Theophylline(thee off ’ i lin)
Elixir: Elixophyllin
Timed-release capsules: Theo-24DNC
Timed-release tablets: TheochronDNC
PREGNANCY CATEGORY C
Drug Classes
Bronchodilator
Xanthine
Therapeutic Actions
Relaxes bronchial smooth muscle, causing bronchodilation and increasing vital capacity that has been impaired by bronchospasm and air trapping; actions may be mediated by inhibition of phosphodiesterase, which increases the concentration of cyclic adenosine monophosphate; in concentrations that may be higher than those reached clinically, it also inhibits the release of slow-reacting substance of anaphylaxis and histamine.
Indications
Symptomatic relief or prevention of bronchial asthma and reversible bronchospasm associated with chronic bronchitis and emphysema
Unlabeled use of 5 mg/kg loading dose, then 3–6 mg/kg/day in divided doses every 6 to 8 hr to maintain serum concentrations between 3 and 5 mcg/mL: Treatment of apnea and bradycardia of prematurity
Contraindications and Cautions
Contraindicated with hypersensitivity to any xanthines, peptic ulcer, active gastritis, pregnancy, underlying seizure disorders (unless receiving appropriate antiepileptic).
Use cautiously with cardiac arrhythmias, acute myocardial injury, HF, cor pulmonale, severe hypertension, severe hypoxemia, renal or hepatic disease, hyperthyroidism, alcoholism, labor (may inhibit uterine contractions), lactation, status asthmaticus.
Available Forms
CR tabletsDNC—100, 200, 300, 450, 600 mg; ER capsulesDNC—100, 200, 300, 400 mg; elixir—80 mg/15 mL; injection—0.8, 1.6, 3.2 mg/mL
Dosages
Maintain serum levels in the therapeutic range of 5–15 mcg/mL; base dosage on lean body mass.
Anhydrous Theophylline Content in Theophylline Derivatives (these products are more water soluble than anhydrous theophylline)
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Adults and children weighing more than 45 kg without risk of impaired excretion
Elixophyllin: Initially, 300 mg/day PO in divided doses every 6–8 hr. After 3 days, may be increased to 400 mg/day PO in divided doses every 6–8 hr. After 3 more days may be increased to 600 mg/day PO in divided doses every 6–8 hr if tolerated and needed.
ER capsule: Initially, 300 mg/day PO in divided doses every 8–12 hr. After 3 days, may be increased to 400 mg/day PO in divided doses every 8–12 hr. After 3 more days, may be increased to 600 mg/day PO in divided doses every 8–12 hr if tolerated and needed.
Theo-24: Initially, 300–400 mg/day PO once every 24 hr. After 3 days, may be increased to 400–600 mg/day PO once every 24 hr. After 3 more days, may be increased based on theophylline level to stay within safe range.
Adults and children with risk factors for impaired clearance, geriatric patients, patients for whom monitoring serum theophylline levels is not feasible
Elixophyllin: Children 1–15 yr: Final dose should not exceed 16 mg/kg/day PO up to a maximum 400 mg/day. Patients 16 yr and older and geriatric patients: Final dose should not exceed 400 mg/day PO.
Theo-24: Children 12–15 yr: Final dose should not exceed 16 mg/kg/day PO up to a maximum 400 mg/day. Patients older than 16 yr and geriatric patients: Final dose should not exceed 400 mg/day PO.
Serum theophylline level 5–10 mcg/mL: Increase dose by about 25% at 3-day intervals until desired response or serum level occurs.
Serum theophylline level 10–14.9 mcg/mL: Maintain dosage; recheck at 6- to 12-mo intervals.
Serum theophylline level 15–19.9 mcg/mL: Consider a decrease in dose by 10% to provide a greater margin of safety.
Serum theophylline level 20–25 mcg/mL: Decrease dose by about 25%; recheck level in 3 days.
Serum theophylline level 25–30 mcg/mL: Skip next dose, and decrease subsequent doses by 25%; recheck level after 3 days.
Serum theophylline level greater than 30 mcg/mL: Skip next two doses and decrease later doses by 50%. Recheck level after 3 days.
Measurement of serum theophylline levels during chronic therapy: Measure serum theophylline in blood sample drawn 1–2 hr after administration of immediate-release preparations, 5–9 hr after administration of most timed-release products.
Adults
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