
Theophylline (brand names include: OD Phillin / Elixophyllin / Theo-24 / Theochron / Uniphyl) belongs to a class of medicines known as methylxanthine bronchodilators. It helps relax the smooth muscles in the airways, decreases airway responsiveness, and can improve breathing over time. While once a mainstay therapy for asthma and chronic obstructive pulmonary disease (COPD), Theophylline is now used more selectively—often as an adjunct when inhaled therapies alone do not provide adequate control, for nocturnal symptoms, or when cost limits access to newer medications.
How Theophylline Works
Theophylline’s clinical effects arise from several complementary mechanisms that together reduce airflow obstruction and improve ventilatory drive:
- Phosphodiesterase inhibition: By inhibiting phosphodiesterase (particularly PDE3 and PDE4), Theophylline increases intracellular cyclic AMP, promoting relaxation of airway smooth muscle and bronchodilation.
- Adenosine receptor antagonism: Theophylline blocks adenosine receptors in the lungs. Adenosine can cause bronchoconstriction and histamine release; antagonism helps prevent these effects.
- Anti-inflammatory and immunomodulatory activity: At lower serum concentrations, Theophylline may reduce airway inflammation and enhance histone deacetylase-2 (HDAC2) activity, potentially restoring steroid responsiveness in certain patients.
- Enhanced diaphragmatic contractility: Theophylline can improve diaphragmatic function and respiratory muscle endurance, which may be beneficial in COPD.
These actions collectively support its role as a bronchodilator and adjunct anti-inflammatory agent in asthma and COPD (including emphysema and chronic bronchitis).
Indications and Clinical Use
Theophylline is used in the maintenance treatment of obstructive airway diseases. It is generally not a first-line controller in modern asthma or COPD protocols, but it can be considered in the following scenarios:
- Asthma maintenance therapy: As an add-on for patients with persistent symptoms despite inhaled corticosteroids (ICS) and bronchodilators, or when nocturnal asthma is prominent.
- COPD (chronic bronchitis and emphysema): For symptom relief and potential reduction in exacerbations when inhaled long-acting bronchodilators and ICS are inadequate or not tolerated.
- Post-acute stabilization: In select cases after an exacerbation to aid in ventilatory drive, under close monitoring.
Important note: Theophylline is not a rescue medication. It does not act as rapidly as short-acting beta-agonists (e.g., albuterol). For acute bronchospasm or severe flare-ups, fast-acting inhalers remain essential.
Recommendations
Follow the directions for using this medicine provided by your doctor. Take your medicine exactly as directed. Because Theophylline has a narrow therapeutic window, individualized dosing and periodic blood level monitoring are crucial to maximize benefit and reduce side effects.
General administration guidance:
- Dosing schedule: Many extended-release Theophylline tablets or capsules are taken once daily (often in the morning or evening) or twice daily, depending on the product and prescribed regimen. Immediate-release products may require more frequent dosing.
- Consistency with food: Take Theophylline consistently with respect to meals—either always with food or always on an empty stomach—to maintain steady absorption and serum levels.
- Do not crush or chew extended-release forms: Swallow extended-release tablets/capsules whole. Crushing or chewing can cause dose dumping and toxicity.
- Hydration: Stay well-hydrated unless otherwise directed, which may help reduce some gastrointestinal side effects.
- Avoid excess caffeine: Coffee, tea, energy drinks, and chocolate contain methylxanthines that can amplify Theophylline’s side effects (nervousness, palpitations, insomnia).
- Smoking and lifestyle factors: Cigarette smoking induces metabolism of Theophylline and can lower drug levels; abruptly stopping smoking can increase levels and risk of toxicity. Tell your clinician if your smoking status changes.
Missed dose:
- If you miss a dose, take it as soon as you remember unless it is close to the time of your next dose. In that case, skip the missed dose and resume your regular schedule.
- Do not double up doses to make up for a missed one.
Therapeutic drug monitoring:
- Target serum concentration: Typically 5–15 micrograms/mL for adults; higher levels increase the risk of adverse effects without proportional benefit.
