Muscarinic receptor antagonists for the treatment of chronic obstructive pulmonary disease

Abstract

Introduction: Long-acting muscarinic receptor antagonists (LAMAs) are central to the treatment of chronic obstructive pulmonary disease (COPD) because of the important role of the cholinergic system in the pathophysiology of this disorder.

Areas covered: LAMAs show clinically meaningful effects in lung function and other important supportive outcomes, such as exacerbations, health-related quality of life, dyspnea, rescue medication use and nighttime/early morning symptoms, and are safe. Muscarinic receptor antagonists could exert other useful actions such as the anti-inflammatory, anti-remodeling, mucus-modifying, and anti-cough effects. Concerns have been raised about possible associations of muscarinic receptor antagonists with cardiovascular morbidity and mortality. Muscarinic receptor antagonists can be combined with long-acting β₂-agonists (LABAs), inhaled corticosteroids (ICSs) and LABA + ICS. There are number of LAMAs that are being identified but only few have reached the clinical development. Fixed-dose combination formulations of both novel and established LAMAs with LABAs are being developed.

Expert opinion: There are important questions concerning the use of LAMAs in the treatment of patients suffering from stable COPD that need conclusive answers.

Keywords::

• aclidinium
• cardiovascular adverse events
• cost-effectiveness of long-acting muscarinic receptor antagonists
• dual bronchodilation
• emerging long-acting muscarinic receptor antagonists
• glycopyrronium
• muscarinic receptor antagonists
• muscarinic receptor subtypes
• tiotropium

Declaration of interest

M Cazzola has received honoraria for speaking and consulting and/or financial support for attending meetings from Abbott, Almirall, AstraZeneca, Boehringer Ingelheim, Chiesi Farmaceutici, Dey, GlaxoSmithKline, Guidotti, Lallemand, Malesci, Menarini Farmaceutici, Mundipharma, Novartis, Pfizer, Sanovel, Sigma Tau, Takeda and Valeas. MG Matera has received honoraria for speaking and consulting and/or financial support for attending meetings from Almirall, AstraZeneca, Boehringer Ingelheim, Chiesi Farmaceutici, GlaxoSmithKline, Novartis, Pfizer and Takeda. P Rogliani has received honoraria for speaking and/or financial support for attending meetings from Almirall, Boehringer Ingelheim, GlaxoSmithKline and Sigma Tau. No funding was received in support of this manuscript.

Notes

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