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Methylxanthines for Chronic Obstructive Pulmonary Disease (COPD)


Generic Name Brand Name
theophylline Elixophyllin, Theo-24

These medicines are available in pill, liquid, injection, or suppository form. One medicine may be available in multiple forms. Your doctor 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 medicines 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, compared to a placebo, theophylline provides a small improvement in lung function as measured by tests (spirometry) in people who have stable COPD.

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

In general, research shows that the small improvement in lung function does not justify the severe side effects for most people who have COPD. In most cases, newer and safer medicines have replaced methylxanthines for treatment of people who have COPD.

Side Effects

All medicines have side effects. But many people don't feel the side effects, or they are able to deal with them. Ask your pharmacist about the side effects of each medicine you take. Side effects are also listed in the information that comes with your medicine.

Here are some important things to think about:

  • Usually the benefits of the medicine are more important than any minor side effects.
  • Side effects may go away after you take the medicine for a while.
  • If side effects still bother you and you wonder if you should keep taking the medicine, call your doctor. He or she may be able to lower your dose or change your medicine. Do not suddenly quit taking your medicine unless your doctor tells you to.

Call your doctor right away if you have:

  • Nausea and vomiting.
  • A seizure.
  • Irregular heartbeat (arrhythmia).

Common side effects of methylxanthines include:

  • Stomach upset and heartburn. The heartburn may make breathing more difficult, especially for people with asthma.
  • Trouble sleeping (insomnia).
  • Headache.
  • Nervousness or irritability.
  • Rapid heart rate (tachycardia).
  • Rapid breathing (tachypnea).

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

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 medicines, which can make it less effective and potentially life-threatening.

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

What To Think About

Other medicines 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 medicines, such as antibiotics, antacids, birth control pills, and those used for seizures. Ask your doctor or pharmacist if a new medicine will affect how much theophylline you take.

Different brands of theophylline get into the bloodstream at different rates. So always use the same generic or brand-name medicine.

Medicines and illnesses can affect how quickly theophylline is cleared from the body. So the amount of theophylline in the blood must be measured regularly to be sure it stays 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 medicine.

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

Taking medicine

Medicine is one of the many tools your doctor has to treat a health problem. Taking medicine as your doctor suggests will improve your health and may prevent future problems. If you don't take your medicines properly, you may be putting your health (and perhaps your life) at risk.

There are many reasons why people have trouble taking their medicine. But in most cases, there is something you can do. For suggestions on how to work around common problems, see the topic Taking Medicines as Prescribed.

Advice for women

If you are pregnant, breastfeeding, or planning to get pregnant, do not use any medicines unless your doctor tells you to. Some medicines can harm your baby. This includes prescription and over-the-counter medicines, vitamins, herbs, and supplements. And make sure that all your doctors know that you are pregnant, breastfeeding, or planning to get pregnant.


Follow-up care is a key part of your treatment and safety. Be sure to make and go to all appointments, and call your doctor if you are having problems. It's also a good idea to know your test results and keep a list of the medicines you take.

Complete the new medication information form (PDF)( What is a PDF document? ) to help you understand this medication.


Other Works Consulted

  • Department of Veterans Affairs, Department of Defense (2014). VA/DoD clinical practice guideline for the management of chronic obstructive pulmonary disease. U.S. Department of Veterans Affairs. http://www.healthquality.va.gov/guidelines/CD/copd. Accessed June 23, 2016.
  • Global Initiative for Chronic Obstructive Lung Disease (2016). Global strategy for diagnosis, management, and prevention of COPD – 2016. Global Initiative for Chronic Obstructive Lung Disease. http://goldcopd.org/gold-reports. Accessed June 23, 2016.


Current as ofSeptember 5, 2018

Author: Healthwise Staff
Medical Review: E. Gregory Thompson, MD - Internal Medicine
Adam Husney, MD - Family Medicine
Hasmeena Kathuria, MD - Pulmonology, Critical Care Medicine, Sleep Medicine

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