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Xanthines and Phosphodiesterase Inhibitors.

D Spina1, C P Page2

  • 1The Sackler Institute of Pulmonary Pharmacology, Institute of Pharmaceutical Science, King's College London, Franklin Wilkins Building, London, SE1 9NH, UK.

Handbook of Experimental Pharmacology
|November 16, 2016
PubMed
Summary
This summary is machine-generated.

Theophylline, a xanthine drug, offers anti-inflammatory benefits for asthma and COPD beyond bronchodilation. Despite a narrow therapeutic window, it remains crucial for patients unresponsive to other treatments.

Keywords:
Adenosine receptor antagonismBamifyllineDoxofyllineHDACPI3δ-kinasePhosphodiesterasesTheophylline

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Area of Science:

  • Pharmacology
  • Respiratory Medicine

Background:

  • Theophylline, an orally acting xanthine, has been a long-standing treatment for asthma and COPD since 1937.
  • Xanthines are now often third-line therapy due to a narrow therapeutic window and drug-drug interactions.
  • Lower doses of theophylline exhibit anti-inflammatory effects relevant to respiratory diseases.

Purpose of the Study:

  • To explore the anti-inflammatory mechanisms of theophylline in respiratory diseases.
  • To discuss the role of xanthines in current asthma and COPD management.
  • To compare theophylline with newer agents like roflumilast.

Main Methods:

  • Review of existing literature on theophylline's pharmacology and clinical use.
  • Discussion of proposed molecular mechanisms of action.
  • Comparison with other xanthines (doxofylline, bamifylline) and PDE4 inhibitors (roflumilast).

Main Results:

  • Theophylline's anti-inflammatory actions are relevant for asthma and COPD treatment.
  • Potential mechanisms include PDE inhibition, phosphoinositide 3-kinase inhibition, adenosine receptor antagonism, and HDAC activation.
  • Xanthines provide clinical benefit in glucocorticosteroid-refractory patients and are essential for disease management.

Conclusions:

  • Theophylline and related xanthines remain important in managing asthma and COPD, especially in refractory cases.
  • Understanding their mechanisms is key to optimizing their use.
  • Newer agents like roflumilast show promise but have dose-limiting side effects.