Long-acting muscarinic antagonists

Abstract

Chronic obstructive pulmonary disease (COPD) is a major cause of death and disability worldwide. Inhaled bronchodilators are the mainstay of COPD pharmacological treatment. Long-acting muscarinic antagonists (LAMAs) are a major class of inhaled bronchodilators. Some LAMA/device systems with different characteristics and dosing schedules are currently approved for maintenance therapy of COPD and a range of other products are being developed. They improve lung function and patient-reported outcomes and reduce acute bronchial exacerbations with good safety. LAMAs are used either alone or associated with long-acting β₂-agonists, eventually in fixed dose combinations. Long-acting β₂-agonist/LAMA combinations assure additional benefits over the individual components alone. The reader will obtain a view of the safety and efficacy of the different LAMA/device systems in COPD patients.

Keywords:

• aclidinium
• bronchodilator
• chronic obstructive pulmonary disease
• dual bronchodilation
• fixed dose combination
• glycopyrronium
• long-acting muscarinic antagonists
• tiotropium
• umeclidinium

Financial and competing interests disclosure

A Melani has served as an advisory board member, has been reimbursed for speaker honoraria and has recieved fees as a consultant for AstraZeneca/Almirall, Chiesi, Guidotti/Malesci, Novartis, Mundipharma, GSK, Sole24 Ore and Artsana. The author has no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Key issues

• Inhaled bronchodilators are the cornerstone of pharmacological treatment of chronic obstructive pulmonary disease (COPD).

• Most treated COPD patients remain symptomatic despite the use of short-acting inhaled bronchodilators and in these situations, guidelines recommend long-term bronchodilator treatment as regular maintenance.

• Inhaled long-acting muscarinic antagonists (LAMAs) and inhaled long-acting β₂-agonists (LABAs) are the currently available long-term bronchodilator drugs for use in stable COPD patients.

• Inhaled LAMAs are indicated for long-term maintenance bronchodilator treatment of stable COPD patients and in real life are often considered as the first-choice long-term bronchodilators.

• A range of LAMA/device systems with different characteristics and dosing schedules are available for maintenance therapy of stable COPD patients.

• Inhaled LAMAs are safe and improve the lung function and patient-reported outcomes and reduce acute bronchial exacerbations of COPD patients.

• When symptoms are not fully controlled despite the regular maintenance use of an inhaled long-term bronchodilator, LAMA and LABA with different mechanisms of action and increasing evidence of favorable crosso-talkings, eventually in a single inhaler, are indicated.

• There is evidence that the combination of LABA and LAMA provides additional benefits over the individual components used alone without significantly increasing the risk of adverse effects.