Theophylline for Asthma

Woman with breathing difficulties puts hand on chest

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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.

Theophylline periodically becomes more popular and then falls out of favor with doctors treating asthma. However, one of its main advantages compared to all other asthma treatments is that it is inexpensive. This makes it much more appealing as an add-on treatment after an inhaled steroid does not sufficiently control asthma symptoms in the minds of many patients.

Because theophylline can last for up to 24 hours, some physicians will use theophylline to gain control of nighttime asthma symptoms, especially for mild persistent or moderate persistent asthma.

How Theophylline Works

Theophylline is a controller medication that works as a bronchodilator and relaxes the muscles that tighten as part of your asthma. Theophylline also has anti-inflammatory and bronchoprotective properties that probably better explain its ability to help control asthma symptoms rather than its bronchodilatory properties alone.

Because of safer alternatives like inhaled steroids (and doctors in training today have much less experience with the drug as we have been in a time where it has fallen out of favor with the medical community), 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 over adding theophylline.

Theophylline requires certain blood levels to be achieved for it to have a therapeutic effect but also can cause adverse side effects when this level is exceeded. Doctors often describe this as a narrow therapeutic range.

Theophylline Brand Names

Theophylline is marketed under the following brand names:

  • Elixophyllin
  • Theo-24
  • Theo-Bid Duracap
  • TheoCap
  • Theochron
  • Theo-Dur
  • Theo-Dur Sprinkle
  • Theolair
  • Theovent LA
  • Slo Bid
  • Slo-Phyllin
  • Uniphyl

Monitoring Theophylline Levels

In 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.

In the distant past, target blood levels of theophylline were 10-20 mcg/ml. More recently, target levels are 5-10 mcg/ml. This lower level of theophylline has made this medication safer, because dangerous side effects don't usually occur until levels exceed 20 mcg/ml.

Potential Contraindications

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 than 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 may lessen the effect.
  • Beta-Blockers may decrease the bronchodilation effect of theophylline.
  • Carbamazepine: Theophylline may decrease blood levels and increase seizure risk.
  • Ciprofloxacin: 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 the 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: The 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.

Indications for Theophylline

There are several general areas where theophylline is used today in the treatment of asthma:

  1. As an adjunctive therapy when inhaled steroids do not control asthma symptoms or when other agents were added (LABAs) or (leukotriene modifiers) and not effective in controlling symptoms.
  2. As a primary maintenance treatment when a patient does not adhere (or it is too difficult or cumbersome) to an inhaled steroid and a leukotriene modifier is not effective.
  3. When a patient is in the intensive care unit with a severe asthma exacerbation and not responding to other treatments.

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 to your doctor if they do not go away, include:

More severe side effects that you need to promptly notify your physician of include:

  • Abnormal heartbeat or rate
  • Seizures
  • Skin rash
  • Vomiting
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Article Sources
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  1. Elias-jones AC, Higenbottam TW, Barnes ND, Godden DJ. Sustained release theophylline in nocturnal asthma. Arch Dis Child. 1984;59(12):1159-61. doi:10.1136/adc.59.12.1159

  2. Nutini S, Martini T, Righi R. Long-term treatment of asthmatic patients with salmeterol vs slow-release theophylline. Respir Med. 1998;92(4):683-90. doi:10.1016/s0954-6111(98)90518-2

  3. Oppenheimer J, Nelson HS. Safety of long-acting beta-agonists in asthma: a review. Curr Opin Pulm Med. 2008;14(1):64-9. doi:10.1097/MCP.0b013e3282f1980b

  4. Pashko S, Simons WR, Sena MM, Stoddard ML. Rate of exposure to theophylline-drug interactions. Clin Ther. 1994;16(6):1068-77.

  5. Mahemuti G, Zhang H, Li J, Tieliwaerdi N, Ren L. Efficacy and side effects of intravenous theophylline in acute asthma: a systematic review and meta-analysis. Drug Des Devel Ther. 2018;12:99-120. doi:10.2147/DDDT.S156509

Additional Reading
  • National Heart, Lung, and Blood Institute. Expert Panel Report 3 (EPR3): Guidelines for the Diagnosis and Management of Asthma