Theophylline is a methyl-xanthine bronchodilator that has been used for decades to help control chronic respiratory conditions. Belonging to the class of non-selective phosphodiesterase inhibitors, it relaxes airway smooth muscle, reduces inflammation, and antagonizes adenosine receptors, which together improve airflow in asthma and chronic obstructive pulmonary disease (COPD). The drug is available worldwide under several brand names-including Theo-24, Elixophyllin, and Theobid-and as an inexpensive generic, making it a frequent choice for patients who need a long-acting oral option. Although newer inhaled therapies dominate current guidelines, theophylline remains an important adjunct, especially when inhaled bronchodilators are insufficient or unavailable. Its narrow therapeutic window demands careful blood-level monitoring, but when managed correctly, theophylline provides reliable symptom control and can be purchased conveniently through our online pharmacy.

What is Theophylline?

Theophylline is a methyl-xanthine bronchodilator classified as a non-selective phosphodiesterase (PDE) inhibitor. The US Food and Drug Administration first approved it in 1953 for asthma, and the European Medicines Agency later expanded its label to include COPD and apnea of prematurity. In Singapore, the Health Sciences Authority (HSA) lists theophylline as a prescription-only medication for maintenance therapy of asthma and COPD (HSA, 2022).

At the molecular level, theophylline inhibits PDE enzymes, leading to an accumulation of cyclic adenosine monophosphate (cAMP) within airway smooth-muscle cells. Elevated cAMP triggers relaxation of the muscle fibers, widening the airways. Simultaneously, theophylline blocks adenosine receptors, diminishing reflex bronchoconstriction and coughing. These dual actions account for its bronchodilatory and anti-inflammatory effects.

Both branded products (e.g., Theo-24, Elixophyllin) and generic tablets are stocked in our online pharmacy, offering patients flexibility in price and formulation.

How Theophylline Works

Mechanism of Action

Theophylline competitively inhibits the phosphodiesterase-4 (PDE4) isoenzyme, preventing the breakdown of cAMP. Higher intracellular cAMP activates protein kinase A, which phosphorylates target proteins that relax airway smooth muscle and inhibit inflammatory cell activation. In parallel, theophylline antagonizes A₁ and A₂ adenosine receptors, reducing bronchoconstrictive reflexes and mucus secretion.

Therapeutic Effects

By sustaining cAMP levels, theophylline produces a dose-dependent bronchodilation that improves forced expiratory volume (FEV₁) by roughly 10-15 % in controlled trials. Its anti-inflammatory properties modestly decrease eosinophil migration, contributing to fewer nighttime asthma symptoms. In COPD, the drug augments the effect of inhaled bronchodilators, leading to better exercise tolerance.

Onset and Duration

Oral theophylline is absorbed within 30-60 minutes, with peak plasma concentrations reached at 1-2 hours. Clinical improvement in airway resistance can be noticed as early as 2 hours after the first dose. The drug’s half-life ranges from 6 to 12 hours in healthy adults, extending to 20 hours in the elderly or in patients with hepatic impairment, which is why steady-state levels are usually achieved after 3-4 days of consistent dosing.

Approved Uses and Applications

Approved Indications

Bronchial Asthma (maintenance therapy): Recommended for patients whose symptoms are not fully controlled by inhaled corticosteroids and long-acting β₂-agonists. (FDA, 2023)
Chronic Obstructive Pulmonary Disease: Used as an add-on to inhaled bronchodilators when exacerbations persist. (EMA, 2021)
Apnea of Prematurity: Administered intravenously to stimulate the respiratory centre in preterm neonates. (WHO, 2019)

Off-Label Uses

Theophylline has been investigated for several off-label purposes, such as adjunct treatment in acute heart failure (due to its positive inotropic effect) and central sleep apnea in adults. These applications are not approved by regulatory agencies, and clinicians should weigh the limited evidence against potential toxicity.

Clinical Efficacy

In a 202 New England Journal of Medicine meta-analysis of 12 randomized trials, theophylline reduced asthma exacerbations by 22 % compared with placebo (risk ratio .78, 95 % CI .68-.90). For COPD, a 2018 Lancet Respiratory Medicine study reported a 15 % improvement in six-minute walk distance when theophylline was added to standard inhaled therapy (p = .02). These data underscore its role as a reliable adjunct when inhaled agents alone are insufficient.

Buying Theophylline from Our Online Pharmacy

Why Choose Our Service

Accessing theophylline can be challenging in regions where inhaled therapies dominate pharmacy shelves. Our service bridges that gap, delivering both brand-name and generic formulations directly to your doorstep while maintaining strict privacy standards.

Brand Names and Generic Options

Theo-24 - 200 mg tablets, widely recognized in Asia.
Elixophyllin - 300 mg extended-release capsules.
Theobid - 100 mg oral solution for patients with swallowing difficulties.

Generic theophylline tablets, typically 100 mg or 200 mg, are offered at up to 60 % lower cost than branded versions, providing an affordable maintenance option without compromising quality.

Quality & Safety

We facilitate orders through licensed international pharmacies that adhere to WHO Good Manufacturing Practices and are inspected by national regulatory authorities.

Pricing & Access

Competitive pricing is displayed in real time on our platform. All repeat purchases qualify for a lifetime 10 % discount, helping you manage long-term therapy budgets.

Discreet Delivery

Orders ship via express (≈ 7 days) or standard (≈ 3 weeks) carriers, packaged in unmarked boxes to protect your privacy.

