Products
Tiotropium bromide is commercially available in the form of capsules for inhalation and has been approved since 2002 (Spiriva). The capsules are inhaled using the Spiriva HandiHaler. The inhalation solution (Spiriva Respimat) was approved in many countries in 2016. Tiotropium bromide is the successor to ipratropium bromide (Atrovent, both Boehringer Ingelheim). In 2016, a fixed-dose combination with olodaterol was approved for the treatment of COPD (Spiolto Respimat).
Structure and properties
Tiotropium bromide (C19H22BrNO4S2, Mr = 472.4 g/mol) is present in drugs as tiotropium bromide monohydrate, a white to yellowish-white powder that is sparingly soluble in water. Tiotropium bromide is non-chiral and structurally related to atropine and ipratropium bromide. The positive charge of the quaternary ammonium compound contributes to the fact that the drug is predominantly locally active in the respiratory tract and is absorbed into the systemic circulation only to a minor extent.
Effects
Tiotropium bromide (ATC R03BB04) has bronchodilator and parasympatholytic properties. It counteracts COPD symptoms, decreases exacerbation rates, and increases quality of life. The effects are due to competitive antagonism at muscarinic receptors in the airways. Unlike ipratropium bromide, tiotropium bromide has a long duration of action of more than 24 hours and is therefore also known as LAMA, Long Acting Muscarinic Antagonist. The long duration of action is an advantage for treatment adherence.
Indications
For symptomatic long-term treatment of chronic obstructive pulmonary disease (COPD).
Dosage
According to the SmPC. Inhaled once daily with the medication.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Combination with other anticholinergics is not recommended because adverse effects may be increased. Tiotropium bromide is excreted via cation transporters. Interactions with substrates of the transporters are possible.
Adverse effects
The most common potential adverse effect is dry mouth.
