Theophylline: Revisiting An Old Asthma Treatment

by Frederic Little, M.D. Health Professional

In this entry, I would like to discuss the use of theophylline for asthma both in the past and present. While this medication has fallen out of favor as a first line medication in the treatment of asthma, it should not be overlooked as an option for many patients with asthma.

Theophylline in the past and present

Theophylline is a drug that has been in use for asthma since the 1950's. Structurally related to caffeine, it was first isolated from tea leaves in the late 19th century. Current drug preparations are synthesized in the laboratory.

In the early days of drug treatment for asthma, there were limited treatments -- most of the drugs had significant side effects because they didn't directly target the breathing tubes of individuals with asthma. The airways of people with asthma could be relaxed but at a cost of side effects on other parts of the body:

  • Steroids weakened bones and the immune system and caused weight gain.

  • Epinephrine was short acting and strained the heart.

Theophylline was recognized as a drug that could loosen tight airways, but for this effect, blood levels needed to be at a point that caused jitteriness and upset stomach (similar to the effects from an "overdose" of caffeine). Because there were few alternatives, most patients with chronic asthma that caused daily symptoms between the 1960s and 1980s were taking some preparation of theophylline.

During the 1980s, there were several developments in asthma treatments that changed the lives of asthma sufferers and decreased the use of theophylline. More selective bronchodilators (drugs that relax the breathing tubes or "airways") with fewer side effects were discovered, such as albuterol. Steroids could be given through an inhaler to deliver medication directly to the lungs without having to go through the rest of the body, thus avoiding side effects of steroids given in pill form or by injection.

Because of these powerful new treatments, as well as the modest benefits of theophylline and its side effects, theophylline fell out of favor. In the late 1990s, theophylline was relegated to second or third line status in the treatment of chronic asthma.

New findings about theophylline

The main limitations to the use of theophylline in the past have been its side effects and the fact that it is a relatively weak bronchodilator compared to albuterol and related inhaled medicines. But recent research has shown that there may be newer, underappreciated effects of theophylline. Theophylline can improve breathing in other ways, such as strengthening the diaphragm, the main muscle that we use to bring air into our lungs. In addition, theophylline has been shown to have so-called 'anti-inflammatory' effects on the airways. This effect directly combats the abnormal inflammation in the airways of asthmatics. Most importantly, this effect is found at levels in the blood well below that which causes the common side effects seen in most people.

While theophylline is still not a reasonable choice as a sole agent in asthma treatment, its use is being reevaluated as an option to add on to existing medications in an individual whose asthma is not optimally controlled.

Closing thoughts

While there are many newer medications for the treatment of chronic asthma with few side effects, some patients may benefit from the addition of theophylline to their current medication regimen. With new treatment guidelines, there are fewer side effects as the target level in the blood is lower than in past times. Whether theophylline is an option for your asthma treatment should be discussed with your doctor.

Frederic Little, M.D.
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Frederic Little, M.D.

Frederic Little is an Assistant Professor in the Department of Medicine at Boston University. He attends on the Allergy Consultation Service as well as the Medical Intensive Care Unit and Pulmonary Consultation Service at Boston Medical Center. He wrote for HealthCentral as a health professional for Asthma and Allergy.