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Role of muscarinic antagonist therapy in COPD

Pharmacologically active anticholinergic alkaloids exist in the roots, seeds, and leaves of a variety of belladonna plants. The most important of these naturally occurring alkaloids are atropine and scopolamine...

With the introduction of ephedrine and epinephrine during the 20th century, the use of atropine and related substances for relief of bronchospasm declined. Anticholinergic therapy has again come to the forefront of bronchodilator therapy with the introduction of the synthetic quaternary derivatives of atropine, including ipratropium bromide and tiotropium bromide.

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Articles of Interest

Antimuscarinic Medications for Chronic Obstructive Pulmonary Disease

Antimuscarinic drugs for COPD management include short-acting and long-acting muscarinic receptor antagonists (SAMAs and LAMAs, respectively). These medications are considered the bronchodilators of choice in the management of COPD because they exhibit minimal cardiac stimulatory effects and have greater effectiveness compared with beta-agonists.

Bronchodilators in COPD: Impact of β-agonists and anticholinergics on severe exacerbations and mortality

The main therapeutic options for the management of COPD are inhaled corticosteroids and bronchodilators. Inhaled corticosteroids significantly reduce inflammatory cells in the lungs, as well as systemic inflammatory markers such as C-reactive protein, compared with placebo. However, there is some evidence that corticosteroids have no antiinflammatory effects in COPD patients who are still smoking.

Long-acting muscarinic receptor antagonists for the treatment of chronic airway diseases

In the clinic, LAMAs showed a significant improvement of forced expiratory volume in 1 second (FEV1), quality of life, dyspnea and reduced the number of exacerbations in COPD and more recently in asthma. This review will focus on the three LAMAs approved in Europe in the treatment of chronic airway diseases.

Muscarinic receptor antagonists, from folklore to pharmacology; finding drugs that actually work in asthma and COPD

Rationally, blocking M3 receptors on airway smooth muscle should inhibit bronchoconstriction. However, while anticholinergic drugs are useful in the laboratory setting, their ability to block bronchoconstriction clinically in humans with asthma and COPD has been mired with problems surrounding efficacious dosing, side effects and muscarinic receptor selectivity.

Safety of long acting muscarinic antagonists: are all these drugs always and equally safe?

Even if inhaled LAMAs are generally considered to be safe, muscarinic receptors are expressed not only in the lungs, but also at the level of heart, digestive and urinary apparatus. Because LAMAs are not fully selective for lung receptors, their use may be associated with adverse events related to stimulation of receptors in these organs. By far, tiotropium has been the most used LAMA. The most common adverse events of subjects receiving tiotropium compared to placebo were dry mouth, constipation and urinary retention, usually mild and seldom causing the stopping of treatment.

The role of long-acting muscarinic antagonist/long-acting β agonist fixed-dose combination treatment for chronic obstructive pulmonary disease...

Based on the characteristics of Chinese COPD patients, we can conclude that LAMA/LABA FDCs are a suitable choice to reduce symptoms and improve the QoL and economic outcomes of patients.