It is a competitive selective antagonist of muscarinic receptors (anticholinergics) with a longer residence time at M3 receptors than at M2 receptors. M3 receptors mediate the contraction of the smooth muscle of the airways , so that their antagonism produces bronchodilation.
Indications
Maintenance bronchodilator therapy to relieve symptoms in adult patients with chronic obstructive pulmonary disease (COPD).
Pharmacokinetics
It is rapidly absorbed from the lung and reaches peak plasma concentrations 15 minutes after administration to COPD patients. The fraction of the inhaled dose that reaches the systemic circulation as unchanged aclidinium is less than 5%. Aclidinium bromide hydrolyzes (chemical and plasma esterase-mediated hydrolysis) rapidly to inactive metabolites. The low absolute bioavailability of inhaled aclidinium bromide (<5%) is due to the fact that aclidinium bromide undergoes extensive systemic and presystemic hydrolysis when deposited in the lung or swallowed. The terminal elimination half-life of aclidinium bromide is between 2 and 3 hours.
Posology
The recommended dose is an inhalation of 375 mcg of aclidinium bromide (equivalent to 322 mcg of aclidinium) twice a day. The 400mcg dose of aclidinium bromide used in the studies is equivalent to the marketed dose of 322mcg of aclidinium. Administration is done by using the inhaler device
Contraindications
Hypersensitivity to aclidinium bromide, atropine or their derivatives, including ipratropium , oxitropium or tiotropium or any of the excipients (contains lactose ).
Precautions
It should not be used in asthma , since it has not been evaluated in this indication. Like other inhaled treatments, it can cause paradoxical bronchospasm. Aclidinium bromide is a maintenance bronchodilator and should not be used for the relief of acute episodes of bronchospasm, as salvage treatment. Due to its anticholinergic effects, it should be used with caution in patients with a history of myocardial infarction (in the previous 6 months), unstable angina , newly diagnosed arrhythmia (in the previous 3 months) or hospitalization due to heart failure of functional classes III. and IV of the NYHA (in the previous 12 months). It should be used with caution in patients with symptomatic prostatic hyperplasia, bladder neck obstruction, ornarrow-angle glaucoma .
Use in special groups
In elderly patients, no dose adjustment is necessary. There is no specific recommendation for use in children and adolescents (under 18 years of age). No dose adjustment is necessary in patients with renal or hepatic impairment . There are no data on its use in pregnancy or lactation . It should only be used in pregnant women if the benefits outweigh the possible risks. It is considered unlikely that, at therapeutic doses, it has an effect on fertility.
Interactions
Its use with other anticholinergic drugs is not recommended, as no corresponding studies have been performed. Based on in vitro tests, no interactions are expected between aclidinium bromide and glycoprotein (P-gp) substrate drugs or drugs metabolized by cytochrome P450 (CYP450) or esterases.