Background: Doxofylline, a methylxanthine derivative, has recently drawn attention because of its better safety profile and similar efficacy over the most widely prescribed analogue, theophylline, indicated for asthma and chronic obstructive pulmonary disease.
Objective: This article attempts to discuss the pharmacodynamics/pharmacokinetics and clinical efficacy of doxofylline.
Method: An extensive search in three electronic databases (Unbound Medline, Pubmed and Sciencedirect) and internet search engines (Scirus and Google Scholar) were used to identify the clinical studies on doxofylline. The literature search was carried out without time constraints to ensure maximum coverage of existing literature on doxofylline.
Results/conclusion: In a relatively large number of comparative studies, doxofylline is indicated to have less affinity for alpha(1) and alpha(2) receptors than theophylline. Unlike theophylline, doxofylline does not antagonize calcium channels, nor does it interfere with the influx of calcium into the cells, which probably reduces the cardiac side effects. Moreover, it does not affect sleep rhythm, gastric secretions, heart rate and rhythm and CNS functioning. Numerous reports available regarding the better tolerability of doxofylline than theophylline prove it as a potential bronchodilator with promising pharmacological behavior. However, despite its superior safety and clinical efficacy, the potential of doxofylline has not been fully exploited.