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Related Concept Videos

Antiasthma Drugs: Methylxanthines01:24

Antiasthma Drugs: Methylxanthines

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Updated: May 11, 2026

Disposable Dosators for Pulmonary Insufflation of Therapeutic Agents to Small Animals
04:22

Disposable Dosators for Pulmonary Insufflation of Therapeutic Agents to Small Animals

Published on: March 30, 2017

Theophylline.

Peter J Barnes1

  • 11 National Heart and Lung Institute, Imperial College, London, United Kingdom.

American Journal of Respiratory and Critical Care Medicine
|May 16, 2013
PubMed
Summary
This summary is machine-generated.

Theophylline, a long-used airway disease treatment, offers anti-inflammatory benefits in asthma and COPD at lower doses. It works by inhibiting phosphodiesterase and activating histone deacetylase-2, potentially reversing corticosteroid resistance.

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Bronchial Thermoplasty: A Novel Therapeutic Approach to Severe Asthma
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Published on: November 4, 2010

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Disposable Dosators for Pulmonary Insufflation of Therapeutic Agents to Small Animals
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Bronchial Thermoplasty: A Novel Therapeutic Approach to Severe Asthma
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Area of Science:

  • Pharmacology
  • Respiratory Medicine
  • Inflammation Biology

Background:

  • Theophylline (dimethylxanthine) has an 80-year history in treating airway diseases, initially as a bronchodilator.
  • High doses led to side effects, reducing its use with the rise of inhaled β2-agonists.
  • Recent research highlights its anti-inflammatory effects in asthma and COPD at lower concentrations.

Purpose of the Study:

  • To explore the molecular mechanisms behind theophylline's bronchodilator and anti-inflammatory effects.
  • To investigate theophylline's role in reversing corticosteroid resistance in severe asthma and COPD.
  • To review theophylline's current therapeutic applications and side effect profiles.

Main Methods:

  • Review of existing literature on theophylline's pharmacological actions.
  • Analysis of molecular pathways including phosphodiesterase (PDE) inhibition and histone deacetylase-2 (HDAC2) activation.
  • Examination of clinical data regarding theophylline's efficacy and safety in asthma and COPD management.

Main Results:

  • Bronchodilatation is mediated by PDE3 inhibition.
  • Anti-inflammatory effects involve PDE4 inhibition and HDAC2 activation, downregulating inflammatory genes.
  • Theophylline reverses corticosteroid resistance, particularly valuable in severe asthma and COPD with reduced HDAC2 activity.

Conclusions:

  • Theophylline's dual action on PDE and HDAC2 offers significant therapeutic potential.
  • It serves as an effective add-on therapy for inadequately controlled asthma and severe COPD.
  • Future applications may focus on low-dose theophylline for corticosteroid resistance in severe airway diseases.