Products
Aclidinium bromide is commercially available as a powder inhalation (Bretaris Genuair, Eklira Genuair). It is administered with the Genuair inhaler and was approved in the EU and US in 2012. In many countries, it entered the market in 2013. In the EU, a fixed-dose combination with formoterol was released in 2014 (Brimica Genuair).
Structure and properties
Aclidinium bromide (C26H30BrNO4S2, Mr = 564.6 g/mol) is a quaternary ammonium ion and an ester derivative of 3-quinuclidinol. It exists as a white powder that is very slightly soluble in water. The positive charge allows for deep oral bioavailability and low crossing of the blood–brain barrier.
Effects
Aclidinium bromide (ATC R03BB05) has bronchodilator and parasympatholytic properties with a long duration of action. The effects are due to antagonism at muscarinic receptors in the airways. Aclidinium bromide binds longer to M3 receptors and shorter to M2 receptors. In plasma, it is rapidly hydrolyzed to an inactive alcohol metabolite and a carboxylic acid metabolite. This reduces the risk of side effects outside the lungs.
Indications
For symptomatic and bronchodilator continuous treatment of chronic obstructive pulmonary disease (COPD).
Dosage
According to the SmPC. The drug is usually inhaled twice daily.
Contraindications
Aclidinium bromide is contraindicated in hypersensitivity to aclidinium bromide and structurally related parasympatholytics. Refer to the drug label for complete precautions.
Interactions
Combination with other anticholinergics is not recommended. Aclidinium bromide does not interact with CYP450.
Adverse effects
Possible adverse effects include headache, nasopharyngitis, sinusitis, blurred vision, rapid pulse, cough, voice disturbance, diarrhea, dry mouth, and urinary retention.
