Theophylline

Prescription ·Exploratory record · not publication-reviewed ·Updated July 13, 2026

Theophylline is an oral methylxanthine bronchodilator used in selected asthma and COPD patients when other therapies are insufficient or unavailable. It has a narrow therapeutic index, variable clearance, and serious toxicity risks including nausea, tachyarrhythmias, seizures, and death, so serum level monitoring and interaction review are essential.

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Publication status

Exploratory record, not a reviewed medical publication.

See the editorial and medical-review policies for the publication gate.

This generated database record has not completed a claim-level review by a qualified human medical reviewer. Bibliography links and evidence labels are not approval. The page remains available for reference and is excluded from search indexing.

In short

What the research says.

A quick, data-only summary. The full evidence, dosing, and sources are below.

Theophylline is an oral methylxanthine bronchodilator used in selected asthma and COPD patients when other therapies are insufficient or unavailable. NutriStack rates the supporting evidence as strong. Common adult dosing is Adults: individualized extended-release dosing commonly starts around 300 to 400 mg daily in divided or once-daily regimens, then titrated by serum concentration and tolerability. Target concentrations are often lower than historical ranges to reduce toxicity., though a prescriber sets the actual dose. With long-term use it can deplete vitamin b6. This profile indexes 4 sources.

What it's good for

Maintenance bronchodilation in selected asthma patients
Maintenance treatment adjunct in COPD
Reduction of nocturnal bronchospasm in some patients³
Potential improvement in respiratory muscle endurance

What to watch for

Nausea
Vomiting
Reflux
Known hypersensitivity to theophylline or methylxanthines^1,2
Use caution or avoid in uncontrolled seizure disorder, serious arrhythmias, active peptic ulcer disease, severe hepatic disease, heart failure, fever, sepsis, or major changes in smoking status²

The bottom line

Evidence rating strong. Most-documented uses: maintenance bronchodilation in selected asthma patients, maintenance treatment adjunct in copd, reduction of nocturnal bronchospasm in some patients. 4 sources indexed (1980–2026), with 0 interaction records on file.

The science

How it works, mechanistically.

Core mechanism

Theophylline inhibits phosphodiesterase nonselectively, antagonizes adenosine receptors, increases catecholamine release, and may enhance diaphragmatic contractility and anti-inflammatory signaling at lower concentrations. Clearance is mainly hepatic through CYP1A2 with contributions from CYP2E1 and CYP3A pathways, so smoking status, fever, liver disease, heart failure, age, and interacting drugs or botanicals can markedly change levels.^1,2

Class

Methylxanthine bronchodilator

Dosing

Dosing & protocol.

Common range

Adults: individualized extended-release dosing commonly starts around 300 to 400 mg daily in divided or once-daily regimens, then titrated by serum concentration and tolerability. Target concentrations are often lower than historical ranges to reduce toxicity.

Recommended form

Extended-release oral tablet or capsule with consistent timing and consistent relationship to meals

Use the same product and take consistently with regard to food because extended-release absorption varies by formulation. Avoid sudden changes in caffeine intake and smoking status without reassessing serum concentrations.

Depletions

What it depletes.

Nutrients this medication can lower over time, and what to replace.

Vitamin B6

Moderate

Theophylline exposure has been associated with reduced pyridoxal phosphate status and may increase neurologic vulnerability in susceptible patients.

Replace Vitamin B6Monitor Plasma pyridoxal-5-phosphate when clinically indicatedOnset Weeks to months

Full Theophylline depletion and interaction guide →

Safety

Full safety detail.

Side effects

Nausea
Vomiting
Reflux
Headache
Insomnia
Tremor
Palpitations
Tachycardia
Hypokalemia
Hyperglycemia
Seizures
Serious ventricular arrhythmias
Toxicity from elevated serum concentrations

Contraindications

Known hypersensitivity to theophylline or methylxanthines^1,2
Use caution or avoid in uncontrolled seizure disorder, serious arrhythmias, active peptic ulcer disease, severe hepatic disease, heart failure, fever, sepsis, or major changes in smoking status²
Avoid duplicate methylxanthine exposure and high caffeine loads¹

Sources

Sources, by evidence tier.

Numbered references. Citations throughout the page link here.

Reviews & position papers

1Global Strategy for the Diagnosis, Management, and Prevention of Chronic Obstructive Pulmonary DiseaseGlobal Initiative for Chronic Obstructive Lung Disease · GOLD Report · 2025
Guidelines emphasize inhaled bronchodilators and note safety limitations of methylxanthines.
2Theophylline poisoning: clinical features and managementShannon M · Medical Toxicology and Adverse Drug Experience · 1993
Review details clinical toxicity and the importance of prompt recognition and serum level management.

Observational studies

3Effect of theophylline therapy on vitamin B6 statusMerrill AH et al. · American Journal of Clinical Nutrition · 1980
Clinical data reported reduced pyridoxal phosphate measures during theophylline therapy, supporting monitoring when neurologic symptoms or poor intake are present.

Reference material

4Theophylline Extended-Release Tablets US Prescribing InformationURLU.S. National Library of Medicine · DailyMed · 2026
Labeling describes variable clearance, therapeutic drug monitoring, toxicity, and numerous clinically important interactions.

FAQ

Common questions.

Quick answers about Theophylline, drawn from the data on this page.

What is Theophylline?

What is Theophylline used for?

Commonly cited benefits of Theophylline include: Maintenance bronchodilation in selected asthma patients; Maintenance treatment adjunct in COPD; Reduction of nocturnal bronchospasm in some patients; Potential improvement in respiratory muscle endurance. NutriStack rates the overall evidence as strong.

What is a typical dose of Theophylline?

A typical adult dose of Theophylline is Adults: individualized extended-release dosing commonly starts around 300 to 400 mg daily in divided or once-daily regimens, then titrated by serum concentration and tolerability. Target concentrations are often lower than historical ranges to reduce toxicity.. The commonly recommended form is Extended-release oral tablet or capsule with consistent timing and consistent relationship to meals. These are general ranges, not personalized advice; confirm the right dose with a clinician.

What are the side effects of Theophylline?

Reported side effects include nausea, vomiting, reflux, headache, insomnia, tremor. This is educational information; check with a healthcare professional before use.

How strong is the evidence for Theophylline?

NutriStack rates this as Strong, meaning multiple high-quality meta-analyses or systematic reviews converge on the same finding. Full tier criteria are at https://nutristackapp.com/methodology/evidence-tiers.

Use this with your stack

Theophylline in NutriStack.

Add it to your stack, see how it interacts with everything else you take, and get a Stack Score that updates the moment it does.

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