What to Know About Theophylline

Used with other asthma therapies, this drug acts as a bronchodilator

In This Article

Theophylline is a drug used in combination with other medications for the treatment of asthma and chronic obstructive pulmonary disease (COPD). Delivered either orally or intravenously, theophylline acts as a bronchodilator to reduce airway reactivity that leads to wheezing and shortness of breath.

Theophylline belongs to a unique class of drugs called methylxanthines derived from naturally-occurring compounds found in tea and cocoa beans.

Common brand names include:

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

Uses

Theophylline is considered a component of a treatment plan. It is typically taken by mouth for the long-term control and maintenance of asthma, COPD (including emphysema and chronic bronchitis), and other chronic lung diseases.

It can also be given intravenously (into a vein) for treatment for severe asthma attacks or COPD exacerbations.

Theophylline works by relaxing the smooth muscles of the airways while relieving inflammation and acting upon the respiratory center of the brain. Doing so helps alleviate the airway hypersensitivity that leads to trouble breathing.

While theophylline has been used in the treatment of asthma since 1922, it has since fallen in and out of favor with doctors and, today, is not as commonly used as it once was.

Doctors who prescribe it most commonly do so for the following purposes:

  • Adjunctive ("add-on") therapy when inhaled steroids are unable to control symptoms
  • Adjunctive therapy when other add-on drugs, such as long-acting beta-agonists (LABAs) or leukotriene modifiers, are unable to provide control
  • Maintenance therapy when adherence to inhaled steroids is poor
  • In intensive care situations when a person is not responding to other traditional treatments

Because theophylline can work for up to 24 hours, some doctors prescribe theophylline to help patients gain control of nighttime wheezing, coughing, and shortness of breath, especially with mild-persistent to moderate-persistent asthma.

Off-Label Uses

Theophylline is sometimes prescribed off-label for the treatment of obstructive sleep apnea.

Before Taking

Theophylline is neither as effective nor as safe as inhaled steroids, LABAs, or leukotriene modifiers. As such, theophylline is typically only prescribed when standard therapies underperform, cause intolerable side effects, or are financially out of reach.

It is rarely used in first-line or even second-line therapies. It is never used on its own.

Precautions and Contraindications

Theophylline has few outright contraindications for use other than a history of hypersensitivity to theophylline or any inactive ingredient in the drug.

With that said, theophylline may cause a worsening of certain medical conditions and may need to be avoided if you have:

Theophylline should be used with caution in people with following medical conditions in whom drug clearance (in general) is more likely to be impaired:

  • Acute pulmonary edema
  • Congestive heart failure
  • Cor pulmonale
  • Cystic fibrosis
  • Enlarged prostate
  • Thyroid disease

Because theophylline stimulates gastric secretions, it should also be used with caution in people with chronic gastritis, gastroesophageal reflux disease (GERD), hiatal hernia, or an active peptic ulcer, as it may exacerbate gastrointestinal symptoms.

Theophylline is a Pregnancy Category C drug, meaning that the drug has not been proven to cause fetal harm but no well-designed human trials are available. Women who are pregnant or intend to get pregnant should fully weigh the benefits and risks of treatment with their doctors.

Doxofylline is a closely related methylxanthine drug that is also used in the treatment of asthma. Studies have shown that doxofylline has similar efficacy to theophylline but with fewer side effects.

Dosage

Theophylline is available as an oral tablet, capsule, or liquid suspension, as well as an injectable solution.

  • Theophylline immediate-release pills are available in 100-milligram (mg), 200-mg, 300-mg, 400-mg, 450-mg, and 600-mg formulations.
  • Theophylline extended-release pills are available in 100-mg, 200-mg, 300-mg, 400-mg, 450-mg, and 600-mg formulations.
  • Theophylline extended-release capsules are available in 100-mg, 200-mg, 300-mg, and 400-mg formulations.
  • Theophylline oral suspension is available in an 80-mg per 15-milliliter (80 mg/15 mL) formulation that is typically for use in younger children.
  • Theophylline injected solution is available in a 25 mg/1 mL formulation for use in emergency situations.

The recommended dosage varies by age as well as the intended use. The lowest dose able to achieve a therapeutic effect should always be used.

Doctors will typically start with a 300-mg dose in adults, children, and the elderly and only increase the dose if blood tests reveal that the drug is being safely cleared from the body.

Theophylline Forms and Dosing by Age Group
  Adults Over 60 Adults Under 60 Children Infants
Oral maintenance
(immediate-release tablets)
Extended-release tablets recommended 300-1,600 mg/day taken every 6-8 hours 300-1,600 mg/day taken every 6-8 hours Dosage based on weight and age in weeks
Oral maintenance
(extended-release tablets)
300-400 mg/day taken every 8-12 hours 300-1,600 mg/day taken every 8-12 hours For children over 6: 300-1,600 mg/day taken every 8-12 hours Do not use
Oral maintenance 
(extend-release capsules)
Extended-release tablets recommended 300-1,600 mg/day taken every 24 hours For children over 12: 300-1,600 mg/day taken every 24 hours Do not use
Intravenous solution Up to 400 mg daily Up to 900 mg daily Up to 400-900 mg daily based on age and weight Dosage based on weight and age by weeks

Modifications

Dose modifications are generally made if you have conditions that impair the clearance of theophylline from the body.

