Methylxanthines for Chronic Obstructive Pulmonary Disease (COPD)

Covers methylxanthines for COPD. Looks at medicines that help relax airways, improve breathing, and help get mucus out of the lungs. Lists generic and brand names such as theophylline (Theo-24). Includes how well they work and side effects.

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
  • Have persistent nighttime
  • 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.

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
  • 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
  • Trouble sleeping
  • Headache.
  • Nervousness or
  • 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

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.

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

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. :// 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. :// Accessed June 23, 2016.


ByHealthwise StaffPrimary Medical Reviewer E. Gregory Thompson, MD – Internal Medicine Adam Husney, MD – Family Medicine Specialist Medical Reviewer Hasmeena Kathuria, MD – Pulmonology, Critical Care Medicine, Sleep Medicine

Current as ofDecember 6, 2017