Products
Umeclidinium bromide is commercially available as a powder for inhalation as a monopreparation (Incruse Ellipta) and as a fixed combination with vilanterol (Anoro Ellipta, LAMA–LABA combination). It was approved in many countries in 2014. In 2017, a combination of umeclidinium bromide, fluticasone furoate, and vilanterol was released in the EU (Trelegy Ellipta), and in many countries in 2018.
Structure and properties
Umeclidinium bromide (C29H34BrNO2, Mr = 508.5 g/mol) is a quinuclidine derivative structurally related to atropine. It exists as a white powder that is sparingly soluble in water.
Effects
Umeclidinium bromide (ATC R03BB07) has anticholinergic and bronchodilator properties. The effects are due to competitive antagonism at muscarinic receptors on airway smooth muscle. Umeclidinium bromide abolishes the effects of bronchoconstrictor acetylcholine.
Indications
For long-term bronchodilator treatment of chronic obstructive pulmonary disease (COPD).
Dosage
According to the SmPC. The drug is inhaled once daily. This is in contrast to previous agents in this group, such as ipratropium bromide.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Because of bronchodilatation, umeclidinium bromide may increase pulmonary absorption of other agents. Umeclidinium is a substrate of P-glycoprotein and CYP2D6. However, this does not appear to be clinically relevant.
Adverse effects
The most common potential adverse effects include upper respiratory tract infection and cough. Occasionally, atrial fibrillation and rapid heart rate have been reported (tachycardia).
