks the bronchoconstrictive effects of acetylcholine. The bronchodilating reaction is observed about 30 minutes after inhalation. Tiotropium dissociates from the M3 receptor much more slowly than ipratropium and atropine. This is the reason for its long duration of action, which allows for a once-a-day application. In COPD, tiotropium reduces the need for additional cortisone administration.

Tiotropium bromide is used as an anticholinergic and bronchodilator in patients with chronic obstructive pulmonary disease(COPD).

Most frequent side effect (16 % of patients): Dry mouth.

Hypersensitivity to lactose monohydrate (excipient), atropine or its derivatives (e.g. ipratropium bromide, oxitropium bromide).

Spiriva©^; the preparation is approved for permanent bronchodilation in patients with chronic obstructive pulmonary disease (COPD).

After inhalation, the ammonium salt acts primarily locally in the bronchi. The absorption of the swallowed portion from the gastrointestinal tract is low (10 to 15 percent). The active substance is hardly metabolized. After inhalation administration, 14 % of the dose is excreted with the urine.