Theophylline: Uses, Safety, and Interactions

When working with Theophylline, a methylxanthine bronchodilator that relaxes airway muscles and improves breathing. Also known as Theolair, it is commonly prescribed for chronic respiratory conditions.

It plays a crucial role in managing asthma, a condition marked by airway inflammation, wheezing, and shortness of breath and COPD, chronic obstructive pulmonary disease, which causes persistent airflow limitation and frequent exacerbations. As a bronchodilator, a drug that opens narrowed airways by relaxing smooth muscle, Theophylline helps keep airways open when other inhalers aren’t enough.

How Theophylline Works and Who Benefits

Theophylline belongs to the methylxanthine, a class of compounds that stimulate the heart, diaphragm, and central nervous system while dilating airways. Its primary action is phosphodiesterase inhibition, which raises cAMP levels and leads to smooth‑muscle relaxation. This mechanism makes it a rescue option for patients who need long‑term control of airway tone, especially those with severe asthma or frequent COPD flare‑ups.

Because Theophylline is taken orally, blood levels can vary widely. Therapeutic drug monitoring is often recommended to keep serum concentrations between 10‑20 µg/mL. Staying within this range minimizes side effects like nausea, tremor, or insomnia while preserving the drug’s bronchodilating effect.

One key advantage is its oral availability, which can be a game‑changer for patients who struggle with inhaler technique. However, it’s not a first‑line therapy for most people; inhaled corticosteroids and long‑acting beta‑agonists usually take priority. Theophylline shines when those inhaled options fall short or when a patient needs an additional oral agent.

Drug interactions are a major consideration. Antibiotics such as erythromycin and clarithromycin, as well as antifungals like fluconazole, can inhibit the enzymes that clear Theophylline, pushing blood levels into the toxic range. Conversely, smoking induces metabolism, potentially lowering effectiveness. Always review a patient’s medication list for these contributors.

When prescribing Theophylline, clinicians weigh benefits against risks. The drug can improve exercise tolerance and reduce hospital visits for asthma exacerbations, but it demands careful dose adjustments and patient education. Patients should be taught to report symptoms like rapid heartbeat, severe headache, or persistent vomiting immediately.

For patients with heart disease, Theophylline’s mild stimulant effect can be useful, but it may also provoke arrhythmias in susceptible individuals. In such cases, cardiology input is advisable before starting therapy.

In practice, many providers use Theophylline as part of a combination therapy—pairing it with inhaled steroids, long‑acting beta‑agonists, or leukotriene modifiers. This multi‑drug approach tackles inflammation, bronchoconstriction, and smooth‑muscle tone simultaneously, offering a more comprehensive control strategy.

Below you’ll find a curated list of articles that dive deeper into specific aspects of Theophylline use—ranging from dosing guides and safety tips to real‑world comparisons with other asthma and COPD treatments. Whether you’re a patient looking for practical advice or a clinician seeking up‑to‑date evidence, the collection will give you actionable insights you can use right away.