Theophylline for COPD

Theophylline is a bronchodilator that’s been used in the treatment of COPD for more than seven decades. It is used to treat wheezing or shortness of breath caused by asthma, bronchitis, emphysema and other breathing disorders. It works by relaxing the muscles in the lungs and chest, making it easier to breathe.

How does theophylline for COPD work?

Theophylline is part of the methylxanthines class. It has two different mechanisms of action in people with reversible lung obstruction: as a bronchodilator, it causes smooth muscle relaxation. Its non-bronchodilator effects suppress the response of the airways to stimuli.

Its mechanism of action is not fully known, although animal studies suggest that the bronchodilation involves the inhibition of two phosphodiesterase enzymes (PDE III and PDE IV) while the suppressive effects are probably due to different mechanisms that do not involve these enzymes.

Theophylline also increases the force of contraction of diaphragmatic muscles, probably due to the increase of intracellular calcium through an adenosine-mediated channel. It hasn’t been used as often as it was in the past as better-tolerated and more effective bronchodilators have come on the market.

Studies of theophylline

Studies of people with COPD have shown that theophylline decreases dyspnea, air trapping, and breathing difficulties, and increases diaphragmatic muscle contraction force.

Indications and side effects

Guidelines for COPD treatment classify theophylline as a third-line bronchodilator, after inhaled anticholinergics (ipratropium and glycopyrrolate) and beta2-agonists (albuterol, arformoterol, formoterol, indacaterol, levalbuterol, salmeterol, vilanterol), or a combination of both. However, theophylline may be helpful in people with COPD for its anti-inflammatory properties, although its use is somewhat controversial. Theophylline’s beneficial effects for COPD patients have a narrow therapeutic index (small differences in dose or blood concentration may lead to serious therapeutic failures or adverse drug reactions). Therefore, toxicity can become a serious problem with chronic use, and it is essential to monitor these patients.

Theophylline comes as a tablet, capsule, or liquid to take by mouth. This is a medication that controls symptoms but doesn’t cure them.

Common side effects may include stomach pain, diarrhea, upset stomach, headache, sweating, insomnia or nervousness.


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