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Methylxanthine Bronchodilator Pregnancy: Theophylline should not be administered during pregnancy unless clearly necessary; neonatal irritability and apnoea have been reported and teratogenic effects have been seen in animals. It is secreted in breast milk and may cause irritability in the infant, so should only be given to breastfeeding women when the anticipated benefits outweigh the risk.

Theophylline (Oral Modified Release)

Brand names: Uniphyllin, Slo-Phyllin, Nuelin SA

Theophylline is an oral xanthine bronchodilator used as add-on therapy in asthma and COPD when other treatments are insufficient.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 200 mg, titrated to 300 mg or 400 mg depending on therapeutic response
Route: Oral (prolonged-release tablets - must be swallowed whole and not broken, crushed or chewed)
Frequency: Every 12 hours (twice daily)
Usual maintenance dose for adults and the elderly. Patients vary in their response to xanthines and it may be necessary to titrate the dose individually; it may be appropriate to give a larger evening or morning dose to cover the period of worst symptoms (e.g. the morning dip in lung function). Plasma theophylline concentrations should ideally be maintained between 10 and 20 micrograms/ml, although 5 to 15 micrograms/ml may be effective; adverse effects can occur within the 10-20 micrograms/ml range and significant adverse reactions are usually seen above 20 micrograms/ml. Monitor plasma concentrations when higher doses are prescribed, when co-morbidities impair clearance, or when co-administered medicines reduce theophylline clearance. Dose reduction and monitoring may be required in the elderly and in cardiac disease/arrhythmias, hepatic disease, exacerbations of lung disease, hypothyroidism, fever, viral infection or risk of hypokalaemia; dose increase may be needed in hyperthyroidism and cystic fibrosis. Dose adjustment may be necessary if smoking is started or stopped during treatment. The SPC notes theophylline may be inappropriate as monotherapy for COPD in elderly patients because of its narrow therapeutic index. Missed dose: if remembered within 4 hours the tablets can be taken straight away and the next dose taken at the normal time. Source product: UNIPHYLLIN 200 mg prolonged release tablets. SPC sections 4.4/4.5 were truncated at the source-fetch limit, so the interaction list below may be incomplete.

Paediatric dose

Dose: 9 mg/kg
Route: Oral (prolonged-release tablets)
Frequency: Twice daily
Max: No numerical maximum is stated for children in this SPC; UNIPHYLLIN tablets must not be used in children below 6 years of age
Usual paediatric maintenance dose for children aged 6 years and above. Some children with chronic asthma require and tolerate much higher doses (10-16 mg/kg twice daily). Clearance is increased in children compared with adults and decreases towards adult values in late teens, so lower (adult-based) dosages may be required for adolescents. Theophylline distributes poorly into body fat, so mg/kg doses should be calculated on lean (ideal) bodyweight. Other dosage forms are available that are more suitable for children under 6 years; theophylline is contraindicated in children under 6 months. Plasma theophylline monitoring applies as for adults. Verify against a children's formulary before prescribing.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Paediatric weight-based calculator

Usual paediatric maintenance dose for children aged 6 years and above. Some children with chronic asthma require and tolerate much higher doses (10-16 mg/kg twice daily). Clearance is increased in children compared with adults and decreases towards adult values in late teens, so lower (adult-based) dosages may be required for adolescents. Theophylline distributes poorly into body fat, so mg/kg doses should be calculated on lean (ideal) bodyweight. Other dosage forms are available that are more suitable for children under 6 years; theophylline is contraindicated in children under 6 months. Plasma theophylline monitoring applies as for adults. Verify against a children's formulary before prescribing.

Verify in a children's formulary

US labelling (FDA)

Reference — US labelling, may differ from UK

DOSAGE AND ADMINISTRATION Theophylline (Anhydrous) Extended-Release Tablets 400 or 600 mg can be taken once a day in the morning or evening. It is recommended that Theophylline (Anhydrous) Extended-Release Tablets be taken with meals. Patients should be advised that if they choose to take Theophylline (Anhydrous) Extended-Release Tablets with food it should be taken consistently with food and if they take it in a fasted condition it should routinely be taken fasted. It is important that the product whenever dosed be dosed consistently with or without food. Theophylline (Anhydrous) Extended-Release Tablets are not to be chewed or crushed because it may lead to a rapid release of theophylline …

Source: US FDA prescribing information (openFDA / DailyMed), label dated 2025-12-04. Accessed 2026-06-12. US dosing and indications can differ from UK practice — use UK sources for prescribing decisions.

Contraindications

  • Hypersensitivity to theophylline and other xanthines or to any of the excipients
  • Patients with porphyria
  • Concomitant administration with ephedrine in children less than 6 years of age (or less than 22 kg)
  • Children under 6 months of age

Side effects

  • Seizures or convulsions
  • Cardiac arrhythmias, sinus tachycardia, atrial tachycardia and palpitations
  • Nausea, vomiting, abdominal pain and gastric irritation / gastro-oesophageal reflux
  • Headache, tremor, dizziness, agitation, anxiety and insomnia
  • Hypokalaemia and hyperuricaemia
  • Urinary retention (elderly males with pre-existing partial urinary tract obstruction) and diuresis

Interactions

  • May increase theophylline plasma concentrations: cimetidine, ciprofloxacin, macrolide antibiotics such as erythromycin, propranolol, isoniazid, oral contraceptives, mexiletine, ranitidine, fluvoxamine
  • Increase theophylline clearance (dose increase may be needed): aminoglutethimide, carbamazepine, isoprenaline, phenytoin, rifampicin, ritonavir, sulphinpyrazone, barbiturates and St John's wort; smoking and alcohol consumption also increase clearance
  • Reduce theophylline clearance (dose reduction may be needed): aciclovir, allopurinol, carbimazole, cimetidine, clarithromycin, diltiazem, disulfiram, erythromycin, fluconazole, interferon, isoniazid, methotrexate, mexiletine, nizatidine, pentoxifylline, propafenone, propranolol (SPC list truncated at the source-fetch limit)

Clinical monograph

How it works

It causes bronchodilation and has some anti-inflammatory effect (via phosphodiesterase inhibition and adenosine antagonism); the mechanism is not fully defined.

Prescribing in practice

  • It has a narrow therapeutic index — toxicity (nausea, palpitations, arrhythmia, seizures) can occur near therapeutic levels, so monitor plasma levels.
  • Many factors alter its level — smoking and enzyme inducers lower it; macrolides, ciprofloxacin, heart failure and liver disease raise it.
  • Modified-release brands differ and are not interchangeable — prescribe by brand.

Monitoring

Monitor plasma theophylline levels (and at dose or interacting-drug changes) and watch for toxicity.

Counselling the patient

  • Stay on the same brand.
  • Report palpitations, persistent vomiting, or feeling shaky or agitated.
  • Tell your clinician if you start or stop smoking, as it changes how the drug works.

Evidence & guidelines

An add-on bronchodilator in asthma/COPD (NICE NG80/NG115), used with level monitoring because of its narrow margin.

Reference: BTS/SIGN Asthma Guidelines 2019; GOLD COPD 2024; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.