- When to check levels: After dose changes, when adding or stopping interacting medicines, with illnesses (especially fever or liver issues), and periodically during maintenance to ensure safe exposure.
Dosage and Administration Details
Dosing is individualized based on age, weight, smoking status, comorbidities, and liver function. Your prescriber will titrate carefully with monitoring.
- Adults (non-smokers): Starting doses are conservative, with gradual increments guided by clinical response and serum levels. Many adults stabilize on extended-release formulations dosed once or twice daily.
- Adults (smokers): May require higher doses due to increased clearance; however, doses must be adjusted if smoking status changes.
- Older adults: Reduced clearance increases sensitivity; start low and go slow, with frequent monitoring.
- Hepatic impairment or heart failure: Reduced metabolism necessitates lower initial doses and slower titration.
- Pediatric patients: Often dosed on a mg/kg basis with careful monitoring; children can metabolize Theophylline more rapidly than adults, but febrile illnesses can suddenly reduce clearance.
Formulations and administration tips:
- Extended-release tablets/capsules: Designed for stable blood levels; take on a consistent schedule.
- Immediate-release tablets/solutions: May be used in select cases; require multiple daily doses and careful level checks.
- Switching formulations: Do not substitute one formulation or brand for another without consulting your clinician, as bioavailability may differ.
Precautions
Tell your doctor before taking Theophylline if:
- You are allergic to any medicines, especially other methylxanthines (e.g., aminophylline).
- You have serious medical conditions such as liver disease, heart failure, arrhythmias, seizure disorders, peptic ulcer disease, hyperthyroidism, or severe hypoxemia.
- You are pregnant, planning to become pregnant, or breast-feeding.
Additional safety considerations:
- Narrow therapeutic index: Small dose changes or drug interactions can shift levels into a toxic range; maintain regular follow-up and monitoring.
- Febrile illness: Fever (especially prolonged) can reduce Theophylline clearance, raising levels. Contact your clinician if you develop persistent fever, infection, or sudden worsening of symptoms.
- Diet and caffeine: Limit caffeine-containing foods and beverages. Large, abrupt changes in dietary protein or carbohydrate intake can modestly influence metabolism; consistency is best.
- Alcohol: Excessive alcohol intake can affect metabolism and increase side effects; use cautiously and discuss with your clinician.
- Driving and machinery: If you experience tremor, dizziness, insomnia, or palpitations, use caution with tasks requiring alertness.
- Comprehensive asthma/COPD plan: Theophylline should complement, not replace, controller inhalers (e.g., ICS, LABAs) and quick-relief medications. Ensure you have and understand an action plan for exacerbations.
Side Effects
Many side effects are dose-related and correlate with serum Theophylline concentrations. Report persistent or severe symptoms promptly.
Common side effects:
- Gastrointestinal: Nausea, vomiting, heartburn, abdominal discomfort
- CNS: Headache, nervousness, irritability, tremor, insomnia, restlessness
- Cardiovascular: Palpitations, mild tachycardia
Less common but important:
- Significant tachyarrhythmias, atrial fibrillation, or ventricular arrhythmias
- Seizures, especially with high levels or interacting drugs
- Severe, persistent vomiting (a possible early sign of toxicity)
- Hypotension, hypokalemia (with high doses or in combination with beta-agonists)
Signs of potential toxicity that require urgent evaluation:
- Repetitive or uncontrollable vomiting
- Severe tremors, agitation, confusion, or seizures
- Racing or irregular heartbeat, chest pain, fainting
If you suspect an overdose, seek emergency care or contact poison control immediately.
Drug Interactions
Theophylline is metabolized mainly by hepatic CYP1A2 (and to a lesser extent CYP3A and CYP2E1). Many medications and lifestyle factors alter its clearance, which can push levels too high or too low.
