• Long-term control of reversible airway obstruction caused by asthma or COPD.

Contraindicated in:

• Hypersensitivity to aminophylline or theophylline.

Use Cautiously in:

• Cardiac arrhythmias
• HF, liver disease, or hypothyroidism (↓ dose)
• Peptic ulcer disease
• Seizure disorders
• OB: Safety not established in pregnancy
• Lactation: Safety not established in breastfeeding
• Pedi: Dose ↓ required for children <1 yr
• Geri: Dose ↓ required for patients >60 yr.

CV: tachycardia, angina, ARRHYTHMIAS, palpitations.

GI: nausea, vomiting, anorexia.

Neuro: anxiety, headache, insomnia, irritability, SEIZURES, tremor.

Drug-Drug:

• Additive CV and CNS side effects with adrenergics (sympathomimetic).
• May ↓ the therapeutic effect of lithium and phenytoin.
• Smoking, barbiturates, carbamazepine, phenytoin, nevirapine and rifampin may ↑ metabolism and may decrease effectiveness.
• Erythromycin, beta blockers, clarithromycin, calcium channel blockers, cimetidine, hormonal contraceptives, disulfiram, doxycycline, estrogens, fluvoxamine, isoniazid, ketoconazole, mexiletine, nefazodone, protease inhibitors, quinidine, some fluoroquinolones, and large doses of allopurinol↓ metabolism and may lead to toxicity.

Drug-Natural Products:

• Caffeine-containing herbs (cola nut, guarana, mate, tea, coffee) may ↑ levels and risk of CNS and CV side effects.
• ↓levels and effectiveness with St. John’s wort.

Drug-Food:

• Excessive regular intake of charcoal-broiled foods may ↓ effectiveness.

(Generic available)

• Extended-release tablets (12 hr): 300 mg; 450 mg;
• Extended-release tablets (24 hr): 400 mg; 600 mg;
• Extended-release capsules (24 hr): 100 mg; 200 mg; 300 mg; 400 mg;
• Elixir (orange/raspberry, mixed fruit, and other flavors): 80 mg/15 mL;
• Premixed infusion: 400 mg/500 mL D5W;

• PO (Adults Healthy, Nonsmoking): Loading dose: 5 mg/kg, followed by 10 mg/kg/day divided every 8–12 hr (not to exceed 900 mg/day).
• PO (Adults with HF, Cor Pulmonale, or Liver Dysfunction): Loading dose: 5 mg/kg, followed by 5 mg/kg/day divided every 8–12 hr (not to exceed 400 mg/day).
• PO (Children 12–16 yr, Nonsmoking): Loading dose: 5 mg/kg, followed by 13 mg/kg/day divided every 8–12 hr.
• PO (Children 9–12 yr, adolescent and adult smokers <50 yr): Loading dose: 5 mg/kg, followed by 16 mg/kg/day divided every 8–12 hr.
• PO (Children 1–9 yr): Loading dose: 5 mg/kg, followed by 20–24 mg/kg/day divided every 8–12 hr.
• PO (Infants 6 mo–1 yr): Loading dose: 5 mg/kg, followed by 12–18 mg/kg/day divided every 6–8 hr.
• PO (Infants 6 wk–6 mo): Loading dose: 5 mg/kg, followed by 10 mg/kg/day divided every 6–8 hr.
• PO (Neonates up to 6 wk): Loading dose: 4 mg/kg, followed by 4 mg/kg/day divided every 12 hr.
• IV (Adults and Children): See aminophylline monograph for IV doses.

Elixophyllin, Theo-24, Theochron

• Inhibit phosphodiesterase, producing increased tissue concentrations of cyclic adenosine monophosphate (cAMP). Increased levels of cAMP result in:
  • Bronchodilation,
  • CNS stimulation,
  • Positive inotropic and chronotropic effects,
  • Diuresis,
  • Gastric acid secretion.

• Bronchodilation.

Therapeutic Classification: bronchodilators

Pharmacologic Classification: xanthines

Absorption: Well absorbed from PO dosage forms; absorption from extended-release dosage forms is slow but complete. IV administration results in complete bioavailability.

Distribution: Widely distributed; 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: 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).

Theo ER

(bronchodilation)

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

• Emphasize the importance of taking only the prescribed dose at the prescribed time intervals. Take missed doses as soon as possible or omit if close to next dose.
• Encourage the patient to drink adequate liquids (2000 mL/day minimum) to decrease the viscosity of the airway secretions.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially OTC cough, cold, or breathing preparations ; may increase side effects and cause arrhythmias.
• Encourage patients not to smoke. A change in smoking habits may necessitate a change in dose.
• Advise patient to minimize intake of xanthine-containing foods or beverages (colas, coffee, chocolate) and not to eat charcoal-broiled foods daily.
• Instruct patient not to change brands without consulting health care professional.
• Advise patient to contact health care professional promptly if the usual dose of medication fails to produce the desired results, symptoms worsen after treatment, or toxic effects occur.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
• Emphasize the importance of having serum levels routinely tested every 6–12 mo.

thee-OFF-i-lin