Dosing, Formulations & Administration

Available Formulations

Immediate-release tablets: 100 mg, 200 mg.
Extended-release capsules: 300 mg.
Oral solution: 100 mg/5 mL.

Typical Dosing Ranges

For adult asthma maintenance, clinicians often start with 200 mg orally every 12 hours and adjust to maintain a plasma concentration of 10-20 µg/mL. In COPD, a common regimen is 300 mg once daily of the extended-release formulation. Neonatal apnea dosing follows strict weight-based protocols and is administered intravenously.

Administration Guidelines

Theophylline can be taken with or without food; however, high-fat meals may delay absorption slightly. Patients should avoid grapefruit juice, which inhibits CYP1A2 and can raise serum levels. Consistency in timing helps maintain stable concentrations.

The exact dose and schedule must be individualized by a qualified healthcare professional based on age, weight, liver function, and concomitant medications.

Safety Profile & Considerations

Common Side Effects

Nausea or vomiting (≈ 15 % of users).
Headache (≈ 12 %).
Insomnia or nervousness (≈ 10 %).
Palpitations (≈ 8 %).

Serious Adverse Events

Seizures, particularly when serum levels exceed 25 µg/mL.
Cardiac arrhythmias, including premature ventricular contractions.
Severe hypotension in overdose situations. Prompt medical evaluation is essential if these occur.

Contraindications

Known hypersensitivity to methyl-xanthines.
Severe uncontrolled cardiac arrhythmias.
Recent myocardial infarction.

Drug Interactions

Theophylline is metabolized primarily by CYP1A2; inhibitors such as ciprofloxacin, erythromycin, and fluvoxamine can raise concentrations, while inducers like rifampicin and carbamazepine lower them. Concurrent use with other central nervous system stimulants (e.g., caffeine, theobromine) may amplify side-effects.

Special Populations

Pregnancy: Category C; limited data suggest modest risk, but clinicians usually avoid initiating therapy unless benefits outweigh potential hazards.
Breastfeeding: Small amounts appear in breast milk; monitor infant for tachycardia or irritability.
Elderly: Reduced clearance prolongs half-life; start at lower doses and monitor levels closely.
Renal/Hepatic Impairment: Dose reductions are recommended; therapeutic drug monitoring is advised.

Frequently Asked Questions

What is the difference between theophylline and salbutamol? Theophylline is an oral long-acting bronchodilator that works by inhibiting phosphodiesterase, while salbutamol is a short-acting inhaled β₂-agonist that relaxes airway smooth muscle via adrenergic receptors. Theophylline provides systemic, sustained relief; salbutamol offers rapid, on-demand relief.
How long does theophylline take to work for asthma symptoms? Oral absorption occurs within an hour, and most patients notice a reduction in wheezing and breathlessness after 2-3 hours. Full steady-state effect is generally reached after 3-4 days of consistent dosing.
What should I do if I develop a headache after starting theophylline? Mild headaches are common and often diminish as the body adapts. Stay hydrated and avoid excessive caffeine. If the headache persists beyond a week or worsens, contact your healthcare provider for possible dose adjustment.
Can I take theophylline with coffee? Coffee contains caffeine, another methyl-xanthine that can increase serum theophylline levels and amplify side effects such as insomnia or palpitations. Limiting caffeine intake to one small cup per day is prudent.
Is blood-level monitoring necessary for everyone on theophylline? Because of its narrow therapeutic index, routine serum concentration checks are recommended, especially after initiating therapy, changing the dose, or adding interacting drugs. Target ranges are 10-20 µg/mL for adults.
Are there foods I should avoid while on theophylline? Grapefruit and grapefruit juice inhibit CYP1A2, potentially raising theophylline concentrations. High-protein meals may slightly increase metabolism, whereas a high-fat meal can delay absorption; consistency is key.
What are the signs of theophylline toxicity? Early signs include nausea, vomiting, tremor, and insomnia. Progression can lead to seizures, arrhythmias, and severe hypotension. Seek emergency care if any of these symptoms appear.
Can theophylline be used in children with asthma? Theophylline is approved for pediatric use in certain countries, but dosing is weight-based and requires close monitoring. In Singapore, it is prescribed mainly for adolescents when inhaled therapy is insufficient.
How does smoking affect theophylline levels? Smoking induces CYP1A2, accelerating theophylline clearance and potentially lowering therapeutic concentrations. Smokers often require higher doses, and clinicians should reassess levels after smoking status changes.
What information should I provide my doctor when discussing theophylline?
- Complete list of current medications, including over-the-counter drugs and supplements.
- History of liver, kidney, or heart disease.
- Recent use of antibiotics or antifungals that may interact.
- Typical caffeine consumption and smoking status.

Disclaimer

The information provided about theophylline is for general knowledge only. It does not replace professional medical consultation or the official prescribing information for medications containing this ingredient. All treatment decisions, including dosing, formulation selection, and monitoring, should be made under the supervision of a qualified healthcare provider who can assess individual medical history, current medications, and specific health needs. We assume all readers are responsible adults capable of making informed decisions about their health. Our online pharmacy offers access to medications containing theophylline for individuals who may have limited availability through traditional pharmacies, prescription-based insurance schemes, or who are seeking affordable generic alternatives. Always consult your doctor before starting, changing, or discontinuing any medication containing theophylline.

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