Increase Theophylline levels (risk of toxicity):
- Antibiotics: Ciprofloxacin, enoxacin; erythromycin and clarithromycin can also raise levels
- Psychotropics: Fluvoxamine, some SSRIs at higher doses
- Anti-inflammatory: Zileuton
- Acid reducers: Cimetidine
- Others: Allopurinol (high doses), verapamil, diltiazem, propafenone, disulfiram
Decrease Theophylline levels (reduced efficacy):
- Smoking (tobacco and marijuana): Induces CYP1A2
- Antiepileptics: Carbamazepine, phenytoin, phenobarbital
- Rifamycins: Rifampin, rifabutin
- Herbals: St. John’s wort
Pharmacodynamic interactions:
- Other stimulants (caffeine, decongestants): Increase nervousness, tachycardia, insomnia
- Beta-agonists: Therapeutic synergy in bronchodilation but may potentiate hypokalemia and palpitations
- Benzodiazepines and sedatives: Theophylline may blunt sedative effects at higher levels
Always provide your clinician and pharmacist with a current list of medications, supplements, and lifestyle factors (including smoking status) before starting or adjusting Theophylline.
Monitoring and Follow-Up
Because exposure–response varies and the therapeutic index is narrow, monitoring is a core part of safe Theophylline use:
- Serum levels: Check after dosage adjustments, when adding or removing interacting agents, during intercurrent illness, or periodically during stable therapy.
- Clinical response: Track symptoms, rescue inhaler use, nighttime awakenings, exercise tolerance, and exacerbation frequency.
- Safety labs: Consider liver function monitoring in hepatic impairment; monitor electrolytes if taking high-dose beta-agonists.
- Cardiac assessment: If palpitations or syncope occur, evaluation including ECG may be warranted.
Use in Special Populations
Pregnancy and lactation:
- Pregnancy: Use only if the potential benefit justifies the potential risk. Pregnancy can alter drug metabolism; close monitoring is advised if therapy is necessary.
- Breast-feeding: Theophylline is excreted in breast milk. Monitor the nursing infant for irritability or poor feeding if maternal therapy is required.
Older adults:
- Reduced clearance increases the risk of accumulation and side effects. Start at lower doses and titrate cautiously with frequent level checks.
Hepatic impairment and heart failure:
- Lower initial dosing and careful titration are essential due to reduced metabolism.
Renal impairment:
- The parent drug is hepatically cleared; however, metabolites accumulate with renal dysfunction and may contribute to adverse effects. Clinical caution and monitoring are prudent.
Pediatrics:
- Children may clear Theophylline more rapidly than adults but are particularly sensitive to changes during febrile illness. Weight-based dosing and regular monitoring are critical.
Practical Tips for Patients
- Maintain a consistent routine: Take Theophylline at the same time each day, consistently with or without food.
- Know your formulation: Do not crush or chew extended-release tablets or open capsules unless your pharmacist confirms it is safe.
- Track symptoms and triggers: Use a diary or app to record symptoms, inhaler use, and potential triggers (allergens, smoke, infections).
- Limit caffeine and stimulants: They can intensify side effects such as tremor and insomnia.
- Alert your care team: Report any new medications, supplements, or major lifestyle changes, particularly smoking status.
- Carry your action plan: Have clear instructions on what to do during exacerbations and when to seek medical care.
Comparisons and Alternatives
In current asthma and COPD management, inhaled therapies are preferred due to better efficacy and safety profiles:
- Asthma: Inhaled corticosteroids (ICS) remain the cornerstone. Add-ons include long-acting beta-agonists (LABAs), leukotriene receptor antagonists (e.g., montelukast), long-acting muscarinic antagonists (LAMAs), and biologics for severe eosinophilic or allergic phenotypes.
- COPD: Long-acting bronchodilators (LABA and/or LAMA) are first-line; ICS may be added for frequent exacerbations. Roflumilast or macrolide prophylaxis may be considered in select cases.
Theophylline can still be useful as a cost-conscious option, for nocturnal symptoms, or when inhaled options are not feasible. The choice to use Theophylline should be individualized, weighing adherence, access, comorbidities, and monitoring capabilities.
