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Concept: Muscarinic antagonists


Abstract “Death rattle” is a term used to describe the noisy sound produced by dying patients caused by the oscillatory movements of secretions in the upper airways. Antimuscarinic drugs, including atropine, scopolamine (hyoscine hydrobromide), hyoscine butylbromide, and glycopyrronium, have been used to diminish the noisy sound by reducing airway secretions. We report on the effectiveness of sublingual atropine eyedrops in alleviating death rattle in a terminal cancer patient. We present a 58-year-old man with pancreatic cancer who was admitted to our hospital because of severe dyspnea, cough, and death rattle with excessive bronchial secretion as a result of multiple lung metastases. We administered 1% atropine eyedrops sublingually to obviate the need for subcutaneous infusions and to prevent somnolence. On the basis of our experience, we conclude that atropine eyedrops, administered sublingually for distressing upper respiratory secretions, may be an effective alternative to the injection of antimuscarinic drugs, or as an option when other antimuscarinic formulations are not available.

Concepts: Cancer, Death, Muscarinic antagonists, Respiratory system, Anticholinergic, Hyoscyamine, Scopolamine, Muscarinic antagonist


Inhaled corticosteroid/long-acting β2-agonist combinations and/or long-acting muscarinic antagonists are recommended first-line therapies for preventing chronic obstructive pulmonary disease (COPD) exacerbation. Comparative effectiveness of budesonide/formoterol combination (BFC, an inhaled corticosteroid/long-acting β2-agonist combination) vs tiotropium (long-acting muscarinic antagonist) in the US has not yet been studied.

Concepts: Medicine, Asthma, Pneumonia, Muscarinic antagonists, Chronic obstructive pulmonary disease, Tiotropium, Muscarinic acetylcholine receptor


QVA149 is a once-daily (o.d.) inhaled dual bronchodilator containing a fixed-dose combination of the long-acting β2-agonist indacaterol and the long-acting muscarinic antagonist glycopyrronium for the treatment of COPD. The QUANTIFY study compared QVA149 with a free-dose bronchodilator combination of tiotropium plus formoterol (TIO+FOR) in improving health-related quality of life (HRQoL) of patients with COPD.

Concepts: Asthma, Life, Muscarinic antagonists, Quality, Quality of life, Chronic obstructive pulmonary disease, Tiotropium, Muscarinic acetylcholine receptor


Randomized, controlled trials comparing long-acting muscarinic antagonist (LAMA) efficacy in COPD are limited. This network meta-analysis (NMA) assessed the relative efficacy of tiotropium 18 µg once-daily (OD) and newer agents (aclidinium 400 µg twice-daily, glycopyrronium 50 µg OD, and umeclidinium 62.5 µg OD).

Concepts: Epidemiology, Medical statistics, Randomized controlled trial, Muscarinic antagonists, Meta-analysis, Muscarinic acetylcholine receptor


Two once-daily long-acting muscarinic antagonists (LAMAs) are currently available for the treatment of chronic obstructive pulmonary disease (COPD) - tiotropium and glycopyrronium. Previous studies have compared glycopyrronium with open-label tiotropium. In the GLOW5 study, we compare glycopyrronium with blinded tiotropium.

Concepts: Asthma, Pneumonia, Muscarinic antagonists, Chronic obstructive pulmonary disease, Tiotropium, Muscarinic acetylcholine receptor


COPD guidelines recommend the combined use of inhaled long-acting beta2-agonists and long-acting muscarinic antagonists if symptoms are not improved by a single agent. This systematic review assessed the efficacy and safety of the fixed-dose combination QVA149 compared with its monocomponents (glycopyrronium and indacaterol) and tiotropium for the treatment of moderate-severe COPD.

Concepts: Muscarinic antagonists, Muscarinic acetylcholine receptor


Oral oxybutynin has been associated with the development of cognitive impairment.

Concepts: Psychology, Cognitive psychology, Muscarinic antagonists, Differential geometry


Long-acting muscarinic antagonists (LAMAs) have been recommended for the treatment of chronic obstructive pulmonary disease and (more recently) asthma. However, the in vitro pharmacological profiles of the four LAMAs currently marketed (tiotropium, umeclidinium, aclidinium and glycopyrronium) have not yet been compared (relative to ipratropium) by using the same experimental approach.

Concepts: Medicine, Asthma, Lung, Pneumonia, Muscarinic antagonists, Chronic obstructive pulmonary disease, Bronchus, Ipratropium


Acute exposure to organic dust (OD) in pig barns induces intense airway inflammation with neutrophilia and hyperresponsiveness. This reaction is likely associated with increased cholinergic activity. Therefore, the involvement of cholinergic mechanisms in the reaction to acute exposure of OD was investigated in mice using the long-acting muscarinic antagonist tiotropium.

Concepts: Inflammation, Muscarinic antagonists, Tiotropium, Anticholinergic, Muscarinic acetylcholine receptor, Exposure


Despite a range of efficacious therapies for asthma, including inhaled corticosteroids (ICS) and long-acting β₂-agonists (LABA), a significant proportion of patients have poor asthma control and retain a risk of future worsening of their symptoms. Long-acting muscarinic antagonist (LAMA) bronchodilators offer a well-tolerated, efficacious, and cost-effective add-on to a patient’s treatment. Of the LAMAs currently under investigation or available for the treatment of asthma, evidence from a comprehensive clinical trial program in adults and children shows that once-daily treatment with tiotropium provides benefits for patients with uncontrolled asthma despite the use of ICS and LABAs. Tiotropium is included in the Global Initiative for Asthma (GINA) strategy document as an add-on therapy option for patients at Step 4 or 5 with a history of asthma exacerbations. Tiotropium Respimat® has demonstrated safety and efficacy in patients with a range of disease severities, ages, and phenotypes. This review describes the evidence for the use of LAMA as add-on therapy for patients with asthma who remain uncontrolled despite the use of ICS and LABA treatments.

Concepts: Medicine, Clinical trial, Asthma, Randomized controlled trial, Effectiveness, Muscarinic antagonists, Chronic obstructive pulmonary disease, Muscarinic acetylcholine receptor