Theophylline

Oral
Intravenous
Class
Bronchodilators
Subclass
Nonselective phosphodiesterase inhibitors
Substance name
Theophylline, 1, 3-dimethylxanthine
Brand names
Elixophyllin®, Uniphyl®
Common formulations
Elixir, Oral solution, Tablet
See also
Theophylline ER (Theo-24®)
Dosage and administration
Adults patients
Symptomatic relief
Reversible airway obstruction in patients with asthma
•
Loading: 5 mg/kg PO × 1 in a patient who has not received any theophylline in the previous 24 hours
•
Subsequently: 300 mg PO daily, in 3-4 divided doses, for 3 days
•
Maintenance: 400-600 mg PO daily, in 3-4 divided doses
Taken with meals.
Reversible airway obstruction in patients with COPD
•
Loading: 5 mg/kg PO × 1 in a patient who has not received any theophylline in the previous 24 hours
•
Subsequently: 300 mg PO daily, in 3-4 divided doses, for 3 days
•
Maintenance: 400-600 mg PO daily, in 3-4 divided doses
Taken with meals.
Treatment
Bradycardia in patients with SND
•
200-400 mg PO daily, in divided doses
Bradycardia in patients with spinal cord injury • Off-label
•
5-10 mg/kg PO daily, in divided doses, titrated to effect
Bradycardia, after heart transplantation • Off-label
•
Loading: 300 mg IV once
•
Subsequently: 5-10 mg/kg PO daily, in divided doses, titrated to a therapeutic serum level of 10-20 mcg/mL
Central sleep apnea in patients with HF • Off-label
•
200-300 mg PO daily, in 3-4 divided doses
Central sleep apnea in patients with high-altitude periodic breathing • Off-label
•
250 mg PO BID
Indications for use
Labeled indications
Adults
•
Symptomatic relief of reversible airway obstruction in patients with asthma
•
Symptomatic relief of reversible airway obstruction in patients with COPD
•
Treatment of bradycardia in patients with SND
Off-label indications
Adults
•
Treatment of bradycardia in patients with spinal cord injury
•
Treatment of bradycardia, after heart transplantation
•
Treatment of central sleep apnea in patients with HF
•
Treatment of central sleep apnea in patients with high-altitude periodic breathing
Safety risks
Contraindications
Hypersensitivity to theophylline or its components
Warnings and precautions
Exacerbation of cardiac arrhythmias
•
Use extreme caution in patients with cardiac arrhythmias (not including bradyarrhythmias).
Exacerbation of peptic ulcer disease
•
Use extreme caution in patients with active peptic ulcer disease.
Increased theophylline levels
•
Use caution in patients with acute pulmonary edema, congestive HF, cor pulmonale, high and/or prolonged fever, hypothyroidism, liver disease, renal impairment, sepsis with multi-organ failure, shock, or cessation of smoking, as well as in the elderly.
Seizure
•
Use extreme caution in patients with seizure disorders.
Specific populations
Renal impairment
eGFR ≥ 15 mL/min/1.73 m²
•
Use acceptable. No dose adjustment required.
eGFR < 15 mL/min/1.73 m²
•
Use with caution. Monitor serum concentrations.
Renal replacement therapy
Continuous renal replacement
•
Use acceptable. No dose adjustment required.
Intermittent hemodialysis
•
Use with caution. Administer the dose after dialysis session.
Peritoneal dialysis
•
Use with caution.
Hepatic impairment
Any severity
•
Use with caution. Reduce dose. Monitor serum concentrations.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: A
•
Generally acceptable for use. Evidence of fetal harm in animals. The 2020 ERS/TSANZ task force statement suggests that theophylline is compatible with pregnancy.
Breastfeeding
Acceptable for use during breastfeeding.
•
The 2020 ERS/TSANZ task force statement suggests that theophylline is compatible with breastfeeding.
Low excretion in breastmilk (5-25%).
Unknown drug levels in breastfed infants.
May potentially cause adverse effects in breastfed infants.
Adverse reactions
Unknown frequency
•
Peptic ulcer disease, intracranial hemorrhage, tachycardia, ↑ urine free cortisol, ↑ blood glucose, ↑ serum total cholesterol, ↓ serum free T3, ↑ serum uric acid, diarrhea, nausea, vomiting, dizziness, headache, insomnia, seizure, tremor, stuttering, irritability, restlessness, fever
Interactions
Drug(s)
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