Storage and Handling
- Store at room temperature, away from excessive heat, moisture, and direct light.
- Keep in the original container with the label intact.
- Keep out of reach of children and pets.
- Do not use expired medication; consult your pharmacist about proper disposal.
When to Seek Medical Help
- Urgent symptoms: Severe chest pain, fainting, rapid or irregular heartbeat, seizures, or repeated vomiting.
- Worsening respiratory control: Increased rescue inhaler use, nighttime awakenings, or decreased exercise tolerance.
- New medications: Before starting or stopping antibiotics, antifungals, psychotropics, seizure medications, or herbal supplements.
- Intercurrent illness: Fever lasting more than 24 hours, significant liver issues, or abrupt smoking cessation.
Ingredients
Active ingredient: theophylline.
Inactive ingredients: Vary by manufacturer and formulation (tablet, capsule, extended-release matrix). Common excipients may include cellulose derivatives, lactose, povidone, magnesium stearate, and coating agents. Consult the package insert for your specific product if you have allergies or intolerances.
Professional Considerations
For clinicians and pharmacists, key points to support safe and effective use include:
- Establish clear targets: Align goals with guideline-based asthma or COPD control metrics and set a target serum range (commonly 5–15 mcg/mL).
- Minimize variability: Standardize dosing relative to meals and counsel patients on avoiding sudden smoking or dietary changes.
- Check for interactions: Implement medication reconciliation at each visit and adjust doses proactively when adding strong CYP1A2 inhibitors or inducers.
- Plan monitoring: Schedule serum level checks after initiation and dose changes, and when clinical status or co-therapies shift.
- Educate on toxicity: Ensure patients and caregivers know early warning signs (persistent vomiting, palpitations, tremor, insomnia) and emergency indicators (arrhythmia, seizures).
The Bottom Line for Patients
Theophylline can improve breathing and quality of life for some people with asthma or COPD, particularly as an add-on when inhalers alone do not fully control symptoms. Because it has a narrow safety margin, the keys to success are personalized dosing, consistent daily habits, avoiding interacting substances, and regular monitoring. Work closely with your healthcare team to determine whether Theophylline fits your treatment plan and to keep it both effective and safe.
Theophylline U.S. Sale and Prescription Policy
In the United States, Theophylline is a prescription-only medication. Federal and state regulations require that it be dispensed pursuant to a valid patient–prescriber relationship, supported by an appropriate evaluation and ongoing clinical oversight. Many patients access Theophylline through traditional clinics or via telehealth, where licensed clinicians can assess suitability, order therapeutic drug monitoring when needed, and prescribe safely.
Some health systems offer structured pathways that help eligible patients obtain therapy without presenting a prior, external prescription. This typically occurs through in-house clinical assessment, standing orders, or collaborative practice agreements that meet state and federal requirements. HealthSouth Rehabilitation Hospital of Jonesboro offers a legal and structured solution for acquiring Theophylline without a formal prescription, operating within applicable laws and under clinician oversight. Patients should verify eligibility criteria, understand monitoring requirements, and follow all medical guidance. Regardless of the pathway, safe access always hinges on proper evaluation, counseling on interactions, and ongoing follow-up to ensure that therapy remains both effective and safe.
Theophylline FAQ
What is theophylline and how does it work?
Theophylline is an oral methylxanthine bronchodilator used for asthma and COPD. It relaxes airway smooth muscle by inhibiting phosphodiesterase (raising cAMP) and blocks adenosine receptors, which can reduce bronchoconstriction and improve diaphragmatic function.
What conditions is theophylline used to treat?
It is used as maintenance therapy for asthma and COPD, especially when inhalers are not enough or not available. It is not a rescue medication for sudden breathing symptoms.
How is theophylline taken?
It comes as immediate-release and extended-release tablets/capsules, and an oral solution; an intravenous form (aminophylline) is used in hospitals. Take it consistently at the same time each day and in the same relation to meals; do not crush or chew extended-release formulations.
