Drug Comparisons

Related to caffeine, theophylline and similar medications belong to a group of chemicals known as methylxanthines, xanthines, or, more commonly, theophyllines. Theophylline was one of the first drugs used to treat asthma in the 1950s. After extended-release products became widely available in the 1960s and 1970s, theophyllines were the mainstay of asthma therapy. Now, newer drugs have replaced them as first-line, long-term treatment. They are still used as add-on therapy, though, when asthma symptoms are not controlled by standard treatment with inhaled corticosteroids or long-acting beta-2 agonists.

Mainly, theophyllines relax muscles in the bronchial tubes (airways) to relieve asthma symptoms. They may have other effects that improve breathing, but the exact ways that they work are not understood very well. Theophyllines must be used regularly and they usually take longer than other asthma drugs to become effective for preventing asthma symptoms. They cannot stop an asthma attack once it begins. In comparison to other asthma medications, theophyllines also have more risk for side effects and interactions. Additionally, doses for them may need frequent adjustment because the blood levels of theophyllines that are effective for treating asthma may be close to levels that cause potentially serious side effects. Therefore, patients taking a theophylline usually need to have blood testing done fairly often.

Drugs in this Class
Theophylline Extended-Release Capsules ()
Theophylline Elixir (Elixophyllin Elixir)

Summarizing the Evidence

• In studies, adding theophylline to inhaled corticosteroid therapy has resulted in improvements roughly equal to a double dose of the corticosteroid or to adding a long-acting beta-2 agonist to the corticosteroid dose.
• In general, theophyllines are less effective at reducing bronchial constriction than other types of asthma medications. In addition, theophyllines have little or no ability to decrease inflammation.
• However, extended-release theophylline may be more effective than oral beta-2 agonists for controlling nocturnal (nighttime) asthma symptoms
• Although oral theophyllines cannot stop an asthma attack that has started, injectable forms of theophylline sometimes may be used in emergency situations to stop a severe asthma attack that does not respond to other treatment.

Dosing and Administration

• Most theophylline products are available in oral dose forms (capsules, liquids, or tablets) that may be more convenient for some asthma patients to take than using an inhaler or a nebulizer.
• Dosing for theophyllines depends on the patient?s age and weight and on other factors such as whether the patient smokes. To be effective, theophyllines must reach a certain level in the patient?s blood and then stay at about that same level.
• Theophyllines have a narrow therapeutic index (also called a narrow therapeutic range), which means that there is only a little difference between an effective dose and a harmful dose. Usually, once a patient?s asthma has been controlled by a specific dose and type of theophylline, the patient should keep taking exactly that dose. Changing from one brand or generic to another generally is not recommended.
• Some extended-release theophyllines can be taken once a day.
• Most theophyllines are taken two times or three times a day. The doses should be spread out equally, if possible. That means twice-daily doses should be 12 hours apart and three-times-a-day doses should be once every 8 hours.
• Sometimes patients are directed to take a larger dose of theophylline in the evening than during the day, if asthma symptoms get worse at night.
• Some types of theophylline need to be taken on an empty stomach (at least one hour before a meal, two hours or more after a meal, or first thing in the morning).

Generic Availability

• Nearly all types of theophyllines are available in generic forms, so they may be less expensive than many other asthma drugs.
• Many brand-name theophylline products have been discontinued by their manufacturers because of low sales.

Drug Interactions

Some interactions between medications can be more severe than others. The best way for you to avoid harmful interactions is to tell your doctor and/or pharmacist what medications you are currently taking, including any over-the-counter products, vitamins, and herbals. For specific information on how the drugs interact and the severity of the interaction, please use our Drug Interactions Checker.

Side Effects

To view specific side effect information, please use our Side Effect Checker.

Additional Information

References

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Last Updated: May 2007
This content was created by members of the DrugDigest team of experts and is solely under DrugDigest's editorial control.

Note: The above information is intended to supplement, not substitute for, the expertise and judgment of your physician, pharmacist, or other healthcare professional. It should not be construed to indicate that the use of the product is safe, appropriate, or effective for you. Consult your healthcare professional before taking any medication.