Methylxanthines for chronic obstructive pulmonary disease (COPD)

Examples

These medications are available in pill, liquid, injection, or suppository form. One medication may be available in multiple forms. Your health professional will help you decide which type is best for you.

How It Works

The actions of methylxanthines are not completely known.

Theophylline may:

• Slightly relax the airways in the lungs (bronchodilator).
• Improve breathing by increasing the strength of the diaphragm (if it is weakened) and by stimulating the breathing control centers in the brain.
• Make it easier to get mucus out of the lungs.

Why It Is Used

Because of their side effects, methylxanthines are not considered first-choice medications to treat chronic obstructive pulmonary disease (COPD). They are prescribed most often for people with COPD who:

• Still have major difficulty breathing despite using both an inhaled beta2-agonist and an inhaled anticholinergic.
• Have persistent nighttime symptoms.
• Have frequent, rapid, and sometimes sudden increase in shortness of breath (COPD exacerbation).

How Well It Works

A few studies have noted that theophylline provides a small improvement in lung function as measured by tests (spirometry) in people with stable COPD compared to a placebo.¹

In a COPD exacerbation, methylxanthines provide a small improvement in lung function as measured by spirometry compared to a placebo.²

In general, research shows that the small improvement in lung function does not justify the severe side effects for most people with COPD.

Side Effects

The side effects of methylxanthines are described as being similar to drinking too much caffeine, including:

• Stomach upset.
• Heartburn.
• Trouble sleeping (insomnia).
• Headache.
• Nervousness or irritability.
• Rapid heart rate (tachycardia).
• Rapid breathing (tachypnea).

People taking the medication may be able to reduce these side effects by avoiding caffeine.

Serious (toxic) side effects are seen in some people. These side effects include:

• Nausea and vomiting.
• Seizures.
• Low blood sugar.
• Irregular heartbeat (arrhythmia).

The difference between a dose of theophylline that helps improve symptoms and a dangerous dose (one that causes serious side effects) is small. Theophylline also has significant interactions with other prescribed medications, which can make it less effective and potentially life-threatening.

Theophylline relaxes the esophagus near the opening into the stomach. This may result in heartburn (acid reflux) if stomach acid moves up into the esophagus. Acid reflux may cause airway obstruction to become worse (making breathing more difficult), particularly in people with asthma. For more information, see the topic Gastroesophageal Reflux Disease (GERD).

See Drug Reference for a full list of side effects. (Drug Reference is not available in all systems.)

What To Think About

Other medications may be a better choice than methylxanthines for treating COPD because the dose needed to improve symptoms is so close to a dose that causes serious side effects.

Theophylline interacts with many different types of medications, such as antibiotics, antacids, birth control pills, and those used for seizures. Ask your health professional or pharmacist if a new medicine will affect how much theophylline you take.

Different brands of theophylline get into the bloodstream at different rates. Therefore, you always should use the same generic or brand-name medication.

Because medications and illnesses can affect how quickly theophylline is cleared from the body, the amount of theophylline in the blood must be measured regularly to be certain it remains at a safe level.

Smoking increases how quickly theophylline is cleared from the body, so a person with COPD who continues to smoke may need larger doses of the medication.

People taking theophylline should avoid caffeine-containing beverages. These may make theophylline's side effects worse, especially jittery nerves and headaches.

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