What is theophylline used for?

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Last updated: February 24, 2025View editorial policy

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From the Guidelines

Theophylline is used as a bronchodilator to treat respiratory conditions such as asthma and chronic obstructive pulmonary disease (COPD), primarily as a long-term control medication or adjunctive therapy with inhaled corticosteroids. The most recent and highest quality study, 1, published in 2015, suggests that oral slow-release theophylline can be used to prevent acute exacerbations of COPD. In asthma, theophylline is typically used as an alternative, not preferred, therapy for mild persistent asthma or as adjunctive therapy with inhaled corticosteroids, as stated in 1. Some key points to consider when using theophylline include:

  • Monitoring of serum theophylline concentration is essential, as noted in 1
  • Theophylline may have mild anti-inflammatory effects, as mentioned in 1
  • It is less commonly prescribed now due to the availability of newer, more targeted medications with fewer side effects, but remains a valuable option for patients who don't respond well to or can't use inhaled therapies
  • Theophylline works by relaxing smooth muscles in the airways and reducing inflammation, which explains its effectiveness in these respiratory conditions. Overall, theophylline is a valuable option for treating respiratory conditions, particularly for patients who don't respond well to or can't use inhaled therapies, as supported by the most recent study 1.

From the FDA Drug Label

Theophylline is indicated for the treatment of the symptoms and reversible airflow obstruction associated with chronic asthma and other chronic lung diseases, e.g., emphysema and chronic bronchitis.

Theophylline is used for the treatment of symptoms and reversible airflow obstruction associated with:

  • Chronic asthma
  • Other chronic lung diseases, such as:
    • Emphysema
    • Chronic bronchitis 2

From the Research

Theophylline Uses

  • Theophylline is an oral methylxanthine bronchodilator used for the treatment of asthma and chronic obstructive pulmonary disease (COPD) 3, 4, 5, 6, 7
  • It is recommended as alternate therapy for the treatment of asthma and COPD 3
  • Theophylline has anti-inflammatory and immunomodulatory effects, especially at low doses 4, 5, 6
  • It is not generally recommended for the treatment of other respiratory disorders such as obstructive sleep apnea (OSA) or hypoxia 3

Clinical Guidelines and Recommendations

  • Current clinical practice guidelines rely on evidence published prior to the year 2000 to make recommendations for theophylline use 3
  • Theophylline is considered a third-line therapy due to its narrow therapeutic window and propensity for drug-drug interactions 5
  • Japanese asthma guidelines recommend theophylline as an additional regimen to inhaled beta-agonists and inhaled corticosteroids for patients whose asthma is not controlled completely 4

Potential Applications and Future Research

  • Theophylline may have a role in the treatment of patients who are refractory to glucocorticosteroid therapy 5
  • Low-dose theophylline may have immunomodulatory and anti-inflammatory effects, making it a potential treatment option for certain patients 4, 5, 6
  • Future research is needed to fully understand the molecular mechanism(s) of action of theophylline and its potential applications in human medicine 5, 6

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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