Anticholinergics Information

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Anticholinergics in asthma e-learning module

Introduction to asthma

  • Asthma is a heterogeneous disease, characterised by chronic airway inflammation and a history of respiratory symptoms, including:1

  • wheeze

  • breathlessness

  • chest tightness

  • cough, varying over time and in intensity

  • expiratory airflow variation greater than that seen in healthy people

  • Bronchial hyper-responsiveness, inflammation, and airway remodelling are key features of asthma, leading to a decline in lung function and increased severity of disease2

Introduction to asthma therapy

  • The current standard of care is initial treatment with low-dose ICS, with SABA as needed, followed by increasing ICS dose or ICS+LABA therapy1

  • Referral to the secondary care setting for investigation and consideration for add-on therapy is recommended in patients with more severe or difficult-to-control asthma1

  • A high proportion of patients with asthma do not achieve control despite receiving standard-of-care asthma therapy, thus highlighting the need for different strategies to address this issue1

  • The importance of acetylcholine in the pathophysiology of asthma and also as a potential treatment target is now widely recognised1

Role of acetylcholine in asthma

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Acetylcholine plays a significant role
in the pathophysiology of asthma1-4

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the effect on the airways

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Anticholinergics in asthma: background

  • Bronchoconstriction is the primary cause of airway obstruction in patients with asthma, predominately owing to the downstream effects of acetylcholine1

  • Anticholinergics target the muscarinic receptors within the airway, reducing the downstream effects of acetylcholine2,3

Short-acting anticholinergics Long-acting anticholinergics
Ipratropium bromide Tiotropium bromide
Oxitropium bromide Aclidinium bromide
  Glycopyrronium bromide
  Umeclidinium bromide

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Tiotropium Respimat®
mechanism of action1-3

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the effect on the airways

Anticholinergics in asthma:
tiotropium Respimat®

  • Add-on therapy to ICS+LABA with tiotropium Respimat® may have additional benefits (e.g. greater bronchodilation) compared with ICS+LABA alone in patients with asthma1,2

  • Anticholinergics block acetylcholine-induced smooth muscle contraction whereas LABAs stimulate adrenergic smooth muscle relaxation1

  • Preclinical studies in animal models, have shown that tiotropium partly prevents airway remodelling and eosinophilic inflammation3

  • Tiotropium Respimat® shows a slower dissociation from the M3 receptor compared with the other anticholinergics

  • The longer duration of action allows for a once-daily dosing pattern3

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Anticholinergics in asthma:
clinical data

  • The first clinical trial of tiotropium Respimat® was in 12 adult male patients with mild allergic asthma

  • Tiotropium Respimat® was associated with prolonged bronchodilator response and protection from methacholine challenge1

  • The early proof-of-concept studies further supported these findings, including in patients with severe asthma2,3

  • The tiotropium Respimat® clinical trial programme in asthma, with Phase II and III trials assessing patients with mild-to-severe and poorly controlled asthma, has been completed4

  • This clinical trial programme included 18 trials with over 6000 patients5

  • This also includes several recently completed clinical trials of tiotropium Respimat® in children and adolescents6–8

A closer look at the studies for
tiotropium Respimat® in asthma

PrimoTinA-asthma®1 MezzoTinA-asthma®2 GraziaTinA-asthma®3
Population Adults, uncontrolled asthma,
despite high-dose ICS
(≥800 µg budesonide
or equivalent) + LABA
Adults, moderated uncontrolled asthma, despite medium-dose
ICS (400-800 µg budesonide or
Adults, uncontrolled asthma,
despite low-to-medium dose
ICS (200-400 µg budesonide or
Trial 1: N = 459
Trial 2: N = 453
Trial 1: N = 1070
Trial 2: N = 1032
N = 465
Comparators 5 µg tiotropium Respimat® qd vs. placebo 5 or 2.5 µg tiotropium Respimat® qd or salmeterol 50 µg bid vs. placebo 5 or 2.5 µg tiotropium Respimat®
 qd vs. placebo
Lung function
Lung function
Asthma control
Lung function
  • Significant lung function improvement

  • Exacerbation reduction

  • Asthma control improvement

  • Comparable safety profile
    with placebo

  • Significant lung function improvement

  • Asthma control improvement (ACQ-7 responder rate)

  • Comparable safety profile with placebo

  • Significant lung function improvement

  • Comparable safety profile with placebo

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  • Acetylcholine binds to muscarinic receptors to trigger airway
    inflammation and hyper-responsiveness seen in patients with asthma

  • Anticholinergics target the M3 muscarinic receptors within the airway to
    reduce the downstream effects of acetylcholine

  • Long-acting anticholinergics have demonstrated benefits in asthma

  • Clinical data suggest that add-on anticholinergics are an option for the treatment and management of patients with asthma

  • Tiotropium Respimat® is the only long-acting anticholinergic approved for the treatment of asthma as an add-on treatment and has demonstrated:

  • Improvements in lung function

  • Reductions in the risk of severe exacerbations and asthma worsening

  • Improvements in asthma control

  • These effects were demonstrated independently of the patient´s baseline characteristics (phenotype)

  • Tiotropium Respimat® is the only long-acting anticholinergic recommended in Steps 4 and 5 of the international GINA strategy

Explore patient profiles for
anticholinergic treatment




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