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Bronchodilator Pregnancy: It is not known whether theophyllines can cause foetal harm; safe use in pregnancy has not been established, though theophyllines have been used in pregnancy without teratogenicity or other adverse foetal effect and their safety when clearly needed is generally not seriously questioned because of the risk of uncontrolled asthma. Aminophylline should only be used during pregnancy if considered essential by the physician. Theophylline crosses the placenta. Breast-feeding: theophylline is distributed into milk and may occasionally induce irritability or other signs of toxicity in nursing infants - should not be used if the mother is breast-feeding her infant.

Aminophylline

Brand names: Phyllocontin

Aminophylline is a soluble salt of theophylline used as a bronchodilator in acute severe asthma and chronic obstructive pulmonary disease.

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: Patients NOT currently receiving theophylline preparations - loading dose: 250-500 mg (5 mg/kg) aminophylline by slow intravenous injection, administered at a rate not exceeding 25 mg aminophylline per minute. Maintenance infusion, otherwise healthy non-smoking adults: 0.5 mg/kg/hour.
Route: Intravenous - slow intravenous injection or intravenous infusion in glucose injection or sodium chloride injection
Frequency: Loading dose given once, administered slowly (rate not exceeding 25 mg aminophylline per minute), followed by a continuous intravenous maintenance infusion expressed in mg/kg/hour
Max: Intravenous administration must not exceed a rate of 25 mg aminophylline per minute. Therapeutic serum theophylline concentrations are considered to range from 10 to 20 micrograms/ml; levels greater than 20 micrograms/ml are often associated with toxic effects. A range of 5 to 15 micrograms/ml may be effective and associated with fewer adverse effects.
Narrow therapeutic index - cautious dosage determination is essential; titrate for each individual, monitor serum theophylline levels and watch for signs of toxicity. Approximate IV aminophylline maintenance doses from the SPC table: children 6 months to 9 years 1 mg/kg/hour; children 10-16 years of age and young adult smokers 0.8 mg/kg/hour; otherwise healthy non-smoking adults 0.5 mg/kg/hour; elderly patients 0.3 mg/kg/hour. If patients experience acute adverse effects while loading doses are being infused, the infusion may be stopped for 5-10 minutes or administered at a slower rate. In patients ALREADY receiving theophylline preparations: determine the time, route, dosage form and dose of the last dose where possible; loading doses are based on the expectation that 0.5 mg/kg (lean body weight) of theophylline will result in a 1 microgram/ml increase in serum theophylline concentration; the loading dose should be deferred until a serum theophylline concentration can be attained, or the clinician must carefully select a dose based on potential benefits and risks - the maintenance doses above may then be considered. Administer cautiously to patients over 55 years of age. Serum potassium must be monitored during regular therapy, especially with beta-2 agonists, corticosteroids or diuretics, or in the presence of hypoxia. Smokers have a shorter theophylline half-life and may require larger doses. US labelling (DailyMed, cross-check only - not the UK SPC) expresses doses as theophylline with aminophylline equivalents, e.g. a loading dose of 4.6 mg/kg theophylline (5.7 mg/kg as aminophylline) over 30 minutes and a non-smoking adult infusion of 0.4 mg/kg/hr theophylline (0.5 mg/kg/hr as aminophylline); do not mix the two labelling conventions.

Paediatric dose

Dose: 1 mg/kg
Route: Intravenous infusion
Frequency: per hour (continuous intravenous maintenance infusion) - i.e. 1 mg/kg/hour, for children 6 months to 9 years of age
Max: Intravenous administration must not exceed a rate of 25 mg aminophylline per minute; therapeutic serum theophylline 10-20 micrograms/ml, levels above 20 micrograms/ml often associated with toxic effects
SPC section 4.2 maintenance table: children 6 months to 9 years 1 mg/kg/hour; children 10-16 years of age (and young adult smokers) 0.8 mg/kg/hour. The use of aminophylline IV in children under 6 months of age is NOT recommended - elimination of theophylline in children younger than 6 months, especially neonates, appears to be reduced (also listed under section 4.3). The SPC does not give an age-separated loading dose; the loading dose stated for patients not already on theophylline is 250-500 mg (5 mg/kg) at a rate not exceeding 25 mg/minute. Children are particularly susceptible to the effects of theophylline and care is required; seizures have been reported in children with theophylline plasma levels within the accepted therapeutic range (section 4.4). Verify all paediatric dosing against a children's formulary and local guidance before administration.

