The efficacy of theophylline as a bronchodilator is well documented. The drug can relieve and prevent bronchospasms in different manifestations of bronchial asthma. However, beta-sympathomimetic agents such as salbutamol are more effective for the treatment of acute asthma attacks. In therapy resistant cases where theophylline was not administered beforehand, theophylline (or aminophylline) can be given intravenously possibly in combination with corticosteroids.

Continuous prophylactic therapy with theophylline slow-release preparations is indicated mainly for children and for nocturnal and early-morning asthma. However, long-acting beta-sympathomimetic agents, such as formoterol or salmeterol, inhaled before retiring to bed are at least as effective for nocturnal asthma. Theophylline can also be beneficial in certain cases of chronic asthma and chronic obstructive airways disease if inhaled corticosteroids and bronchodilators do not offer sufficient relief; however, efficacy and tolerance must be monitored closely.

Theophylline is used against apnea of prematurity (as an alternative to caffeine). After a few hours it is also suited for the prevention of sleep apnea in adults and for the treatment of leg cramps.

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