Arformoterol tartrate in the treatment of bronchoconstriction in patients with chronic obstructive pulmonary disease.
Arformoterol tartrate inhalational solution is a nebulized bronchodilator that has been approved for long-term, twice-daily maintenance therapy for bronchoconstriction in patients with chronic obstructive pulmonary disease (COPD). It is a single-isomer ([R,R]-formoterol), selective, long-acting, full beta(2)-agonist with affinity for both subtypes of beta-adrenergic receptor, and 2-fold higher affinity for the beta(2) receptor versus racemic formoterol. It is 1,000-fold more potent in receptor-binding affinity compared to (S,S)-enantiomer of formoterol. More than 2,000 COPD patients have participated in 16 completed clinical trials, including phase III pivotal and open-label trials to evaluate the efficacy and safety of arformoterol at doses ranged from 15 to 50 microg. These studies demonstrated that treatment with arformoterol significantly improved various lung function parameters, overall clinical status and ability to function, as well as significantly reduced COPD exacerbations and use of rescue medication. In terms of safety, arformoterol was found to be well tolerated in doses up to 50 microg/day with no reports of significant clinical, laboratory or cardiovascular adverse events, such as changes in QTc interval or cardiac arrhythmias. Recent asthma literature has alluded to caution with the use of long-acting beta-agonists (LABAs) (except probably in combination with inhaled corticosteroids) citing possible increase in the risk of asthma-related mortality. However, there is no comparable data available with regards to the use of LABAs in COPD patients.
Madaan
Arvind
A
Danville ENT Associates, Danville, Virginia, USA. arvind.madaan@gmail.com
D000280:Administration, Inhalation; D016084:Bronchoconstriction / Q000187:drug effects*; D001993:Bronchodilator Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D002986:Clinical Trials as Topic; D004305:Dose-Response Relationship, Drug; D004983:Ethanolamines / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D000068759:Formoterol Fumarate; D006801:Humans; D029424:Pulmonary Disease, Chronic Obstructive / Q000188:drug therapy / Q000503:physiopathology
D001993:Bronchodilator Agents; D004983:Ethanolamines; D000068759:Formoterol Fumarate