Dose adjustments

Renal

No numeric dose adjustment is stated. Section 4.4 advises that aminophylline should be given with caution to patients with cardiac failure, chronic obstructive pulmonary disease, renal or hepatic dysfunction and in chronic alcoholism, since clearance of aminophylline is decreased.

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

SPC section 4.2 maintenance table: children 6 months to 9 years 1 mg/kg/hour; children 10-16 years of age (and young adult smokers) 0.8 mg/kg/hour. The use of aminophylline IV in children under 6 months of age is NOT recommended - elimination of theophylline in children younger than 6 months, especially neonates, appears to be reduced (also listed under section 4.3). The SPC does not give an age-separated loading dose; the loading dose stated for patients not already on theophylline is 250-500 mg (5 mg/kg) at a rate not exceeding 25 mg/minute. Children are particularly susceptible to the effects of theophylline and care is required; seizures have been reported in children with theophylline plasma levels within the accepted therapeutic range (section 4.4). Verify all paediatric dosing against a children's formulary and local guidance before administration.

Verify in a children's formulary

Contraindications

  • Hypersensitivity to ethylenediamine, or allergy to the theophyllines, caffeine or theobromine, or to any of the excipients listed in section 6.1
  • Must not be administered concomitantly with other xanthine drugs - simultaneous administration of aminophylline and/or theophylline by more than one route or in more than one preparation increases the hazard of serious toxicity
  • Acute porphyria
  • Use of aminophylline IV in children under 6 months of age is not recommended

Side effects

  • Cardiac: palpitations, tachycardia, cardiac arrhythmias, hypotension - hypotension, arrhythmias and convulsions may follow intravenous injection, particularly if the injection is too rapid, and sudden deaths have been reported
  • Gastrointestinal: nausea, vomiting, abdominal pain, diarrhoea, gastro-oesophageal reflux, gastrointestinal bleeding
  • Nervous system: headache, confusion, restlessness, hyperventilation, vertigo/dizziness, tremor; higher doses may lead to maniacal behaviour, delirium and convulsions
  • Metabolic: hypokalaemia, hypophosphataemia, hyponatraemia
  • Psychiatric: insomnia, anxiety. Skin: rash, maculo-papular rash, erythema, pruritus, urticaria, exfoliative dermatitis. Hypersensitivity reactions may occur

Interactions

  • Fluvoxamine - increases plasma theophylline; concomitant use should usually be avoided, and where not possible the theophylline dose should be halved and plasma theophylline monitored closely
  • Cimetidine; macrolide antibiotics (e.g. erythromycin, clarithromycin); quinolone antibiotics (e.g. ciprofloxacin, norfloxacin); fluconazole; isoniazid - may increase plasma theophylline concentrations
  • Propranolol; calcium channel blockers, diltiazem, verapamil; mexiletine, propafenone - may increase plasma theophylline concentrations
  • High-dose allopurinol (e.g. 600 mg daily); oral contraceptives; disulfiram; interferon alfa and influenza vaccine; methotrexate; zafirlukast; tacrine; thiabendazole; thyroid hormones - may increase plasma theophylline concentrations
  • Other xanthine medicines must not be given concurrently. The section 4.5 list of drugs that DECREASE plasma theophylline was truncated at the source-fetch limit and is not reproduced here - check the SPC.

Clinical monograph

How it works

It is a methylxanthine that inhibits phosphodiesterase and antagonises adenosine receptors, relaxing bronchial smooth muscle and enhancing respiratory function.

Prescribing in practice

  • It has a narrow therapeutic index with a risk of arrhythmias and convulsions, and serum theophylline concentrations must guide dosing.
  • Numerous drug interactions and factors such as smoking, heart failure and hepatic impairment markedly alter clearance.
  • Loading regimens differ in patients already taking oral theophylline, so prior therapy must be established before intravenous loading.

Monitoring

Monitor serum theophylline concentrations, heart rate and rhythm, and serum potassium, particularly during intravenous use.

Counselling the patient

  • Report palpitations, persistent vomiting, tremor or seizures promptly.
  • Tell clinicians if your smoking habits change as this alters how the drug is handled.
  • Do not change brands or formulations without advice.

Evidence & guidelines

Therapeutic drug monitoring of theophylline is well established owing to its narrow margin between effective and toxic concentrations.

Reference: BTS/SIGN Asthma 2023; NICE; 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.