Products
Glycopyrronium bromide is commercially available in the form of hard capsules with a powder for inhalation (Seebri Breezhaler). It was approved in the EU in 2012 and in many countries in April 2013. Glycopyrronium bromide is also combined fixed with indacaterol (Ultibro Breezhaler, approved in many countries in 2014). In 2020, a combination of indacaterol with glycopyrronium bromide and mometasone furoate was registered for asthma treatment (Enerzair Breezhaler). In 2018, a fixed-dose combination with formoterol and beclometasone was released in the EU (Riarify), and in many countries in 2020 (Trimbow). Also registered was a combination with formoterol (Bevespi Aerosphere).
Structure and properties
Glycopyrronium bromide (C19H28BrNO3, Mr = 398.3 g/mol) is an anticholinergic with a quaternary ammonium structure. It is structurally related to atropine and exists as a white, odorless, crystalline powder that is readily soluble in water.
Effects
Glycopyrronium bromide (ATC R03BB06) has parasympatholytic and bronchodilator properties. The effects are due to the abolition of the effects of acetylcholine on airway smooth muscle cells, which induces bronchoconstriction. Glycopyrronium bromide binds mainly to the M1 to M3 muscarinic receptors responsible for bronchoconstriction. It has a rapid onset of action and a long duration of action. Therefore, unlike other agents in this group – such as ipratropium bromide – it only needs to be administered once daily.
Indications
For bronchodilator maintenance therapy for symptom relief in chronic obstructive pulmonary disease (COPD) or bronchial asthma.
Dosage
According to the SmPC. The powder in the capsules is inhaled once daily at the same time of day.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Glycopyrronium bromide should not be combined with other parasympatholytics. Cimetidine, an inhibitor of organic cation transport, decreases elimination of glycopyrronium bromide and increases exposure.
Adverse effects
The most common potential adverse effects include nasopharyngitis, sleep disturbances, headache, dry mouth, gastroenteritis, and urinary tract infections.