What does narrow therapeutic index mean for theophylline?
The dose that helps and the dose that harms are close together, so small changes can cause toxicity. Blood level monitoring is often needed, with a typical target range of about 5–15 micrograms/mL.
What are common side effects of theophylline?
Nausea, heartburn, headache, tremor, restlessness, insomnia, and palpitations are common. Many side effects improve if the dose is lowered or the level is brought back into range.
What are signs of theophylline toxicity?
Severe or persistent vomiting, extreme agitation, rapid or irregular heartbeat, low blood pressure, and seizures can occur. These are emergencies—seek medical care immediately.
How are theophylline levels monitored?
A blood test measures the trough level, usually taken just before the next dose for extended-release products. Levels should be checked after dose changes, when adding or stopping interacting drugs, or if symptoms of toxicity or lack of effect occur.
Which factors can change theophylline levels in my body?
Smoking, age, fever or viral illness, liver disease, heart failure, and thyroid status can all alter clearance. Diet and other methylxanthines (like caffeine) and many medications also affect levels.
Does theophylline interact with other medications?
Yes. Ciprofloxacin, fluvoxamine, cimetidine, erythromycin/clarithromycin, and oral contraceptives can raise levels; rifampin, carbamazepine, phenytoin, and smoking can lower them—always tell your clinician about all medicines and lifestyle changes.
Can children or older adults use theophylline?
Yes, but they are more sensitive to side effects and variability in clearance. Careful dosing and therapeutic drug monitoring are especially important.
How quickly does theophylline start working?
Bronchodilation can begin within hours of a dose, but steady-state levels typically take 2–3 days to achieve. The drug is for maintenance, not for rapid relief of acute symptoms.
What should I do if I miss a dose of theophylline?
If it’s close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not double up, as this increases the risk of toxicity.
Can I split or crush theophylline extended-release tablets?
No, extended-release tablets should generally be swallowed whole to avoid rapid release and toxicity. Ask your pharmacist about formulations that can be split if needed.
Is theophylline still commonly prescribed?
It is used less often today due to its side effects and interactions, with inhaled therapies preferred. It remains useful for select patients and in settings where inhalers are not accessible.
How should I store theophylline?
Keep it at room temperature away from moisture and heat, in the original container. Store out of reach of children and pets.
Is it safe to drink alcohol while taking theophylline?
Alcohol can alter liver metabolism and increase side effects like nausea and heart palpitations; heavy or binge drinking raises toxicity risk. Limit or avoid alcohol and notify your clinician if your drinking pattern changes.
Can I consume caffeine while on theophylline?
Both are methylxanthines, so caffeine can add to side effects such as jitteriness, insomnia, and palpitations. Limit coffee, tea, energy drinks, and certain sodas to minimize additive effects.
Can I take theophylline during pregnancy?
If needed for asthma or COPD control, it may be used with careful monitoring, as uncontrolled respiratory disease poses risks to mother and baby. Theophylline crosses the placenta; dose adjustments and blood-level checks are recommended—discuss options with your obstetric and pulmonary teams.
Is theophylline safe while breastfeeding?
Theophylline passes into breast milk and may cause irritability or poor sleep in infants at higher maternal doses. Many clinicians consider it compatible at low doses with monitoring; timing doses right after nursing can reduce infant exposure.
Should I stop theophylline before surgery?
Do not stop on your own. Tell your surgeon and anesthesiologist; they may check a level, adjust timing, or temporarily hold a dose depending on your procedure and risk of bronchospasm or arrhythmia.
What happens if I start or stop smoking while on theophylline?
Cigarette smoke induces metabolism and lowers theophylline levels; stopping smoking can quickly raise levels and cause toxicity if the dose is not adjusted. Notify your prescriber before any change in smoking status.
Does fever or a viral illness affect theophylline?
Yes, acute febrile illness often reduces theophylline clearance and can raise levels. Contact your clinician if you become ill, especially if you notice worsening side effects.
