Theophylline

Theophylline is a prescription medication used to treat asthma, bronchitis, and emphysema (acute bronchospasm). 

• Theophylline is available under the following different brand names: Theo 24, Theochron, Elixophyllin, Aminophylline, Uniphyl.

Adult and pediatric dosage

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

Adult dosage

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• Patients not currently taking theophylline: 5-7 mg/kg IV/Orally; 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 orally (extended release) every 12 hours 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 orally (extended release) every 8 hours
• Coadministration with drugs that decrease theophylline clearance (eg, cimetidine, ciprofloxacin, and erythromycin and other macrolides): 0.2-0.3 mg/kg/hr IV or orally (extended release) every 12-24 hours
• Congestive heart failure: 0.39 mg/kg/hr IV for next 12 hours after loading dose, then 0.08-0.16 mg/kg/hr

Bronchospasm 

Pediatric dosage

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• No theophylline administered in previous 24 hours: 5-7 mg/kg IV/Orally; IV infused over 2-30 minutes

Maintenance

• Children 1.5-6 months: 0.5mg/kg/hr IV or 10 mg/kg/day orally in divided doses
• Children 6-12 months: 0.6-0.7 mg/kg/hr IV or 12-18 mg/kg/day orally in divided doses
• Children 1-9 years: 1 mg/kg/hr IV or 8 mg/kg orally (extended release) every 8 hours
• Children 9-12 years: 0.8-0.9 mg/kg/hr IV or 6.4 mg/kg orally (extended release) every 8 hours
• Children 12-16 years: 0.7 mg/kg/hr IV or 5.6 mg/kg orally (extended release) every 8 hours

Neonatal Apnea

• Loading: 4-5 mg/kg orally/IV once
• Maintenance: 3-6 mg/kg/day orally/IV divided every 8 hours

Dosage Considerations – Should be Given as Follows: 

• See "Dosages."

Common side effects of Theophylline include:

• nausea, 
• vomiting, 
• diarrhea, 
• headache, 
• sleep problems (insomnia), 
• tremors, 
• sweating, 
• restlessness, and 
• irritableness

Serious side effects of Theophylline include:

• hives, 
• difficulty breathing, 
• swelling in the face, lips, tongue, or throat, 
• severe or continued vomiting, 
• ongoing headache, 
• trouble sleeping, 
• rapid heartbeats, 
• seizure, 
• fever, 
• leg cramps, 
• constipation, 
• irregular heartbeats, 
• fluttering in the chest, 
• increased thirst or urination, 
• numbness or tingling, 
• muscle weakness, 
• limp feeling, 
• dry mouth, and
• fruity breath odor

Rare side effects of Theophylline include:

• none 

This is not a complete list of side effects and other serious side effects or health problems may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

• Theophylline has severe interactions with the following drugs:
  • dipyridamole
  • febuxostat
  • riociguat
• Theophylline has serious interactions with at least 31 other drugs.
• Theophylline has moderate interactions with at least 148 other drugs.
• Theophylline has minor interactions with at least 25 other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this drug, tell your doctor or pharmacist of all the drugs you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Contraindications

• Hypersensitivity 

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Theophylline?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Theophylline?”

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 theophylline clearance occurs
• Avoid extravasation; vesicant; ensure proper placement of catheter 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 less than 10 mcg//mL

Pregnancy and Lactation

• Use with caution in pregnancy if benefits outweigh risks.
• 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