Theophylline is a methylxanthine that is both a bronchodilator and may have mild anti-inflammatory effects. While it may be used as an adjunctive, alternative treatment with an inhaled steroid, this is not a preferred drug when persistent asthma requires additional medication for asthma control.
How Theophylline WorksTheophylline is a controller medication that works as a bronchodilator and relaxes the muscles that tighten as part of your asthma. Theophylline also has mild anti-inflammatory properties. Because of safer alternatives like inhaled steroids, long-acting beta agonists (LABAs) and leukotriene modifiers, theophylline is not usually prescribed as a first-line or second-line treatment for asthma by your doctor.
The reason theophylline has fallen out of favor is that it does not appear to work as well as other asthma medications. Studies have not shown that theophylline is equivalent to inhaled steroids in the treatment of asthma. Similarly, studies have shown that LABAs are more effective when adding a second drug than adding theophylline.
Theophylline is marketed under the following brand names:
- Theo-Bid Duracap
- Theo-Dur Sprinkle
- Theovent LA
- Slo Bid
Monitoring Theophylline LevelsIn addition to side effects, one thing patients do not like about using theophylline is that you will need to have blood drawn to monitor theophylline levels in your blood. Depending on how you are doing, you may need to do this as much as once per month until you achieve a stable, effective theophylline level in your blood. Generally, your doctor is trying to get a theophylline level in the blood of 5-15 µg/ml. If your theophylline level is above this level, you have a greater chance of experiencing side effects.
Additionally, it is important to let any physician you see know that you are on theophylline. Because theophylline interacts with many types of medication, any doctor you see needs to know you are on theophylline. Studies have shown more 35% of patients on theophylline are prescribed some medication that adversely interacts with theophylline. Some medications that interact with theophylline include:
- Allopurinol: May increase blood levels of theophylline.
- Benzodiazepines: Theophylline may lessen effect.
- Beta-Blockers: May decrease bronchodilatation effect of theophylline.
- Carbamazepine: Theophylline may decrease blood levels and increase seizure risk.
- Ciprofloxocin: Theophylline levels increase with this antibiotic and all other antibiotics in this class. If you receive IV theophylline and IV ciprofloxacin through the same IV line, crystallization can occur.
- Formoterol: Theophylline increases risk of low potassium.
- Zafirlukast: Theophylline may decrease the blood levels of zafirlukast.
- Zileuton: May increase the serum concentration of theophylline.
Also, if you have certain medical problems or conditions you need to be careful if you take theophylline:
- Liver disease: If you have liver problems your body does not metabolize theophylline as quickly as a normal person, and your dose needs to be decreased.
- Congestive heart failure: Dose needs to be decreased as with liver disease
- Smoking: If you smoke, you may need a higher dose of theophylline. Also, if you decide to quit smoking you may need to decrease your theophylline dose.
Theophylline Side Effects
One of the main reasons theophylline is not commonly used anymore is because of side effects. Many patients, however, do not experience any side effects on theophylline. Some patients also experience side effects during the first week of treatment with theophylline. If you can tolerate it initially, your body will more than likely become tolerant. Symptoms that your body will get used to, but you need to talk with your doctor if they do not go away, include:
- Abdominal discomfort or pain
More severe side effects that you need to notify your physician promptly of include:
- Abnormal heart beats or rate
- Skin rash
Pashko S, Simons WR, Sena MM, Stoddard ML. Rate of exposure to theophylline-drug interactions. Clin Ther. 1994 Nov-Dec;16(6):1068-77.
UpToDate. Accessed September 18, 2011.Theophylline: Patient drug information
National Heart, Lung, and Blood Institute. Accessed: September 13, 2011. Expert Panel Report 3 (EPR3): Guidelines for the Diagnosis and Management of Asthma