section name header

Indications

REMS

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CNS: SEIZURES, anxiety, headache, insomnia, irritability.

CV: ARRHYTHMIAS, tachycardia, angina, palpitations.

GI: nausea, vomiting, anorexia.

Neuro: tremor.

Interactions

Drug-Drug:

Drug-Natural Products:

Drug-Food:

Availability

(Generic available)

Route/Dosage

see Calculator

Dose should be determined by theophylline serum level monitoring. Loading dose should be or eliminated if theophylline preparation has been used in preceding 24 hr. Aminophylline is 80% theophylline (100 mg aminophylline = 80 mg theophylline). Extended-release (controlled-release, sustained-release) products may be given q 8–24 hr, depending upon the formulation.

US Brand Names

Elixophyllin, Theo-24, Theochron

Action

Therapeutic Effects:

Classifications

Therapeutic Classification: bronchodilators

Pharmacologic Classification: xanthines

Pharmacokinetics

Absorption: Well absorbed from PO dosage forms; absorption from extended-release dosage forms is slow but complete.

Distribution: Widely distributed; crosses the placenta and into breast milk; does not distribute into adipose tissue.

Metabolism/Excretion: 90% metabolized by the liver to several metabolites (including the active metabolites, caffeine, and 3–methylxanthine); metabolites are renally excreted; 10% excreted unchanged by the kidneys.

Half-life: Theophylline — Premature infants: 20–30 hr; Term infants: 11–25 hr; Children 1–4 yr: 3.4 hr; Children 6–17 yr: 3.7 hr; Adults: 9–10 hr ( in patients >60 yr, patients with HF or liver disease; in cigarette smokers).

Canadian Brand Names

Pulmophylline, Theolair, Uniphyl

Time/Action Profile

(bronchodilation)

ROUTEONSET†PEAKDURATION
POrapid1–2 hr6 hr
PO-ERdelayed4–8 hr8–24 hr
IVrapidend of infusion6–8 hr

†Provided that a loading dose has been given and steady-state blood levels exist.

Patient/Family Teaching

Pronunciation

thee-OFF-i-lin audio

Code

NDC Code*