Dosing & Uses
Dosage Forms & Strengths
capsule, extended-release (24 hours)
- 100mg
- 200mg
- 300mg
- 400mg
tablet, extended release (12 hours)
- 100mg
- 200mg
- 300mg
- 450mg
tablet, extended-release (24 hours)
- 400mg
- 600mg
oral elixir
- 80mg/15mL
intravenous solution
- 400mg/250mL D5W
- 400mg/500mL D5W
- 800mg/500mL D5W
Acute Bronchospasm
Loading
- Patients not currently taking theophylline: 5-7 mg/kg IV/PO; not to exceed 25 mg/min IV
- Aminophylline: 6-7 mg/kg IV infused over 20 minutes
Maintenance
- 0.4-0.6 mg/kg/hr IV or 4.8-7.2 mg/kg PO (extended release) q12hr to maintain levels 10-15 mg/L
- Smokers: 0.79 mg/kg/hr IV for next 12 hours after loading dose, then 0.63 mg/kg/hr or 5 mg/kg PO (extended release) q8hr
- Coadmininstration with drugs that decrease theophylline clearance (eg, cimetidine, ciprofloxacin, and erythromycin and other macrolides): 0.2-0.3 mg/kg/hr IV or PO (extended release) q12-24hr
- Congestive heart failure: 0.39 mg/kg/hr IV for next 12 hours after loading dose, then 0.08-0.16 mg/kg/hr
Dosage Modifications
Hepatic impairment: After loading dose, 0.39 mg/kg/hr IV for next 12 hours, then 0.08-0.16 mg/kg/hr
Dosing Considerations
For PO loading, use immediate-release theophylline
If patient is already taking theophylline, give smaller loading dose
Use ideal body weight to calculate dose
1 mg/kg results in 2 mg/L (34.4 mmol/L) increase in serum theophylline
Therapeutic range: 10-20 mg/L (172-344 mmol/L)
Aminophylline
- All dosages expressed as aminophylline; use ideal body weight (theophylline distributes poorly into body fat) to calculate dose; individualize dose based on steady-state serum concentrations
- If administering aminophylline, increase dose by 25% (aminophylline is approximately 79-86% theophylline)
- Treatment of asthma and acute COPD exacerbations with aminophylline is not recommended by current clinical practice guidelines
Dosage Forms & Strengths
capsule, extended-release (24 hours)
- 100mg
- 200mg
- 300mg
- 400mg
tablet, extended-release (12 hours)
- 100mg
- 200mg
- 300mg
- 450mg
tablet, extended-release (24 hours)
- 400mg
- 600mg
oral elixir
- 80mg/15mL
intravenous solution
- 400mg/250mL D5W
- 400mg/500mL D5W
- 800mg/500mL D5W
Bronchospasm
Loading
Maintenance
- 1.5-6 months: 0.5 mg/kg/hr IV or 10 mg/kg/day PO in divided doses
- 6-12 months: 0.6-0.7 mg/kg/hr IV or 12-18 mg/kg/day PO in divided doses
- 1-9 years: 1 mg/kg/hr IV or 8 mg/kg PO (extended release) q8hr
- 9-12 years: 0.8-0.9 mg/kg/hr IV or 6.4 mg/kg PO (extended release) q8hr
- 12-16 years: 0.7 mg/kg/hr IV or 5.6 mg/kg PO (extended release) q8hr
Neonatal Apnea
Maintenance: 3-6 mg/kg/day PO/IV divided q8hr
Dosing Considerations
If administering aminophylline, increase dose by 20-25% (aminophylline is approximately 79-86% theophylline)
Use ideal body weight to calculate dose
1 mg/kg results in 2 mg/L (34.4 mmol/L) increase in serum theophylline
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
Frequency Not Defined
Peak serum concentration <20 mcg/mL
- Central nervous system excitement, headache, insomnia, irritability, restlessness, seizure
- Diarrhea, nausea, vomiting
- Diuresis (transient)
- Exfoliative dermatitis
- Skeletal muscle tremors
- Tachycardia, flutter
- Hypercalcemia (with concomitant hyperthyroid disease)
- Difficulty urinating (elderly males with prostatism)
Peak serum concentration >30 mcg/mL
- Acute myocardial infarction
- Seizures (resistant to anticonvulsants)
- Urinary retention
Warnings
Contraindications
Hypersensitivity
Cautions
Patients, who develop CNS abnormalities, reported (rarely) to experience nonconvulsive status epilepticus
Theophylline clearance may decrease in patients with congestive heart failure, acute pulmonary edema, hepatic disease, cor pulmonale, acute hepatitis, hypothyroidism, cirrhosis, fever, or sepsis with multiorgan failure and shock; severe and potentially fatal toxicity may occur if reduced theophylling clearance occurs
Avoid extravasation; vesicant; ensure proper placement of catherer prior to and during infusion
Use with caution in patients with hyperthyroidism, seizure disorder, peptic ulcer, or cardiovascular disease
Some dosage forms may contain propylene glycol; use caution; seizures, hyperosmolality, lactic acidosis, and respiratory depression reported associated with use of large amounts of propylene glycol
Measure serum levels and withhold subsequent doses if patient develops signs and symptoms of theophylline toxicity
Use caution in patients with cardiac arrhythmia, excluding bradyarrhythmia; use may exacerbate arrhythmia
Use with caution in patients with cystic fibrosis; increased theophylline clearance may occur
Use with caution in patients with seizure disorders; use may exacerbate seizure disorder
Do not increase dose in response to acute exacerbation of symptoms unless steady state serum theophylline concentration of <10 mcg//mL
Pregnancy & Lactation
Pregnancy category: C
Lactation: Theophylline is excreted into breast milk and may cause irritability or other signs of mild toxicity in nursing human infants; serious adverse effects in infant are unlikely unless mother has toxic serum theophylline concentration
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Theophylline relaxes smooth muscles of respiratory tract and suppresses the response of the airways to stimuli
May increase tissue concentration of cyclic adenine monophosphate (cAMP) by inhibiting 2 isoenzymes of phosphodiesterase (PDE III and, to a lesser extent, PDE IV), which ultimately induces release of epinephrine from the adrenal medulla cells
Absorption
Onset: Variable
Duration: Variable
Peak plasma time: 1-2 hr
Peak plasma concentration: 10 mcg/mL
Distribution
Protein bound: 40-55%
Vd: 0.3-0.7 L/kg
Metabolism
Metabolized in liver by CYP1A2 and CYP3A4
Metabolites: 1,3-Dimethyluric acid, 1-methyluric acid, 3-methylxanthine
Elimination
Half-life: Nonsmoker, 8 hr; smoker, 4-5 hr
Clearance: 1.45 mL/min/kg
Excretion: Urine
Administration
IV Incompatibilities
Additive: Clindamycin, dobutamine, epinephrine, erythromycin, meperdine, morphine, norepinephrine, vancomycin, vitamins B and C
Y-site: Amiodarone, dobutamine, fenoldopam
Not specified: Carbenicillin, tetracycline
IV Compatibilities
Additive: Calcium gluconate, dopamine, esmolol, heparin, hydrocortisone, hydroxyzine, lidocaine, nitroglycerin, pentobarbital, potassium chloride, sodium bicarbonate, verapamil
Syringe: Heparin, pentobarbital
Y-site: Ampicillin, cefazolin, esmolol, heparin, potassium chloride, vitamins B and C
Not specified: Diazepam
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Patient Handout
Formulary
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- Compare formulary status to other drugs in the same class.
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