Theophylline is mainly excreted in stool and, to a lesser degree, in urine. If the drug cannot be cleared adequately, toxicity can occur.

To ensure the appropriate drug concentrations are being maintained—ideally between 5 and 10 mcg/mL—therapeutic drug monitoring (TDM) blood tests will be performed routinely. Any value over this threshold may require a dose adjustment.

Among the conditions for which dose adjustment may be needed:

  • Liver disease: Do not exceed 400 mg/day if there is cirrhosis, acute hepatitis, or liver failure. Intravenous doses should not exceed 0.2 mg/kg/per for children under 16 years of age or 16 mg/kg/per for anyone older.
  • Kidney impairment: Reduce the dose by 50% infants under 3 months.
  • Smoking: Tobacco smoke speeds the clearance of theophylline from the body. If you smoke, you may need a higher dose of theophylline. TDM monitoring will help determine the appropriate dose.
  • Prolonged fever: Prolonged fever over 102 degrees F can reduce the clearance of theophylline from the body. In such cases, a short-term reduction in the dose may be needed.

How to Take and Store

Oral theophylline can be taken with or without food. However, if you experience an upset stomach, taking the dose with food may help relieve symptoms.

Do not crush or chew tablets or capsules.

Because the drug half-life of theophylline is relatively short (eight hours in non-smoking adults), you need to take it on a strict daily dose to maintain optimal blood concentrations. This means taking it at the prescribed time, whether that be every six, eight, 12, or 24 hours.

If you miss a dose by a couple of hours, simply take it once you remember. However, if the missed dose is near the time of your next scheduled dose, simply skip the missed dose and continue as normal.

Never double up theophylline doses either to "catch up" following a missed dose or to "load up" if you plan to be out and don't want to carry your medication along with you.

Unless otherwise indicated, most oral formulations can be stored at room temperature, ideally between 68 degrees F and 77 degrees F. Do not store theophylline in your glove compartment or direct sunlight. Keep the medications in their original light-resistant containers.

Never use a drug past beyond its expiration date.

Side Effects

Like any drug, theophylline may cause side effects. Many are caused by the drug's caffeine-like properties.

Not everyone will experience them, and some may only have side effects during the first week of treatment.

Common

Common side effects of theophylline include:

  • Abdominal discomfort or pain
  • Diarrhea
  • Headache
  • Insomnia
  • Irritability
  • Dizziness
  • Restlessness
  • Nausea and vomiting
  • Skin redness and flaking
  • Increased urination
  • Difficulty urinating (mainly in older men)

Side effects like these may be more pronounced if caffeine (e.g., coffee, chocolate) is also consumed.

Severe

You need to take theophylline regularly before it has any therapeutic effect. However, doing so may cause side effects if the drug accumulates beyond a certain blood concentration. This is referred to as a narrow therapeutic range.

When concentrations exceed 20 micrograms per milliliter (mcg/mL), serious and potentially life-threatening symptoms may develop.

Given this, and to avoid drug toxicity, users must be prepared to submit to regular therapeutic drug monitoring.

When to Call 911

Seek emergency care if you experience the following severe symptoms while on theophylline:

  • Abnormal heart rhythms
  • Shortness of breath or weak breathing
  • Chest pains
  • LIghtheadedness or fainting
  • Bluish or pale skin color
  • Inability to urinate
  • Seizures

These may be signs of theophylline toxicity, a rare condition that can lead to cardiac arrest and irreversible brain damage if not treated immediately.

Interactions

Some medications are known to interact with theophylline, including:

  • Accolate (zafirlukast): May be less effective if taken with theophylline.
  • Allopurinol: May increase blood concentrations of theophylline.
  • Benzodiazepines: May be less effective if taken with theophylline.
  • Beta-blockers: May be less effective if taken with theophylline.
  • Cipro (ciprofloxacin) and other quinolone antibiotics: May decrease theophylline concentrations and raise antibiotic concentrations, increasing the risk of antibiotic side effects.
  • Formoterol: May cause hypokalemia (low potassium) if taken with theophylline.
  • Tegretol (carbamazepine): May increase the risk of seizures if taken with theophylline.
  • Zyflo (zileuton): May increase blood concentrations of theophylline.

To avoid drug interactions, let your doctor known about any medications you may be taking whether they are prescription, over-the-counter, herbal, nutritional, or recreational.

A Word From Verywell

Theophylline is sometimes used to support the treatment of asthma or COPD if you are not adherent to your daily inhaled steroid treatment.

But rather than simply taking another drug to overcome an adherence problem, speak with your doctor about ways to improve your adherence, including daily cell phone reminders or psychotherapy if you have anxiety or depression (both of which can influence adherence).

By committing to a daily drug regimen, you are likely to experience fewer and less severe attacks or complications of asthma or COPD, which may make use of theophylline unnecessary.

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