Synopsis

Source of validity: Scientific
Rating (out of 5): 3

Theophylline has a well-established history in the treatment of asthma, supported by scientific evidence. It is a methylxanthine drug that acts as a bronchodilator, primarily by inhibiting phosphodiesterase, leading to increased cyclic AMP levels in airway smooth muscle and resulting in relaxation of the airways. Additionally, it has mild anti-inflammatory effects and improves diaphragmatic contractility. Theophylline was once a first-line therapy for asthma, but its use has declined due to the development of more effective and safer inhaled corticosteroids and beta-agonists. Numerous clinical trials from the mid-20th century through the early 2000s have demonstrated that theophylline can provide symptomatic improvement and reduce bronchospasm in asthmatic patients. However, the therapeutic window is narrow, and side effects—including nausea, cardiac arrhythmias, and seizures—are common at higher blood concentrations. Because of these risks and the need for regular blood monitoring, theophylline is now considered a second- or third-line agent, typically reserved for patients who do not respond to or cannot tolerate standard therapies. Major clinical guidelines (such as GINA and NHLBI/NAEPP) still acknowledge a role for theophylline, particularly as add-on therapy when inhaled medications are insufficient. Thus, while the scientific evidence supports its efficacy, its risk-benefit profile limits its use in modern practice.

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