theophylline

theophylline is evaluated for the following indications with varying evidence strength: Chronic asthma (evidence tier B), Chronic obstructive pulmonary disease (evidence tier B), Apnea of prematurity (evidence tier F). See the full indication matrix with dosing and citations above on this page.

Common side effects of theophylline (≥ 1 in 100): Nausea, vomiting, abdominal pain, Headache, insomnia, anxiety, Tachycardia, Tremor, Increased urination. See the Safety section for uncommon and serious reactions.

FDA category C. FDA category C. Used in pregnancy for asthma when inhaled therapy is insufficient. Theophylline clearance changes by trimester: in the second and third trimesters it falls, dose reduction and more frequent serum monitoring are required. Newborns of mothers on theophylline in the third trimester may have irritability, tachycardia, tremor, and vomiting.

Theophylline passes into breast milk at about 70 percent of maternal plasma concentration. Infant irritability, poor sleep, and tremor are possible. LactMed lists it as conditionally compatible with breastfeeding; newborns and preterm infants require monitoring. Nursing is best timed just before the next maternal dose.

theophylline is contraindicated in: Allergy to theophylline or other methylxanthines; Acute porphyria; History of hemorrhagic stroke; Retinal hemorrhage; Poorly controlled epilepsy (seizure risk at toxic concentrations). Full list in the Safety section.

theophylline is produced synthetically; the natural methylxanthine underlies caffeine. Theophylline has one of the narrowest therapeutic windows in current pharmacology – a 2–3-fold gap between therapeutic and toxic concentrations.

aminophylline (ethylenediamine salt of theophylline) is theophylline. All safety rules apply. In acute severe asthma, aminophylline offers no advantage over high-dose inhaled therapy and systemic corticosteroids; international guidelines have removed it from the standard of care.

caffeine is another methylxanthine, effects are additive. In patients on theophylline, intake above 200 mg of caffeine daily worsens tachycardia, tremor, and insomnia. Caffeine is limited to 100 mg/day.