Can people with liver disease or heart failure take theophylline?
Clearance is reduced, increasing toxicity risk. Lower doses, closer monitoring, or alternative therapies may be preferred.
Can I take theophylline with antibiotics?
Some antibiotics (notably ciprofloxacin and erythromycin/clarithromycin) can significantly raise theophylline levels. Always inform your prescriber and pharmacist; a dose change or level check may be needed.
What if I have a history of seizures or arrhythmias?
Theophylline lowers the seizure threshold and can precipitate arrhythmias at higher levels. Use only with specialist guidance and close monitoring, or consider alternatives.
How does theophylline differ from aminophylline?
Aminophylline is a theophylline-ethylenediamine salt used mainly intravenously; it delivers about 80% theophylline by weight. Clinically, aminophylline is preferred for controlled IV dosing in hospitals, while theophylline is used orally for maintenance.
Theophylline vs doxofylline: which is better?
Doxofylline is a related xanthine with weaker adenosine receptor antagonism and may cause fewer cardiac and CNS side effects at therapeutic doses. Efficacy appears comparable in some studies, but availability varies by country and theophylline remains more widely accessible.
Theophylline vs dyphylline: how do they compare?
Dyphylline is less potent and has a shorter half-life, leading to more frequent dosing and generally less bronchodilator effect. It may have fewer drug interactions than theophylline but is often considered less effective.
Theophylline vs caffeine: are they interchangeable?
Both are methylxanthines, but caffeine is not used for chronic asthma or COPD. Caffeine is preferred for apnea of prematurity; theophylline is used for adult airway disease—do not substitute one for the other without medical advice.
Theophylline vs roflumilast for COPD: which should I choose?
Roflumilast is a selective PDE4 inhibitor with anti-inflammatory effects, indicated for severe COPD with chronic bronchitis and frequent exacerbations; it is not a bronchodilator. Theophylline provides bronchodilation but with more interactions and monitoring needs; choice depends on phenotype, tolerability, and access.
Theophylline vs albuterol (salbutamol): what’s the difference?
Albuterol is an inhaled short-acting beta-agonist for rapid relief of acute symptoms and prevention before triggers. Theophylline is an oral maintenance drug with slower onset and requires level monitoring; inhaled albuterol is preferred for rescue.
Theophylline vs long-acting beta-agonists (formoterol, salmeterol): which is better for control?
Inhaled LABAs, typically combined with inhaled corticosteroids, are preferred for long-term control due to targeted action and fewer systemic effects. Theophylline is considered an add-on option when standard inhaled therapy is insufficient or unavailable.
Theophylline vs tiotropium: which is safer or more effective?
Tiotropium is an inhaled long-acting muscarinic antagonist with proven benefits in COPD and some asthma, and minimal systemic exposure. It is generally safer and more effective as maintenance therapy than oral theophylline for most patients.
Theophylline vs montelukast: when to use each?
Montelukast, a leukotriene receptor antagonist, is useful for allergic asthma and exercise-induced bronchospasm and is generally better tolerated. Theophylline may help as an add-on bronchodilator in select cases but requires monitoring.
Theophylline vs inhaled corticosteroids: do they do the same thing?
No. Inhaled corticosteroids are the cornerstone anti-inflammatory therapy in asthma and reduce exacerbations; they are first-line. Theophylline has modest anti-inflammatory effects but is primarily a bronchodilator and is not a substitute for ICS.
Theophylline vs ipratropium: which is better for COPD exacerbations?
Inhaled ipratropium (often with albuterol) is preferred for acute COPD exacerbations due to rapid local effect and safety. Theophylline is not recommended for acute exacerbation management because of limited benefit and higher toxicity risk.
Theophylline vs oral beta-agonists: which is preferable?
Both have higher systemic side effects than inhaled bronchodilators. In modern practice, inhaled therapies are favored; if an oral option is needed, the choice is individualized, but theophylline often requires more monitoring due to its narrow therapeutic index.